penicillin antibiotics. Penicillin is the progenitor of modern antibiotics Antibiotic protected penicillins

Antipyretics for children are prescribed by a pediatrician. But there are emergency situations for fever when the child needs to be given medicine immediately. Then the parents take responsibility and use antipyretic drugs. What is allowed to give to infants? How can you bring down the temperature in older children? What medicines are the safest?

ANTIBIOTICS OF THE PENICILLIN GROUP

According to the modern classification, antibiotics of the penicillin group are divided into short-acting biosynthetic penicillins (benzylpenicillin sodium salt, benzylpenicillin potassium salt, benzylpenicillin novocaine salt, phenoxymethylpenicillin), long-acting biosynthetic penicillins (bicillin-1, bicillin-5, benzathine benzylpenicillin), semi-synthetic penicillins: aminopenicillins (amoxicillin, ampicillin, bacampicillin, penicillin, timentin), isoxazolylpenicillins (cloxacillin, oxacillin, flucloxacillin), carboxypenicillins (carbenicillin), ureidopenicillins (azlocillin, mezlocillin, piperacillin).

AZLOCILLIN (Azlocillin)

Synonyms: Securopen, Azlyn.

Semisynthetic beta-lactam antibiotic of the acylureidopenicillin group.

Pharmachologic effect. It has a bactericidal (destroying bacteria) effect on a large number of pathogenic (pathogenic) gram-negative, indol-positive and gram-positive microorganisms. Not resistant to beta-lactamases (enzymes secreted by microbes and destroying penicillins). Proved synergism (increased effect when used together) with aminoglycoside antibiotics.

Indications for use. Urogenital infections (infectious diseases of the urinary and genital organs), septic conditions (diseases associated with the presence of microbes in the blood) of various origins, bone and soft tissue infections, respiratory ( respiratory tract), biliary, gastrointestinal infections, serositis (inflammation of the membrane lining the cavity of the body, for example, the peritoneum), infected (infected with microbes) large areas of burns, etc. For local washing in the form of drainage (introduction through a tube into the cavity of an organ or tissue) the drug is prescribed for osteomyelitis (inflammation of the bone marrow and adjacent bone tissue), pleuroempyema (accumulation of pus between the membranes of the lungs), the presence of purulent cavities, fistulas (channels formed as a result of the disease connecting body cavities or hollow organs with the external environment or among themselves).

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. The drug is administered intravenously, rarely intramuscularly. The average daily dose for adults is from 8 g (2 g -4 times) to 15 g (5 g 3 times), with severe

infections, the appointment of 20 g per day (5 g - 4 times) is allowed. Premature babies weighing 1.5; 2.0 and 2.5 kg of the drug is administered in a single dose of 50 mg/kg 2 times a day. The average daily dose for newborns is 100 mg / kg of body weight 2 times; for infants under the age of 1 year - 100 mg / kg 3 times; for children aged 1 to 14 years - 75 mg / kg 3 times. Duration of treatment - at least 3 days after normalization of temperature and disappearance clinical symptoms. Apply in the form of a 10% aqueous solution, administered intravenously (stream or drip) at a rate of 5 ml / min, for 20-30 minutes.

Patients with impaired renal function require dose adjustment of azlocillin. Children with creatinine clearance values (the rate of blood purification from the end product of nitrogen metabolism - creatinine) is less than 30 ml / min, a 2-fold decrease in the daily dose of the drug is required. For adult patients with creatinine clearance of more than 30 ml / min, the drug is prescribed 5 g every 12 hours. With a creatinine clearance of less than 10 ml / min, the initial dose of the drug is 5 g, then 3.5 g is prescribed every 12 hours. With concomitant impaired liver function these doses should be further reduced.

Side effect. Nausea, vomiting, flatulence (accumulation of gases in the intestines), liquid stool, diarrhea (diarrhea); transient (transient) increase in the blood concentration of hepatic transaminases and alkaline phosphatase (enzymes); rarely - an increase in the concentration of bilirubin (bile pigment) in the blood. Sometimes - skin rash, itching, urticaria, rarely - drug-induced fever (a sharp rise in body temperature in response to the administration of azlocillin), acute interstitial nephritis (inflammation of the kidney with a primary lesion connective tissue), vasculitis (inflammation of the walls blood vessels). In some cases - anaphylactic shock; leukopenia (decrease in the level of leukocytes in the blood), thrombocytopenia (decrease in the number of platelets in the blood), pancytopenia (decrease in the content of all formed elements in the blood - erythrocytes, leukocytes, platelets, etc.). These side effects disappear after discontinuation of the drug. Violations of taste and smell (these effects occur when the rate of administration of the solution exceeds 5 ml / min). Rarely - erythema (limited reddening of the skin), soreness or thrombophlebitis (inflammation of the vein wall with its blockage) at the injection site. In some cases, hypokalemia (decrease in the level of potassium in the blood), an increase in the concentration of creatinine and residual nitrogen in the blood serum. With the introduction of high doses of the drug, due to an increase in its concentration in the liquor (cerebrospinal fluid), convulsions may develop.

With prolonged or repeated use of azlocillin, superinfection may develop (severe, rapidly developing forms of an infectious disease caused by drug-resistant microorganisms that were previously in the body, but do not manifest themselves).

Contraindications. Hypersensitivity to penicillins and cephalosporins.

Release form. Lyophilized (dehydrated by freezing in a vacuum) powder for the preparation of an injection solution in vials of 0.5; 1.0; 2.0 g in a pack of 5 and 10 pieces.

Storage conditions. List B. In a dry, cold and dark room.

AMOXICILLIN (Amoxicillin)

Synonyms: Amine, Amoxillate, Amoxicillin-Rati ofpharm, Amoxicillin-Teva, Apo-Amoxi, Gonoform, Grunamox, Dedoxil, Isoltil, Ospamox, Taysil, Flemoxin Solutab, Hikontsil.

Pharmachologic effect. bactericidal (killing bacteria) antibiotic synthetic penicillins. It has a wide spectrum of activity, including gram-positive and gram-negative cocci, some gram-negative rods (E. coli, shigella, salmonella, klebsiella). Microorganisms producing penicillinase (an enzyme that destroys penicillins) are resistant to the drug. The drug is acid-resistant, in the intestine is absorbed quickly and almost completely.

Indications for use. Bacterial infections: bronchitis (inflammation of the bronchi), pneumonia (inflammation of the lungs), tonsillitis, pyelonephritis (inflammation of the tissue of the kidney and renal pelvis), urethritis (inflammation of the urethra), colienteritis (inflammation small intestine caused by Escherichia coli), gonorrhea, etc., caused by microorganisms sensitive to the drug.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Doses of the drug are set individually, taking into account the severity of the infection and the sensitivity of the pathogen. Adults and children over 10 years old (weighing more than 40 kg) the drug is prescribed 0.5 g 3 times a day; in severe infections, the dose may be increased to 1.0 g 3 times a day. Children aged 5-10 years are prescribed 0.25 g 3 times a day. Children aged from

2 to 5 years appoint 0.125 g 3 times a day. Children under 2 years of age are prescribed a daily dose of 20 mg / kg of body weight in 3 divided doses. For children under the age of 10 years, it is advisable to prescribe the drug in the form of a suspension (suspension in a liquid). In the treatment of acute uncomplicated gonorrhea,

3 g once, it is desirable to simultaneously prescribe 1 g of probenecid. In the treatment of gonorrhea in women, the indicated dose is recommended to be repeated.

Side effect. Allergic reactions: urticaria, erythema (limited reddening of the skin), angioedema, rhinitis (inflammation of the nasal mucosa), conjunctivitis (inflammation of the outer membrane of the eye); rarely - fever (a sharp increase in body temperature), joint pain, eosinophilia (an increase in the number of eosinophils in the blood); extremely rarely - anaphylactic (allergic) shock. It is possible to develop superinfections (severe, rapidly developing forms of an infectious disease caused by drug-resistant microorganisms that were previously in the body, but do not manifest themselves), especially in patients with chronic diseases or reduced resistance (resistance) of the body.

Contraindications. Hypersensitivity to penicillins, Infectious mononucleosis(acute viral disease occurring with a high rise in body temperature, an increase in the palatine lymph nodes, liver).

With caution, the drug is prescribed to pregnant women; patients prone to allergic reactions. In patients with hypersensitivity to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

Release form. Tablets of 1.0 g, film-coated; capsules of 0.25 g and 0.5 g; forte capsules; solution for oral (by mouth) use (1 ml - 0.1 g); suspension for oral administration (5 ml - 0.125 g); dry matter for injections 1 g.

Storage conditions.

AUGMENTIN (Augmentm)

Synonyms: amoxicillin, potentiated by clavulanate, Amoxiclav, Amoklavin, Clavocin.

Pharmachologic effect. Broad spectrum antibiotic. It has a bacteriolytic (destroying bacteria) effect. Active against a wide range of aerobic (developing only in the presence of oxygen) and anaerobic (able to exist in the absence of oxygen) gram-positive and aerobic gram-negative microorganisms, including strains that produce beta-lactamase (an enzyme that destroys penicillins). The clavulanic acid, which is part of the preparation, ensures the stability of amoxicillin to the effects of beta-lactamases, expanding the spectrum of its action.

Indications for use. Bacterial infections caused by microorganisms sensitive to the drug: infections of the upper respiratory tract - acute and chronic bronchitis (inflammation of the bronchi), lobar bronchopneumonia (combined inflammation of the bronchi and lungs), empyema (accumulation of pus), abscesses (abscesses) of the lungs; bacterial infections of the skin and soft tissues; urinary tract infections - cystitis (inflammation Bladder), urethritis (inflammation of the urethra), pyelonephritis (inflammation of the tissue of the kidney and renal pelvis); sepsis (infection of the blood with microbes from the focus of purulent inflammation) during abortion, infections of the pelvic organs, syphilis, gonorrhea; osteomyelitis (inflammation of the bone marrow and adjacent bone tissue); septicemia (a form of blood infection by microorganisms); peritonitis (inflammation of the peritoneum); postoperative infections.

For children under the age of 1 year, the drug is prescribed in the form of drops. Single dose for children up to 3 months. - 0.75 ml, for children from 3 months. up to a year - 1.25 ml. In severe cases, an intravenous single dose for children aged 3 months. up to 12 years is 30 mg / kg of body weight; the drug is administered every 6-8 hours. For children under 3 months, a single dose of 30 mg / kg of body weight is administered: for premature babies and children in the perinatal period (on the 7th day of life of newborns) - every 12 hours, then every 8 hours. Treatment the drug should not be continued for more than 14 days without a review of the clinical situation.

Children under the age of 12 are prescribed the drug in the form of a syrup or suspension. A single dose depends on age and is: for children aged 7-12 years - 10 ml (0.156 g / 5 ml) or 5 ml (0.312 g / 5 ml); for children aged 2-7 years - 5 ml (0.156 g / 5 ml); children over the age of 9 months. before

2 years - 2.5 ml of syrup (0.156 g / 5 ml) 3 times a day. In severe infections, these doses can be doubled.

Adults and children over 12 years of age with mild and moderate infections are prescribed 1 tablet (0.375 g) 3 times a day. In severe infections, a single dose is 1 tab. 0.625 g or 2 tab. 0.375 g each

3 times a day. It is also possible to administer the drug intravenously in a single dose of 1.2 g every 6-8 hours. If necessary, the drug can be administered every 6 hours. The maximum single dose is 1.2 g, the maximum allowable daily dose for intravenous administration is 7.2 g.

Patients with impaired renal excretory function of moderate or severe degree require correction of the dosing regimen of the drug. With creatinine clearance (the rate of blood purification from the end product of nitrogen metabolism -: creatinine) more than 30 ml / min, no change in dosing regimen is required; at 10-30 ml / min - the initial dose of the drug is 1.2 g intravenously, then 0.6 g every 12 hours. With creatinine clearance less than 10 ml / min, the initial dose of the drug is 1.2 g, then 0.6 g every 24 hours. Augmentin is excreted during dialysis (a method of purifying the blood). In the case of the use of the drug in patients on dialysis, an additional intravenous administration of the drug is prescribed at a dose of 0.6 g during and 0.6 g at the end of the dialysis procedure.

Augmentin should not be mixed in the same syringe or dropper with aminoglycoside antibiotics, as inactivation (loss of activity) of the latter occurs. The drug should not be mixed with blood products and protein-containing (protein-containing) fluids.

Side effect. Rarely - dyspepsia (digestive disorders). The severity of dyspeptic side effects may decrease when taking the drug with food. Separate cases of liver dysfunction, development of hepatitis, cholestatic jaundice (jaundice associated with stagnation of bile in the biliary tract) are described. There are isolated reports of the development of pseudomembranous colitis (intestinal colic, characterized by bouts of abdominal pain and the release of large amounts of mucus in the feces). Rarely - urticaria, Quincke's edema (allergic edema); very rarely - anaphylactic (allergic) shock, erythema multiforme (an infectious-allergic disease characterized by redness of symmetrical areas of the skin and a rise in temperature), Stevens-Johnson cider (a disease characterized by redness and hemorrhage in the mucous membranes of the mouth, urethra and conjunctiva / outer shell of the eye /), exfoliative dermatitis (reddening of the skin of the whole body with its pronounced peeling). Rarely, candidiasis fungal disease) and other types of superinfection (severe, rapidly developing forms of an infectious disease caused by drug-resistant microorganisms that were previously in the body, but do not manifest themselves). In some cases, it is possible to develop phlebitis (inflammation of the vein) at the injection site.

Contraindications. Hypersensitivity to the components of the drug.

Intravenous administration should be used with caution in patients with severe hepatic impairment. Treatment should be discontinued if urticaria or an erythematous rash occurs.

It is not recommended to use the drug during pregnancy (especially in the first trimester) and breastfeeding.

The drug should be administered with caution to patients with an indication of allergic reactions in history (case history).

Release form. Tablets of 0.375 g (0.25 g of amoxicillin and 0.125 g of clavulanic acid); tablets of 0.625 g (0.5 g of amoxicillin and 0.125 g of clavulanic acid). Syrup in vials (5 ml contain 0.156 g / 0.125 g of amoxicillin and 0.03125 g of clavulanic acid / or 0.312 g / 0.25 g of amoxicillin and 0.0625 g of clavulanic acid /).

Dry matter for the preparation of a suspension (1 measuring spoon contains 0.125 g of amoxicillin and 0.031 g of clavulanic acid) and suspension-forte (1 measuring spoon contains 0.25 g of amoxicillin and 0.062 g of clavulanic acid). Dry matter for the preparation of drops (1 ml of drops contains 0.05 g of amoxicillin and 0.0125 g of clavulanic acid). IN dosage forms for oral (by mouth) use, amoxicillin is in the form of a trihydrate, and clavulanic acid is in the form of a potassium salt.

Powder for injection 0.6 g (0.5 g amoxicillin and 0.1 g clavulanic acid) in vials. Powder for injection 1.2 g (1.0 g amoxicillin and 0.2 g clavulanic acid). In dosage forms for intravenous use, amoxicillin is in the form of a sodium salt, and clavulanic acid is in the form of a potassium salt. Each 1.2 g vial contains approximately 1.0 mmol potassium and 3.1 mmol sodium.

Storage conditions. List B. In a dry, cool place.

KLONACOM-X (Clonacom-X)

Pharmachologic effect. Combined preparation containing semi-synthetic penicillins. The combination of amoxicillin with penicillinase-resistant (resistant to the action of an enzyme that destroys penicillins) cloxacillin expands the spectrum and in some cases enhances the effect of each drug individually. Amoxicillin has a wide spectrum of activity, is active against most gram-negative (with the exception of Pseudomonas aeruginosa) and gram-positive bacteria (with the exception of penicillinase-forming / forming an enzyme that destroys penicillins - penicillinase / staphylococci). Not resistant to penicillinase. Cloxacillin is similar in spectrum of action to benzylpenicillin, but differs in resistance to penicillinase.

Indications for use. Infectious diseases caused by microorganisms sensitive to the drug: infections of the upper respiratory tract, bronchitis (inflammation of the bronchi), pneumonia (inflammation of the lungs), urinary tract infections, infections of the skin and soft tissues, infections of the gastrointestinal tract, infections of the bones and joints, gonorrhea.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults are advised to take 1 capsule every 6-8 hours, depending on the severity of the disease. With impaired renal function, a dose reduction is necessary.

Side effect.

Contraindications. Infectious mononucleosis (an acute viral disease that occurs with a high rise in body temperature, an increase in palatine lymph nodes, liver). Hypersensitivity to antibiotics penicillin series. The drug should be administered with caution to patients with an indication of allergic reactions in history (case history).

Release form. Capsules in a package of 100 pieces. One capsule contains amoxicillin trihydrate and cloxacillin sodium in amounts corresponding to 0.25 g of amoxicillin and 0.25 g of cloxacillin.

Storage conditions. List B. In a dry, dark place. . .

AMPICILLIN (AmpiciUinum)

Synonyms: Pentrexil, Abetaten, "Acidocycline, Aniline, Acrocilin, Agnopen, Albercilin, Amiel, Amecillin, Ampen, Ampeksin, Ampifen, Ampilin, Ampiopenil, Amplenil, Amplital, Bactipen, Biampen, Binotal, Britapen, Broadocylin, Tsimeksillin, Diacycline, Dicillin, Domicillin , Domipen, Eurocillin, Fortapen, Grampenil, Isticillin, Lifitillin, Maxibiotic, Maxipred, Morepen, Negopen, Opicilin, Oracilina, Penberin, Penybrin, Pentrex, Polycilin, Riomycin, Roscillin, Semicillin, Sintelin, Sinpenin, Totacillin, Ultrabion, Vampen, Vexampil , Vidopen, Zimopen, Apo-Ampi, Mencilin, Standacillin, Dedoompil, Campicillin, etc.

Pharmachologic effect. Ampicillin is a semi-synthetic antibiotic obtained by acylation of 6-aminopenicillanic acid with an amino-phenylacetic acid residue.

The drug is not destroyed in acidic environment stomach, well absorbed when taken orally. Active against gram-positive microorganisms, which are affected by benzylpenicillin. In addition, it acts on a number of gram-negative microorganisms (Salmonella, Shigella, Proteus, Escherichia coli, Klebsiella pneumonia / Friedlander's stick /, Pfeiffer's stick / influenza stick /) and is therefore considered as a broad-spectrum antibiotic and is used in diseases caused by mixed infections.

On penicillinase-forming (forming penicillinase - an enzyme that destroys penicillins) staphylococci resistant to benzylpenicillin, ampicillin does not work, as it is destroyed by penicillinase.

Indications for use. Ampicillin is used to treat patients with pneumonia (inflammation of the lungs), bronchopneumonia (combined inflammation of the bronchi and lungs), with abscesses (abscesses) of the lungs, tonsillitis, peritonitis (inflammation of the peritoneum), cholecystitis (inflammation of the gallbladder), sepsis (infection of the blood with microbes from a focus of purulent inflammation), intestinal infections, postoperative soft tissue infections and other infections caused by microorganisms sensitive to it. The drug has high efficiency with infections urinary tract caused by Escherichia coli, Proteus, Enterococcus or mixed infection, as it is excreted unchanged in the urine in high concentrations. In large quantities, ampicillin also enters the bile. The drug is effective in the treatment of gonorrhea.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Assign ampicillin inside (regardless of the intake of food). A single dose for adults is 0.5 g, daily - 2-3 g. Children are prescribed at the rate of 100 mg / kg. daily dose divided into 4-6 receptions.

The duration of treatment depends on the severity of the disease and the effectiveness of therapy (from 5-10 days to 2-3 weeks or more).

Side effect. In the treatment of ampiillin, allergic reactions may occur in the form of skin rash, urticaria, Quincke's edema, etc., in rare cases, anaphylactic shock (mainly with the introduction of ampicillin sodium salt).

In case of occurrence allergic reactions it is necessary to stop the administration of the drug and conduct desensitizing (preventing or inhibiting allergic reactions) therapy. When signs of anaphylactic shock appear, urgent measures must be taken to remove the patient from this state.

With long-term treatment with ampicillin in debilitated patients, it is possible to develop superinfection (severe, rapidly developing forms of an infectious disease caused by drug-resistant microorganisms that were previously in the body, but do not manifest themselves), caused by drug-resistant microorganisms (yeast-like fungi, gram-negative microorganisms). It is advisable for these patients to simultaneously prescribe vitamins of group B and vitamin C, if necessary - nystatin or levorin.

Contraindications. The drug is contraindicated in case of hypersensitivity to penicillin. In hepatic insufficiency, it is used under the control of liver function; at bronchial asthma, hay fever and other allergic diseases only when absolutely necessary. At the same time, desensitizing agents are prescribed.

Ampicillin enhances the effect of oral anticoagulants (taken by mouth medicines that prevent blood clotting).

The drug should be administered with caution to patients with an indication of allergic reactions in history (case history).

Release form. Tablets and capsules 0.25 each. g in a package of 10 or 20 pieces. Powder for the preparation of a suspension (slurry) in orange glass jars of 60 g (5 g of active substance). White powder with a yellowish tint (sweet in taste), with a specific odor (contains sugar, vanillin and other fillers). It is taken orally in the same dose as ampicillin based on the content of the active substance. Mix the powder with water or drink it with water.

Storage conditions.

AMPIOKS (Ampioxum)

Combined preparation containing ampicillin and oxacillin. For oral administration, Ampiox is produced, which is a mixture of ampicillin trihydrate and oxacillin sodium salt (1: 1), and for parenteral use - Ampiox-sodium (Ampioxum-natrium), which is a mixture of sodium salts of ampicillin and oxacillin (2: 1).

Pharmachologic effect. The drug combines the spectrum of antimicrobial action of ampicillin and oxacillin; acts on gram-positive (staphylococcus, streptococcus, pneumococcus) and gram-negative (gonococcus, meningococcus, E. coli, Pfeiffer bacillus / influenza bacillus /, salmonella, shigella, etc.) microorganisms. Due to the content of oxacillin, it is active against penicillinase-forming (forming penicillinase - an enzyme that destroys penicillins) staphylococci.

The drug penetrates well into the blood when taken orally and parenterally (bypassing the digestive tract) administration.

Indications for use. It is used for infections of the respiratory tract and lungs (bronchitis - inflammation of the bronchi, pneumonia - inflammation of the lungs, etc.), with tonsillitis, cholangitis (inflammation bile ducts), cholecystitis (inflammation of the gallbladder), pyelitis (inflammation of the renal pelvis), pyelonephritis (inflammation of the tissue of the kidney and renal pelvis), cystitis (inflammation of the bladder), infected wounds, skin infections, etc. Especially indicated in cases of severe diseases: sepsis (infection of the blood with microbes from the focus of purulent inflammation), endocarditis (inflammation of the internal cavities of the heart), postpartum infection, etc. With an unidentified antibiogram (the spectrum of antibiotic activity characterizing the sensitivity of pathogens to it) and an unidentified pathogen, with a mixed infection caused by sensitive and insensitive to benzylpenicillin by staphylococci or streptococci and gram-negative bacteria, with burn disease, kidney infections. It is used to prevent purulent postoperative complications in surgical operations and for the prevention and treatment of infections in newborns.

In the treatment of gonorrhea, ampiox is used in cases caused by resistant (resistant) to benzylpenicillin strains of gonococci.

With parenteral administration, a single dose of ampiox-sodium for adults is 0.5-1.0 g, daily - 2-4 g.

Newborns, premature babies and children under 1 year of age are administered in a daily dose of 100-200 mg per 1 kg of body weight; children from 1 to 7 years old - 100 mg / kg per day; from 7 to 14 years - 50 mg / kg per day; children over the age of 14 are prescribed the adult dose. In severe infections, doses can be increased by 1.5-2 times.

To prepare solutions for intramuscular injection, add 2 ml of sterile water for injection to the contents of the vial with ampiox-sodium (0.1; 0.2; 0.5 g).

The duration of treatment ranges from 5-7 days to 3 weeks. and more.

For intravenous administration (jet), a single dose of the drug is dissolved in 10-15 ml of sterile water for injection or isotonic sodium chloride solution and injected slowly over 2-3 minutes. For intravenous drip in adults, the drug is dissolved in 100-200 ml of isotonic sodium chloride solution or 5% glucose solution and administered at a rate of 60-80 drops per minute. With drip administration, children use 5-10% glucose solution (30-100 ml) as a solvent. Intravenously administered for 5-7 days, followed by the transition (if necessary) to intramuscular injection. Solutions are used immediately after preparation; mixing them with other medicines is unacceptable.

When taken orally, a single dose of Ampiox for adults is 0.5-1.0 g, daily - 2-4 g. Children from 3 to 7 years old are prescribed 100 mg / kg per day, from 7 to 14 years old - 50 mg / kg per day, over 14 years old - at the adult dose. Duration of treatment - from 5-7 days to 2 weeks. and more. The daily dose is divided into 4-6 doses.

Side effect. Possible side effects: with parenteral (bypassing the digestive tract) administration of ampiox-sodium - pain at the injection site and allergic reactions, in rare cases - anaphylactic (allergic) shock; when taking Ampiox inside - nausea, vomiting, loose stools, allergic reactions. If necessary, desensitizing (preventing or inhibiting allergic reactions) agents are prescribed.

Contraindications. Ampioks and ampioks-sodium are contraindicated if there is a history (medical history) of data on toxic-allergic reactions to drugs of the penicillin group.

Release form. For parenteral administration, ampioks-sodium is released in vials of 0.1; 0.2 or 0.5 g labeled "Intravenous" or "Intramuscular". For oral administration, Ampiox is available in capsules of 0.25 g in a package of 20 pieces.

Storage conditions.

AMPICILLIN SODIUM SALT (Ampicillinum-natrium)

Synonyms: Penbritin, Penbrock, Policillin, Ampicid.

Pharmachologic effect. Semi-synthetic broad-spectrum penicillin. Active against coccal microorganisms (staphylococci that do not form penicillinase / an enzyme that destroys penicillins /, streptococci, pneumococci, gonococci and meningococci) and most gram-negative bacteria (E. coli, Salmonella, Shigella, Proteus mirabilis, H. influenzae and some strains of KJ. pneumoniae).

It is quickly absorbed into the blood, penetrates into tissues and body fluids. It is excreted mainly by the kidneys. It does not have cumulative properties (the ability to accumulate in the body). Low toxicity (does not have a pronounced damaging effect on the body).

Indications for use. Inflammatory diseases of the respiratory tract: pneumonia (inflammation of the lungs), bronchitis (inflammation of the bronchi), pharyngitis (inflammation of the pharynx), etc.; urological diseases: pyelonephritis (inflammation of the tissue of the kidney and renal pelvis), cystitis (inflammation of the bladder), prostatitis (inflammation of the prostate gland), intestinal infections: dysentery, salmonellosis, enterocolitis (inflammation of the small and large intestine), septic endocarditis (inflammation of the internal cavities of the heart due to the presence of microbes in the blood), meningitis (inflammation of the meninges), erysipelas, etc.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. It is used for intramuscular and intravenous (jet or drip) administration. With both routes of administration, a single dose of the drug for adults is 0.25-0.5 g; daily - 1-3 g. In severe infections, the daily dose can be increased to 10 g or more. With meningitis - up to 14 g per day. Multiplicity of introduction - 6-8 times. For newborns, the drug is prescribed in a daily dose of 100 mg / kg, for children of other age groups - 50 mg / kg. In severe infectious diseases, these doses can be doubled.

The daily dose is administered in 4-6 doses at intervals of 4-6 hours.

Solution for intramuscular injection prepare ex tempore (before use) by adding 2 ml of sterile water to the contents of the vial (0.25 or 0.5 g). injections. The duration of treatment is 7-14 days or more.

For intravenous jet administration, a single dose of the drug (no more than 2 g) is dissolved in 5-10 ml of sterile water for injection or isotonic sodium chloride solution and injected slowly over 3-5 minutes (1-2 g over 10-15 minutes). With a single dose exceeding 2 g, the drug is administered intravenously. For intravenous drip, a single dose of the drug is dissolved in a small volume of sterile water for injection (7.5-15.0 ml, respectively), then the resulting antibiotic solution is added to 125-250 ml of isotonic sodium chloride solution or 5-10% glucose solution and administered at a rate of 60-80 drops per minute. With drip administration to children, a 5-10% glucose solution is used as a solvent (30-50 ml, depending on age). Solutions are used immediately after preparation; addition of other drugs to them is unacceptable. The daily dose is divided into 3-4 injections. The duration of treatment is 5-7 days, followed by the transition (if necessary) to intramuscular injection.

Side effect. Allergic reactions.

Contraindications. Allergy to penicillin preparations, impaired liver function.

The drug should be administered with caution to patients with an indication of allergic reactions in history (case history).

Release form. In vials of sterile powder complete with a solvent of 0.25 g, 0.5 g; powder 5 g in a vial for suspension; disks of 10 mcg, in a package of 100 pieces.

Storage conditions. List B. In a dry, dark place at room temperature.

AMPICILLIN TRIHYDRATE (Ampicillinum trihydras)

Synonyms: A-Pen.

Pharmachologic effect. Same as ampicillin and its sodium salt. It differs from ampicillin by the presence of 3 molecules of crystallized water in the structure.

Indications for use. Same as for ampicillin.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Inside, 0.5 g every 4-6 hours, with severe infections, up to 10 g or more per day; children under 13 years old - 0.1-0.2 g (kg / day). The course of treatment is 7-14 days or more.

Side effects and contraindications are the same as for ampicillin.

Release form. Tablets of 0.25 g in a package of 24 pieces; capsules of 0.25 g in a package of 6 pieces.

Storage conditions. List B. In a dry, dark place at room temperature.

KLONACOM-R (Clonacom-P)

Pharmachologic effect. Combined preparation containing semi-synthetic penicillins. The combination of ampicillin with penicillinase-resistant (resistant to the action of an enzyme that destroys penicillins) cloxacillin expands the spectrum and in some cases enhances the effect of each drug individually. Ampicillin has a wide spectrum of activity, is active against most gram-negative (with the exception of Pseudomonas aeruginosa) and gram-positive bacteria (with the exception of penicillinase-forming / forming penicillinase - an enzyme that destroys penicillins / staphylococci). Not resistant to penicillinase. Cloxacillin is similar in spectrum of action to benzylpenicillin, but differs in resistance to penicillinase.

Indications for use. Infectious diseases caused by microorganisms sensitive to the drug: infections of the upper respiratory tract, bronchitis (inflammation of the bronchi), pneumonia (inflammation of the lungs), infections of the urinary tract, skin and soft tissues, gastrointestinal tract, bones and joints, gonorrhea.

With impaired renal function, a dose reduction is necessary.

Side effect. Allergic reactions, skin rash; possible diarrhea, nausea, vomiting; in some cases, pseudomembranous colitis (intestinal colic, characterized by bouts of abdominal pain and the release of large amounts of mucus with feces) may develop.

The drug should be administered with caution to patients with an indication of allergic reactions in history (case history).

Release form. Capsules in a package of 100 pieces. One capsule contains 0.25 g of ampicillin and 0.25 g of cloxacillin.

Storage conditions. List B. In a dry, dark place.

SULTAMICILLIN (Sultamicillin)

Synonyms: Sulaiillin, Betamp, Unazin.

Combined preparation containing ampicillin-sodium and sulbactam-sodium in a ratio of 2: 1.

Pharmachologic effect. Sulbactam-sodium does not have a pronounced antibacterial activity, but irreversibly inhibits (suppresses activity) beta-lactamase (an enzyme that destroys the beta-lactam core of the penis). When used together with penicillins, sulbactam protects the latter from hydrolysis (decomposition involving water) and inactivation (partial or complete loss of biological activity). Unazine (sulbactam + ampicillin combination) is a highly effective drug that acts on gram-positive and gram-negative aerobes (microorganisms that develop only in the presence of oxygen) and anaerobes (microorganisms that can exist in the absence of oxygen), including penicillin-resistant strains.

Indications for use. Unazine is used for pneumonia (pneumonia), bronchitis (inflammation of the bronchi), otitis media (inflammation of the ear cavity), sinusitis (inflammation of the paranasal sinuses), purulent surgical infections (abscesses - ulcers, phlegmon - acute, clearly not delimited purulent inflammation, osteomyelitis - inflammation bone marrow and adjacent bone tissue, etc.), peritonitis (inflammation of the peritoneum), urological (urinary tract) and gynecological infections, for the prevention of postoperative purulent complications, gonorrhea and other infections.

Children weighing less than 30 kg - 25-50 mg / kg per day in 2 doses, depending on the severity of the infection and at the discretion of the doctor. With a body weight of 30 kg or more - as in adults, i.e. 375-750 mg (1-2 tablets) 2 times a day. For children, the drug can be prescribed in the form of a suspension (suspension).

The course of treatment is usually from 5 to 14 days, but if necessary, can be extended. After the temperature normalizes and the main pathological symptoms disappear, treatment continues for another 48 hours.

In the treatment of uncomplicated gonorrhea, sultamicillin can be prescribed as a single dose of 2.25 g (6 tablets of 375 g). To prolong the residence time of sulbactam and ampicillin in blood plasma, in

as a concomitant agent, a 1 g sample of Necida should be prescribed.

In gonorrhea patients with suspected syphilis, microscopic tests should be performed during treatment and monthly serological tests for at least 4 months.

In the treatment of any infection caused by hemolytic streptococci, to prevent the occurrence of rheumatism or glomerulonephritis (kidney disease), it is recommended to carry out antibiotic therapy for 10 days.

In patients with severely impaired renal function (creatinine clearance / rate of blood clearance from the end product of nitrogen metabolism - creatinine / less than 30 ml / min), the dynamics of the release of sulbactam and ampicillin are equally affected, therefore, the ratio of one to the other in plasma will remain constant. In such patients, the dose of sultamicillin is administered at large intervals in accordance with the usual practice of using ampicillin.

After dilution, the suspension should be stored in the refrigerator for no more than 14 days.

Side effect. The most common side effect is diarrhea (diarrhea), but also nausea, vomiting, pain in the epigastric region (the area of the abdomen located directly under the convergence of the costal arches and the sternum), abdominal pain and colic. As with other antibiotics of the ampicillin series, enterocolitis (inflammation of the small and large intestines) and pseudomembranous colitis (intestinal colic characterized by bouts of abdominal pain and the release of large amounts of mucus with feces) have been reported in rare cases. Rash, itching and other skin reactions. Drowsiness, malaise, headache. In rare cases, anemia (decrease in hemoglobin in the blood), thrombocytopenia (decrease in the number of platelets in the blood), eosinophilia (increase in the number of eosinophils in the blood) and leukopenia (decrease in the level of leukocytes in the blood). These effects disappear after treatment is stopped. Perhaps a transient increase in the level of enzymes alanine transferase and asparagine transferase. With intramuscular injection, pain at the injection site is possible. In isolated cases - the development of phlebitis (inflammation of the vein) after intravenous administration of the drug.

Contraindications. Allergy to any of the penicillins in history (previously).

The drug should be used with caution in patients with a history of allergic reactions.

Release form. Sterile powder for intramuscular and intravenous administration 0.75 g in 10 ml vials (ampicillin sodium 0.5 g, sodium sulfabactam 0.25 g). Sterile powder for intramuscular and intravenous administration 1.5 g in 20 ml vials (sodium ampicillin 1.0 g, sodium sulfabactam 0.5 g). Sterile powder for intramuscular and intravenous administration 3 g in 20 ml vials (ampicillin sodium 2.0 g, sodium sulfabactam 1.0 g). Tablets of 0.375 g of the drug. Powder for the preparation of a suspension (5 ml - 0.25 g of the drug).

Storage conditions. List B. In a dark place.

Familiar today antibacterial drugs less than a century ago made a real revolution in medicine. Mankind has received a powerful weapon to fight infections that were previously considered fatal.

The first were the antibiotics penicillins, which saved many thousands of lives during the Second World War, and are relevant in modern medical practice. It was with them that the era of antibiotic therapy began and thanks to them all other antimicrobial drugs were obtained.

Main title	Antimicrobial activity	Analogues
Benzylpenicillin potassium and sodium salts	Influence mainly gram-positive microorganisms. Currently, most strains have developed resistance, but spirochetes are still sensitive to the substance.	Gramox-D, Ospen, Star-Pen, Ospamox
benzylpenicillin procaine	Indicated for the treatment of streptococcal and pneumococcal infections. Compared to potassium and sodium salts, it acts longer, as it dissolves and is absorbed more slowly from the intramuscular depot.	Benzylpenicillin-KMP (-G, -Teva, -G 3 mega)
Bicillins (1, 3 and 5)	It is used for chronic rheumatism with a prophylactic purpose, as well as for the treatment of infectious diseases of moderate and mild severity caused by streptococci.	Benzicillin-1, Moldamine, Extincillin, Retarpin
Phenoxymethylpenicillin	It has a therapeutic effect similar to the previous groups, but is not destroyed in an acidic gastric environment. Produced in the form of tablets.	V-Penicillin, Kliacil, Ospen, Penicillin-Fau, Vepicombin, Megacillin Oral, Pen-os, Star-Pen
Oxacillin	Active against staphylococci that produce penicillinase. It is characterized by low antimicrobial activity, it is completely ineffective against penicillin-resistant bacteria.	Oxamp, Ampiox, Oxamp-Sodium, Oxamsar
Ampicillin	Extended spectrum of antimicrobial activity. In addition to the main spectrum inflammatory diseases Gastrointestinal tract, treats and caused by Escherichia, Shigella, Salmonella.	Ampicillin AMP-KID (-AMP-Forte, -Ferein, -AKOS, -trihydrate, -Innotek), Zetsil, Pentrixil, Penodil, Standacillin
Amoxicillin	It is used to treat inflammation of the respiratory and urinary tract. After clarifying the bacterial origin of gastric ulcers, Helicobacter pylori is used for eradication.	Flemoxin solutab, Hikoncil, Amosin, Ospamox, Ecobol
Carbenicillin	The spectrum of antimicrobial action includes Pseudomonas aeruginosa and enterobacteria. The digestibility and bactericidal effect is higher than that of Carbenicillin.	Securopen
Piperacillin	Similar to the previous one, but the level of toxicity is increased.	Isipen, Pipracil, Picillin, Piprax
Amoxicillin/clavulanate	Due to the inhibitor, the spectrum of antimicrobial activity is expanded compared to the unprotected agent.	Augmentin, Flemoklav solutab, Amoxiclav, Amklav, Amovikomb, Verklav, Ranklav, Arlet, Klamosar, Rapiclav
Ampicillin/sulbactam		Sulacillin, Liboksil, Unazine, Sultasin
Ticarcillin/clavulanate	The main indication for use is nosocomial infections.	Gimentin
Piperacillin/tazobactam	The main indication for use is nosocomial infections.	Tazocin

The information provided is for informational purposes and is not a guide to action. All appointments are made exclusively by a doctor, and therapy is under his control.

Despite the low toxicity of penicillins, their uncontrolled use leads to serious consequences: the formation of resistance in the pathogen and the transition of the disease to a chronic form that is difficult to cure. It is for this reason that most strains of pathogenic bacteria are resistant to first-generation ABP today.

Use for antibiotic therapy should be exactly the medication that was prescribed by a specialist. Independent attempts to find cheap analogue and savings can lead to deterioration.

For example, the dosage of the active substance in a generic may differ up or down, which will negatively affect the course of treatment.

When you have to replace the medicine due to an acute lack of finances, you need to ask the doctor about it, since only a specialist can choose the best option.

Penicillins: definition and properties

Preparations of the penicillin group belong to the so-called beta-lactams - chemical compounds that have a beta-lactam ring in their formula.

This structural component is of decisive importance in the treatment of bacterial infectious diseases: it prevents bacteria from producing a special peptidoglycan biopolymer necessary for building the cell membrane. As a result, the membrane cannot form and the microorganism dies. There is no destructive effect on human and animal cells for the reason that they do not contain peptidoglycan.

Medications based on the waste products of mold fungi are widely used in all areas of medicine due to the following properties:

High bioavailability - drugs are quickly absorbed and distributed through the tissues. The weakening of the blood-brain barrier during inflammation of the meninges also contributes to the penetration into the cerebrospinal fluid.
Broad spectrum of antimicrobial action. Unlike first-generation chemicals, modern penicillins are effective against the vast majority of gram-negative and positive bacteria. They are also resistant to penicillinase and the acidic environment of the stomach.
The lowest toxicity among all ABPs. They are allowed for use even during pregnancy, and the correct intake (as prescribed by the doctor and according to the instructions) almost completely eliminates the development of side effects.

In the process of research and experiments, many medications with different properties were obtained. For example, when belonging to the general series, penicillin and ampicillin are not the same thing. All penicillin antibiotics are well compatible with most others. medicines. Concerning complex therapy with other types of antibacterial drugs, then the combined use with bacteriostatics weakens the effectiveness of penicillins.

Classification

Careful study of the properties of the first antibiotic showed its imperfection. Despite a fairly wide range of antimicrobial activity and low toxicity, natural penicillin turned out to be sensitive to a special destructive enzyme (penicillinase) produced by some bacteria. In addition, it completely lost its qualities in an acidic gastric environment, therefore it was used exclusively in the form of injections. In search of more effective and stable compounds, various semi-synthetic drugs have been created.

Currently, penicillin antibiotics full list which are listed below are divided into 4 main groups.

Biosynthetic

Produced by the fungi Penicillium notatum and Penicillium chrysogenum, benzylpenicillin is an acid molecular structure. For medical purposes, it combines chemically with sodium or potassium to form salts. The resulting compounds are used to prepare injection solutions that are rapidly absorbed.

The therapeutic effect is noted within 10-15 minutes after injection, but lasts no more than 4 hours, which requires frequent repeated injections into muscle tissue (in special occasions sodium salt can be administered intravenously).

These drugs penetrate well into the lungs and mucous membranes, and to a lesser extent into the cerebrospinal and synovial fluids, myocardium and bones. However, with inflammation of the meninges (meningitis), the permeability of the blood-brain barrier increases, which allows for successful treatment.

To prolong the effect of the drug, natural benzylpenicillin combines with novocaine and other substances. The resulting salts (novocaine, Bicillin-1, 3 and 5) after intramuscular injection form a drug depot at the injection site, from where the active substance enters the blood constantly and at a low speed. This property allows you to reduce the number of injections up to 2 times a day while maintaining therapeutic effect potassium and sodium salts.

These drugs are used for long-term antibiotic therapy of chronic rheumatism, syphilis, focal streptococcal infection.
Phenoxymethylpenicillin is another form of benzylpenicillin used to treat mild infections. It differs from those described above in resistance to hydrochloric acid of gastric juice.

This quality allows the drug to be produced in the form of tablets for oral administration (from 4 to 6 times a day). Most pathogenic bacteria are currently resistant to biosynthetic penicillins, except for spirochetes.

See also: Instructions for the use of penicillin in injections and tablets

Semi-synthetic antistaphylococcal

Natural benzylpenicillin is inactive against strains of staphylococcus that produce penicillinase (this enzyme destroys the beta-lactam ring of the active substance).

For a long time, penicillin was not used to treat staphylococcal infections, until oxacillin was synthesized on its basis in 1957. It inhibits the activity of beta-lactamases of the pathogen, but is ineffective against diseases caused by benzylpenicillin-sensitive strains. This group also includes cloxacillin, dicloxacillin, methicillin and others, almost not used in modern medical practice due to increased toxicity.

Antibiotics of the penicillin group in broad spectrum tablets

This includes two subgroups of antimicrobials intended for oral use and having a bactericidal effect against most pathogens (both gram+ and gram-).

Aminopenicillins

Compared with the previous group, these compounds have two significant advantages. Firstly, they are active against a wider range of pathogens, and secondly, they are available in tablet form, which greatly facilitates the use. The disadvantages include sensitivity to beta-lactamase, that is, aminopenicillins (ampicillin and amoxicillin) are unsuitable for the treatment of staphylococcal infections.

However, in combination with oxacillin (Ampioks) they become resistant.

The preparations are well absorbed and act for a long time, which reduces the frequency of use to 2-3 times per 24 hours. The main indications for use are meningitis, sinusitis, otitis, infectious diseases of the urinary and upper respiratory tract, enterocolitis and eradication of Helicobacter (causative agent of stomach ulcers). A common side effect of aminopenicillins is a characteristic non-allergic rash that disappears immediately after withdrawal.

Antipseudomonal

They are a separate penicillin series of antibiotics, from the name of which the purpose becomes clear. Antibacterial activity is similar to aminopenicillins (with the exception of Pseudomonas) and is pronounced against Pseudomonas aeruginosa.

According to the degree of efficiency are divided into:

Carboxypenicillins, the clinical significance of which has recently been declining. Carbenicillin, the first of this subgroup, is also effective against ampicillin-resistant Proteus. Currently, almost all strains are resistant to carboxypenicillins.
Ureidopenicillins are more effective against Pseudomonas aeruginosa, and can also be prescribed for inflammation caused by Klebsiella. The most effective are Piperacillin and Azlocillin, of which only the latter remains relevant in medical practice.

To date, the vast majority of strains of Pseudomonas aeruginosa are resistant to carboxypenicillins and ureidopenicillins. For this reason, their clinical significance is reduced.

Inhibitor-protected combined

The ampicillin group of antibiotics, highly active against most pathogens, is destroyed by penicillinase-forming bacteria. Since the bactericidal action of oxacillin resistant to them is much weaker than that of ampicillin and amoxicillin, combined drugs were synthesized.

In combination with sulbactam, clavulanate and tazobactam, antibiotics receive a second beta-lactam ring and, accordingly, immunity to beta-lactamases. In addition, inhibitors have their own antibacterial effect, enhancing the main active ingredient.

Inhibitor-protected drugs successfully treat severe nosocomial infections, strains of which are resistant to most drugs.

See also: About the modern classification of antibiotics by group of parameters

Penicillins in medical practice

An extensive spectrum of action and good tolerance by patients made penicillin the optimal treatment for infectious diseases. At the dawn of the era of antimicrobial drugs, benzylpenicillin and its salts were the drugs of choice, but at the moment most pathogens are resistant to them. Nevertheless, modern semi-synthetic penicillin antibiotics in tablets, injections and other dosage forms occupy one of the leading places in antibiotic therapy in various fields of medicine.

Pulmonology and otolaryngology

Another discoverer noted the special effectiveness of penicillin against pathogens of respiratory diseases, so the drug is most widely used in this area. Almost all of them have a detrimental effect on bacteria that cause sinusitis, meningitis, bronchitis, pneumonia and other diseases of the lower and upper respiratory tract.

Inhibitor-protected agents treat even particularly dangerous and persistent nosocomial infections.

Venereology

Spirochetes are one of the few microorganisms that have retained susceptibility to benzylpenicillin and its derivatives. Benzylpenicillins are also effective against gonococci, which makes it possible to successfully treat syphilis and gonorrhea with minimal negative effects on the patient's body.

Gastroenterology

Inflammation of the intestines caused by pathogenic microflora responds well to therapy with acid-resistant drugs.

Of particular importance are aminopenicillins, which are part of the complex eradication of Helicobacter.

Gynecology

In obstetric and gynecological practice, many penicillin preparations from the list are used both to treat bacterial infections of the female reproductive system and to prevent infection in newborns.

Ophthalmology

Here, penicillin antibiotics also occupy a worthy place: eye drop, ointments and solutions for injection are treated keratitis, abscesses, gonococcal conjunctivitis and other eye diseases.

Urology

Diseases of the urinary system, which are of bacterial origin, respond well to therapy only with inhibitor-protected drugs. The remaining subgroups are ineffective, since the strains of pathogens are highly resistant to them.

Penicillins are used in almost all areas of medicine for inflammation caused by pathogenic microorganisms, and not only for treatment. For example, in surgical practice, they are prescribed to prevent postoperative complications.

Features of therapy

Treatment with antibacterial medications in general and penicillins in particular should be carried out only on prescription. Despite the minimal toxicity of the drug itself, its improper use seriously harms the body. In order for antibiotic therapy to lead to recovery, it is necessary to observe medical recommendations and know the characteristics of the drug.

Indications

The scope of application of penicillin and various preparations based on it in medicine is due to the activity of the substance with respect to specific pathogens. Bacteriostatic and bactericidal effects are manifested in relation to:

Gram-positive bacteria - gonococci and meningococci;
Gram-negative - various staphylococci, streptococci and pneumococci, diphtheria, Pseudomonas aeruginosa and anthrax, Proteus;
Actinomycetes and spirochetes.

Low toxicity and a broad spectrum of action make antibiotics of the penicillin group the best treatment for tonsillitis, pneumonia (both focal and lobar), scarlet fever, diphtheria, meningitis, blood poisoning, septicemia, pleurisy, pyemia, osteomyelitis in acute and chronic forms, septic endocarditis, various purulent infections of the skin, mucous membranes and soft tissues, erysipelas, anthrax, gonorrhea, actinomycosis, syphilis, blennorrhea, as well as eye diseases and ENT diseases.

Contraindications

Strict contraindications include only individual intolerance to benzylpenicillin and other drugs in this group. Also, endolumbar (injection into spinal cord) administration of drugs to patients diagnosed with epilepsy.

During pregnancy, antibiotic therapy with penicillin preparations should be treated with extreme caution. Despite the fact that they have a minimal teratogenic effect, it is worth prescribing tablets and injections only in case of urgent need, assessing the degree of risk to the fetus and the pregnant woman herself.

Since penicillin and its derivatives freely penetrate from the bloodstream into breast milk, it is advisable to refuse breastfeeding for the duration of therapy. The medicine can provoke a severe allergic reaction in the baby even at the first use. To prevent lactation, milk must be expressed regularly.

Side effect

Among other antibacterial agents, penicillins are favorably distinguished by their low toxicity.

TO undesirable consequences uses include:

Allergic reactions. Most often manifested by skin rash, itching, urticaria, fever and swelling. Extremely rarely, in severe cases, anaphylactic shock is possible, requiring the immediate administration of an antidote (adrenaline).
Dysbacteriosis. Imbalance of the natural microflora leads to digestive disorders (flatulence, bloating, constipation, diarrhea, abdominal pain) and the development of candidiasis. In the latter case, the mucous membranes are affected oral cavity(in children) or the vagina.
neurotoxic reactions. The negative effect of penicillin on the central nervous system manifested by increased reflex excitability, nausea and vomiting, convulsions, and sometimes coma.

To prevent the development of dysbacteriosis and avoid allergies, timely medical support of the body will help. It is desirable to combine antibiotic therapy with the intake of pre- and probiotics, as well as desensitizers (if sensitivity is increased).

Penicillin antibiotics for children: application features

For children, tablets and injections should be prescribed carefully, taking into account the possible backlash, and the choice of a particular drug should be approached thoughtfully.

In the first years of life, benzylpenicillin is used in case of sepsis, pneumonia, meningitis, otitis media. For treatment respiratory infections, sore throats, bronchitis and sinusitis, the safest antibiotics from the list are selected: Amoxicillin, Augmentin, Amoxiclav.

The body of a child is much more sensitive to drugs than that of an adult. Therefore, you should carefully monitor the condition of the baby (penicillin is excreted slowly and, accumulating, can cause convulsions), and also take preventive measures. The latter include the use of pre- and probiotics to protect the intestinal microflora, diet and comprehensive strengthening of immunity.

A little theory:

Historical information

The discovery that made a real revolution in medicine at the beginning of the 20th century was made by accident. I must say that the antibacterial properties of mold fungi were noticed by people in ancient times.

Alexander Fleming - discoverer of penicillin

The Egyptians, for example, even 2500 years ago treated inflamed wounds with compresses from moldy bread, but scientists took up the theoretical side of the issue only in the 19th century. European and Russian researchers and doctors, studying antibiosis (the property of some microorganisms to destroy others), made attempts to derive practical benefits from it.

Alexander Fleming, a British microbiologist, succeeded in this, who in 1928, on September 28, found mold in Petri dishes with staphylococcus colonies. Its spores, which fell on the crops due to the negligence of the laboratory staff, germinated and destroyed the pathogenic bacteria. Interested Fleming carefully studied this phenomenon and isolated a bactericidal substance called penicillin. For many years, the discoverer worked on obtaining a chemically pure stable compound suitable for treating people, but others invented it.

In 1941, Ernst Chain and Howard Flory were able to purify penicillin from impurities and conducted clinical trials with Fleming. The results were so successful that by the year 1943, the United States organized mass production of the drug, which saved many hundreds of thousands of lives during the war. The merits of Fleming, Cheyne and Flory before mankind were appreciated in 1945: the discoverer and developers became Nobel Prize winners.

Subsequently, the initial chemical preparation was constantly improved. This is how modern penicillins appeared, resistant to the acidic environment of the stomach, resistant to penicillinase and more effective in general.

Read a fascinating article: The Inventor of Antibiotics or the History of Mankind's Salvation!

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Mushrooms are the kingdom of living organisms. Mushrooms are different: some of them get into our diet, some cause skin diseases, some are so poisonous that they can cause death. But mushrooms of the genus Penicillium save millions of human lives from pathogenic bacteria.

Antibiotics of the penicillin series based on this mold (mold is also a fungus) are still used in medicine.

The discovery of penicillin and its properties

In the 30s of the last century, Alexander Fleming conducted experiments with staphylococci. He studied bacterial infections. After growing a group of these pathogens in a nutrient medium, the scientist noticed that there were areas in the cup that were not surrounded by live bacteria. The investigation showed that the usual green mold, which likes to settle on stale bread, is to blame for these spots. The mold was called Penicillium and, as it turned out, produced a substance that kills staphylococci.

Fleming went deeper into the subject and soon isolated pure penicillin, which became the world's first antibiotic. The principle of action of the drug is as follows: when a bacterial cell divides, each half restores its cell membrane with the help of a special chemical element, peptidoglycan. Penicillin blocks the formation of this element, and the bacterial cell simply "resolves" in the environment.

But difficulties soon arose. Bacteria cells learned to resist the drug - they began to produce an enzyme called "beta-lactamase", which destroys beta-lactams (the basis of penicillin).

The next 10 years there was an invisible war between pathogens that destroy penicillin, and scientists that modify this penicillin. So many modifications of penicillin were born, which now form the entire penicillin series of antibiotics.

Pharmacokinetics and principle of action

The drug for any kind of application spreads rapidly throughout the body, penetrating almost all its parts. Exceptions: cerebrospinal fluid, prostate gland and visual system. In these places, the concentration is very low, under normal conditions it does not exceed 1 percent. With inflammation, a rise of up to 5% is possible.

Antibiotics do not affect the cells of the human body, since the latter do not contain peptidoglycan.

The drug is quickly excreted from the body, after 1-3 hours most of it is excreted through the kidneys.

Watch a video on this topic

Classification of antibiotics

All drugs are divided into: natural (short and prolonged action) and semi-synthetic (anti-staphylococcal, broad-spectrum drugs, antipseudomonal).

Natural

These drugs obtained directly from the mold. At the moment, most of them are obsolete, as pathogens have become immune to them. In medicine, benzylpenicillin and Bicillin are most often used, which are effective against gram-positive bacteria and cocci, some anaerobic and spirochetes. All these antibiotics are used only in the form of injections into the muscles, since the acidic environment of the stomach quickly destroys them.

Benzylpenicillin in the form of sodium and potassium salts is a short-acting natural antibiotic. Its action stops after 3-4 hours, so frequent repeated injections are necessary.

Trying to eliminate this drawback, pharmacists have created natural long-acting antibiotics: Bicillin and novocaine salt of benzylpenicillin. These drugs are called "depot-forms", because after injection into the muscle they form a "depot" in it, from which the drug is slowly absorbed into the body.

Examples of drugs: benzylpenicillin salt (sodium, potassium or novocaine), Bicillin-1, Bicillin-3, Bicillin-5.

Semi-synthetic antibiotics of the penicillin group

Several decades after receiving penicillin pharmacists were able to isolate its main active ingredient, and the modification process began. Most drugs, after improvement, acquired resistance to the acidic environment of the stomach, and semi-synthetic penicillins began to be produced in tablets.

Isoxazolpenicillins are drugs that are effective against staphylococci. The latter have learned to produce an enzyme that destroys benzylpenicillin, and drugs from this group prevent the production of the enzyme. But you have to pay for the improvement - drugs of this type are less absorbed into the body and have a smaller spectrum of action compared to natural penicillins. Examples of drugs: Oxacillin, Nafcillin.

Aminopenicillins are broad-spectrum drugs. They are inferior to benzylpenicillins in terms of strength in the fight against gram-positive bacteria, but they capture a larger range of infections. Compared to other drugs, they stay in the body longer and better penetrate some of the body's barriers. Examples of drugs: Ampicillin, Amoxicillin. You can often find Ampiox - Ampicillin + Oxacillin.

Carboxypenicillins and ureidopenicillins antibiotics effective against Pseudomonas aeruginosa. At the moment, they are practically not used, since infections quickly acquire resistance to them. Occasionally, you can find them as part of a comprehensive treatment.

Examples of drugs: Ticarcillin, Piperacillin

List of drugs

Pills

Sumamed

Active ingredient: azithromycin.

Indications: Respiratory infections.

Contraindications: intolerance, severe renal failure, childhood up to 6 months.

Price: 300-500 rubles.

Oxacillin

Active ingredient: oxacillin.

Indications: infections sensitive to the drug.

Price: 30-60 rubles.

Amoxicillin Sandoz

Indications: respiratory tract infections (including tonsillitis, bronchitis), urinary tract infections, skin infections, other infections.

Contraindications: intolerance, children under 3 years of age.

Price: 150 rubles.

Ampicillin trihydrate

Indications: pneumonia, bronchitis, tonsillitis, other infections.

Contraindications: hypersensitivity, liver failure.

Price: 24 rubles.

Phenoxymethylpenicillin

Active ingredient: phenoxymethylpenicillin.

Indications: streptococcal diseases, infections of mild and moderate severity.

Price: 7 rubles.

Amoxiclav

Active ingredient: amoxicillin + clavulanic acid.

Indications: infections of the respiratory tract, urinary system, infections in gynecology, other infections sensitive to amoxicillin.

Contraindications: hypersensitivity, jaundice, mononucleosis and lymphocytic leukemia.

Price: 116 rubles.

injections

Bicillin-1

Active ingredient: benzathine benzylpenicillin.

Indications: acute tonsillitis, scarlet fever, wound infections, erysipelas, syphilis, leishmaniasis.

Contraindications: hypersensitivity.

Price: 15 rubles per injection.

Ospamox

Active ingredient: amoxicillin.

Indications: infections of the lower and upper respiratory tract, gastrointestinal tract, genitourinary system, gynecological and surgical infections.

Contraindications: hypersensitivity, severe gastrointestinal infections, lymphocytic leukemia, mononucleosis.

Price: 65 rubles.

Ampicillin

Active ingredient: ampicillin.

Indications: infections of the respiratory and urinary tract, gastrointestinal tract, meningitis, endocarditis, sepsis, whooping cough.

Contraindications: hypersensitivity, impaired renal function, childhood, pregnancy.

Price: 163 rubles.

Benzylpenicillin

Indications: severe infections, congenital syphilis, abscesses, pneumonia, erysipelas, anthrax, tetanus.

Contraindications: intolerance.

Price: 2.8 rubles per injection.

Benzylpenicillin novocaine salt

Active ingredient: benzylpenicillin.

Indications: Similar to benzylpenicillin.

Contraindications: intolerance.

Price: 43 rubles for 10 injections.

For the treatment of children, Amoxiclav, Ospamox, Oxacillin are suitable. But Before using the medicine, you must always consult with your doctor to adjust the dose.

Indications for use

Antibiotics of the penicillin group are prescribed for infections, the type of antibiotics is selected based on the type of infection. It can be various cocci, bacilli, anaerobic bacteria, and so on.

Most often, antibiotics treat infections of the respiratory tract and genitourinary system.

Application features

In the case of treating children, you need to follow the instructions of the doctor, who will prescribe the desired antibiotic and adjust the dose.

In case of pregnancy, antibiotics should be used with extreme caution, as they penetrate the fetus. During lactation, it is better to switch to mixtures, as the medicine also penetrates into milk.

Not for the elderly special instructions, although the doctor should take into account the condition of the patient's kidneys and liver when prescribing treatment.

Contraindications and side effects

The main and often the only contraindication is individual intolerance. It occurs frequently - in about 10% of patients. Additional contraindications depend on the specific antibiotic and are prescribed in the instructions for use.

List of side effects

The development of allergies, from itching and fever to anaphylactic shock and coma.
Instantaneous development of an allergic reaction in response to the introduction of the drug into a vein.
Dysbacteriosis, candidiasis.

In case of appearance side effects need to contact immediately medical care, stop the drug and carry out symptomatic treatment.

FAQ

Where does penicillin mold grow?

Almost everywhere. This mold includes dozens of subspecies, and each of them has its own habitat. The most notable are the penicillin mold that grows on bread (which also infects apples, causing them to rot quickly) and the mold used in the production of some cheeses.

How to replace penicillin antibiotics?

If the patient is allergic to penicillin, non-penicillin antibiotics can be used. Names of drugs: Cefadroxil, Cefalexin, Azithromycin. The most popular option is Erythromycin. But you need to know that Erythromycin often causes dysbacteriosis and indigestion.

Antibiotics from the penicillin series - strong remedy against infections caused by various bacteria. There are quite a few of them, and treatment must be selected in accordance with the type of pathogen.

They seem harmless to the body due to the fact that the only contraindication is a hypersensitivity reaction, but improper treatment or self-medication can provoke resistance of the pathogen to the antibiotic, and you will have to select another treatment that is more dangerous and less effective.

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Antibiotics of the penicillin group are the first drugs created from the waste products of certain types of bacteria. IN general classification Penicillin antibiotics belong to the beta-lactam class of drugs. In addition to them, non-penicillin antibiotics are also included here: monobactams, cephalosporins and carbapenems.

The similarity is due to the fact that these drugs contain four-membered ring. All antibiotics of this group are used in chemotherapy and play an important role in the treatment of infectious diseases.

Properties of penicillin and its discovery

Before the discovery of antibiotics, many diseases seemed simply incurable, scientists and doctors around the world wanted to find a substance that could help defeat pathogenic microorganisms, while not causing damage to human health. People died from sepsis, wounds infected with bacteria, gonorrhea, tuberculosis, pneumonia and other dangerous and serious diseases.

A key moment in medical history is 1928 It was in this year that penicillin was discovered. Millions of human lives for this discovery are due to Sir Alexander Fleming. The accidental appearance of mold on the nutrient medium of the Penicillium notatum group in Fleming's laboratory and the observation of the scientist himself gave a chance to fight against infectious diseases.

After the discovery of penicillin, scientists faced only one task - to isolate this substance in its pure form. This case turned out to be quite complicated, but in the late 30s of the 20th century, two scientists Ernst Cheyne and Howard Flory managed to create a drug with an antibacterial effect.

Properties of antibiotics of the penicillin group

antibiotic penicillin inhibits the emergence and development pathogenic organisms such as:

meningococci;
gonococci;
streptococci;
staphylococci;
tetanus stick;
pneumococci;
anthrax;
botulism stick;
diphtheria bacillus, etc.

This is only a small list of those pathogenic bacteria in which penicillin and all penicillin preparations suppress vital activity.

The antibiotic effect of penicillin is bactericidal or bacteriostatic. In the latter case, we are talking about the complete destruction of pathogenic organisms that caused the disease, most often acute and extremely severe. For diseases of moderate severity, antibiotics with a bacteriostatic effect are used - they do not allow bacteria to divide.

Penicillin is an antibiotic with a bactericidal effect. Microbes in their structure have a cell wall in which the main substance is peptidoglycan. This substance gives the bacterial cell stability, preventing it from dying even in very unsuitable conditions for life. By acting on the cell wall, penicillin destroys its integrity and disables its work.

In the human body, cell membranes do not contain peptidoglycan and therefore antibiotics of the penicillin group do not have a negative effect on our body. Also, we can talk about a small toxicity of these funds.

Penicillins have a wide range of dosages used, which is safer for the human body, since it makes it possible for a particular patient to choose a therapeutic dosage with minimal side effects.

The main part of penicillin is excreted from the body by the kidneys with urine (more than 70%). Some antibiotics of the penicillin group are excreted using the biliary system, that is, they are excreted with bile.

List of drugs and classification of penicillins

The basis of the chemical compound of the penicillin group is beta-lactam ring, therefore they belong to beta-lactama drugs.

Since penicillin has been used in medical practice for more than 80 years, some microorganisms have developed resistance to this antibiotic in the form of the beta-lactamase enzyme. The mechanism of the enzyme's work consists in the connection of the hydrolytic enzyme of a pathogenic bacterium with the beta-lactam ring, which, in turn, facilitates their binding, and as a result, the inactivation of the drug.

To date, semi-synthetic antibiotics are most often used: it is taken as a basis chemical composition natural antibiotic and undergoes useful modifications. Due to this, humanity can still resist various bacteria that constantly produce different antibiotic resistance mechanisms.

To date, the Federal Guidelines for the Use of Medicinal Products provides such a classification of penicillins.

Short acting natural antibiotics

Natural antibiotics do not contain beta-lactamase inhibitors, so they are never used against diseases caused by staphylococcus aureus.

Benzylpenicillin is active during treatment:

lobar pneumonia;
anthrax;
bronchitis;
pleurisy;
peritonitis;
sepsis;
diseases of the genitourinary system;
meningitis (in adults and in children from 2 years old);
skin infections;
wound infections;
ENT diseases.

Side effects: for all antibiotics of the penicillin series, the main side effect is an allergic response of the body in the form of urticaria, anaphylactic shock, hyperthermia, Quincke's edema, skin rashes, nephritis. Possible failures in the work of the heart. During the introduction of significant dosages - convulsions (in children).

Restrictions on use and contraindications: hay fever, allergy to penicillin, impaired kidney function, arrhythmia, bronchial asthma.

Natural antibiotics with prolonged action

Benzylpenicillin benzathine is used in cases of:

inflammation of the tonsils;
syphilis;
wound infections;
scarlet fever.

It is also used to prevent complications after surgery.

Side effects: anemia, allergic response, abscess at the injection site of the antibiotic, headache, thrombocytopenia and leukopenia.

Contraindications: hay fever, bronchial asthma, propensity to allergies to penicillin.

Benzylpenicillin procaine is used in the treatment of:

septic endocarditis,
acute inflammatory diseases of the respiratory organs;
osteomyelitis;
meningitis;
processes of inflammation of the biliary and urinary tract;
peritonitis;
eye diseases;
dermatoses;
wound infections.

It is used for relapses of erysipelas and rheumatism.

Side effect: convulsions, nausea, allergic reaction.

Contraindications: hypersensitivity to procaine and penicillin.

Antistaphylococcal agents

Oxacillin is the main representative of this group of antibiotics. The result of treatment is similar to benzylpenicillin, but unlike the second, this drug can destroy staphylococcal infections.

Side effects: skin rashes, urticaria. Rarely - anaphylactic shock, edema, fever, digestive disorders, vomiting, nausea, hematuria (in children), jaundice.

Contraindications: allergic reactions to penicillin.

Broad spectrum drugs

As an active substance, ampicillin is used in many antibiotics. Used to treat acute infections of the urinary and respiratory tract, infectious diseases digestive system, chlamydial infections, endocarditis, meningitis.

List of antibiotics that contain ampicillin: Ampicillin sodium salt, Ampicillin trihydrate, Ampicillin-Inotec, Ampicillin AMP-Forte, Ampicillin-AKOS, etc.

Amoxicillin is modified derivative of ampicillin. It is considered the main antibiotic, which is taken orally only. Used for meningococcal infections, acute respiratory diseases, Lyme disease, processes of inflammation of the gastrointestinal tract. It is used to prevent anthrax in women during pregnancy and children.

List of antibiotics that contain amoxicillin: Amoxicillin Sandoz, Amoxicar, Amoxicillin DS, Amoxicillin-ratiopharm, etc.

Side effects: dysbacteriosis, dyspeptic disorders, allergies, candidiasis, superinfection, CNS disorders.

Contraindications for this group of penicillins: hypersensitivity, mononucleosis, impaired liver function. Ampicillin is prohibited for newborns up to one month.

Antipseudomonal antibiotics

Carboxypenicillins contain active ingredient - carbenicillin. In this case, the name of the antibiotic is the same as the active ingredient. It is used in the treatment of diseases that are caused by Pseudomonas aeruginosa. Today, they are almost never used in medicine due to the availability of more powerful drugs.

Ureidopenicillins include: Azlocillin, Piperacillin, Mezlocillin.

Side effect: nausea, eating disorders, urticaria, vomiting. Possible headache, drug-induced fever, superinfection, impaired renal function.

Contraindications: pregnancy, high sensitivity to penicillin.

Features of the use of antibiotics of the penicillin group in children

The use of antibiotics in pediatric treatment much attention is constantly paid, since the child's body has not yet fully formed and most of the organs and systems still not fully functional. Therefore, the choice of antibiotics for infants and growing children, doctors must be treated with great responsibility.

Penicillin in newborns is used for toxic diseases and sepsis. In the first years of life in children, it is used to treat otitis, pneumonia, meningitis, pleurisy.

With angina, SARS, cystitis, bronchitis, sinusitis, as a rule, children are prescribed Flemoxin, Amoxicillin, Augmentin, Amoxiclav. These antibiotics in relation to the child's body are the least toxic and the most effective.

Dysbacteriosis is one of the complications of antibiotic therapy, since beneficial microflora in children dies simultaneously with pathogenic microorganisms. Therefore, antibiotic treatment must be combined with the intake of probiotics. A rare side effect is an allergy to penicillin. in the form of a skin rash.

In infants, the excretory work of the kidneys is not sufficiently developed and the accumulation of penicillin is likely in the body. The result of this is the appearance of seizures.

Treatment with any antibiotics, even the latest generation, always has a significant impact on health. Naturally, from the main infectious disease they relieve, however, overall immunity is also significantly reduced. Since not only pathogenic bacteria die, but also healthy microflora. Therefore, it will take some time to restore the protective forces. If side effects are pronounced, especially those associated with the gastrointestinal tract, then a sparing diet is necessary.

Be sure to use probiotics and prebiotics (Bifidumbacterin, Linex, Bifiform, Acipol, etc.). The start of reception must occur simultaneously with the start of use antibacterial agent. At the same time, after a course of antibiotics, prebiotics and probiotics must be used for about 14 more days to populate the stomach with beneficial bacteria.

When antibiotics have a toxic effect on the liver, the use of hepatoprotectors can be recommended. These drugs will protect healthy liver cells and repair damaged ones.

Since immunity is reduced, the body is particularly susceptible to colds. Therefore, you need to take care of yourself and not overcool. Use immunomodulators, while it is desirable that they be of plant origin (purple Echinacea, Immunal).

If the disease is of viral etiology, then in this case antibiotics are powerless, even the latest generation and a wide spectrum of action. They can only serve as a prophylaxis in joining a bacterial viral infection. Antivirals are used to treat viruses.

In order to reduce the use of antibiotics and get sick less often, it is necessary to healthy lifestyle life. The most important thing is not to overdo it with the use of antibacterial agents in order to prevent the development of bacterial resistance to them. Otherwise, it will not be possible to cure any infection. Therefore, always consult your doctor before using any antibiotic.

Antibiotics of the penicillin series are several types of drugs that are divided into groups. In medicine, drugs are used to treat various diseases infectious and bacterial origin. The drugs have a minimum number of contraindications and are still used to treat various patients.

Discovery history

Once Alexander Fleming in his laboratory was engaged in the study of pathogens. He created a nutrient medium and grew staphylococcus aureus. The scientist was not particularly clean, he simply put beakers and cones in the sink and forgot to wash them.

When Fleming needed the dishes again, he found that they were covered with fungus - mold. The scientist decided to test his conjecture and examined one of the containers under a microscope. He noticed that where there is mold, there is no staphylococcus aureus.

Alexander Fleming continued his research, he began to study the effect of mold on pathogenic microorganisms and found that the fungus has a destructive effect on the membranes of bacteria and leads to their death. The public could not be skeptical about the research.

The discovery helped save many lives. Saved humanity from those diseases that previously caused panic among the population. Naturally, modern medicines have a relative similarity with those drugs that were used in late XIX century. But the essence of medicines, their action has not changed so dramatically.

Penicillin antibiotics were able to revolutionize medicine. But the joy of discovery did not last long. It turned out that pathogenic microorganisms, bacteria can mutate. They mutate and become insensitive to drugs. As a result, penicillin-type antibiotics have undergone significant changes.

For almost the entire 20th century, scientists have been "fighting" against microorganisms and bacteria, trying to create the perfect drug. Efforts were not in vain, but such improvements have led to the fact that antibiotics have changed significantly.

New generation drugs are more expensive, act faster, have a number of contraindications. If we talk about those preparations that were obtained from mold, then they have a number of disadvantages:

Badly digested. Gastric juice acts on the fungus in a special way, reduces its effectiveness, which undoubtedly affects the result of treatment.
Penicillin antibiotics are drugs of natural origin, for this reason they do not differ in a wide spectrum of action.
Medicines are quickly excreted from the body, approximately 3-4 hours after injection.

Important: There are practically no contraindications for such medicines. It is not recommended to take them in the presence of individual intolerance to antibiotics, as well as in the event of an allergic reaction.

Modern antibacterial agents are significantly different from penicillin, which is familiar to many. In addition to the fact that today you can easily buy medicines of this class in tablets, there are a great many varieties of them. Classification, the generally accepted division into groups, will help to understand the preparations.

Antibiotics: classification

Antibiotics of the penicillin group are conditionally divided into:

Natural.
Semi-synthetic.

All medicines based on mold are antibiotics of natural origin. Today, such medicines are practically not used in medicine. The reason is that pathogenic microorganisms have become immune to them. That is, the antibiotic does not act on bacteria in the proper way, to achieve the desired result in the treatment is obtained only with the introduction of a high dose of the drug. The means of this group include: Benzylpenicillin and Bicillin.

The drugs are available in the form of a powder for injection. They effectively affect: anaerobic microorganisms, gram-positive bacteria, cocci, etc. since medicines are of natural origin, they cannot boast of a long-term effect, injections are often done every 3-4 hours. This allows not to reduce the concentration of the antibacterial agent in the blood.

Penicillin antibiotics of semi-synthetic origin are the result of modification of preparations made from a mold fungus. Medicines belonging to this group managed to give some properties, first of all, they became insensitive to the acid-base environment. That allowed to produce antibiotics in tablets.

And also there were medicines that acted on staphylococci. This class of drugs is different from natural antibiotics. But the improvements have had a significant impact on the quality of drugs. They are poorly absorbed, have a not so wide sector of action, and have contraindications.

Semi-synthetic drugs can be divided into:

Isoxazolpenicillins are a group of drugs that act on staphylococci, examples include the names the following drugs: Oxacillin, Nafcillin.
Aminopenicillins - several drugs belong to this group. They differ in a wide sector of action, but are significantly inferior in strength to antibiotics of natural origin. But they can fight a large number of infections. Means from this group remain in the blood longer. Such antibiotics are often used to treat various diseases, for example, 2 very well-known drugs can be given: Ampicillin and Amoxicillin.

Attention! The list of medicines is quite large, they have a number of indications and contraindications. For this reason, before starting antibiotics, you should consult a doctor.

Indications and contraindications for taking drugs

Antibiotics belonging to penicillin group are appointed by the doctor. Drugs are recommended to be taken in the presence of:

Diseases of an infectious or bacterial nature (pneumonia, meningitis, etc.).
Respiratory tract infections.
Diseases of the inflammatory and bacterial nature of the genitourinary system (pyelonephritis).
Skin diseases of various origins (erysipelas, caused by staphylococcus aureus).
Intestinal infections and many other diseases of an infectious, bacterial or inflammatory nature.

Reference: Antibiotics are prescribed for extensive burns and deep wounds, gunshot or stab wounds.

In some cases, taking medication can save a person's life. But you should not prescribe yourself such drugs yourself, as this can lead to the development of addiction.

What are the contraindications for drugs:

Do not take medication during pregnancy or lactation. Drugs can affect the growth and development of the child. Able to change the quality of milk and its taste characteristics. There are a number of drugs that are conditionally approved for the treatment of pregnant women, but a doctor must prescribe such an antibiotic. Since only a doctor can determine the acceptable dosage and duration of treatment.
It is not recommended to use antibiotics from the groups of natural and synthetic penicillins for the treatment of children. Drugs in these classes can have a toxic effect on the child's body. For this reason, medications are prescribed with caution, determining the optimal dosage.
You should not use medications without visible indications. Use drugs for a long period of time.

Direct contraindications for the use of antibiotics:

Individual intolerance to drugs of this class.
Tendency to allergic reactions of various kinds.

Attention! The main side effect of taking medications is considered prolonged diarrhea and candidiasis. They are due to the fact that drugs affect not only pathogens, but also beneficial microflora.

The penicillin series of antibiotics is characterized by the presence of a small number of contraindications. For this reason, drugs in this class are prescribed very often. They help to quickly cope with the disease and return to a normal rhythm of life.

Medicines of the latest generation have a wide spectrum of action. Such antibiotics do not have to be taken for a long time, they are well absorbed and, with adequate therapy, can “put a person on their feet” in 3-5 days.

List of drugs that doctors prescribe to patients

The question is which antibiotics are best? can be considered rhetorical. There are a number of drugs that doctors, for one reason or another, prescribe more often than others. In most cases, the names of drugs are well known to the general public. But still it is worth studying the list of drugs:

Sumamed is a drug used to treat infectious diseases of the upper respiratory tract. The active ingredient is erythromycin. The drug is not used to treat patients with acute or chronic renal failure, is not prescribed for children under 6 months of age. The main contraindication to the use of Sumamed should still be considered an individual intolerance to the antibiotic.
Oxacillin - available in powder form. The powder is diluted, and then the solution is used for intramuscular injections. The main indication for the use of the drug should be considered infections that are sensitive to this drug. Hypersensitivity should be considered a contraindication to the use of Oxacillin.
Amoxicillin belongs to a number of synthetic antibiotics. The drug is quite well-known, it is prescribed for sore throat, bronchitis and other respiratory tract infections. Amoxicillin can be taken for pyelonephritis (inflammation of the kidneys) and other diseases of the genitourinary system. The antibiotic is not prescribed to children under 3 years of age. A direct contraindication is also considered intolerance to the drug.
Ampicillin - the full name of the drug: Ampicillin trihydrate. An indication for the use of the drug should be considered infectious diseases of the respiratory tract (tonsillitis, bronchitis, pneumonia). The antibiotic is excreted from the body by the kidneys and liver, for this reason Ampicillin is not prescribed to people with acute liver failure. Can be used to treat children.
Amoxiclav is a drug that has a combined composition. It belongs to the latest generation of antibiotics. Amoxiclav is used to treat infectious diseases of the respiratory system, the genitourinary system. It is also used in gynecology. A contraindication to the use of the drug should be considered hypersensitivity, jaundice, mononucleosis, etc.

List or list of antibiotics of the penicillin series, which is available in powder form:

Benzylpenicillin novocaine salt is an antibiotic of natural origin. Indications for the use of the drug can be considered severe infectious diseases, including congenital syphilis, abscesses various etiologies, tetanus, anthrax and pneumonia. The drug has practically no contraindications, but in modern medicine it is used extremely rarely.
Ampicillin - used to treat the following infectious diseases: sepsis (blood poisoning), whooping cough, endocarditis, meningitis, pneumonia, bronchitis. Ampicillin is not used to treat children, people with severe renal insufficiency. Pregnancy can also be considered a direct contraindication to the use of this antibiotic.
Ospamox is prescribed for the treatment of diseases of the genitourinary system, infections of a gynecological and other nature. It is prescribed in the postoperative period, if there is a high risk of developing inflammatory process. Antibiotics are not prescribed for severe infectious diseases Gastrointestinal tract, in the presence of individual intolerance to the drug.

Important: Called an antibiotic, the drug should have an antibacterial effect on the body. All those medicines that affect viruses have nothing to do with antibiotics.

Prices for medicines

Sumamed - the cost varies from 300 to 500 rubles.

Amoxicillin tablets - the price is about 159 rubles. for packing.

Ampicillin trihydrate - the cost of tablets is 20–30 rubles.

Ampicillin in the form of a powder intended for injection - 170 rubles.

Oxacillin - the average price of the drug varies from 40 to 60 rubles.

Amoxiclav - cost-120 rubles.

Ospamox - the price varies from 65 to 100 rubles.

Benzylpenicillin novocaine salt - 50 rubles.

Benzylpenicillin - 30 rubles.

Antibiotics for a child

Preparations based on penicillin (mold fungus) for the treatment of children are used only if indicated.

Most often, doctors prescribe to small patients:

Amoxiclav can be prescribed to a newborn child, as well as an infant under the age of 3 months. The dosage is calculated according to the scheme, based on the condition of the child, his weight and the severity of the symptoms.
Oxacillin - the drug is taken under the supervision of a doctor, it can be prescribed to a newborn if indicated. Antibacterial therapy is carried out under the supervision of a physician.
Ospamox - the doctor calculates the dosage for children. It is determined according to the scheme (30-60 mg is divided per kg of weight and the number of doses per day).

Carefully! Conducting antibiotic therapy in children has its own nuances. For this reason, you should not independently prescribe such medicines to a child. There is a risk of making a mistake with the dosage and causing serious harm to the health of the baby.

Antibiotics related to penicillins are quite effective. They were discovered at the end of the 19th century and have found wide application in medicine. Despite the fact that pathogenic microorganisms often mutate, drugs of this class are still in demand.

Mushrooms are the kingdom of living organisms. Mushrooms are different: some of them get into our diet, some cause skin diseases, some are so poisonous that they can lead to death. But mushrooms of the genus Penicillium save millions of human lives from pathogenic bacteria.

Antibiotics of the penicillin series based on this mold (mold is also a fungus) are still used in medicine.

But difficulties soon arose. Bacteria cells learned to resist the drug - they began to produce an enzyme called "beta-lactamase", which destroys beta-lactams (the basis of penicillin).

Antibiotics do not affect the cells of the human body, since the latter do not contain peptidoglycan.

The drug is quickly excreted from the body, after 1-3 hours most of it is excreted through the kidneys.

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All drugs are divided into: natural (short and prolonged action) and semi-synthetic (anti-staphylococcal, broad-spectrum drugs, antipseudomonal).

Benzylpenicillin in the form of sodium and potassium salts is a short-acting natural antibiotic. Its action stops after 3-4 hours, so frequent repeated injections are necessary.

Examples of drugs: benzylpenicillin salt (sodium, potassium or novocaine), Bicillin-1, Bicillin-3, Bicillin-5.

Examples of drugs: Ticarcillin, Piperacillin

Sumamed

Active ingredient: azithromycin.

Indications: Respiratory infections.

Contraindications: intolerance, severe renal failure, children under 6 months of age.

Price: 300-500 rubles.

Oxacillin

Active ingredient: oxacillin.

Indications: infections sensitive to the drug.

Price: 30-60 rubles.

Amoxicillin Sandoz

Indications: respiratory tract infections (including tonsillitis, bronchitis), urinary tract infections, skin infections, other infections.

Contraindications: intolerance, children under 3 years of age.

Price: 150 rubles.

Ampicillin trihydrate

Indications: pneumonia, bronchitis, tonsillitis, other infections.

Contraindications: hypersensitivity, liver failure.

Price: 24 rubles.

Phenoxymethylpenicillin

Active ingredient: phenoxymethylpenicillin.

Indications: streptococcal diseases, infections of mild and moderate severity.

Price: 7 rubles.

Amoxiclav

Active ingredient: amoxicillin + clavulanic acid.

Indications: infections of the respiratory tract, urinary system, infections in gynecology, other infections sensitive to amoxicillin.

Contraindications: hypersensitivity, jaundice, mononucleosis and lymphocytic leukemia.

Price: 116 rubles.

injections

Bicillin-1

Active ingredient: benzathine benzylpenicillin.

Indications: acute tonsillitis, scarlet fever, wound infections, erysipelas, syphilis, leishmaniasis.

Contraindications: hypersensitivity.

Price: 15 rubles per injection.

Ospamox

Active ingredient: amoxicillin.

Indications: infections of the lower and upper respiratory tract, gastrointestinal tract, genitourinary system, gynecological and surgical infections.

Contraindications: hypersensitivity, severe gastrointestinal infections, lymphocytic leukemia, mononucleosis.

Price: 65 rubles.

Ampicillin

Active ingredient: ampicillin.

Indications: infections of the respiratory and urinary tract, gastrointestinal tract, meningitis, endocarditis, sepsis, whooping cough.

Contraindications: hypersensitivity, impaired renal function, childhood, pregnancy.

Price: 163 rubles.

Benzylpenicillin

Indications: severe infections, congenital syphilis, abscesses, pneumonia, erysipelas, anthrax, tetanus.

Contraindications: intolerance.

Price: 2.8 rubles per injection.

Benzylpenicillin novocaine salt

Active ingredient: benzylpenicillin.

Indications: Similar to benzylpenicillin.

Contraindications: intolerance.

Price: 43 rubles for 10 injections.

For the treatment of children, Amoxiclav, Ospamox, Oxacillin are suitable. But Before using the medicine, you must always consult with your doctor to adjust the dose.

Indications for use

Antibiotics of the penicillin group are prescribed for infections, the type of antibiotics is selected based on the type of infection. It can be various cocci, bacilli, anaerobic bacteria, and so on.

Most often, antibiotics treat infections of the respiratory tract and genitourinary system.

In the case of treating children, you need to follow the instructions of the doctor, who will prescribe the desired antibiotic and adjust the dose.

In case of pregnancy, antibiotics should be used with extreme caution, as they penetrate the fetus. During lactation, it is better to switch to mixtures, as the medicine also penetrates into milk.

For the elderly, there are no special instructions, although the doctor should take into account the condition of the patient's kidneys and liver when prescribing treatment.

In case of side effects, you should immediately seek medical help, stop the drug and carry out symptomatic treatment.

Where does penicillin mold grow?

How to replace penicillin antibiotics?

Antibiotics from the penicillin series are a strong remedy against infections caused by various bacteria. There are quite a few of them, and treatment must be selected in accordance with the type of pathogen.

How to forget about pain in the joints and spine?

Does pain limit your movement and fulfilling life?
Are you worried about discomfort, crunching and systemic pain?
Perhaps you have tried a bunch of medicines, creams and ointments?
People who have learned bitter experience for the treatment of joints use ... >>

Read the opinion of doctors on this issue

Familiar today antibacterial drugs less than a century ago made a real revolution in medicine. Mankind has received a powerful weapon to fight infections that were previously considered fatal.

This section presents complete list current antimicrobial drugs. In addition to the characteristics of the main compounds, all trade names and analogues.

Main title	Antimicrobial activity	Analogues
Benzylpenicillin potassium and sodium salts	Influence mainly gram-positive microorganisms. Currently, most strains have developed resistance, but spirochetes are still sensitive to the substance.	Gramox-D, Ospen, Star-Pen, Ospamox
benzylpenicillin procaine	Indicated for the treatment of streptococcal and pneumococcal infections. Compared to potassium and sodium salts, it acts longer, as it dissolves and is absorbed more slowly from the intramuscular depot.	Benzylpenicillin-KMP (-G, -Teva, -G 3 mega)
Bicillins (1, 3 and 5)	It is used for chronic rheumatism with a prophylactic purpose, as well as for the treatment of infectious diseases of moderate and mild severity caused by streptococci.	Benzicillin-1, Moldamine, Extincillin, Retarpin
Phenoxymethylpenicillin	It has a therapeutic effect similar to the previous groups, but is not destroyed in an acidic gastric environment. Produced in the form of tablets.	V-Penicillin, Kliacil, Ospen, Penicillin-Fau, Vepicombin, Megacillin Oral, Pen-os, Star-Pen
Oxacillin	Active against staphylococci that produce penicillinase. It is characterized by low antimicrobial activity, it is completely ineffective against penicillin-resistant bacteria.	Oxamp, Ampiox, Oxamp-Sodium, Oxamsar
Ampicillin	Extended spectrum of antimicrobial activity. In addition to the main spectrum of inflammatory diseases of the gastrointestinal tract, it also treats those caused by Escherichia, Shigella, Salmonella.	Ampicillin AMP-KID (-AMP-Forte, -Ferein, -AKOS, -trihydrate, -Innotek), Zetsil, Pentrixil, Penodil, Standacillin
Amoxicillin	It is used to treat inflammation of the respiratory and urinary tract. After clarifying the bacterial origin of gastric ulcers, Helicobacter pylori is used for eradication.	Flemoxin solutab, Hikoncil, Amosin, Ospamox, Ecobol
Carbenicillin	The spectrum of antimicrobial action includes Pseudomonas aeruginosa and enterobacteria. The digestibility and bactericidal effect is higher than that of Carbenicillin.	Securopen
Piperacillin	Similar to the previous one, but the level of toxicity is increased.	Isipen, Pipracil, Picillin, Piprax
Amoxicillin/clavulanate	Due to the inhibitor, the spectrum of antimicrobial activity is expanded compared to the unprotected agent.	Augmentin, Flemoklav solutab, Amoxiclav, Amklav, Amovikomb, Verklav, Ranklav, Arlet, Klamosar, Rapiclav
Ampicillin/sulbactam		Sulacillin, Liboksil, Unazine, Sultasin
Ticarcillin/clavulanate	The main indication for use is nosocomial infections.	Gimentin
Piperacillin/tazobactam	The main indication for use is nosocomial infections.	Tazocin

The information provided is for informational purposes and is not a guide to action. All appointments are made exclusively by a doctor, and therapy is under his control.

Use for antibiotic therapy should be exactly the medication that was prescribed by a specialist. Independent attempts to find a cheap analogue and save money can lead to a deterioration in the condition.

For example, the dosage of the active substance in a generic may differ up or down, which will negatively affect the course of treatment.

When you have to replace the medicine due to an acute lack of finances, you need to ask the doctor about it, since only a specialist can choose the best option.

Preparations of the penicillin group belong to the so-called beta-lactams - chemical compounds that have a beta-lactam ring in their formula.

Medications based on the waste products of mold fungi are widely used in all areas of medicine due to the following properties:

High bioavailability - drugs are quickly absorbed and distributed through the tissues. The weakening of the blood-brain barrier during inflammation of the meninges also contributes to the penetration into the cerebrospinal fluid.
Broad spectrum of antimicrobial action. Unlike first-generation chemicals, modern penicillins are effective against the vast majority of gram-negative and positive bacteria. They are also resistant to penicillinase and the acidic environment of the stomach.
The lowest toxicity among all ABPs. They are allowed for use even during pregnancy, and the correct intake (as prescribed by the doctor and according to the instructions) almost completely eliminates the development of side effects.

In the process of research and experiments, many medications with different properties were obtained. For example, when belonging to the general series, penicillin and ampicillin are not the same thing. All penicillin antibiotics are well compatible with most other drugs. As for complex therapy with other types of antibacterial drugs, the combined use with bacteriostatics weakens the effectiveness of penicillins.

To date, penicillin antibiotics, a complete list of which is given below, are divided into 4 main groups.

Produced by the fungi Penicillium notatum and Penicillium chrysogenum, benzylpenicillin is an acid in molecular structure. For medical purposes, it combines chemically with sodium or potassium to form salts. The resulting compounds are used to prepare injection solutions that are rapidly absorbed.

The therapeutic effect is noted within 10-15 minutes after administration, but lasts no more than 4 hours, which requires frequent repeated injections into muscle tissue (in special cases, sodium salt can be administered intravenously).

See also: Instructions for the use of penicillin in injections and tablets

Natural benzylpenicillin is inactive against strains of staphylococcus that produce penicillinase (this enzyme destroys the beta-lactam ring of the active substance).

This includes two subgroups of antimicrobials intended for oral use and having a bactericidal effect against most pathogens (both gram+ and gram-).

However, in combination with oxacillin (Ampioks) they become resistant.

According to the degree of efficiency are divided into:

Carboxypenicillins, the clinical significance of which has recently been declining. Carbenicillin, the first of this subgroup, is also effective against ampicillin-resistant Proteus. Currently, almost all strains are resistant to carboxypenicillins.
Ureidopenicillins are more effective against Pseudomonas aeruginosa, and can also be prescribed for inflammation caused by Klebsiella. The most effective are Piperacillin and Azlocillin, of which only the latter remains relevant in medical practice.

To date, the vast majority of strains of Pseudomonas aeruginosa are resistant to carboxypenicillins and ureidopenicillins. For this reason, their clinical significance is reduced.

Inhibitor-protected drugs successfully treat severe nosocomial infections, strains of which are resistant to most drugs.

See also: About the modern classification of antibiotics by group of parameters

Inhibitor-protected agents treat even particularly dangerous and persistent nosocomial infections.

Inflammation of the intestines caused by pathogenic microflora responds well to therapy with acid-resistant drugs.

Of particular importance are aminopenicillins, which are part of the complex eradication of Helicobacter.

In obstetric and gynecological practice, many penicillin preparations from the list are used both to treat bacterial infections of the female reproductive system and to prevent infection in newborns.

Here, penicillin antibiotics also occupy a worthy place: keratitis, abscesses, gonococcal conjunctivitis and other eye diseases are treated with eye drops, ointments and injection solutions.

Treatment with antibacterial medications in general and penicillins in particular should be carried out only on prescription. Despite the minimal toxicity of the drug itself, its improper use seriously harms the body. In order for antibiotic therapy to lead to recovery, you should follow medical recommendations and know the characteristics of the drug.

Gram-positive bacteria - gonococci and meningococci;
Gram-negative - various staphylococci, streptococci and pneumococci, diphtheria, Pseudomonas aeruginosa and anthrax, Proteus;
Actinomycetes and spirochetes.

Low toxicity and a broad spectrum of action make antibiotics of the penicillin group the best treatment for tonsillitis, pneumonia (both focal and croupous), scarlet fever, diphtheria, meningitis, blood poisoning, septicemia, pleurisy, pyemia, osteomyelitis in acute and chronic forms, septic endocarditis, various purulent infections of the skin, mucous membranes and soft tissues, erysipelas, anthrax, gonorrhea, actinomycosis, syphilis, blennorrhea, as well as eye diseases and ENT diseases.

Strict contraindications include only individual intolerance to benzylpenicillin and other drugs in this group. Also, endolumbar (injection into the spinal cord) administration of drugs to patients with diagnosed epilepsy is not allowed.

Among other antibacterial agents, penicillins are favorably distinguished by their low toxicity.

Undesirable effects of use include:

Allergic reactions. Most often manifested by skin rash, itching, urticaria, fever and swelling. Extremely rarely, in severe cases, anaphylactic shock is possible, requiring the immediate administration of an antidote (adrenaline).
Dysbacteriosis. Imbalance of the natural microflora leads to digestive disorders (flatulence, bloating, constipation, diarrhea, abdominal pain) and the development of candidiasis. In the latter case, the mucous membranes of the oral cavity (in children) or the vagina are affected.
neurotoxic reactions. The negative effect of penicillin on the central nervous system is manifested by increased reflex excitability, nausea and vomiting, convulsions, and sometimes coma.

For children, tablets and injections should be prescribed carefully, given the possible negative reaction, and the choice of a particular drug should be approached thoughtfully.

In the first years of life, benzylpenicillin is used in case of sepsis, pneumonia, meningitis, otitis media. For the treatment of respiratory infections, tonsillitis, bronchitis and sinusitis, the safest antibiotics from the list are selected: Amoxicillin, Augmentin, Amoxiclav.

The body of a child is much more sensitive to drugs than that of an adult. Therefore, you should carefully monitor the condition of the baby (penicillin is excreted slowly and, accumulating, can cause convulsions), as well as take preventive measures. The latter include the use of pre- and probiotics to protect the intestinal microflora, diet and comprehensive strengthening of immunity.

A little theory:

Alexander Fleming - discoverer of penicillin

Read a fascinating article: The Inventor of Antibiotics or the History of Mankind's Salvation!

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Antibiotics of the penicillin series are several types of drugs that are divided into groups. In medicine, funds are used to treat various diseases of infectious and bacterial origin. The drugs have a minimum number of contraindications and are still used to treat various patients.

The discovery helped save many lives. Saved humanity from those diseases that previously caused panic among the population. Naturally, modern medicines have a relative similarity with those drugs that were used at the end of the 19th century. But the essence of medicines, their action has not changed so dramatically.

New generation drugs are more expensive, act faster, have a number of contraindications. If we talk about those preparations that were obtained from mold, then they have a number of disadvantages:

Badly digested. Gastric juice acts on the fungus in a special way, reduces its effectiveness, which undoubtedly affects the result of treatment.
Penicillin antibiotics are drugs of natural origin, for this reason they do not differ in a wide spectrum of action.
Medicines are quickly excreted from the body, approximately 3-4 hours after injection.

Antibiotics of the penicillin group are conditionally divided into:

Natural.
Semi-synthetic.

Semi-synthetic drugs can be divided into:

Isoxazolpenicillins are a group of drugs that act on staphylococci, as an example, the names of the following drugs can be given: Oxacillin, Nafcillin.
Aminopenicillins - several drugs belong to this group. They differ in a wide sector of action, but are significantly inferior in strength to antibiotics of natural origin. But they can fight a large number of infections. Means from this group remain in the blood longer. Such antibiotics are often used to treat various diseases, for example, 2 very well-known drugs can be given: Ampicillin and Amoxicillin.

Attention! The list of medicines is quite large, they have a number of indications and contraindications. For this reason, before starting antibiotics, you should consult a doctor.

Antibiotics belonging to the penicillin group are prescribed by a doctor. Drugs are recommended to be taken in the presence of:

Diseases of an infectious or bacterial nature (pneumonia, meningitis, etc.).
Respiratory tract infections.
Diseases of the inflammatory and bacterial nature of the genitourinary system (pyelonephritis).
Skin diseases of various origins (erysipelas, caused by staphylococcus aureus).
Intestinal infections and many other diseases of an infectious, bacterial or inflammatory nature.

Reference: Antibiotics are prescribed for extensive burns and deep wounds, gunshot or stab wounds.

In some cases, taking medication can save a person's life. But you should not prescribe yourself such drugs yourself, as this can lead to the development of addiction.

What are the contraindications for drugs:

Do not take medication during pregnancy or lactation. Drugs can affect the growth and development of the child. Able to change the quality of milk and its taste characteristics. There are a number of drugs that are conditionally approved for the treatment of pregnant women, but a doctor must prescribe such an antibiotic. Since only a doctor can determine the acceptable dosage and duration of treatment.
It is not recommended to use antibiotics from the groups of natural and synthetic penicillins for the treatment of children. Drugs in these classes can have a toxic effect on the child's body. For this reason, medications are prescribed with caution, determining the optimal dosage.
You should not use medications without visible indications. Use drugs for a long period of time.

Direct contraindications for the use of antibiotics:

Individual intolerance to drugs of this class.
Tendency to allergic reactions of various kinds.

Attention! The main side effect of taking medications is considered prolonged diarrhea and candidiasis. They are due to the fact that drugs affect not only pathogens, but also beneficial microflora.

Sumamed is a drug used to treat infectious diseases of the upper respiratory tract. The active ingredient is erythromycin. The drug is not used to treat patients with acute or chronic renal failure, is not prescribed for children under 6 months of age. The main contraindication to the use of Sumamed should still be considered an individual intolerance to the antibiotic.
Oxacillin - available in powder form. The powder is diluted, and then the solution is used for intramuscular injections. The main indication for the use of the drug should be considered infections that are sensitive to this drug. Hypersensitivity should be considered a contraindication to the use of Oxacillin.
Amoxicillin belongs to a number of synthetic antibiotics. The drug is quite well-known, it is prescribed for sore throat, bronchitis and other respiratory tract infections. Amoxicillin can be taken for pyelonephritis (inflammation of the kidneys) and other diseases of the genitourinary system. The antibiotic is not prescribed to children under 3 years of age. A direct contraindication is also considered intolerance to the drug.
Ampicillin - the full name of the drug: Ampicillin trihydrate. An indication for the use of the drug should be considered infectious diseases of the respiratory tract (tonsillitis, bronchitis, pneumonia). The antibiotic is excreted from the body by the kidneys and liver, for this reason Ampicillin is not prescribed to people with acute liver failure. Can be used to treat children.
Amoxiclav is a drug that has a combined composition. It belongs to the latest generation of antibiotics. Amoxiclav is used to treat infectious diseases of the respiratory system, the genitourinary system. It is also used in gynecology. A contraindication to the use of the drug should be considered hypersensitivity, jaundice, mononucleosis, etc.

List or list of antibiotics of the penicillin series, which is available in powder form:

Benzylpenicillin novocaine salt is an antibiotic of natural origin. Indications for the use of the drug can be considered severe infectious diseases, including congenital syphilis, abscesses of various etiologies, tetanus, anthrax and pneumonia. The medicine has practically no contraindications, but in modern medicine it is used extremely rarely.
Ampicillin - used to treat the following infectious diseases: sepsis (blood poisoning), whooping cough, endocarditis, meningitis, pneumonia, bronchitis. Ampicillin is not used to treat children, people with severe renal insufficiency. Pregnancy can also be considered a direct contraindication to the use of this antibiotic.
Ospamox is prescribed for the treatment of diseases of the genitourinary system, infections of a gynecological and other nature. It is prescribed in the postoperative period, if the risk of developing an inflammatory process is high. The antibiotic is not prescribed for severe infectious diseases of the gastrointestinal tract, in the presence of individual intolerance to the drug.

Important: Called an antibiotic, the drug should have an antibacterial effect on the body. All those medicines that affect viruses have nothing to do with antibiotics.

Sumamed - the cost varies from 300 to 500 rubles.

Amoxicillin tablets - the price is about 159 rubles. for packing.

Ampicillin trihydrate - the cost of tablets is 20–30 rubles.

Ampicillin in the form of a powder intended for injection - 170 rubles.

Oxacillin - the average price of the drug varies from 40 to 60 rubles.

Amoxiclav - cost-120 rubles.

Ospamox - the price varies from 65 to 100 rubles.

Benzylpenicillin novocaine salt - 50 rubles.

Benzylpenicillin - 30 rubles.

Penicillins (penicillina)- a group of antibiotics produced by many types of molds of the genus penicillium, active against most gram-positive, as well as some gram-negative microorganisms (gonococci, meningococci and spirochetes). Penicillins belong to the so-called. beta-lactam antibiotics (beta-lactams).

Beta-lactams are a large group of antibiotics, which have in common the presence of a four-membered beta-lactam ring in the molecule structure. Beta-lactams include penicillins, cephalosporins, carbapenems, monobactams. Beta-lactams are the most numerous group of antimicrobial drugs used in clinical practice, which occupies a leading position in the treatment of most infectious diseases.

Historical information. In 1928, the English scientist A. Fleming, who worked at St. Mary`s Hospital in London, discovered the ability of a green mold filamentous fungus (Penicillium notatum) cause the death of staphylococci in cell culture. The active substance of the fungus, which has antibacterial activity, A. Fleming called penicillin. In 1940, in Oxford, a group of researchers led by H.W. Flory and E.B. Cheyna isolated in pure form significant amounts of the first penicillin from culture Penicillium notatum. In 1942, the outstanding domestic researcher Z.V. Yermolyeva received penicillin from a mushroom Penicillium crustosum. Since 1949, practically unlimited quantities of benzylpenicillin (penicillin G) have become available for clinical use.

The penicillin group includes natural compounds produced by various types of molds. Penicillium, and a number of semi-synthetic ones. Penicillins (like other beta-lactams) have a bactericidal effect on microorganisms.

The most common properties of penicillins include: low toxicity, a wide range of dosages, cross-allergy between all penicillins and partially cephalosporins and carbapenems.

Antibacterial effect beta-lactams is associated with their specific ability to disrupt the synthesis of the bacterial cell wall.

The cell wall of bacteria has a rigid structure, it gives the microorganisms their shape and protects them from destruction. It is based on a heteropolymer - peptidoglycan, consisting of polysaccharides and polypeptides. Its cross-linked mesh structure gives the cell wall strength. The composition of polysaccharides includes such amino sugars as N-acetylglucosamine, as well as N-acetylmuramic acid, which is found only in bacteria. Amino sugars are associated with short peptide chains, including some L- and D-amino acids. In gram-positive bacteria, the cell wall contains 50-100 layers of peptidoglycan, in gram-negative bacteria - 1-2 layers.

About 30 bacterial enzymes are involved in the process of peptidoglycan biosynthesis, this process consists of 3 stages. It is believed that penicillins disrupt the late stages of cell wall synthesis, preventing the formation of peptide bonds by inhibiting the transpeptidase enzyme. Transpeptidase is one of the penicillin-binding proteins that beta-lactam antibiotics interact with. In addition to transpeptidases, penicillin-binding proteins, enzymes involved in the final stages of bacterial cell wall formation, include carboxypeptidases and endopeptidases. They are present in all bacteria (for example, in Staphylococcus aureus there are 4 of them Escherichia coli- 7). Penicillins bind to these proteins with different speed with the formation of a covalent bond. In this case, inactivation of penicillin-binding proteins occurs, the strength of the bacterial cell wall is impaired, and the cells undergo lysis.

Pharmacokinetics. When taken orally, penicillins are absorbed and distributed throughout the body. Penicillins penetrate well into tissues and body fluids (synovial, pleural, pericardial, bile), where they quickly reach therapeutic concentrations. The exceptions are the cerebrospinal fluid, the internal environment of the eye and the secret of the prostate gland - here the concentrations of penicillins are low. The concentration of penicillins in the cerebrospinal fluid may be different depending on the conditions: normally - less than 1% of serum, with inflammation it can increase up to 5%. Therapeutic concentrations in the cerebrospinal fluid are created with meningitis and the administration of drugs in high doses. Penicillins are rapidly excreted from the body, mainly by the kidneys by glomerular filtration and tubular secretion. Their half-life is short (30-90 minutes), the concentration in the urine is high.

There are several classifications Drugs belonging to the group of penicillins: by molecular structure, by sources of production, by spectrum of activity, etc.

According to the classification presented by D.A. Kharkevich (2006), penicillins are classified as follows (the classification is based on a number of features, including differences in the ways of obtaining):

I. Preparations of penicillins obtained by biological synthesis (biosynthetic penicillins):

I.1. For parenteral administration (destroyed in the acidic environment of the stomach):

Short acting:

benzylpenicillin (sodium salt),

benzylpenicillin (potassium salt);

Long lasting:

benzylpenicillin (novocaine salt),

Bicillin-1,

Bicillin-5.

I.2.

phenoxymethylpenicillin (penicillin V).

II. Semi-synthetic penicillins

II.1. For parenteral and enteral administration (acid-resistant):

Penicillinase resistant:

oxacillin (sodium salt),

nafcillin;

Broad spectrum of action:

ampicillin,

amoxicillin.

II.2. For parenteral administration (destroyed in the acidic environment of the stomach)

Broad spectrum of action, including Pseudomonas aeruginosa:

carbenicillin (disodium salt),

ticarcillin,

azlocillin.

II.3. For enteral administration (acid-resistant):

carbenicillin (indanyl sodium),

carfecillin.

According to the classification of penicillins given by I.B. Mikhailov (2001), penicillins can be divided into 6 groups:

1. Natural penicillins (benzylpenicillins, bicillins, phenoxymethylpenicillin).

2. Isoxazolpenicillins (oxacillin, cloxacillin, flucloxacillin).

3. Amidinopenicillins (amdinocillin, pivamdinocillin, bacamdinocillin, acidocillin).

4. Aminopenicillins (ampicillin, amoxicillin, talampicillin, bacampicillin, pivampicillin).

5. Carboxypenicillins (carbenicillin, carfecillin, carindacillin, ticarcillin).

6. Ureidopenicillins (azlocillin, mezlocillin, piperacillin).

The source of receipt, the spectrum of action, as well as the combination with beta-lactamases, were taken into account when creating the classification given in the Federal Guide (formular system), edition VIII.

1. Natural:

benzylpenicillin (penicillin G),

phenoxymethylpenicillin (penicillin V),

benzathine benzylpenicillin,

benzylpenicillin procaine,

benzathine phenoxymethylpenicillin.

2. Antistaphylococcal:

oxacillin.

3. Extended spectrum (aminopenicillins):

ampicillin,

amoxicillin.

4. Active towards Pseudomonas aeruginosa:

Carboxypenicillins:

ticarcillin.

Ureidopenicillins:

azlocillin,

piperacillin.

5. Combined with beta-lactamase inhibitors (inhibitor-protected):

amoxicillin / clavulanate,

ampicillin/sulbactam,

ticarcillin/clavulanate.

Natural (natural) penicillins are narrow-spectrum antibiotics that affect Gram-positive bacteria and cocci. Biosynthetic penicillins are obtained from a culture medium on which certain mold strains are grown. (Penicillium). There are several varieties of natural penicillins, one of the most active and persistent of them is benzylpenicillin. In medical practice, benzylpenicillin is used in the form of various salts - sodium, potassium and novocaine.

All natural penicillins have similar antimicrobial activity. Natural penicillins are destroyed by beta-lactamases, therefore, they are ineffective for the treatment of staphylococcal infections, because. in most cases, staphylococci produce beta-lactamase. They are effective mainly against gram-positive microorganisms (incl. Streptococcus spp., including Streptococcus pneumoniae, Enterococcus spp.), Bacillus spp., Listeria monocytogenes, Erysipelothrix rhusiopathiae, Gram-negative cocci (Neisseria meningitidis, Neisseria gonorrhoeae), some anaerobes (Peptostreptococcus spp., Fusobacterium spp.), spirochete (Treponema spp., Borrelia spp., Leptospira spp.). Gram-negative organisms are usually resistant, except Haemophilus ducreyi And Pasteurella multocida. With regard to viruses (causative agents of influenza, poliomyelitis, smallpox, etc.), mycobacterium tuberculosis, the causative agent of amoebiasis, rickettsia, fungi, penicillins are ineffective.

Benzylpenicillin is active mainly against gram-positive cocci. The spectra of antibacterial action of benzylpenicillin and phenoxymethylpenicillin are almost identical. However, benzylpenicillin is 5-10 times more active than phenoxymethylpenicillin against sensitive Neisseria spp. and some anaerobes. Phenoxymethylpenicillin is prescribed for infections of moderate severity. The activity of penicillin preparations is determined biologically by the antibacterial effect on a specific strain. Staphylococcus aureus. The activity of 0.5988 μg of chemically pure crystalline sodium salt of benzylpenicillin is taken per unit of action (1 ED).

Significant disadvantages of benzylpenicillin are its instability to beta-lactamases (when the beta-lactam ring is enzymatically cleaved by beta-lactamases (penicillinases) with the formation of penicillanic acid, the antibiotic loses its antimicrobial activity), slight absorption in the stomach (necessitates injection routes of administration) and relatively low activity against most Gram-negative organisms.

Under normal conditions, benzylpenicillin preparations do not penetrate well into the cerebrospinal fluid, however, with inflammation of the meninges, the permeability through the BBB increases.

Benzylpenicillin, used in the form of highly soluble sodium and potassium salts, acts for a short time - 3-4 hours, because. is rapidly excreted from the body, and this requires frequent injections. In this regard, poorly soluble salts of benzylpenicillin (including novocaine salt) and benzathine benzylpenicillin have been proposed for use in medical practice.

Prolonged forms of benzylpenicillin, or depot-penicillins: Bicillin-1 (benzathine benzylpenicillin), as well as combined drugs based on them - Bicillin-3 (benzathine benzylpenicillin + benzylpenicillin sodium + benzylpenicillin novocaine salt), Bitsillin-5 (benzathine benzylpenicillin + benzylpenicillin novocaine salt) ), are suspensions that can only be administered intramuscularly. They are slowly absorbed from the injection site, creating a depot in muscle tissue. This allows you to maintain the concentration of the antibiotic in the blood for a significant time and thus reduce the frequency of drug administration.

All salts of benzylpenicillin are used parenterally, tk. they are destroyed in the acidic environment of the stomach. Of the natural penicillins, only phenoxymethylpenicillin (penicillin V) has acid-stable properties, although to a weak degree. Phenoxymethylpenicillin differs chemically from benzylpenicillin by the presence of a phenoxymethyl group instead of a benzyl group in the molecule.

Benzylpenicillin is used for infections caused by streptococci, including Streptococcus pneumoniae (community-acquired pneumonia, meningitis), Streptococcus pyogenes(streptococcal tonsillitis, impetigo, erysipelas, scarlet fever, endocarditis), with meningococcal infections. Benzylpenicillin is the antibiotic of choice in the treatment of diphtheria, gas gangrene, leptospirosis, and Lyme disease.

Bicillins are indicated, first of all, if it is necessary to maintain effective concentrations in the body for a long time. They are used for syphilis and other diseases caused by pale treponema (yaws), streptococcal infections (excluding infections caused by group B streptococci) - acute tonsillitis, scarlet fever, wound infections, erysipelas, rheumatism, leishmaniasis.

In 1957, 6-aminopenicillanic acid was isolated from natural penicillins and the development of semi-synthetic drugs began on its basis.

6-Aminopenicillanic acid - the basis of the molecule of all penicillins ("penicillin core") - a complex heterocyclic compound consisting of two rings: thiazolidine and beta-lactam. A side radical is associated with the beta-lactam ring, which determines essential pharmacological properties the resulting drug molecule. In natural penicillins, the structure of the radical depends on the composition of the medium on which they grow. Penicillium spp.

Semi-synthetic penicillins are obtained by chemical modification by adding various radicals to the molecule of 6-aminopenicillanic acid. Thus, penicillins were obtained with certain properties:

Resistant to the action of penicillinases (beta-lactamase);

Acid-resistant, effective when administered orally;

Possessing a wide spectrum of action.

Isoxazolpenicillins (isoxazolyl penicillins, penicillinase-stable, antistaphylococcal penicillins). Most staphylococci produce a specific enzyme beta-lactamase (penicillinase) and are resistant to benzylpenicillin (80-90% of strains are penicillinase-forming). Staphylococcus aureus).

The main antistaphylococcal drug is oxacillin. The group of penicillinase-resistant drugs also includes cloxacillin, flucloxacillin, methicillin, nafcillin and dicloxacillin, which, due to high toxicity and / or low efficacy, have not found clinical use.

The spectrum of antibacterial action of oxacillin is similar to that of benzylpenicillin, but due to the resistance of oxacillin to penicillinase, it is active against penicillinase-forming staphylococci that are resistant to benzylpenicillin and phenoxymethylpenicillin, as well as resistant to other antibiotics.

By activity against gram-positive cocci (including staphylococci that do not produce beta-lactamase), isoxazolpenicillins, incl. oxacillin are significantly inferior to natural penicillins, therefore, in diseases caused by microorganisms sensitive to benzylpenicillin, they are less effective than the latter. Oxacillin is not active against gram-negative bacteria (except Neisseria spp.), anaerobes. In this regard, drugs of this group are indicated only in cases where it is known that the infection is caused by penicillinase-forming strains of staphylococci.

The main pharmacokinetic differences between isoxazolpenicillins and benzylpenicillin:

Rapid, but not complete (30-50%) absorption from the gastrointestinal tract. You can use these antibiotics both parenterally (in / m, in / in) and inside, but 1-1.5 hours before meals, because. they have low resistance to hydrochloric acid;

A high degree of binding to plasma albumin (90-95%) and the inability to remove isoxazolpenicillins from the body during hemodialysis;

Not only renal, but also hepatic excretion, no need to adjust the dosing regimen in mild renal failure.

The main clinical value of oxacillin is the treatment of staphylococcal infections caused by penicillin-resistant strains. Staphylococcus aureus(excluding infections caused by methicillin-resistant Staphylococcus aureus, MRSA). It should be borne in mind that strains are common in hospitals Staphylococcus aureus resistant to oxacillin and methicillin (methicillin, the first penicillinase-resistant penicillin, has been discontinued). Nosocomial and community-acquired strains Staphylococcus aureus Oxacillin/methicillin-resistant bacteria are usually multi-resistant—they are resistant to all other beta-lactams, and often also to macrolides, aminoglycosides, and fluoroquinolones. The drugs of choice for MRSA infections are vancomycin or linezolid.

Nafcillin is slightly more active than oxacillin and other penicillinase-resistant penicillins (but less active than benzylpenicillin). Nafcillin penetrates through the BBB (its concentration in the cerebrospinal fluid is sufficient to treat staphylococcal meningitis), is excreted mainly with bile (the maximum concentration in bile is much higher than serum), to a lesser extent - by the kidneys. Can be used orally and parenterally.

Amidinopenicillins - These are penicillins of a narrow spectrum of action, but with predominant activity against gram-negative enterobacteria. Amidinopenicillin preparations (amdinocillin, pivamdinocillin, bacamdinocillin, acidocillin) are not registered in Russia.

Penicillins with an extended spectrum of activity

In accordance with the classification presented by D.A. Kharkevich, semi-synthetic broad-spectrum antibiotics are divided into the following groups:

I. Drugs that do not affect Pseudomonas aeruginosa:

Aminopenicillins: ampicillin, amoxicillin.

II. Drugs active against Pseudomonas aeruginosa:

Carboxypenicillins: carbenicillin, ticarcillin, carfecillin;

Ureidopenicillins: piperacillin, azlocillin, mezlocillin.

Aminopenicillins - broad-spectrum antibiotics. All of them are destroyed by beta-lactamases of both gram-positive and gram-negative bacteria.

Amoxicillin and ampicillin are widely used in medical practice. Ampicillin is the ancestor of the aminopenicillin group. With regard to gram-positive bacteria, ampicillin, like all semi-synthetic penicillins, is inferior in activity to benzylpenicillin, but superior to oxacillin.

Ampicillin and amoxicillin have similar action spectra. Compared to natural penicillins, the antimicrobial spectrum of ampicillin and amoxicillin extends to susceptible strains of enterobacteria, Escherichia coli, Proteus mirabilis, Salmonella spp., Shigella spp., Haemophilus influenzae; better than natural penicillins act on Listeria monocytogenes and susceptible enterococci.

Of all oral beta-lactams, amoxicillin has the highest activity against Streptococcus pneumoniae, resistant to natural penicillins.

Ampicillin is not effective against penicillinase-forming strains Staphylococcus spp., all strains Pseudomonas aeruginosa, most strains Enterobacter spp., Proteus vulgaris(indole positive).

Combined preparations are produced, for example, Ampiox (ampicillin + oxacillin). The combination of ampicillin or benzylpenicillin with oxacillin is rational, because. the spectrum of action with this combination becomes wider.

The difference between amoxicillin (which is one of the leading oral antibiotics) and ampicillin is its pharmacokinetic profile: when taken orally, amoxicillin is more quickly and well absorbed in the intestine (75-90%) than ampicillin (35-50%), bioavailability does not depend on food intake . Amoxicillin penetrates better into some tissues, incl. into the bronchopulmonary system, where its concentration is 2 times higher than the concentration in the blood.

The most significant differences in the pharmacokinetic parameters of aminopenicillins from benzylpenicillin:

Possibility of appointment inside;

Insignificant binding to plasma proteins - 80% of aminopenicillins remain in the blood in free form - and good penetration into tissues and body fluids (with meningitis, concentrations in the cerebrospinal fluid can be 70-95% of concentrations in the blood);

The multiplicity of appointment of combined drugs - 2-3 times a day.

The main indications for the appointment of aminopenicillins are infections of the upper respiratory tract and ENT organs, infections of the kidneys and urinary tract, infections of the gastrointestinal tract, eradication Helicobacter pylori(amoxicillin), meningitis.

A feature of the undesirable effect of aminopenicillins is the development of an "ampicillin" rash, which is a maculopapular rash of a non-allergic nature, which quickly disappears when the drug is discontinued.

One of the contraindications to the appointment of aminopenicillins is infectious mononucleosis.

Antipseudomonal penicillins

These include carboxypenicillins (carbenicillin, ticarcillin) and ureidopenicillins (azlocillin, piperacillin).

Carboxypenicillins - These are antibiotics that have a spectrum of antimicrobial activity similar to aminopenicillins (with the exception of the action on Pseudomonas aeruginosa). Carbenicillin is the first antipseudomonal penicillin, inferior in activity to other antipseudomonas penicillins. Carboxypenicillins act on Pseudomonas aeruginosa (Pseudomonas aeruginosa) and indole-positive proteus species (Proteus spp.) resistant to ampicillin and other aminopenicillins. The clinical significance of carboxypenicillins is currently declining. Although they have a wide spectrum of action, they are inactive against most strains. Staphylococcus aureus, Enterococcus faecalis, Klebsiella spp., Listeria monocytogenes. Almost do not pass through the BBB. Multiplicity of appointment - 4 times a day. Secondary resistance of microorganisms develops rapidly.

Ureidopenicillins - these are also antipseudomonal antibiotics, their spectrum of action coincides with carboxypenicillins. The most active drug from this group is piperacillin. Of the drugs in this group, only azlocillin retains its importance in medical practice.

Ureidopenicillins are more active than carboxypenicillins in relation to Pseudomonas aeruginosa. They are also used in the treatment of infections caused by Klebsiella spp.

All antipseudomonal penicillins are destroyed by beta-lactamases.

Pharmacokinetic features of ureidopenicillins:

Enter only parenterally (in / m and / in);

Excretion involves not only the kidneys, but also the liver;

Multiplicity of application - 3 times a day;

Secondary bacterial resistance develops rapidly.

Due to the emergence of strains with high resistance to antipseudomonal penicillins and the lack of advantages over other antibiotics, antipseudomonal penicillins have practically lost their significance.

The main indications for these two groups of antipseudomonal penicillins are nosocomial infections caused by susceptible strains. Pseudomonas aeruginosa, in combination with aminoglycosides and fluoroquinolones.

Penicillins and other beta-lactam antibiotics have high antimicrobial activity, but many of them can develop microbial resistance.

This resistance is due to the ability of microorganisms to produce specific enzymes - beta-lactamases (penicillinases), which destroy (hydrolyze) the beta-lactam ring of penicillins, which deprives them of antibacterial activity and leads to the development of resistant strains of microorganisms.

Some semi-synthetic penicillins are resistant to the action of beta-lactamases. In addition, to overcome acquired resistance, compounds have been developed that can irreversibly inhibit the activity of these enzymes, the so-called. beta-lactamase inhibitors. They are used in the creation of inhibitor-protected penicillins.

Beta-lactamase inhibitors, like penicillins, are beta-lactam compounds, but they themselves have minimal antibacterial activity. These substances bind irreversibly to beta-lactamases and inactivate these enzymes, thereby protecting beta-lactam antibiotics from hydrolysis. Beta-lactamase inhibitors are most active against beta-lactamases encoded by plasmid genes.

Inhibitor-protected penicillins are a combination of a penicillin antibiotic with a specific beta-lactamase inhibitor (clavulanic acid, sulbactam, tazobactam). Beta-lactamase inhibitors are not used alone, but are used in combination with beta-lactams. This combination allows you to increase the resistance of the antibiotic and its activity against microorganisms that produce these enzymes (beta-lactamases): Staphylococcus aureus, haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Escherichia coli, Klebsiella spp., Proteus spp., anaerobes, incl. Bacteroides fragilis. As a result, strains of microorganisms resistant to penicillins become sensitive to the combined drug. The spectrum of antibacterial activity of inhibitor-protected beta-lactams corresponds to the spectrum of penicillins contained in their composition, only the level of acquired resistance differs. Inhibitor-protected penicillins are used to treat infections of various localizations and for perioperative prophylaxis in abdominal surgery.

Inhibitor-protected penicillins include amoxicillin/clavulanate, ampicillin/sulbactam, amoxicillin/sulbactam, piperacillin/tazobactam, ticarcillin/clavulanate. Ticarcilin/clavulanate has antipseudomonal activity and is active against Stenotrophomonas maltophilia. Sulbactam has its own antibacterial activity against gram-negative cocci of the family Neisseriaceae and families of non-fermenting bacteria Acinetobacter.

Indications for the use of penicillins

Penicillins are used for infections caused by susceptible pathogens. They are mainly used for infections of the upper respiratory tract, in the treatment of tonsillitis, scarlet fever, otitis media, sepsis, syphilis, gonorrhea, gastrointestinal infections, urinary tract infections, etc.

It is necessary to use penicillins only as directed and under the supervision of a physician. It must be remembered that the use of insufficient doses of penicillins (as well as other antibiotics) or too early termination of treatment can lead to the development of resistant strains of microorganisms (especially natural penicillins). If resistance occurs, further antibiotic therapy should be continued.

The use of penicillins in ophthalmology. In ophthalmology, penicillins are applied topically in the form of instillations, subconjunctival and intravitreal injections. Penicillins do not pass well through the blood-ophthalmic barrier. Against the background of the inflammatory process, their penetration into the internal structures of the eye increases and the concentrations in them reach therapeutically significant. So, when instilled into the conjunctival sac, therapeutic concentrations of penicillins are determined in the stroma of the cornea; when applied topically, they practically do not penetrate into the moisture of the anterior chamber. With subconjunctival administration, drugs are determined in the cornea and moisture of the anterior chamber of the eye, in vitreous body- concentrations below therapeutic.

Solutions for topical application are prepared extempore. Penicillins are used to treat gonococcal conjunctivitis (benzylpenicillin), keratitis (ampicillin, benzylpenicillin, oxacillin, piperacillin, etc.), canaliculitis, especially caused by actinomycetes (benzylpenicillin, phenoxymethylpenicillin), abscess and phlegmon of the orbit (ampicillin / clavulanate, ampicillin / sulbact am, phenoxymethylpenicillin and etc.) and other eye diseases. In addition, penicillins are used to prevent infectious complications in eyelid and orbital injuries, especially when a foreign body penetrates into the tissues of the orbit (ampicillin / clavulanate, ampicillin / sulbactam, etc.).

The use of penicillins in urological practice. In urological practice, inhibitor-protected drugs are widely used among penicillin antibiotics (the use of natural penicillins, as well as the use of semi-synthetic penicillins as drugs of choice, is considered not justified due to high level resistance of uropathogenic strains.

Side effects and toxic effects of penicillins. Penicillins have the lowest toxicity among antibiotics and a wide range of therapeutic effects (especially natural ones). Most serious side effects are associated with hypersensitivity to them. Allergic reactions are observed in a significant number of patients (according to various sources, from 1 to 10%). Penicillins are more common than other drugs pharmacological groups are the cause of drug allergy. In patients who had allergic reactions to the introduction of penicillins in history, with subsequent use, these reactions are observed in 10-15% of cases. Less than 1% of people who have not previously experienced such reactions develop an allergic reaction to penicillin with repeated administration.

Penicillins can cause an allergic reaction at any dose and in any dosage form.

When using penicillins, both allergic reactions are possible immediate type, and slow. It is believed that the allergic reaction to penicillins is associated mainly with the intermediate product of their metabolism - the penicillin group. It is called the major antigenic determinant and is formed when the beta-lactam ring is broken. Small antigenic determinants of penicillins include, in particular, unchanged molecules of penicillins, benzylpenicilloate. They are formed in vivo, but are also determined in solutions of penicillins prepared for administration. It is believed that early allergic reactions to penicillins are mediated mainly by IgE antibodies to small antigenic determinants, delayed and late (urticaria) - usually by IgE antibodies to a large antigenic determinant.

Hypersensitivity reactions are caused by the formation of antibodies in the body and usually occur within a few days after the start of penicillin use (the timing can vary from several minutes to several weeks). In some cases, allergic reactions are manifested in the form of skin rash, dermatitis, fever. In more severe cases, these reactions are manifested by swelling of the mucous membranes, arthritis, arthralgia, kidney damage and other disorders. Possible anaphylactic shock, bronchospasm, pain in the abdomen, swelling of the brain and other manifestations.

A severe allergic reaction is an absolute contraindication to the introduction of penicillins in the future. The patient must be explained that even a small amount of penicillin that has entered the body with food or during a skin test can be deadly for him.

Sometimes the only symptom of an allergic reaction to penicillins is fever (it can be constant, remittent or intermittent in nature, sometimes accompanied by chills). Fever usually disappears within 1-1.5 days after discontinuation of the drug, but sometimes it can last for several days.

All penicillins are characterized by cross-sensitization and cross-allergic reactions. Any preparations containing penicillin, including cosmetics and foods, may cause sensitization.

Penicillins can cause various side and toxic effects of a non-allergic nature. These include: when taken orally - an irritant effect, incl. glossitis, stomatitis, nausea, diarrhea; with the / m introduction - pain, infiltrate, aseptic necrosis of muscles; with a / in the introduction - phlebitis, thrombophlebitis.

It is possible to increase the reflex excitability of the central nervous system. When using high doses, neurotoxic effects may occur: hallucinations, delusions, dysregulation of blood pressure, convulsions. Seizures more likely in patients receiving high doses of penicillin and/or in patients with severe hepatic impairment. Due to the risk of severe neurotoxic reactions, penicillins cannot be administered endolumbally (with the exception of benzylpenicillin sodium salt, which is administered extremely carefully, according to vital indications).

In the treatment of penicillins, the development of superinfection, candidiasis of the oral cavity, vagina, intestinal dysbacteriosis is possible. Penicillins (more often ampicillin) can cause antibiotic-associated diarrhea.

The use of ampicillin leads to the appearance of an "ampicillin" rash (in 5-10% of patients), accompanied by itching, fever. This side effect occurs more frequently on days 5-10 of high-dose ampicillin use in children with lymphadenopathy and viral infections or with concomitant allopurinol, as well as in almost all patients with infectious mononucleosis.

specific adverse reactions when using bicillins, there are local infiltrates and vascular complications in the form of Onet's syndromes (ischemia and gangrene of the extremities when accidentally injected into an artery) or Nicolau (embolism of the pulmonary and cerebral vessels when injected into a vein).

When using oxacillin, hematuria, proteinuria, and interstitial nephritis are possible. The use of antipseudomonal penicillins (carboxypenicillins, ureidopenicillins) may be accompanied by the appearance of allergic reactions, symptoms of neurotoxicity, acute interstitial nephritis, dysbacteriosis, thrombocytopenia, neutropenia, leukopenia, eosinophilia. When using carbenicillin, hemorrhagic syndrome is possible. Combined drugs containing clavulanic acid can cause acute liver damage.

Application during pregnancy. Penicillins pass through the placenta. Although adequate and strictly controlled safety studies in humans have not been conducted, penicillins, incl. inhibitor-protected, are widely used in pregnant women, with no complications reported.

In studies on laboratory animals with the introduction of penicillins in doses 2-25 (for different penicillins) higher than therapeutic, fertility disorders and effects on reproductive function were not found. No teratogenic, mutagenic, embryotoxic properties have been identified with the introduction of penicillins to animals.

In accordance with the generally recognized recommendations of the FDA (Food and Drug Administration), which determine the possibility of using drugs during pregnancy, penicillin drugs in terms of their effect on the fetus belong to the FDA category B (the study of reproduction in animals did not reveal an adverse effect of drugs on the fetus, but adequate and strictly controlled studies in pregnant women have not been conducted).

When prescribing penicillins during pregnancy, one should (as with any other means) take into account the duration of pregnancy. During therapy, it is necessary to strictly monitor the condition of the mother and fetus.

Use during breastfeeding. Penicillins pass into breast milk. Although no significant complications have been reported in humans, the use of penicillins by nursing mothers can lead to sensitization of the child, changes in the intestinal microflora, diarrhea, the development of candidiasis and the appearance of skin rashes in infants.

Pediatrics. When using penicillins in children, no specific pediatric problems have been reported, however, it should be borne in mind that underdeveloped kidney function in newborns and children early age can lead to the accumulation of penicillins (in this regard, it is noted increased risk neurotoxic effect with the development of seizures).

Geriatrics. No specific geriatric problems have been reported with the use of penicillins. However, it should be remembered that older people are more likely to age-related impairment of kidney function, and therefore dose adjustment may be required.

Impaired kidney and liver function. With renal / hepatic insufficiency, cumulation is possible. With moderate and severe insufficiency of kidney and / or liver function, dose adjustment and an increase in the periods between antibiotic injections are required.

Interaction of penicillins with other drugs. Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) have an antagonistic effect. Care must be taken when combining penicillins active against Pseudomonas aeruginosa (Pseudomonas aeruginosa), with anticoagulants and antiplatelet agents (potential risk of increased bleeding). It is not recommended to combine penicillins with thrombolytics. When combined with sulfonamides, the bactericidal effect may be weakened. Oral penicillins may reduce the effectiveness of oral contraceptives due to impaired enterohepatic estrogen circulation. Penicillins can slow down the excretion of methotrexate from the body (inhibit its tubular secretion). The combination of ampicillin with allopurinol increases the likelihood of a skin rash. The use of high doses of the potassium salt of benzylpenicillin in combination with potassium-sparing diuretics, potassium preparations, or ACE inhibitors increases the risk of hyperkalemia. Penicillins are pharmaceutically incompatible with aminoglycosides.

Due to the fact that with long-term oral administration of antibiotics, the intestinal microflora that produces vitamins B 1, B 6, B 12, PP can be suppressed, it is advisable for patients to prescribe vitamins of group B to prevent hypovitaminosis.

In conclusion, it should be noted that penicillins are a large group of natural and semi-synthetic antibiotics with a bactericidal effect. The antibacterial action is associated with a violation of the synthesis of peptidoglycan of the cell wall. The effect is due to the inactivation of the transpeptidase enzyme, one of the penicillin-binding proteins located on the inner membrane of the bacterial cell wall, which is involved in the later stages of its synthesis. Differences between penicillins are associated with the features of their spectrum of action, pharmacokinetic properties and the spectrum of undesirable effects.

Over several decades of successful use of penicillins, problems have arisen associated with their misuse. Thus, the prophylactic administration of penicillins at risk of bacterial infection is often unreasonable. Incorrect treatment regimen - incorrect dose selection (too high or too low) and the frequency of administration can lead to the development of side effects, reduced efficacy and the development of drug resistance.

Thus, at present, most strains Staphylococcus spp. resistant to natural penicillins. IN last years increased frequency of detection of resistant strains Neisseria gonorrhoeae.

The main mechanism of acquired resistance to penicillins is associated with the production of beta-lactamase. To overcome the acquired resistance that is widespread among microorganisms, compounds have been developed that can irreversibly inhibit the activity of these enzymes, the so-called. beta-lactamase inhibitors - clavulanic acid (clavulanate), sulbactam and tazobactam. They are used in the creation of combined (inhibitor-protected) penicillins.

It should be remembered that the choice of one or the other antibacterial drug, incl. penicillin, should be due, first of all, to the sensitivity of the pathogen that caused the disease to it, as well as the absence of contraindications to its appointment.

Penicillin antibiotics are β-lactam antibiotics. β-lactam antibiotics β-lactams, which are united by the presence of a β-lactam ring in their structure, include penicillins, cephalosporins, carbapen

ema and monobactams, which have a bactericidal effect. The similarity of the chemical structure determines, firstly, the same mechanism of action of all β-lactams - inhibition of penicillin-binding proteins (PBP), enzymes involved in the process of synthesis of the bacterial cell wall (under conditions of PBP inhibition, this process is disrupted, which entails lysis of the bacterial cell) , and, secondly, cross-allergy to them in some patients.

It is important that the cellular structures of bacteria that are the target of β-lactams are absent in mammals; therefore, specific toxicity to the macroorganism is not typical for these antibiotics.

Penicillins, cephalosporins and monobactams are sensitive to the hydrolyzing action of special enzymes - β-lactamases produced by many bacteria. Carbapenems are characterized by a significantly higher resistance to β-lactamases.
Given the high clinical efficacy and low toxicity, β-lactam antibiotics have been the basis of antimicrobial chemotherapy for many years, occupying a leading position in the treatment of most bacterial infections.

Antibiotics of the penicillin group

Penicillins- the first antimicrobial preparations developed on the basis of biologically active substances produced by microorganisms. The ancestor of all penicillins, benzylpenicillin, was obtained in the early 40s. XX century. His discovery marked a kind of revolutionary revolution in medicine, because, firstly, it transferred many bacterial infections from the category of inevitably lethal to potentially curable, and secondly, it determined the fundamental direction on the basis of which the development of many other antibacterial drugs was going on.

Currently, the group of penicillins includes more than ten antibiotics, which, depending on the sources of production, structural features and antimicrobial activity, are divided into several subgroups. At the same time, some antibiotics, primarily carboxypenicillins and ureidopenicillins, have lost their original significance and are not used as monopreparations.

General properties of penicillins

Antibacterial drugs from the penicillin group have the following properties:

They have bactericidal action.
They are well distributed in the body, penetrate into many organs, tissues and environments, with the exception of non-inflamed meninges, eyes, prostate, organs and tissues. Creates high concentrations in the lungs, kidneys, intestinal mucosa, reproductive organs, bones, pleural and peritoneal fluid.
Small amounts pass through the placenta and pass into breast milk.
Poorly penetrate the BBB (with meningitis, the permeability increases, and the concentration of penicillin in the cerebrospinal fluid is 5% of the serum level), the blood-ophthalmic barrier (HOB), into the prostate gland.
Excreted by the kidneys, mainly by active excretion by the renal tubules.
The half-life is 0.5 hours.
The therapeutic level in the blood is maintained within 4-6 hours.

Side effects of penicillin ov

allergic reactions(according to various sources, in 1-10% of cases): urticaria; rash; Quincke's edema; fever; eosinophilia; bronchospasm.

The most dangerous is anaphylactic shock, which gives up to 10% mortality (in the US, about 75% of deaths from anaphylactic shock are due to the introduction of penicillin).

Local irritant action with the / m introduction (soreness, infiltrates).

Neurotoxicity: convulsions, which are more common in children, with the use of very high doses of penicillin, in patients with renal insufficiency, with the introduction of more than 10 thousand units endolumbally.

Violations electrolyte balance - in patients with heart failure, with the introduction of large doses of sodium salt, edema may increase, and with hypertension - an increase blood pressure(AD) (1 million units contains 2.0 mmol sodium).

Sensitization. It should be borne in mind that in some people the degree of sensitization to penicillin may vary over time. In 78% of them, skin tests become negative after 10 years. Therefore, the claim of penicillin allergy as a lifelong clinical diagnosis is incorrect.

Prevention measures

Careful history taking, use of freshly prepared solutions of penicillin, observation of the patient for 30 minutes after the first injection of penicillin, detection of hypersensitivity by skin testing.

Measures to help with the development of anaphylactic shock: ensuring airway patency (if necessary, intubation), oxygen therapy, adrenaline, glucocorticoids.

It should be noted that in bronchial asthma and other allergic diseases, the risk of developing allergic reactions to penicillins (as well as to other antibiotics) is slightly increased, and if they occur, they can be more severe. However, the prevailing point of view that penicillins should not be prescribed to people with allergic diseases at all is erroneous.

Indications for the use of penicillins

GABHS infections: tonsillopharyngitis, erysipelas, scarlet fever, acute rheumatic fever.
Meningitis in children older than 2 years and in adults.
Infective endocarditis (mandatory in combination with gentamicin or streptomycin).
Syphilis.
Leptospirosis.
Anthrax.
Anaerobic infections: gas gangrene, tetanus.
Actinomycosis.

Preparations of natural penicillins

Preparations of natural penicillins include the following:

Benzylpenicillin;
Benzylpenicillin sodium salt;
Benzylpenicillin novocaine salt;
Phenoxymethylpecillin;
Ospen 750;
Bicillin-1;
Retarpen.

Phenoxymethylpenicillin

A preparation of natural penicillin intended for oral administration.
According to the spectrum of activity, it practically does not differ from penicillin. Compared to penicillin, it is more acid-resistant. Bioavailability is 40-60% (slightly higher when taken on an empty stomach).

The drug does not create high concentrations in the blood: taking 0.5 g of phenoxymethylpenicillin inside approximately corresponds to the introduction of 300 thousand units of penicillin / m. The half-life is about 1 hour.

Side effects

Allergic reactions.
Gastrointestinal tract (GIT) - pain or discomfort in the abdomen, nausea; rarely vomiting, diarrhea.

Indications for use

Prevention of pneumococcal infections in individuals after splenectomy.

Benzathine phenoxymethylpenicillin

A derivative of phenoxymethylpenicillin. Compared with it, it is more stable in the gastrointestinal tract, absorbed faster, better tolerated. Bioavailability is independent of food.

Indications for use

Streptococcal (GAB) infections of mild to moderate severity: tonsillopharyngitis, infections of the skin and soft tissues.

Prolonged penicillin preparations

Prolonged penicillin preparations, or the so-called depot penicillins, include b enzylpenicillin novocaine salt And benzathine benzyl penicillin, as well as combined preparations created on their basis.

Side effects long-acting penicillin preparations

Allergic reactions.
Soreness, infiltrates at the injection site.
She syndrome (Hoigne) - ischemia and gangrene of the extremities with accidental injection into the artery.
Nicolau's syndrome (Nicholau) - embolism of the vessels of the lungs and brain when injected into a vein.

Prevention vascular complications: strict adherence to the technique of introduction - in / m into the upper outer quadrant of the buttocks using a wide needle, with the obligatory horizontal position patient. Before insertion, it is necessary to pull the plunger of the syringe towards you to make sure that the needle is not in the vessel.

Indications for use

Infections caused by micro-organisms highly sensitive to penicillin: streptococcal (GABHS) tonsillopharyngitis; syphilis (except neurosyphilis).
Prevention of anthrax after contact with spores (benzylpenicillin novocaine salt).
Year-round prevention of rheumatic fever.
Prevention of diphtheria, streptococcal cellulitis.

Benzylpenicillin novocaine salt

With the / m administration, the therapeutic concentration in the blood is maintained for 12-24 hours, however, it is lower than with the introduction of an equivalent dose of benzylpenicillin sodium salt. The half-life is 6 hours.

It has a local anesthetic effect, it is contraindicated in case of allergy to procaine (novocaine). In case of an overdose, mental disorders are possible.

Benzathine Benzylpenicillin

It acts longer than benzylpenicillin novocaine salt, up to 3-4 weeks. After intramuscular administration, the peak concentration is observed after 24 hours in children and after 48 hours in adults. The half-life is several days.

Pharmacokinetic studies of domestic preparations of benzathine benzylpenicillin, conducted at the State Scientific Center for Antibiotics, showed that when they are used, the therapeutic concentration in blood serum remains no more than 14 days, which requires their more frequent administration than their foreign counterpart, Retarpen.

Combined drugs penicillins

Bicillin-3, Bicillin-5.

Isoxazolylpenicillins (anti-staphylococcal penicillins)

The drug isoxazolylpenicillins - Oxacillin.

The first isoxazolylpenicillin with antistaphylococcal activity was methicillin, which was later discontinued due to lack of advantages over newer analogues and nephrotoxicity.

Currently, the main drug of this group in Russia is oxacillin. Nafcillin, cloxacillin, dicloxacillin and flucloxacillin are also used abroad.

Oxacillin

Activity spectrum
Oxacillin is resistant to penicillinase, which is produced by more than 90% of S. aureus strains. Therefore, they are active against penicillin-resistant S. aureus (PRSA) and a number of strains of S. epidermidis resistant to the action of natural penicillins, amino-, carboxy- and ureidopenicillins. This is the main clinical significance of this drug.

At the same time, oxacillin is much less active against streptococci (including S. pneumoniae). It has practically no effect on most other microorganisms sensitive to penicillin, including gonococci and enterococci.

One of serious problems is the spread of strains (especially nosocomial) S. aureus resistant to isoxazolylpenicillins and received, based on the name of the first of them, the abbreviation MRSA (raeticillin-resistant S. aureus). In fact, they are multi-resistant, as they are resistant not only to all penicillins, but also to cephalosporins, macrolides, tetracyclines, lincosamides, carbapenems, fluoroquinolones and other antibiotics.

Side effects

Allergic reactions.
Gastrointestinal tract - abdominal pain, nausea, vomiting, diarrhea.
Moderate hepatotoxicity - increased activity of liver transaminases, especially with the introduction of high doses (more than 6 g / day); as a rule, it is asymptomatic, but sometimes it can be accompanied by fever, nausea, vomiting, eosinophilia (a liver biopsy shows signs of nonspecific hepatitis).
Decreased hemoglobin level, neutropenia.
Transient hematuria in children.

Indications for use

Confirmed or suspected staphylococcal infections of various localization (with sensitivity to oxacillin or an insignificant risk of the spread of methicillin resistance):

bone and joint infections;
pneumonia;
infective endocarditis;
meningitis;
sepsis.

Aminopenicillins

The aminopencillins are ampicillin And amoxicillin. Compared to natural penicillins and isoxazolylpenicillins their antimicrobial spectrum is extended by some Gram-negative bacteria of the Enterobacteriaceae family and H. influenzae.

Ampicillin

Differences from penicillin in the spectrum of antibacterial activity

It acts on a number of gram (-) bacteria: E. coli, P. mirabilis, salmonella, shigella (the latter are resistant in many cases), H. influenzae (strains that do not produce β-lactamase).
More active against enterococci (E. faecalis) and listeria.
Somewhat less active against streptococci (GABHS, S. pneumoniae), spirochetes, anaerobes.

Ampicillin has no effect on Gram-negative pathogens of nosocomial infections, such as Pseudomonas aeruginosa (P. aeruginosa), Klebsiella, Serratia, Enterobacter, Acinetobacter, etc.

It is destroyed by staphylococcal penicillinase, therefore it is inactive against most staphylococci.

Side effects

Allergic reactions.
Gastrointestinal disorders - abdominal pain, nausea, vomiting, most often diarrhea.
"Ampicillin" rash (in 5-10% of patients), according to most experts, is not associated with an allergy to penicillins.

The rash is maculopapular in nature, is not accompanied by itching, and may resolve without discontinuation of the drug. Risk factors: infectious mononucleosis (rash occurs in 75-100% of cases), cytomegaly, chronic lymphocytic leukemia.

Indications for use

Acute bacterial infections of the upper respiratory tract ( otitis media, rhinosinusitis - if necessary, parenteral administration).
Community-acquired pneumonia (if necessary, parenteral administration).
Urinary tract infections (UTIs) - cystitis, pyelonephritis (not recommended for empirical therapy due to the high level of resistance of pathogens).
Intestinal infections (salmonellosis, shigellosis).
Meningitis.
Infective endocarditis.
Leptospirosis.

Warnings and precautions

Ampicillin can only be dissolved in water for injection or in 0.9% sodium chloride solution. Freshly prepared solutions must be used. When stored for more than 1 hour, the activity of the drug decreases sharply.

Amoxicillin

It is a derivative of ampicillin with improved pharmacokinetics.

According to the antimicrobial spectrum, amoxicillin is close to ampicillin (the microflora has cross-resistance to both drugs).

amoxicillin - the most active among all oral penicillins and cephalosporins against S. pneumoniae, including pneumococci with an intermediate level of resistance to penicillin;
somewhat stronger than ampicillin, acts on E. faecalis;
clinically ineffective against Salmonella and Shigella, regardless of the results of in vitro susceptibility testing;
highly active in vitro and in vivo against H. pylori.

Similarly to ampicillin, amoxicillin is destroyed by β-lactamases.

Side effects

Allergic reactions.
"Ampicillin" rash.
Gastrointestinal tract - mostly moderate abdominal discomfort, nausea; diarrhea is much less common than with ampicillin.

Indications for use

Upper respiratory tract infections - acute otitis media, acute rhinosinusitis.
Lower respiratory tract infections - exacerbation of chronic obstructive pulmonary disease (COPD), community-acquired pneumonia.
Urinary tract infections - cystitis, pyelonephritis (not recommended for empirical therapy due to the high level of resistance of pathogens).
H. pylori eradication (in combination with antisecretory drugs and other antibiotics).
Tick-borne borreliosis (Lyme disease).
Prevention of infective endocarditis.
Prevention of anthrax (in pregnant women and children).

Warnings

Do not use in the treatment of shigellosis and salmonellosis.
Amoxicillin preparations - Ampicillin-AKOS, Ampicillin-Ferein, Ampicillin sodium salt, Amoxicillin, Amoxicillin Sandoz, Amosin, Ospamox, Flemoxin Solutab, Hikontsil.

Carboxypenicillins

Carboxypenicillins include carbenicillin (discontinued and no longer available) and ticarcillin (part of the ticarcillin/clavulanate combination).

Their main advantage for a long time was their activity against R. aeruginosa, as well as some Gram-negative bacteria resistant to aminopenicillins (Enterobacter, Proteus, Morganella, etc.). However, to date, carboxypenicillins have practically lost their "antipseudomonal" value due to the high level of resistance to them by Pseudomonas aeruginosa and many other microorganisms, as well as poor tolerance.

They have the greatest neurotoxicity among penicillins, can cause a violation of platelet aggregation, thrombocytopenia, electrolyte imbalance - hypernatremia, hypokalemia.

Ureidopenicillins

Ureidopenicillins include azlocillin (not currently used) and piperacillin (used as part of the combination drug piperacillin + tazobactam. Compared to carboxypenicillins, they have a broader antimicrobial spectrum and are somewhat better tolerated.

Initially, they were more active than carboxypenicillins against P. aeruginosa, but now most strains of Pseudomonas aeruginosa are resistant to ureidopenicillins.

Inhibitor-protected penicillins

The main mechanism for the development of bacterial resistance to β-lactam antibiotics is the production of special enzymes, β-lactamases, which destroy the β-lactam ring - the most important structural element of these drugs, providing their bactericidal effect. This protective mechanism is one of the leading ones for such clinically important pathogens as S. aureus, H. influenzae, M. catarrhalis, K. pneumoniae, B. fragilis, and many others.

Simplified approach to the systematization of β-lactamases produced by microorganisms, depending on the direction of action, they can be divided into several types:

1) penicillinases that destroy penicillins;

2) cephalosporinases that destroy cephalosporins of I-II generations;

3) extended-spectrum β-lactamases (ESBLs), which combine the properties of the first two types and, in addition, destroy cephalosporins of III and IV generations;

4) metallo-β-lactamases, which destroy almost all β-lactams (except for monobactams).

In order to overcome this resistance mechanism, β-lactamase inactivating compounds were obtained: clavulanic acid (clavulanate), sulbactam and tazobactam.

On this basis, combined preparations containing a penicillin antibiotic (ampicillin, amoxicillin, piperacillin, ticarcillin) and one of the β-lactamase inhibitors have been created.

Such drugs are called inhibitor-protected penicillins.

As a result of the combination of penicillins with β-lactamase inhibitors, the natural (primary) activity of penicillins against many staphylococci (except MRSA), gram-negative bacteria, non-spore-forming anaerobes is restored, and their antimicrobial spectrum is also expanded due to a number of gram-negative bacteria (Klebsiella, etc.) with natural resistance to penicillins.

It should be emphasized that β-lactamase inhibitors make it possible to overcome only one of the mechanisms of bacterial resistance. Therefore, for example, tazobactam cannot increase the sensitivity of P. aeruginosa to piperacillin, since resistance in this case is caused by a decrease in the permeability of the outer membrane of the microbial cell for β-lactams.

Amoxicillin + clavulanate

The drug consists of amoxicillin and potassium clavulanate. The ratio of components in preparations for oral administration is from 2:1, 4:1 and 8:1, and for parenteral administration - 5:1. Clavulanic acid, used as a potassium salt, is one of the most potent inhibitors of microbial β-lactamase. Therefore, amoxicillin in combination with clavulanate is not destroyed by β-lactamases, which significantly expands the spectrum of its activity.

Spectrum of antibacterial activity

Amoxicillin + clavulanate acts on all microorganisms sensitive to amoxicillin. In addition, unlike amoxicillin:

has a higher antistaphylococcal activity: acts on PRSA and some strains of S. epidermidis;
acts on enterococci producing (3-lactamase;
active against gram (-) flora producing (3-lactamase (H. influenzae, M. catarrhalis, N. gonorrhoeae, E. coli, Proteus spp., Klebsiella spp., etc.), except for ESBL producers;
has high antianaerobic activity (including B. fragilis).
Does not affect Gram (-) bacteria resistant to aminopenicillins: P. aeruginosa, Enterobacter, Citrobacter, Serration, Providence, Morganella.

Side effects

Like amoxicillin. In addition, due to the presence of clavulanate, in rare cases (more often in the elderly), hepatotoxic reactions (increased transaminase activity, fever, nausea, vomiting) are possible.

Indications for use

Bacterial infections of the upper respiratory tract (acute and chronic rhinosinusitis, acute otitis media, epiglottitis).
Bacterial infections of the lower respiratory tract (exacerbation of COPD, community-acquired pneumonia).
Infections of the biliary tract (acute cholecystitis, cholangitis).
Urinary tract infections (acute pyelonephritis, cystitis).
intra-abdominal infections.
Infections of the pelvic organs.
Bone and joint infections.

Amoxicillin + sulbactam

The drug consists of amoxicillin and sulbactam in ratios of 1:1 and 5:1 for oral administration and 2:1 for parenteral administration.
The spectrum of activity is close to amoxicillin + clavulanate. Sulbactam, in addition to inhibiting β-lactamases, exhibits moderate activity against Neisseria spp., M. catarrhalis, Acinetobacter spp.
Side effects

Like amoxicillin.

Indications for use

Infections of the urinary tract (acute pyelonephritis, cystitis).
intra-abdominal infections.
Infections of the pelvic organs.
Infections of the skin and soft tissues (including wound infections after bites).
Bone and joint infections.
Perioperative antibiotic prophylaxis.

Ampicillin + sulbactam

The drug consists of ampicillin and sulbactam in a ratio of 2:1. For oral administration, the prodrug sultamicillin is intended, which is a combination of ampicillin and sulbactam. During absorption, hydrolysis of sultamicillin occurs, with the bioavailability of ampicillin and sulbactam exceeding that of an equivalent dose of conventional ampicillin.

Ampicillin + sulbactam is similar in most parameters to amoxicillin + clavulanate and amoxicillin + sulbactam.

Indications for use

Bacterial infections of the upper respiratory tract (acute and chronic rhinosinusitis, acute otitis media, epiglottitis).
Bacterial infections of the NDP (exacerbation of COPD, community-acquired pneumonia).
Infections of the gastrointestinal tract (acute cholecystitis, cholangitis).
MBP infections (acute pyelonephritis, cystitis).
intra-abdominal infections.
Infections of the pelvic organs.
Infections of the skin and soft tissues (including wound infections after bites).
Bone and joint infections.
Perioperative antibiotic prophylaxis.

It has an advantage over amoxicillin + clavulanate in infections caused by Acinetobacter.

Warning

When administered intramuscularly, the drug should be diluted with a 1% solution of lidocaine.

Ticarcillin + clavulanate

Combination of carboxypenicillin ticarcillin with clavulanate in a ratio of 30:1. Unlike inhibitor-protected aminopenicillins, it acts on P. aeruginosa (but many strains are resistant) and surpasses them in activity against nosocomial strains of enterobacteria.

Gram-positive cocci: staphylococci (including PRSA), streptococci, enterococci (but inferior in activity to inhibitor-protected aminopenicillins).
Gram-negative rods: representatives of the Enterobacteriaceae family (E. coli, Klebsiella spp., Proteus spp., Enterobacter spp., Serratia spp., C. diversus, etc.); P. aeruginosa (but not superior to ticarcillin); non-fermenting bacteria - S. maltophilia (surpasses other β-lactams in activity).
Anaerobes: spore-forming and non-spore-forming, including B. fragilis.

Side effects

Allergic reactions.
Neurotoxicity (tremor, convulsions).
Electrolyte disorders (hypernatremia, hypokalemia - especially in patients with heart failure).
Violation of platelet aggregation.

Indications for use

Severe, predominantly nosocomial infections of various localization:

intra-abdominal infections;
infections of the pelvic organs;
skin and soft tissue infections;
bone and joint infections;
sepsis.

Piperacillin + tazobactam

The combination of ureidopenicillin piperacillin with tazobactam in a ratio of 8:1. Tazobactam surpasses sulbactam in the degree of β-lactamase inhibition and is approximately equivalent to clavulanate. Piperacillin + tazobactam is regarded as the most potent inhibitor-protected penicillin.

Spectrum of antibacterial activity

Gram-positive cocci: staphylococci (including PRSA), streptococci, enterococci.
Gram-negative rods: representatives of the Enterobacteriaceae family (E. coli, Klebsiella spp., Proteus spp., Enterobacter spp., Serratia spp., C. diversus, etc.); P. aeruginosa (but not superior to piperacillin); non-fermenting bacteria - S. maltophilia.
Anaerobes: spore-forming and non-spore-forming, including B. frailis.

Side effects

Same as Ticarcillin + clavulanate.

Indications for use

Severe, predominantly nosocomial infections of various localization, caused by multiresistant and mixed (aerobic-anaerobic) microflora:

lower respiratory tract infections (pneumonia, lung abscess, pleural empyema);
complicated urinary tract infections;
intra-abdominal infections;
infections of the pelvic organs;
skin and soft tissue infections;
bone and joint infections;
sepsis.

Preparations of inhibitor-protected penicillins

(Amoxicillin + clavulanate) - Amovikomb, Amoxiclav, Amoxivan, Arlet, Augmentin, Bactoclav, Betaklav, Verklav, Klamosar, Medoklav, Panklav 2X, Rapiclav, Fibell, Flemoklav Solutab, Foraklav, Ecoklav.

(Amoxicillin + sulbactam) - Trifamox IBL, Trifamox IBL DUO.

(Ampicillin + sulbactam)— Ampiside, Libaktsil, Sultasin.

(Ticarcillin + clavulanate) - Timentin.

(Piperacillin + tazobactam) - Santaz, Tazocin, Tazrobida, Tacillin J.