List of penicillin antibiotics, indications for taking drugs. List of penicillin antibiotics: description and treatment Synthetic penicillin preparations

Antipyretics for children are prescribed by a pediatrician. But there are emergency situations with fever when the child needs to be given medicine immediately. Then the parents take responsibility and use antipyretic drugs. What is allowed to be given to infants? How can you lower the temperature in older children? What medications 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 benzyl-penicillin), semi-synthetic penicillins: aminopenicillins (amoxicillin, ampicillin, bacampicillin, penicillin, timentin), isoxazolylpenicillins (cloxacillin, oxacillin, flucloxacillin), carboxypenicillins (carbenicillin), ureidopenicillins (azlocillin, mezlocillin, piperacillin).

AZLOCILLIN (Azlocillin)

Synonyms: Securopen, Azlin.

Semi-synthetic beta-lactam antibiotic of the acylureidopenicillin group.

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

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, infections of bones and soft tissues, respiratory ( respiratory tract), bile, gastrointestinal infections, serositis (inflammation of the membrane lining the cavity of the body, for example, the peritoneum), infected (contaminated with microbes) large areas of burns, etc. For local rinsing 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 (canals formed as a result of the disease, connecting body cavities or hollow organs with the external environment or with each other).

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora 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), for severe

infections, 20 g per day is allowed (5 g - 4 times). Premature babies weighing 1.5; 2.0 and 2.5 kg, 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 body weight 2 times; for infants under 1 year of age - 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 the temperature normalizes and disappears clinical symptoms. Used 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 whose creatinine clearance values (the rate of blood purification from the final product of nitrogen metabolism - creatinine) are less than 30 ml/min require a 2-fold reduction in the daily dose of the drug. For adult patients with creatinine clearance more than 30 ml/min, the drug is prescribed 5 g every 12 hours. For creatinine clearance 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 liver dysfunction These doses should be further reduced.

Side effect. Possible nausea, vomiting, flatulence (accumulation of gases in the intestines), loose stool, diarrhea (diarrhea); transient (transient) increase in the concentration of hepatic transaminases in the blood and alkaline phosphatase(enzymes); rarely - increased concentration of bilirubin (bile pigment) in the blood. Sometimes - skin rash, itching, urticaria, rarely - drug 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 - red blood cells, leukocytes, platelets, etc.). These side effects disappear after discontinuation of the drug. Impaired taste and smell (these effects occur when the rate of administration of the solution exceeds 5 ml/min). Rarely - erythema (limited redness of the skin), soreness or thrombophlebitis (inflammation of the vein wall with its blockage) at the injection site. In some cases, hypokalemia (low potassium levels in the blood), increased concentrations of creatinine and residual nitrogen in the blood serum. With the introduction of increased doses of the drug, due to an increase in its concentration in the cerebrospinal fluid (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 bottles of 0.5; 1.0; 2.0 g in packs of 5 and 10 pieces.

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

AMOXICILLIN

Synonyms: Amine, Amoxillat, amoxicillin-Rati ofarm, Amoxicillin-Teva, Apo-Amoxi, Gonoform, Grunamox, Dedoxil, Isoltil, Ospamox, Taysil, Flemoxin solutab, Hiconcil.

Pharmachologic effect. Bactericidal (bacteria-destroying) antibiotic from the group of semisynthetic penicillins. It has a wide spectrum of action, including gram-positive and gram-negative cocci, some gram-negative bacilli (Escherichia coli, Shigella, Salmonella, Klebsiella). Microorganisms that produce penicillinase (an enzyme that destroys penicillins) are resistant to the drug. The drug is acid-resistant and is absorbed quickly and almost completely in the intestine.

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

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora 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. For adults and children over 10 years of age (with a body weight of more than 40 kg), the drug is prescribed 0.5 g 3 times a day; in case of severe infection, the dose can 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

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

3 g once, it is advisable to simultaneously prescribe 1 g probenecid. When treating gonorrhea in women, it is recommended to repeat the indicated dose.

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

Contraindications. Hypersensitivity to penicillins, infectious mononucleosis (acute viral disease, occurring with a high rise in body temperature, enlargement of the palatine lymph nodes and liver).

Prescribe the drug to pregnant women with caution; patients prone to allergic reactions. In patients who are hypersensitive to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

Release form. 1.0 g tablets, 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 use (5 ml - 0.125 g); dry substance for injection 1 g.

Storage conditions.

AUGMENTIN (Augmentm)

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

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

Indications for use. Bacterial infections caused by microorganisms sensitive to the drug: upper respiratory tract infections - acute and chronic bronchitis (inflammation of the bronchi), lobar bronchopneumonia (combined inflammation of the bronchi and lungs), empyema (accumulation of pus), abscesses (ulcers) of the lungs; bacterial infections of the skin and soft tissues; genitourinary tract infections - cystitis (inflammation Bladder), urethritis (inflammation of the urethra), pyelonephritis (inflammation of the kidney tissue and renal pelvis); sepsis (blood infection by microbes from a source of purulent inflammation) during abortion, pelvic organ infections, 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 1 year of age, 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 one year - 1.25 ml. In severe cases, a single intravenous dose for children over 3 months of age. up to 12 years of age is 30 mg/kg body weight; the drug is administered every 6-8 hours. Children under 3 months are administered single dose 30 mg/kg body weight: for premature infants and children in the perinatal period (up to the 7th day of life of newborns) - every 12 hours, then every 8 hours. Treatment with the drug should not be continued for more than 14 days without reviewing the clinical situation.

Children under 12 years of age 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 aged 9 months and older. before

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

Adults and children over 12 years of age with mild to moderate infections are prescribed 1 tablet (0.375 g) 3 times a day. For severe infection, the single dose is 1 tablet. 0.625 g or 2 tablets. 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 permissible daily dose for intravenous administration is 7.2 g.

Patients with moderate or severe renal excretory dysfunction require adjustment of the drug dosage regimen. When creatinine clearance (the rate of blood purification from the final product of nitrogen metabolism - creatinine) is more than 30 ml/min, no change in dosage 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 blood purification). When using the drug in patients on dialysis, 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). Severity of dyspeptic side effects may decrease when taking the drug with food. Isolated cases of liver dysfunction, the development of hepatitis, and cholestatic jaundice (jaundice associated with stagnation of bile in the biliary tract) have been described. There are isolated reports of the development of pseudomembranous colitis (intestinal colic, characterized by attacks of abdominal pain and the release of large amounts of mucus in the stool). 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 syndrome (a disease characterized by redness and hemorrhage in the mucous membranes of the mouth, urethra and conjunctiva / outer membrane of the eye /), exfoliative dermatitis (redness of the skin of the entire body with severe peeling). Rarely - candidiasis ( fungal disease) and other types of superinfection (severe, rapidly developing forms of infectious disease caused by drug-resistant microorganisms that were previously in the body, but do not manifest themselves). In some cases, phlebitis (inflammation of the vein) may develop at the injection site.

Contraindications. Hypersensitivity to the components of the drug.

Intravenous administration should be used with caution in patients with severe liver dysfunction. If urticaria or erythematous rash appears, treatment should be discontinued.

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

The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

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

Dry substance for the preparation of 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 substance 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 cool, dry place.

CLONACOM-X

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

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

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

Side effect.

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

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

Storage conditions. List B. In a dry place, protected from light. . .

AMPICILLIN (AmpiciUinum)

Synonyms: Pentrexil, Abetaten," Acidocycline, Aniline, Acrocilin, Agnopen, Albercilin, Amil, Amecillin, Ampen, Ampeksin, Ampiphen, Ampilin, Ampiopenil, Amplenil, Amplital, Bactipen, Biampen, Binotal, Britapen, Broadocillin, Cimexillin, Diacyclin, Dicillin, Domicillin , Домипен, Эуроциллин, Фортапен, Грампенил, Истициллин, Лифициллин, Максибиотик, Максипред, Морепен, Негопен, Опицилин, Орацилина, Пенберин, Пенибрин, Пентрекс, Полицилин, Риомицин, Росциллин, Семициллин, Синтелин, Синпенйн, Тотациллин, Ультрабион, Вампен, Вексампил , Vidopen, Zimopen, Apo-Ampi, Mencillin, Standacillin, Dedoompil, Campicillin, etc.

Pharmachologic effect. ampicillin is a semisynthetic 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 affected by benzylpenicillin. In addition, it acts on a number of gram-negative microorganisms (Salmonella, Shigella, Proteus, Escherichia coli, Klebsiella pneumoniae /Friedlander's bacillus/, Pfeiffer's bacillus /influenza bacillus/) and is therefore considered as a broad-spectrum antibiotic and is used for diseases caused by mixed infections.

Ampicillin has no effect on penicillinase-forming (forming penicillinase, an enzyme that destroys penicillins) staphylococci that are resistant to benzylpenicillin, since 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 (ulcers) of the lungs, tonsillitis, peritonitis (inflammation of the peritoneum), cholecystitis (inflammation of the gallbladder), sepsis (blood poisoning by microbes from a purulent focus). inflammation), intestinal infections, postoperative soft tissue infections and other infections caused by microorganisms sensitive to it. The drug has high efficiency for infections urinary tract caused by Escherichia coli, Proteus, enterococci or a mixed infection, since it is excreted unchanged in the urine in high concentrations. Ampicillin also enters the bile in large quantities. The drug is effective in the treatment of gonorrhea.

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

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. When treated with ampicillin, allergic reactions may occur in the form of skin rash, urticaria, angioedema, etc., and in rare cases, anaphylactic shock (mainly with the administration of ampicillin sodium salt).

In case of allergic reactions it is necessary to stop administering the drug and carry out desensitizing (preventing or inhibiting allergic reactions) therapy. If signs of anaphylactic shock appear, urgent measures should be taken to remove the patient from this state.

With long-term treatment with ampicillin in weakened 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 B vitamins and vitamin C, and, if necessary, nystatin or levorin.

Contraindications. The drug is contraindicated in case of hypersensitivity to penicillin. For liver failure, use under monitoring of liver function; for bronchial asthma, hay fever and other allergic diseases only if absolutely necessary. At the same time, desensitizing agents are prescribed.

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

The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

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

Storage conditions.

AMPIOX (Ampioxum)

A combination drug 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 the 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's 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).

Indications for use. Used for infections of the respiratory tract and lungs (bronchitis - inflammation of the bronchi, pneumonia - inflammation of the lungs, etc.), tonsillitis, cholangitis (inflammation bile ducts), cholecystitis (inflammation of the gallbladder), pyelitis (inflammation of the renal pelvis), pyelonephritis (inflammation of the kidney tissue and renal pelvis), cystitis (inflammation of the bladder), infected wounds, skin infections, etc. Especially indicated in cases of severe disease: sepsis (blood infection by microbes from the focus of purulent inflammation), endocarditis (inflammation of the internal cavities of the heart), postpartum infection, etc. With an unknown antibiogram (the spectrum of antibiotic activity characterizing the sensitivity of pathogenic microorganisms to it) and an unisolated pathogen, with a mixed infection caused by sensitive and insensitive to benzylpenicillin by staphylococci or streptococci and gram-negative bacteria, for burn disease, kidney infections. Used for the prevention of 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 benzylpenicillin-resistant strains of gonococci.

When administered parenterally, a single dose of ampiox sodium for adults is 0.5-1.0 g, daily - 2-4 g.

For newborns, premature babies and children under 1 year of age, a daily dose of 100-200 mg per 1 kg of body weight is administered; children from 1 year to 7 years - 100 mg/kg per day; from 7 to 14 years - 50 mg/kg per day; Children over 14 years of age are prescribed the adult dose. In case of severe infection, 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 bottle 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 administered slowly over 2-3 minutes. For intravenous drip administration to 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. For drip administration to children, a 5-10% glucose solution (30-100 ml) is used as a solvent. It is administered intravenously for 5-7 days, followed by a transition (if necessary) to intramuscular administration. Solutions are used immediately after preparation; It is unacceptable to mix them with other medications.

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 - in 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 orally - nausea, vomiting, loose stools, allergic reactions. If necessary, desensitizing (preventing or inhibiting allergic reactions) agents are prescribed.

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

Release form. For parenteral administration, ampiox sodium is produced in bottles of 0.1; 0.2 or 0.5 g, indicating “Intravenous” or “Intramuscular” on the label. 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, Penbrok, Policillin, Ampicid.

Pharmachologic effect. Broad-spectrum semi-synthetic 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 and penetrates into the tissues and fluids of the body. It is excreted mainly by the kidneys. 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 respiratory tract: pneumonia (pneumonia), bronchitis (inflammation of the bronchi), pharyngitis (inflammation of the pharynx), etc.; urological diseases: pyelonephritis (inflammation of the kidney tissue 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 intestines), septic endocarditis (inflammation of the internal cavities of the heart due to the presence of microbes in the blood), meningitis (inflammation of the membranes of the brain), erysipelas, etc.

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

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

A solution for intramuscular administration is prepared ex tempore (before use) by adding 2 ml of sterile water to the contents of the bottle (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 administered slowly over 3-5 minutes (1-2 g over 10-15 minutes). For a single dose exceeding 2 g, the drug is administered intravenously. For intravenous drip administration, 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. For drip administration to children, a 5-10% glucose solution (30-50 ml depending on age) is used as a solvent. Solutions are used immediately after preparation; It is unacceptable to add other medications to them. The daily dose is divided into 3-4 injections. The duration of treatment is 5-7 days, followed by a transition (if necessary) to intramuscular administration.

Side effect. Allergic reactions.

Contraindications. Allergy to penicillin drugs, liver dysfunction.

The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

Release form. The bottles contain sterile powder complete with a solvent of 0.25 g, 0.5 g each; powder 5 g in a bottle for suspension; 10 mcg discs, 100 pieces per pack.

Storage conditions. List B. In a dry place, protected from light, at room temperature.

AMPICILLIN TRHYDRATE (Ampicillium trihydras)

Synonyms: A-Pen.

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

Indications for use. Same as for ampicillin.

Method of administration and dose. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora that caused the disease in this patient. Orally 0.5 g every 4-6 hours, for 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 place, protected from light, at room temperature.

CLONACOM-P

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

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

If renal function is impaired, a dose reduction is necessary.

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

The drug should be prescribed with caution to patients with a history of allergic reactions (medical history).

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

Storage conditions. List B. In a dry place, protected from light.

SULTAMICILLIN

Synonyms: Sulaillin, Betamp, Unazin.

A combined drug containing ampicillin-sodium and sulbactam-sodium in a 2:1 ratio.

Pharmachologic effect. Sulbactam sodium does not have pronounced antibacterial activity, but irreversibly inhibits (suppresses the activity) beta-lactamase (an enzyme that destroys the beta-lactam nucleus of the penis). When used together with penicillins, sulbactam protects the latter from hydrolysis (decomposition with water) and inactivation (partial or complete loss biological activity). Unazine (a combination of sulbactam + ampicillin) 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. Unasin is used for pneumonia (inflammation of the lungs), bronchitis (inflammation of the bronchi), otitis (inflammation of the ear cavity), sinusitis (inflammation of the paranasal sinuses), purulent surgical infections (abscesses - ulcers, phlegmon - acute, not clearly demarcated purulent inflammation, osteomyelitis - inflammation of the 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 divided doses, depending on the severity of the infection and at the discretion of the doctor. With a body weight of 30 kg or more - the same as for 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 usually lasts from 5 to 14 days, but can be extended if necessary. After normalization of temperature and disappearance of the main pathological symptoms, 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 extend the residence time of sulbactam and ampicillin in the blood plasma,

As a concomitant drug, 1 g of necid should be prescribed.

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

When treating any infection caused by hemolytic streptococci, to prevent the occurrence of rheumatism or glomerulonephritis (kidney disease), it is recommended to carry out antibacterial therapy within 10 days.

In patients with severe renal impairment (creatinine clearance / rate of blood clearance from the final product of nitrogen metabolism - creatinine / less than 30 ml/min), the dynamics of the release of sulbactam and ampicillin are subject to the same effect, therefore, the ratio of one to the other in plasma will remain constant. In such patients, the dose of sultamicillin is prescribed 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), nausea, vomiting, epigastric pain (the area of the abdomen located directly below the junction of the costal arches and the sternum), abdominal pain and colic. As with treatment with other ampicillin antibiotics, enterocolitis (inflammation of the small and large intestines) and pseudomembranous colitis (intestinal colic, characterized by attacks of abdominal pain and the release of large amounts of mucus in the stool) are observed in rare cases. Rash, itching and other skin reactions. Drowsiness, malaise, headache. In rare cases, anemia (decreased hemoglobin content in the blood), thrombocytopenia (decreased number of platelets in the blood), eosinophilia (increased number of eosinophils in the blood) and leukopenia (decreased level of leukocytes in the blood). These effects disappear after stopping treatment. There may be a transient increase in the levels of alanine transferase and asparagine transferase enzymes. When administered intramuscularly, pain at the injection site is possible. In isolated cases, the development of phlebitis (inflammation of a vein) after intravenous administration of the drug.

Contraindications. History of allergies to any of the penicillins (previous).

The drug should be prescribed with caution to patients with a history of allergic reactions.

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

Storage conditions. List B. In a place protected from light.

groups penicillins , depends on what kind of medicine we are talking about.

Currently, four groups are used:

natural penicillins;
semisynthetic penicillins;
aminopenicillins, which have an extended spectrum of action;
penicillins, which have a wide antibacterial spectrum of influence.

Release form

Injectable preparations are available, as well as penicillin tablets.

The injection product is produced in glass bottles, which are closed with rubber stoppers and metal caps. The vials contain different doses of penicillin. It is dissolved before administration.

Penicillin-ecmoline tablets are also produced for resorption and oral administration. Sucking tablets contain 5000 units of penicillin. In tablets for oral administration - 50,000 units.

Penicillin tablets with sodium citrate may contain 50,000 and 100,000 units.

pharmachologic effect

Penicillin - this is the first antimicrobial agent that was obtained using waste products of microorganisms as a basis. The history of this medicine begins in 1928, when the inventor of the antibiotic Alexander Fleming isolated it from a strain of the fungus species Penicillium notatum. In the chapter that describes the history of the discovery of penicillin, Wikipedia testifies that the antibiotic was discovered by accident; after the bacteria entered the culture from the external environment of a mold fungus, its bactericidal effect was noted. Later, the formula of penicillin was determined, and other specialists began to study how to obtain penicillin. However, the answer to the questions of what year this drug was invented and who invented the antibiotic is clear.

The further description of penicillin on Wikipedia testifies to who created and improved the drugs. In the forties of the twentieth century, scientists in the USA and Great Britain worked on the industrial production process of penicillin. The first use of this antibacterial drug for the treatment of bacterial infections occurred in 1941. And in 1945, for the invention of penicillin, the Nobel Prize was received by its creator Fleming (the one who invented penicillin), as well as by the scientists who worked on its further improvement - Flory and Chain.

Speaking about who discovered penicillin in Russia, it should be noted that the first samples were obtained in the Soviet Union in 1942 by microbiologists Balezina And Ermolyeva. Then industrial production of the antibiotic began in the country. In the late fifties, synthetic penicillins appeared.

When this drug was invented, for a long time it remained the main antibiotic used clinically throughout the world. And even after other antibiotics without penicillin were invented, this antibiotic remained an important drug for the treatment of infectious diseases. There is a statement that the medicine is obtained using cap mushrooms, but today there is different methods its production. Currently, so-called protected penicillins are widely used.

The chemical composition of penicillin indicates that the drug is an acid, from which various salts are subsequently obtained. Penicillin antibiotics include Phenoxymethylpenicillin (penicillin V), Benzylpenicillin (penicillin G), etc. The classification of penicillins involves their division into natural and semi-synthetic.

Biosynthetic penicillins provide bactericidal and bacteriostatic effects, inhibiting the synthesis of the cell wall of microorganisms. They act on some gram-positive bacteria ( Streptococcus spp., Staphylococcus spp., Bacillus anthracis, Corynebacterium diphtheria), some gram-negative bacteria ( Neisseria meningitidis, Neisseria gonorrhoeae), into anaerobic spore-forming rods ( Spirochaetaceae Actinomyces spp.) and etc.

The most active of penicillin drugs is . Strains demonstrate resistance to the influence of benzylpenicillin Staphylococcus spp., which produce penicillinase.

Penicillin is not effective means in relation to bacteria of the enteric-typhoid-dysenteric group, causative agents of tularemia, brucellosis, plague, cholera, as well as whooping cough, tuberculosis, Friedlander's, Pseudomonas aeruginosa and viruses, rickettsia, fungi, protozoa.

Pharmacokinetics and pharmacodynamics

The most effective method is administered intramuscularly. After such use, the active component reaches the patient very quickly. The highest concentration of the product is observed 30-60 minutes after application. After a single administration, only trace concentrations are determined.

It is quickly detected in muscles, wound exudate, in joint cavities, and in muscles.

A small amount of it is observed in the cerebrospinal fluid. A small amount will also enter the pleural cavities and abdominal cavity, so direct local action of the drug is required if necessary.

Penetrates to the fetus through the placenta. It is excreted from the body through the kidneys, so about 50% of the drug is eliminated. Also, part of it is excreted in bile.

If a patient takes penicillin tablets, he needs to take into account that when taken orally, the antibiotic is poorly absorbed, and part of it is destroyed under the influence of gastric juice and beta-lactamase, which is produced by intestines .

Indications for use

Antibiotics of the penicillin group, the names of which will be prompted directly by the attending physician, are used to treat diseases caused by microorganisms sensitive to penicillin:

pneumonia (lobar and focal);
pleural empyema;
septic endocarditis in acute and subacute forms;
sepsis ;
pyemia;
septicemia;
in acute and chronic form;
infectious diseases biliary and urinary tract;
purulent infectious diseases of the skin, mucous membranes, soft tissues;
erysipelas;
anthrax;
actinomycosis;
gynecological purulent-inflammatory diseases;
ENT diseases;
eye diseases;
gonorrhea, , blenorrhea.

Contraindications

Tablets and injections are not used in the following cases:

with high sensitivity to this antibiotic;
at , , and others;
when patients exhibit high sensitivity to sulfonamides, antibiotics, as well as other drugs.

Side effects

During use, the patient must understand what penicillin is and what side effects it can cause. During treatment, allergy symptoms sometimes appear. As a rule, such manifestations are associated with sensitization of the body due to earlier use of these drugs. Also may occur due to prolonged use of the drug. When using the medicine for the first time, allergies are observed less frequently. There is a possibility of sensitization of the fetus during pregnancy if a woman takes penicillin.

The following side effects may also develop during the course of treatment:

Digestive system: nausea, , vomit.
Central nervous system : neurotoxic reactions, signs of meningism, convulsions .
Allergy:, fever, rash on mucous membranes and skin, eosinophilia,. Cases recorded and death. If such manifestations occur, you should immediately administer intravenously.
Manifestations associated with chemotherapeutic effects: oral cavity, vaginal candidiasis.

Instructions for use of penicillin (Method and dosage)

Antimicrobial action is observed with local and resorptive action of penicillin.

Instructions for the use of penicillin in injections

The drug can be administered subcutaneously, intramuscularly, or intravenously. The drug is also injected into the spinal canal. For therapy to be as effective as possible, the dose must be calculated so that there is 0.1–0.3 units of penicillin in 1 ml of blood. Therefore, the drug is administered every 3-4 hours.

For treatment pneumonia , , cerebrospinal meningitis, etc. a special regimen is prescribed by the doctor.

Instructions for use of penicillin tablets

The dosage of penicillin tablets depends on the disease and on the treatment regimen prescribed by the attending physician. As a rule, patients are prescribed 250-500 mg, the drug should be taken every 8 hours. If necessary, the dose is increased to 750 mg. It is recommended to take tablets half an hour before meals or two hours after meals. The duration of treatment depends on the disease.

Overdose

It should be borne in mind that when taking large doses of penicillin, an overdose may occur, which may cause unpleasant symptoms as nausea, vomiting, diarrhea . But this condition is not life-threatening.

With intravenous administration of potassium salt in patients suffering from renal failure , can develop hyperkalemia .

When large doses of the drug are administered intraventricularly or intravenously, epileptic seizures may occur. But such a symptom appears in adult patients only after administration of at least 50 million units. medicines. In this case, the patient is prescribed barbiturates or benzodiazepines.

Interaction

When taking an antibiotic, the elimination process may slow down from the body due to inhibition of its tubular secretion.

Terms of sale

The drugs are sold by prescription; the doctor writes a prescription to the patient in Latin.

Storage conditions

It should be stored at a temperature of no more than 25 degrees, in a dry place.

Best before date

The shelf life of penicillin is 5 years.

special instructions

Before using penicillin, it is important to conduct tests and determine sensitivity to the antibiotic.

Prescribe the medicine with caution to people who have impaired renal function, as well as to patients with acute heart failure , people who have a tendency to allergic manifestations or severe sensitivity to cephalosporins .

If 3-5 days after the start of treatment there is no improvement in the patient’s condition, it is important to consult a doctor who will prescribe other antibiotics or combination treatment.

Since in the process of taking antibiotics there is a high probability of manifestations fungal superinfection , it is important to take antifungal medications during treatment. It is also important to consider that when using subtherapeutic doses of the drug or with an incomplete course of therapy, the emergence of resistant strains of pathogens is possible.

When taking the drug orally, you should take it with plenty of liquid. It is important to strictly follow the instructions on how to dilute the product.

During treatment with penicillins, it is necessary to strictly follow the prescribed treatment regimen and not skip doses. If a dose is missed, the dose should be taken as soon as possible. You cannot interrupt the course of treatment.

Since expired medicine may be toxic, it should not be taken.

Analogs

Level 4 ATX code matches:

There are a number of penicillin drugs; the most optimal antibiotic is determined by the doctor individually.

With alcohol

For children

It is used to treat children only after a doctor’s prescription and under his supervision.

Penicillin during pregnancy and lactation

It is advisable to prescribe an antibiotic during pregnancy only if the expected benefit outweighs the likelihood of negative effects. Lactation should be stopped during the period of taking the drugs, since the substance passes into the milk and can provoke the development of severe allergic manifestations in the child.

Penicillin antibiotics are universal drugs that allow a person to get rid of bacterial pathologies in a timely and effective manner. These medicines are based on mushrooms, living organisms that save millions of people around the world every year.

The history of the discovery of penicillin antibacterial agents dates back to the 30s of the 20th century, when scientist Alexander Fleming, who was studying bacterial infections, accidentally identified an area in which bacteria did not grow. As additional research showed, such a place in the bowl was the mold that usually covers stale bread.

As it turned out, this substance easily killed staphylococci. After additional research, the scientist was able to isolate penicillin in its pure form, which became the first antibacterial agent.

The principle of action of this substance is as follows: during bacterial cell division, to restore its own damaged membrane, these substances use elements called peptidoglycans. Penicillin does not allow this substance to form, which is why bacteria lose the ability not only to reproduce, but also to develop further, and are destroyed.

However, not everything went smoothly; after some time, bacterial cells began to actively produce an enzyme called beta-lactamase, which began to destroy beta-lactams, which form the basis of penicillins. To solve this problem, additional components were added to the composition of antibacterial agents, for example, clavulonic acid.

Spectrum of action

After penetration into the human body, the drug easily spreads throughout all tissues and biological fluids. The only areas where it penetrates in very small quantities (up to 1%) are the cerebrospinal fluid, organs of the visual system and the prostate gland.

The drug is eliminated outside the body through the kidneys, after about 3 hours.

The antibiotic effect of the natural variety of the drug is achieved by combating the following bacteria:

gram-positive (staphylococci, pneumococci, streptococci, bacilli, listeria);
gram-negative (gonococci, meningococci);
anaerobic (clostridia, actiminocetes, fusobacteria);
spirochetes (pallid, leptospira, borrelia);
effective against Pseudomonas aeruginosa.

Penicillin antibiotics are used to treat various pathologies:

infectious diseases of moderate severity;
diseases of ENT organs (scarlet fever, tonsillitis, otitis media, pharyngitis);
infections respiratory organs(bronchitis, pneumonia);
diseases of the genitourinary system (cystitis, pyelonephritis);
gonorrhea;
syphilis;
skin infections;
osteomyelitis;
blenorrhea occurring in newborns;
leptospirosis;
meningitis;
actinomycosis;
bacterial lesions of mucous and connective tissues.

Antibiotics classification

Penicillin antibiotics have different ways production, as well as properties, which allows us to divide them into 2 large groups.

Natural ones that were discovered by Fleming.
Semi-synthetic, were created a little later in 1957.

Experts have developed a classification of antibiotics from the penicillin group.

Natural ones include:

phenoxylmethylpenicillin (Ospen, as well as its analogues);
benzathine benzylpenicillin (Retarpen);
benzylpenicillin sodium salt (Procaine penicillin).

The group of semi-synthetic products usually includes:

aminopenicillins (amoxicillins, ampicillins);
antistaphylococcal;
antipeseudomonas (ureidopenicillins, carboxypenicillins);
inhibitor-protected;
combined.

Natural penicillins

Natural antibiotics have one weakness: they can be destroyed by beta-lactamase, as well as gastric juice.

Medicines classified in this group are in the form of solutions for injection:

with extended action: this includes a penicillin substitute - bicillin, as well as novocaine salt of benzylpenicillins;
with little effect: sodium and potassium salts of benzylpenicillins.

Long-acting penicillins are administered intramuscularly once a day, and novocaine salt is administered 2 to 3 times a day.

Biosynthetic

The penicillin series of antibiotics consists of acids, which, through the necessary manipulations, are combined with sodium and potassium salts. Such compounds are characterized by rapid absorption, which allows them to be used for injection.

As a rule, the therapeutic effect is noticeable within a quarter of an hour after administration of the drug, and it lasts for 4 hours (therefore, the drug requires repeated administration).

To prolong the effect of natural benzylpenicillin, it was combined with novocaine and some other components. The addition of novocaine salts to the main substance made it possible to lengthen the achieved therapeutic effect. Now it has become possible to reduce the number of injections to two or three per day.

Biosynthetic penicillins are used to treat the following diseases:

chronic rheumatism;
syphilis;
streptococcus.

For the treatment of moderately severe infections, phenoxylmethylpenicillin is used. This variety is resistant to the destructive effects of hydrochloric acid, which is contained in gastric juice.

This substance is available in tablets, which can be taken orally (4-6 times a day). Biosynthetic penicillins work against most bacteria, with the exception of spirochetes.

Semi-synthetic antibiotics belonging to the penicillin series

This type of medication includes several subgroups of medications.

Aminopenicillins actively work against: enterobacteria, Haemophilus influenzae, Helicobacter pylori. These include the following drugs: ampicillin series (Ampicillin), amoxicillin (Flemoxin Solutab).

The activity of both subgroups of antibacterial agents extends to similar types of bacteria. However, ampicillins are not very effective against pneumococci, but some of their varieties (for example, Ampicillin trihydrate) easily cope with Shigella.

Drugs in this group are used as follows:

Ampicillin by intravenous and intramuscular infections.
Amoxicillin by oral administration.

Amoxicillins actively fight Pseudomonas aeruginosa, but, unfortunately, some of the representatives of this group can be destroyed under the influence of bacterial penicillinases.

The antistaphylococcal subgroup includes: Methicillin, Naficillin, Oxacillin, Fluxocillin, Dicloxacillin. These drugs are resistant to staphylococci.

The antipseudomonas subgroup, as the name implies, actively fights Pseudomonas aeruginosa, which provokes the appearance of severe forms of tonsillitis and cystitis.

This list includes two types of drugs:

Carboxypenicillins: Carbecin, Timentin (for the treatment of severe lesions of the urinary tract and respiratory organs), Pyopen, disodium Carbinicillin (used only in adult patients by intramuscular, intravenous administration).
Ureidopenicillins: Picillin piperacillin (used more often for pathologies caused by Klebsiella), Securopen, Azlin.

Combination antibiotics from the penicillin series

Combination drugs are also called inhibitor-protected, which means that they block bacterial beta-lactamases.

The list of beta-lactamase inhibitors is very large, the most common are:

clavulonic acid;
sulbactam;
tazobactam.

For the purpose of treating pathologies of the respiratory and genitourinary systems, the following antibacterial compounds are used:

amoxicillin and clavulonic acid (Augmentin, Amoxil, Amoxiclav);
ampicillin and sulbactam (Unasin);
ticarcillin and clavulonic acid (Timentin);
piperacillin and tazobactam (Tazocin);
ampicillin and oxacillin (Ampiox sodium).

Penicillins for adults

Semi-synthetic drugs are actively used to combat sinusitis, otitis, pneumonia, pharyngitis, and tonsillitis. For adults there is a list of the most effective drugs:

Augmentin;
Amoxicar;
Ospamox;
Amoxicillin;
Amoxiclav;
Ticarcillin;
Flemoxin Solutab.

To get rid of pyelonephritis (purulent, chronic), cystitis (bacterial), urethritis, salpingitis, endometritis, use:

Augmentin;
Honeyclave;
amoxiclav;
Ticarcillin with clavulonic acid.

When a patient suffers from an allergy to penicillin drugs, he may have an allergic reaction in response to taking such drugs (this can be simple hives, or a severe reaction leading to anaphylactic shock). If such reactions occur, the patient is advised to use drugs from the macrolide group.

Ampicillin;
Oxacillin (if the pathogen is staphylococcus);
Augmentin.

In case of intolerance penicillin group, the doctor may recommend the use of a group of reserve antibiotics in relation to penicillins: cephalosporins (Cefazolin) or macrolides (Clarithromycin).

Penicillins for the treatment of children

Many antibacterial agents have been created based on penicillins, some of them are approved for use in patients childhood. These drugs are characterized by low toxicity and high efficiency, which allows their use in young patients.

For children, inhibitor-protected drugs are used orally.

The following antibiotics are prescribed to children:

Flemoklav Solutab;
Augmentin;
Amoxiclav;
Amoxicillin;
Flemoxin.

Non-penicillin forms include Vilprafen Solutab, Unidox Solutab.

The word “solutab” means that the tablets dissolve under the influence of liquid. This fact makes it easier for young patients to take medications.

Many antibiotics of the penicillin group are produced in the form of suspensions that look like a sweet syrup. To determine the dosage for each patient, it is necessary to take into account his age and body weight.

Assign antibacterial agents Only a specialist can do this for children. Self-medication with the use of such drugs is not allowed.

Contraindications side effects of penicillins

The use of penicillin drugs, despite all their effectiveness and benefits, is not possible for all categories of patients; the instructions for the drugs contain a list of conditions when the use of such drugs is prohibited.

Contraindications:

hypersensitivity, personal intolerance or strong reactions to components medicine;
previous reactions to cephalosporins, penicillins;
dysfunction of the liver and kidneys.

Each drug has its own list of contraindications, indicated in the instructions; you should familiarize yourself with it before starting drug therapy.

As a rule, penicillin antibiotics are well tolerated by patients. But, in rare cases, more negative manifestations may occur.

Side effects:

allergic reactions are manifested by skin rash, urticaria, tissue swelling, itching, other rashes, Quincke's edema, anaphylactic shock;
from the gastrointestinal tract, nausea, epigastric pain, and digestive disorders may appear;
circulatory system: increase in indicators blood pressure, heart rhythm disturbances;
liver and kidneys: development of insufficiency in the functioning of these organs.

To prevent the development of adverse reactions, it is very important to take antibiotics only as prescribed by the doctor, be sure to use auxiliary agents (for example, probiotics) that he recommends.

- penicillins, cephalosporins, carbopenems - form the basis of modern chemotherapy. They have a bactericidal effect due to the destruction of peptidoglycan, a mucopeptide of the bacterial cell wall. The drugs have synergism against gram-negative flora with aminoglycosides and fluoroquinolones, but they cannot be mixed in the same syringe or infusion system due to physicochemical incompatibility. To overcome resistance, they are combined with beta-lactamase inhibitors.

Side effects: allergic rashes, eosinophilia, less often other immediate hypersensitivity reactions (angioedema, urticaria), anaphylactic shock in children is extremely rare, as are neutro- and thrombocytopenia, hemolytic anemia, interstitial nephritis, phlebitis at the injection site. Ampicillin and cephalosporins rarely cause. Only benzylpenicillin sodium salt is administered endolumbarally - extremely carefully for health reasons. When prescribing to patients with renal failure, the content of potassium and sodium in the preparations is taken into account.

Contraindications. Individuals with a history of anaphylaxis, urticaria, or severe rash immediately after penicillin administration are at risk of developing a reaction immediate type to other drugs in this group and should not be administered to them. Patients allergic to a penicillin drug will react allergically to all penicillins, but only 10% of them will react allergically to cephalosporins and other beta-lactams. Individuals with a history of minimal rash (not a confluent rash on a small surface area of the body) or a rash that occurred 72 hours or more after penicillin administration may not be allergic to penicillins; they should not refuse its use for serious infections, providing everything for the treatment of anaphylaxis.

Penicillins

Penicillins penetrate well into body tissues and fluids, incl. in the CSF during inflammation of the meninges and the administration of high doses. They are excreted mainly in the urine. Carbenicillin has lost its importance; ticarcillin and ureidopenicillins are used only in combination with lactamase inhibitors.

Drug interactions. They increase the risk of bleeding when used with direct and indirect anticoagulants, NSAIDs, and salicylates. When taken together with potassium supplements, potassium-sparing diuretics, ACE inhibitors, hyperkalemia is possible. Increases the toxicity of methotrexate.

Natural penicillins

Benzylpenicillin(in Russia more often called penicillin) is a low-toxic drug that creates high concentrations(at a dose of 50 mg/kg IM - 15-25 mcg/ml in the blood and 60-70% of it in the tissues). Pneumococci in Russia retain 90-95% sensitivity to penicillin; sensitivity is lower in children in kindergartens and, especially, in boarding schools. Benzylpenicillin derivatives have the same antibacterial spectrum; Due to its lower effectiveness, phenoxymethylpenicillin should not be used to treat serious infections. In children with otitis and uncomplicated otitis, phenoxymethylpenicillin-benzathine (Ospen-syrup) has proven its worth; its concentration in the blood at a dose of 50 mg/kg is 4-6 mcg/ml.

Benzathine benzylpenicillin provides a prolonged effect when administered intramuscularly; it is used for infections caused by highly sensitive pathogens (GABHS, spirochete pallidum) to maintain a low therapeutic concentration for a long time.

Side effects. Jarisch-Herzheimer reaction (treatment of syphilis and other infections caused by spirochetes) - associated with the release of endotoxins.

Benzylpenicillin

Indications. Spicy otitis media, pneumococcal infection (, meningitis), streptococcal infections (acute, erysipelas, scarlet fever, endocarditis, necrotizing fasciitis), meningococcal infection, tick-borne borreliosis, leptospirosis, anthrax; actinomycosis, gas gangrene, syphilis.

Dosing: IM or IV slowly or by infusion: children from 1 month to 12 years, 100-200 thousand units/kg per day in 2-3 doses, for severe diseases - up to 500,000 units/kg/day vital indications (see below). Syphilis - see Section 6.3.

Side effects. At doses >20 million units/day - DNS disorders, increased creatinine levels.

Release form: powder for the preparation of solution for intravenous and intramuscular injections of 250,000, 500,000 and 1 million units (1 mg = 1610 units) (Benzylpenicillin - Russia)

Phenoxymethylpenicillin - Penicillin V (phenoxymethylpenicillin)

Indications: Streptococcal pharyngitis, secondary prevention of rheumatism; prevention of relapses of pneumococcal meningitis after traumatic brain injury, pneumococcal infection in children after splenectomy or with hypogammaglobulinemia; for the treatment of acute otitis media; erysipelas.

Dosage: orally, children over 12 years old - 500 mg every 6 hours, children under 1 year old - 50 mg/kg/day, from 1 to 6 years old - 30 mg/kg/day, 6-12 years old - 20-30 mg/day kg/day in 3-4 doses. Secondary prevention of rheumatism: orally, children - 500 mg 1-2 times a day.

Side effects: See above, also nausea and diarrhea.

Release form: Phenoxymethylpenicillin-benzathine syrup 750 mg/5 ml (Ospen-750 - Sandoz, Austria), tablet. 100 mg, 250 mg, dragee 100,000 units, powder for suspension: 250 mg/5 ml, 60 mg/ml (Phenoxymethylpenicillin - Russia).

Benzathine benzylpenicillin

Indications: acute streptococcal group A, erysipelas, prevention of rheumatism, treatment of diphtheria carriers; syphilis.

Contraindications: neurosyphilis. Do not administer intravenously or intra-arterially.

Carefully: renal failure.

Dosing. In the treatment of acute tonsillitis, scarlet fever, erysipelas, wound infections in the acute phase, therapy begins with penicillin, benzathine continues with benzyl-penicillin: 1-2 injections of 1.2 million units once a week. For rheumatism, 2.4 million units intramuscularly every 15 days. For the prevention of scarlet fever in children under 7 years of age (or weighing up to 25 kg) 600,000 units, over 7 years of age (or weighing more than 25 kg) - 1,200,000 units. For the treatment of tonsillitis and the treatment of diphtheria carriers, these doses are once, for the prevention of rheumatism - same doses every 2 weeks, Syphilis: see Section 6.3.

Side effects: Rarely embolism; pain and inflammation at the injection site.

Release form: Por. d/prig. solution for intramuscular injection, benzathine benzylpenicillin in bottles: 300, 600 thousand, 1.2 and 2.4 million units. (Bicillin-1 (Russia); 1.2 and 2.4 million units (Retarpen, Extencillin - Sandoz, Austria).

Antistaphylococcal penicillins

Oxacillin

Oxacillin is used to treat infections caused by staphylococci, incl. producing beta-lactamase, but not MRSA. The rest of the spectrum of action is the same as that of natural penicillins, but the sensitivity of pneumococci and streptococci to it is lower than to penicillin. Bioavailability when taken orally is low.

Indications: Infectious diseases caused by staphylococci, incl. producing beta-lactamase: acute sinusitis, septicemia, abscesses, phlegmon, cholecystitis, infected burns, bacterial endocarditis.

Carefully: bronchial asthma, chronic renal failure; liver failure.

Dosage: IM or IV for newborns - 20-40 mg/kg/day for 2 injections, for children 100-150 (up to 200) mg/kg/day - max, up to 12 g/day for 2-4 injections.

Side effects. Rarely - liver dysfunction, jaundice at high doses (in adults >12 g/day). Fever, nausea, vomiting, eosinophilia, anemia, neutropenia, transient hematuria in children.

Release form: Lyophilisate d/prig. solution for intravenous and intramuscular administration 250 mg, 500 mg (Oxacillin - Russia).

Aminopenicillins

Ampicillin and amoxicillin, unlike natural pencillins, act on some gram-negative microorganisms, in particular, H. influenzae, which in Russia remains sensitive to aminopenicillins due to the low frequency of production of beta-lactamases. Ampicillin acts on E. fecalis, which in Russia is 90% sensitive to it. Activity against Salmonella and Shigella varies geographically. The value of empirical therapy with IMG1 is limited due to the high frequency of secondary resistance of E. coli. The drugs are inactivated by beta-lactamase produced by S. aureus, M. catarrhalis, N. gonorrhoeae, and enterobacteria.

Amoxicillin acts better than ampicillin and penicillin on; when taken orally, it has 2-2.5 times greater bioavailability than ampicillin (especially in the form of Solutab dispersible tablets), gives higher concentrations in plasma and tissues and is less likely to cause diarrhea. Ampicillin is used only parenterally.

Contraindications. Leukemoid reactions of the lymphatic type, lymphocytic leukemia.

Carefully. Acute (possible mononucleosis), erythematous rashes characteristic of infectious mononucleosis, lactation. Increased diaper rash - does not prevent repeated use.

Side effects. A feature of aminopenicillins is the development (about 7% of courses) of a maculopapular (“ampicillin”) rash (especially against the background of infection with the Ensteia-Barra virus - most recognize its non-allergic nature) on days 3-5 of treatment; the rash disappears without stopping the drug. Rarely vomiting, diarrhea, very rarely -.

Interaction. Reduce the contraceptive effect of estrogen-containing drugs. Allopurinol increases the risk of ampicillin rash.

Ampicillin

Indications. Acute otitis media, acute sinusitis, community-acquired, UTI, IZhP, shigellosis, salmonellosis, meningitis, bacterial endocarditis, septic infection of newborns (in combination with gentamicin), erysipelas.

Dosing: IM, slow IV or IV infusion. 100-200 mg/kg/day, meningitis, endocarditis - 200-300 mg/kg/day. (up to 8-12 g/day).

Release form: Powder for the preparation of solution for injection 250 mg, 500 mg, 1 and 2 g (Ampicillin - Russia).

Amoxicillin

Indications: upper respiratory tract infections (sinusitis, acute otitis media),: UTI. systemic tick-borne borreliosis (Lyme disease); prevention of endocarditis: eradication of H. pylori, dysentery, salmonellosis, salmonellosis carriage in the presence of sensitivity.

Dosage: orally, children 45 mg/kg/day, dose if there is a possibility of pneumococcal resistance (antibiotic treatment, visiting a child care facility) - 80-100 mg/kg/day. The course of treatment is 5-12 days.

Release form: dispersible tablets. 0.125, 025, 0.5 and 1 g. caps., tab. 0.25 and 0.5 g; table, p/obol. 0.5 and 1.0 g; por. and gran, d/prig. susp. 125 mg/5 ml and 250 mg/5 ml: por. d/prig. drops, 0.1 g/ml (Flemoxin Solutab - Astellas Pharma Europe B.B.. Netherlands. Amoxicillin - Russia Ospamox - Sanoz, Austria. Hiconcil - KRKA, Slovenia).

Inhibitor-protected penicillins

They are a combination penicillin drug and an inhibitor (beta-lactamase. The most widely used is amoxicillin/clavulanate, active against resistant H. influenzae, E. coli, M. catarrhalis, S. aureus, (but not MRSA); more active against pneumococci with reduced sensitivity than ceftriaxone. Ticarcillin/clavulanate is effective against Serratia, Citrobacter, as well as some strains of P. aeruginosa and Acinetobacter. The addition of beta-lactamase inhibitors does not overcome the resistance of Pseudomonas aeruginosa. Only 20-30% of P. aeruginosa strains are sensitive to ticarcillin. All drugs bactericidal against anaerobes, including B. fragilis, Prevotella melaninogenicus. Used for perioperative prophylaxis in abdominal surgery. Sulbactam has its own clinically significant antibacterial activity against Neisseria and Acinetobacter.

Side effects. Nausea and vomiting, diarrhea, rarely - hepatitis, cholestatic jaundice. There have been cases of vasculitis, serum sickness, erythema multiforme (including Stevens-Johnson syndrome), exfoliative; Surface plaque on teeth is possible when using the suspension.

Interaction. Antacids, laxatives, and glucosamine reduce the absorption of protected penicillins.

Amoxicillin/clavulanic acid

Indications. Infections of the respiratory tract, skin and soft tissues, bones, genitourinary and abdominal, caused by beta-lactamase-producing microorganisms. As a drug of first choice, it is used in children recently discharged from hospital or treated with antibiotics for a period of 3 months before the present illness, as well as in groups increased risk on the resistance of pneumotropic flora (boarding schools, kindergartens). Drug of choice for anaerobic infections (Vincenta, lung abscess, deep wounds), abscesses, fasciitis and phlegmon, animal bites, dental infections, as well as for antibacterial prophylaxis during organ operations abdominal cavity and small pelvis.

Contraindications. History of jaundice or hepatic dysfunction associated with the use of clavulanic acid. Increased diaper rash - does not prevent repeated use.

Carefully. Kidney, liver failure; erythematous rashes characteristic of infectious mononucleosis, chronic lymphocytic leukemia.

Dosage (for amoxicillin): Orally for children under 12 years of age - 45 mg/kg/day in 2 divided doses (up to 750 mg/day), over 12 years of age and adults - 1750 mg per day in 2 divided doses (875×2). If necessary, the dose is increased to 80-100 mg/kg/day, preferably using drugs with a ratio of amoxicillin to clavulanate of 7:1 or higher. IV for newborns - 60 mg/kg/day for 2 injections, for children from 1 month. up to 12 years old - 40-60 (up to 90-120) mg/kg/day, over 12 years old and adults - 3-4 (up to 6) g/day for 3-4 administrations.

Release form. Amoxicillin to clavulanate ratio:

2:1 - table. 0.25/0.125 g (Augmentin - original amoxicillin/clavulanate produced by GlaxoSmithKline, UK, Medoklav - Medohsmi, Cyprus, Amoxiclav - Lek, Slovenia);
4:1 - table. 500/125 mg, por. d/prig. susp. 125 mg/31.25 mg/5 ml, 250 mg/62.5 mg/5 ml (Amoxiclav, Augmentin, Medoclav);
4:1 - table. dispersible 125 mg/31.25 mg; 250 mg/62.5 mg and 500 mg/125 mg (Flemoklav Solutab - Astellas Pharma Europe B.V., the Netherlands). 5:1 - time. for IV solution 500/100 mg, 1000/200 mg (Augmentin, Amoxiclav, Medoclav) 7:1 - table. 0.875/0.125 g (Amoxiclav)
7:1 - table. 0.875/0.125 g, por. d/prig. susp. 200/28.5 mg/5 ml and 400/57 mg/5 ml (Augmentin - dosing forms 2 times a day with the best ratio of amoxicillin and clavulanate).

Ampicillin/sulbactam

Indications and contraindications. Same as amoxicillin/clavulanate, hypersensitivity to sulbactam.

Dosing. Children of all ages, including newborns - 150 mg/kg/day, (100 mg/kg/day ampicillin and 50 mg/kg/day sulbactam) for 3-4 (for newborns - for 2) administrations, adults - 1.5-12 g per day for 2-4 administrations IM or IV.

Release forms: por. d/prig. solutions 0.5/0.25 g, 1/0.5 g, 2/1 g (Unasin-Pfizer, USA).

Ticarcillin + clavulanic acid (ticarcilliri/clavulanic acid)

Indications. Severe (lungs, abdominal cavity, bones, soft tissues, urinary tract), caused by multiresistant gram-negative flora, including anaerobic.

Dosage (for ticarcillin): children over 3 months. with a weight of up to 60 kg - 200-300 mg/kg/day for 4-6 injections, for children weighing 60 kg or more, as well as adults - 12-18 g for 4-6 injections intravenously (in 30 minutes) .

Side effects: dizziness, neutropenia, hypokalemia.

Release form: liof. por. d/prig. 1500/100 mg and 3000/200 mg (15:1) (Timentin-GlaxoSmith-Klein, UK).

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 are classified as 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 structure of the molecule. Beta-lactams include penicillins, cephalosporins, carbapenems, and monobactams. Beta-lactams are the largest group of antimicrobial drugs used in clinical practice, occupying a leading place 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 filamentous green mold fungus (Penicillium notatum) cause the death of staphylococci in cell culture. Active substance A fungus with antibacterial activity was called penicillin by A. Fleming. In 1940, in Oxford, a group of researchers led by H.W. Flory and E.B. Cheyna isolated significant amounts of the first penicillin from culture in pure form. Penicillium notatum. In 1942, the outstanding domestic researcher Z.V. Ermolyeva received penicillin from a mushroom Penicillium crustosum. Since 1949, virtually unlimited quantities of benzylpenicillin (penicillin G) have become available for clinical use.

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

To the most general properties penicillins include: low toxicity, 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 bacterial cell walls.

The cell wall of bacteria has a rigid structure; it gives microorganisms their shape and protects them from destruction. Its basis is a heteropolymer - peptidoglycan, consisting of polysaccharides and polypeptides. Its cross-linked network structure gives the cell wall strength. Polysaccharides include amino sugars such as N-acetylglucosamine, as well as N-acetylmuramic acid, which is found only in bacteria. Associated with amino sugars are 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 enzyme transpeptidase. Transpeptidase is one of the penicillin-binding proteins with which beta-lactam antibiotics interact. Penicillin-binding proteins—enzymes that take part in the final stages of bacterial cell wall formation—in addition to transpeptidases, include carboxypeptidases and endopeptidases. All bacteria have them (for example, Staphylococcus aureus there are 4 of them, Escherichia coli- 7). Penicillins bind to these proteins with at different speeds with the formation of a covalent bond. In this case, inactivation of penicillin-binding proteins occurs, the strength of the bacterial cell wall is disrupted 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 media of the eye and the secretion of the prostate gland - here the concentrations of penicillins are low. The concentration of penicillins in the cerebrospinal fluid may vary depending on the conditions: normally - less than 1% serum, with inflammation it can increase to 5%. Therapeutic concentrations in the cerebrospinal fluid are created during meningitis and the administration of drugs in high doses. Penicillins are quickly eliminated from the body, mainly by the kidneys through glomerular filtration and tubular secretion. Their half-life is short (30-90 min), the concentration in urine is high.

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

According to the classification presented by D.A. Kharkevich (2006), penicillins are divided as follows (classification is based on a number of characteristics, including differences in production routes):

I. Penicillin preparations 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. Isoxazolepenicillins (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 production, spectrum of action, as well as combination with beta-lactamases were taken into account when creating the classification given in the Federal Guide (formulary system), issue 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 in relation Pseudomonas aeruginosa:

Carboxypenicillins:

ticarcillin.

Ureidopenicillins:

azlocillin,

piperacillin.

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

amoxicillin/clavulanate,

ampicillin/sulbactam,

ticarcillin/clavulanate.

Natural (natural) penicillins - These are narrow-spectrum antibiotics that affect gram-positive bacteria and cocci. Biosynthetic penicillins are obtained from the culture medium on which certain strains of molds 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, and therefore are ineffective for the treatment of staphylococcal infections, because in most cases, staphylococci produce beta-lactamases. They are effective primarily 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 microorganisms are usually resistant, with the exception of Haemophilus ducreyi And Pasteurella multocida. Penicillins are ineffective against viruses (causative agents of influenza, polio, smallpox, etc.), mycobacterium tuberculosis, the causative agent of amebiasis, rickettsia, and fungi.

Benzylpenicillin is active mainly against gram-positive cocci. The antibacterial action spectra 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 moderate infections. The activity of penicillin preparations is determined biologically by their antibacterial effect on a specific strain Staphylococcus aureus. The activity of 0.5988 mcg of chemically pure crystalline sodium salt of benzylpenicillin is taken as a unit of action (1 unit).

Significant disadvantages of benzylpenicillin are its instability to beta-lactamases (with enzymatic cleavage of the beta-lactam ring by beta-lactamases (penicillinases) to form penicillanic acid, the antibiotic loses its antimicrobial activity), insignificant absorption in the stomach (requiring injection routes of administration) and relatively low activity against most gram-negative microorganisms.

Under normal conditions, benzylpenicillin preparations penetrate poorly into the cerebrospinal fluid, but with inflammation of the meninges, 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 quickly eliminated from the body and requires frequent injections. In this regard, poorly soluble salts of benzylpenicillin (including novocaine salt) and benzathine benzylpenicillin were proposed for use in medical practice.

Prolonged forms of gasylpenicillin, or depot-disylline: Bicillin-1 (Benzatin gasolinecylline), as well as combined drugs based on them-bicillin-3 (Benzatin gasylpenicillin sodium + gasylpenicillin Novokaina SC), bicillin-5 (gasoline-gasoline gasolinetylpyillin + gasylpenicillin 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 benzylpenicillin salts are used parenterally, because 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 extent. Phenoxymethylpenicillin differs in chemical structure from benzylpenicillin in the presence of a phenoxymethyl group in the molecule instead of a benzyl group.

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, when it is necessary to maintain effective concentrations in the body for a long time. They are used for syphilis and other diseases caused by Treponema pallidum (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 semisynthetic drugs began on its basis.

6-Aminopenicillanic acid is 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 significant pharmacological properties the resulting drug molecule. In natural penicillins, the structure of the radical depends on the composition of the medium in which they grow Penicillium spp.

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

Penicillinase (beta-lactamase) resistant;

Acid-resistant, effective when administered orally;

Having a wide spectrum of action.

Isoxazolepenicillins (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 effectiveness 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.

In terms of activity against gram-positive cocci (including staphylococci that do not produce beta-lactamase), isoxazolepenicillins, incl. oxacillin are significantly inferior to natural penicillins, therefore, for diseases caused by microorganisms sensitive to benzylpenicillin, they are less effective compared to the latter. Oxacillin does not show activity 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 isoxazolepenicillins and benzylpenicillin:

Rapid, but not complete (30-50%) absorption from the gastrointestinal tract. These antibiotics can be used both parenterally (IM, IV) and orally, but 1-1.5 hours before meals, because they have low resistance to hydrochloric acid;

High degree of binding to plasma albumin (90-95%) and the impossibility of removing isoxazolepenicillins from the body during hemodialysis;

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

The main clinical value of oxacillin is the treatment of staphylococcal infections caused by penicillin-resistant strains Staphylococcus aureus(except infections caused by methicillin-resistant Staphylococcus aureus, MRSA). It should be taken into account that strains are common in hospitals Staphylococcus aureus, resistant to oxacillin and methicillin (methicillin - the first penicillinase-resistant penicillin, discontinued). Nosocomial and community-acquired strains Staphylococcus aureus, resistant to oxacillin/methicillin, are usually multidrug-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 the BBB (its concentration in the cerebrospinal fluid is sufficient to treat staphylococcal meningitis), is excreted primarily in bile (the maximum concentration in bile is much higher than the serum concentration), and to a lesser extent by the kidneys. Can be used orally and parenterally.

Amidinopenicillins - These are penicillins with 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 founder of the aminopenicillin group. In relation to gram-positive bacteria, ampicillin, like all semisynthetic 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 sensitive strains of enterobacteria, Escherichia coli, Proteus mirabilis, Salmonella spp., Shigella spp., Haemophilus influenzae; act better than natural penicillins on Listeria monocytogenes and sensitive enterococci.

Of all the oral beta-lactams, amoxicillin has the greatest 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).

Combination drugs are available, 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 absorbed more quickly and well 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 concentrations are 2 times higher than those in the blood.

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

Possibility of administration internally;

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);

Multiplicity of appointment combination drugs- 2-3 times a day.

The main indications for prescribing aminopenicillins are infections of the upper respiratory tract and ENT organs, kidney and urinary tract infections, gastrointestinal infections, 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 administration of aminopenicillins is infectious mononucleosis.

Antipseudomonas penicillins

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

Carboxypenicillins are antibiotics that have a spectrum of antimicrobial action similar to aminopenicillins (except for the effect on Pseudomonas aeruginosa). Carbenicillin is the first antipseudomonas penicillin, and is 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 decreasing. Although they have a broad spectrum of action, they are inactive against most strains Staphylococcus aureus, Enterococcus faecalis, Klebsiella spp., Listeria monocytogenes. Almost do not pass through the BBB. The frequency of administration is 4 times a day. Secondary resistance of microorganisms quickly develops.

Ureidopenicillins - These are also antipseudomonas 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 against Pseudomonas aeruginosa. They are also used in the treatment of infections caused by Klebsiella spp.

All antipseudomonas penicillins are destroyed by beta-lactamases.

Pharmacokinetic features of ureidopenicillins:

Administered only parenterally (i.m. and i.v.);

Not only the kidneys, but also the liver take part in excretion;

Frequency of application - 3 times a day;

Secondary bacterial resistance develops rapidly.

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

The main indications for these two groups of antipseudomonas 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 microbial resistance can develop to many of them.

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 semisynthetic penicillins are resistant to 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 to create inhibitor-protected penicillins.

Beta-lactamase inhibitors, like penicillins, are beta-lactam compounds but have minimal antibacterial activity on their own. These substances irreversibly bind 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 makes it possible to increase the stability 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 the penicillins they contain, only the level of acquired resistance differs. Inhibitor-protected penicillins are used to treat infections of various locations 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 pathogens sensitive to them. They are mainly used for upper respiratory tract infections, in the treatment of sore throat, scarlet fever, otitis, sepsis, syphilis, gonorrhea, gastrointestinal infections, urinary tract infections, etc.

Penicillins should only be used 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 stopping treatment too early can lead to the development of resistant strains of microorganisms (this is especially true for natural penicillins). If resistance occurs, therapy with other antibiotics should be continued.

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

Solutions for topical use are prepared ex tempore. Penicillins are used to treat gonococcal conjunctivitis (benzylpenicillin), keratitis (ampicillin, benzylpenicillin, oxacillin, piperacillin, etc.), canaliculitis, especially caused by actinomycetes (benzylpenicillin, phenoxymethylpenicillin), abscess and orbital phlegmon (ampicillin/clavulanate, ampicillin/s ulbactam, phenoxymethylpenicillin and etc.) and other eye diseases. In addition, penicillins are used to prevent infectious complications in injuries of the eyelids and orbit, especially when a foreign body penetrates into the orbital tissue (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 unjustified due to the high level of resistance of uropathogenic strains.

Side 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 related to hypersensitivity. Allergic reactions are observed in a significant number of patients (according to various sources, from 1 to 10%). Penicillins are more likely than drugs from other pharmacological groups to cause drug allergies. In patients who have had a history of allergic reactions to the administration of penicillins, with subsequent use these reactions are observed in 10-15% of cases. Less than 1% of people who have not previously experienced such reactions have an allergic reaction to penicillin when given again.

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

When using penicillins, both immediate and delayed allergic reactions are possible. It is believed that an allergic reaction to penicillins is associated mainly with an intermediate product of their metabolism - the penicillin group. It is called a large antigenic determinant and is formed when the beta-lactam ring ruptures. Small antigenic determinants of penicillins include, in particular, unchanged penicillin molecules and benzyl penicilloate. They are formed in vivo, but are also determined in penicillin solutions 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 large antigenic determinants.

Hypersensitivity reactions are caused by the formation of antibodies in the body and usually occur within a few days of starting penicillin use (times can range from a few minutes to several weeks). In some cases, allergic reactions manifest themselves in the form of skin rash, dermatitis, and 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, abdominal pain, cerebral edema and other manifestations.

A severe allergic reaction is an absolute contraindication to future administration of penicillins. The patient must be explained that even a small amount of penicillin that enters the body with food or during a skin test can be fatal to him.

Sometimes the only symptom of an allergic reaction to penicillins is fever (which can be constant, remitting or intermittent in nature, sometimes accompanied by chills). Fever usually disappears 1-1.5 days after stopping 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 - irritating effects, incl. glossitis, stomatitis, nausea, diarrhea; with intramuscular administration - painful sensations, infiltrate, aseptic muscle necrosis; with intravenous administration - phlebitis, thrombophlebitis.

There may be an increase in 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 severely impaired liver function. Due to the risk of severe neurotoxic reactions, penicillins cannot be administered endolumbarally (with the exception of benzylpenicillin sodium salt, which is administered extremely carefully, for health reasons).

When treated with penicillins, the development of superinfection, candidiasis of the oral cavity, vagina, and intestinal dysbiosis is possible. Penicillins (usually 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 and fever. This side effect most often occurs on the 5-10th day of using large doses of ampicillin in children with lymphadenopathy and viral infections or with concomitant use of 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 Aune syndrome (ischemia and gangrene of the limbs when accidentally introduced into an artery) or Nicolau syndrome (embolism of pulmonary and cerebral vessels when it enters a vein).

When using oxacillin, hematuria, proteinuria, and interstitial nephritis are possible. The use of antipseudomonas 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.

Use 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 recorded.

In studies on laboratory animals, when penicillins were administered in doses 2-25 (for different penicillins) higher than therapeutic ones, fertility disorders and effects on reproductive function were not found. Teratogenic, mutagenic, embryotoxic properties were not detected when penicillins were administered to animals.

In accordance with the internationally recognized FDA (Food and Drug Administration) recommendations, which determine the possibility of using drugs during pregnancy, drugs of the penicillin group for their effect on the fetus belong to FDA category B (reproduction studies in animals did not reveal any adverse effects of drugs on the fetus, but adequate and There are no strictly controlled studies in pregnant women).

When prescribing penicillins during pregnancy, one should (as with any other drugs) 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 intestinal microflora, diarrhea, the development of candidiasis and the appearance of skin rashes in infants.

Pediatrics. No specific pediatric problems have been reported with the use of penicillins in children, but it should be borne in mind that insufficiently developed kidney function in newborns and children early age may lead to the accumulation of penicillins (due to this, there is an increased risk of neurotoxicity with the development of seizures).

Geriatrics. No specific geriatric problems have been reported with the use of penicillins. However, it should be remembered that in older people, age-related renal dysfunction is more likely, and therefore dose adjustment may be required.

Impaired kidney and liver function. In case of renal/liver failure, cumulation is possible. In case of moderate and severe insufficiency of renal and/or liver function, dose adjustment and an increase in the periods between administrations of the antibiotic 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. Caution must be exercised 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 disruption of the enterohepatic circulation of estrogen. Penicillins can slow down the elimination of methotrexate from the body (inhibit its tubular secretion). When ampicillin is combined with allopurinol, the likelihood of skin rash increases. The use of high doses of benzylpenicillin potassium salt in combination with potassium-sparing diuretics, potassium supplements or ACE inhibitors increases the risk of hyperkalemia. Penicillins are pharmaceutically incompatible with aminoglycosides.

Due to the fact that long-term oral administration of antibiotics can suppress the intestinal microflora that produces vitamins B1, B6, B12, PP, it is advisable to prescribe B vitamins to patients to prevent hypovitaminosis.

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

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

Thus, currently most strains Staphylococcus spp. resistant to natural penicillins. IN last years the frequency of detection of resistant strains is increasing Neisseria gonorrhoeae.

The main mechanism of acquired resistance to penicillins is associated with the production of beta-lactamases. To overcome the widespread acquired resistance 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 to create combined (inhibitor-protected) penicillins.

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