Penicillin analogues. Antibiotics of the penicillin group: indications, instructions for use

Penicillin is the very first in the world, which became a real salvation for millions of people. With its help, doctors were able to declare war on diseases that were considered fatal at that time: pneumonia, tuberculosis,. However, treatment of pathologies with antibiotics should be carried out only after an accurate diagnosis has been established and strictly as prescribed by the doctor.

History of discovery

The discovery of the antibacterial properties of penicillin occurred in 1928. The famous scientist Alexander Fleming, as a result of conducting a routine experiment with colonies, discovered stains of ordinary mold in some cups with cultures.

As it turned out upon further study, there were no harmful bacteria in the cups with mold stains. Subsequently, it was from ordinary green mold that a molecule was derived that was capable of killing bacteria. This is how the first modern antibiotic, Penicillin, appeared.

Penicillium group

Nowadays, penicillins are a whole group of antibiotics produced by certain types of mold (genus Penicillium).

They can be active against entire groups of gram-positive microorganisms, as well as some gram-negative ones: staphylococci, spirochetes, meningococci.

Penicillins belong to a large group of beta-lactam antibiotics, which contain a special beta-lactam ring molecule.

Indications

Antibiotics of the penicillin group are used in the treatment of a huge number of infectious diseases. They are prescribed when pathogenic microorganisms are sensitive to the drug for the treatment of the following pathologies:

• many types of pneumonia;
• osteomyelitis;
• infections of the genitourinary system, most of the gastrointestinal tract;
• scarlet fever;
• diphtheria;
• anthrax;
• gynecological diseases;
• diseases of the ENT organs;
• syphilis, gonorrhea and many others.

This type of antibiotic is also used in the treatment of wounds infected with bacteria. As a prevention of purulent complications, the drug is prescribed in the postoperative period.

The drug can be used in childhood for umbilical sepsis, pneumonia, otitis in newborns and infants, also early age. Penicillin is also effective for purulent pleurisy and meningitis.

Use of penicillin in medicine:

Contraindications

Application penicillin series for the treatment of infections is not always possible. People who are highly sensitive to the drug are strictly prohibited from taking the drug.

The use of this antibiotic is also contraindicated in patients suffering from asthma of various origins, hay fever, or a history of other active substances.

Release form

Modern pharmacological companies produce penicillin preparations for injections or in tablet form. Means for intramuscular injection are produced in bottles (made of glass), sealed with rubber stoppers and metal caps on top. Before administration, the substrate is diluted with sodium chloride or water for injection.

Tablets are produced in cell packaging in dosages from 50 to 100 thousand units. It is also possible to produce ecmoline lozenges. The dosage in this case does not exceed 5 thousand units.

Mechanism of action

The mechanism of action of penicillin is the inhibition of enzymes involved in the formation of the cell membrane of microorganisms. The cell membrane protects bacteria from environmental influences; disruption of its synthesis leads to the death of pathogenic agents.

This is the bactericidal effect of the drug. It acts on some types of gram-positive bacteria (streptococci and staphylococci), as well as several types of gram-negative ones.

It is worth noting that penicillins can only act on multiplying bacteria. In inactive cells, membranes are not built, so they do not die due to enzyme inhibition.

Instructions for use

The antibacterial effect of penicillin is achieved by intramuscular administration, oral administration, and local action. More often, the injection form is used for treatment. When administered intramuscularly, the drug is quickly absorbed into the blood.

However, after 3-4 hours it completely disappears from the blood. Therefore, regular administration of the drugs at equal intervals from 4 times a day is recommended.

The drug can be administered intravenously, subcutaneously, or into the spinal canal. For the treatment of complex pneumonia, meningitis or syphilis, a special regimen is prescribed, which can only be prescribed by a doctor.

When taking penicillin in tablet form, the dosage must also be determined by your doctor. As a rule, for bacterial infections, 250-500 mg is prescribed every 6-8 hours. If necessary, a single dose can be increased to 750 mg. The tablets should be taken half an hour before meals or 2 hours after. The duration of the course will be determined by the doctor.

Side effects

Since penicillins are a natural drug, they have minimal toxicity among other groups of artificially bred antibiotics. However, allergic reactions are still possible.

The tablet form of penicillin should be taken with plenty of liquid. During treatment with penicillin antibiotics, it is important not to skip the recommended doses, since the effect of the drug may be weakened. If this happens, the missed dose should be taken as quickly as possible.

It happens that after 3-5 days after regular use or administration of the drug, improvement does not occur, then you should consult a doctor to adjust the course of treatment or dose of the drug. It is not recommended to interrupt the course of treatment without consulting a doctor.

Rules for the use of antibiotics:

drug interaction

When prescribing penicillin, attention should be paid to its interaction with other drugs used. Cannot be combined this antibiotic with the following medications:

1. reduces the effectiveness of penicillin antibiotics.
2. Aminoglycosides can conflict with penicillin in a chemical aspect.
3. Sulfonamides also reduce the bactericidal effect.
4. Thrombolytics.

Penicillin price

Penicillin is considered one of the most inexpensive antibacterial drugs. The price of 50 bottles of powder to create a solution varies from 280 to 300 rubles. The cost of 250 mg tablets numbered 30 is just over 50 rubles.

Cheap

Cheap analogues of penicillin include Ampicillin and Bicillin. Their cost in tablet form also does not exceed 50 rubles.

Drug synonyms

Synonyms for the drug are Procaine-benzylpenicillin, Benzylpenicillin sodium, potassium, novocaine salt.

Natural analogues

Natural medicinal penicillins include:

• Phenkoxymethylpenicillin;
• Benzathine benzylpenicillin;
• Benzylpenicillin salts (sodium, potassium, novocaine).

Terms of dispensing from pharmacies

On prescription.

Storage conditions and shelf life

Penicillin analogues have opened up new opportunities for doctors in the treatment of infectious diseases. They are more resistant to the aggressive environment of the stomach and have fewer side effects.

About penicillins

Penicillins are the oldest known antibiotics. They have many species, but some of them have lost their relevance due to resistance. The bacteria were able to adapt and became insensitive to the effects of these drugs. This forces scientists to create new types of mold, analogues of penicillin, with new properties.

Penicillins have low toxicity to the body, are widely used and have a good bactericidal effect, but they are found much more often than doctors would like. This is explained by the organic nature of antibiotics. Another negative quality is the difficulty in combining them with other medications, especially those of a similar class.

Story

The first mention of penicillins in literature took place in 1963, in a book about Indian healers. They used mixtures of fungi for medicinal purposes. For the first time in the enlightened world, Alexander Fleming managed to obtain them, but this did not happen on purpose, but by accident, like all great discoveries.

Before World War II, English microbiologists worked on the issue of industrial production of medicine in the required volumes. The same problem was solved in parallel in the USA. From that moment on, penicillin became the most common medicine. But over time, others were isolated and synthesized, which gradually displaced him from the podium. In addition, microorganisms began to develop resistance to this drug, which complicated the treatment of severe infections.

Principle of antibacterial action

The cell wall of bacteria contains a substance called peptidoglycan. The penicillin group of antibiotics affects the process of synthesis of this protein, suppressing the formation of necessary enzymes. The microorganism dies due to the inability to renew the cell wall.

However, some bacteria have learned to resist such brutal invasion. They produce beta-lactamase, which destroys enzymes that affect peptidoglycans. In order to overcome this obstacle, scientists had to create analogues of penicillin that could also destroy beta-lactamase.

Danger to humans

At the very beginning of the era of antibiotics, scientists began to think about how toxic they would become for the human body, because almost all living matter consists of proteins. But after conducting a sufficient amount of research, we found out that there is practically no peptidoglycan in our bodies, which means that the drug cannot cause any serious harm.

Spectrum of action

Almost all types of penicillins act on gram-positive bacteria of the genus staphylococcus, streptococcus, and the causative agent of plague. Also, their spectrum of action includes all gram-negative microorganisms, gonococci and meningococci, anaerobic bacilli and even some fungi (for example, actinomycetes).

Scientists are inventing more and more new types of penicillins, trying to prevent bacteria from becoming accustomed to their bactericidal properties, but this group of drugs is no longer suitable for treatment. One of the negative properties of this type of antibiotics is dysbiosis, since the human intestines are colonized by bacteria that are sensitive to the effects of penicillin. This is worth remembering when taking medications.

Main types (classification)

Modern scientists propose a modern division of penicillins into four groups:

1. Natural, which are synthesized by fungi. These include benzylpenicillins and phenoxymethylpenicillin. These drugs have a narrow spectrum of action, mainly on
2. Semi-synthetic drugs that are resistant to penicillinases. Used to treat a wide range of pathogens. Representatives: methicillin, oxacillin, nafcillin.
3. Carboxypenicillins (carbpenicillin).
4. A group of drugs with a wide spectrum of action:
   - ureidopenicillins;
   - amidopenicillins.

Biosynthetic forms

As an example, it is worth citing several of the currently most common medications that correspond to this group. Probably the most famous of the penicillins can be considered “Bicillin-3” and “Bicillin-5”. They discovered a group of natural antibiotics and were the leaders in their category until more advanced forms of antimicrobial drugs appeared.

1. "Extencillin". The instructions for use state that it is a long-acting beta-lactam antibiotic. Indications for its use are exacerbations of rheumatic disease and diseases caused by treponemes (syphilis, yaws and pinta). Available in powders. "Extencillin" instructions for use do not recommend combining it with non-steroidal anti-inflammatory drugs (NSAIDs), as a competitive interaction is possible. This may negatively affect the effectiveness of treatment.
2. "Penicillin-V" belongs to the group of phenoxymethylpenicillins. It is used to treat infectious diseases of the ENT organs, skin and mucous membranes, gonorrhea, syphilis, tetanus. It is used as preventive measure after surgical interventions, to maintain remission in rheumatism, chorea minor, bacterial endocarditis.
3. The antibiotic "Ospen" is an analogue of the previous drug. It is available in the form of tablets or granules. It is not recommended to combine with NSAIDs and oral contraceptives. Often used in the treatment of childhood diseases.

Semi-synthetic forms

This group of drugs includes chemically modified antibiotics obtained from mold fungi.

1. The first on this list is Amoxicillin. Instructions for use (price - about one hundred rubles) indicate that the drug has a wide spectrum of action and is used for bacterial infections of almost any localization. Its advantage is that it is stable in acidic environment stomach, and after absorption the concentration in the blood is higher than that of other representatives of this group. But you should not idealize Amoxicillin. Instructions for use (price may vary in different regions) warn that the drug should not be prescribed to patients with mononucleosis, allergy sufferers and pregnant women. Long-term use is not possible due to the significant amount adverse reactions.
2. Oxacillin sodium salt is prescribed when bacteria produce penicillinase. The drug is acid-resistant, can be taken orally, and is well absorbed in the intestine. It is quickly excreted by the kidneys, so it is necessary to constantly maintain the desired concentration in the blood. The only contraindication is an allergic reaction. Available in tablet form or in bottles as liquid for injection.
3. The last representative of semisynthetic penicillins is ampicillin trihydrate. Instructions for use (tablets) indicate that it has a wide spectrum of action, affecting both gram-negative and gram-positive bacteria. Well tolerated by patients, but should be prescribed with caution to those taking anticoagulants (for example, people with pathology of cardio-vascular system), since the drug potentiates their effect.

Solvent

Penicillins are sold in pharmacies in the form of powder for injection. Therefore, for intravenous or intramuscular administration they must be dissolved in liquid. At home, you can use distilled water for injection, sodium chloride or a solution of two percent novocaine. It must be remembered that the solvent should not be too warm.

Indications, contraindications and side effects

Indications for antibiotic treatment are the following diagnoses: lobar and focal pneumonia, pleural empyema, sepsis and septicemia, septic endocarditis, meningitis, osteomyelitis. The field of action includes bacterial tonsillitis, diphtheria, scarlet fever, anthrax, gonorrhea, syphilis, purulent skin infections.

There are few contraindications to treatment with the penicillin group. Firstly, the presence of hypersensitivity to the drug and its derivatives. Secondly, an established diagnosis of epilepsy, which does not make it possible to administer the drug inside the spinal column. As for pregnancy and lactation, in this case the expected benefit should significantly exceed possible risks, because the placental barrier is permeable to penicillins. While taking the medicine, the child must be temporarily switched to another method of feeding, since the drug passes into the milk.

Side effects can occur on several levels at once.

From the central nervous system, nausea, vomiting, excitability, meningism, convulsions and even coma are possible. Allergic reactions manifest themselves in the form of skin rashes, fever, joint pain and swelling. There have been cases of anaphylactic shock and deaths. Due to the bactericidal effect, candidiasis of the vagina and oral cavity, as well as dysbacteriosis, is possible.

Features of use

Caution should be used in patients with impaired liver and kidney function and established heart failure. It is not recommended to use them for people prone to allergic reactions, as well as for those who are hypersensitive to cephalosporins.

If five days after the start of therapy there are no changes in the patient’s condition, then it is necessary to use penicillin analogues or replace the group of antibiotics. At the same time as prescribing, for example, the substance "Bicillin-3", care must be taken to prevent fungal superinfection. For this purpose, antifungal drugs are prescribed.

It is necessary to clearly explain to the patient that interrupting the medication without good reason causes resistance of microorganisms. And to overcome it, you will need stronger drugs that cause severe side effects.

Penicillin analogues have become indispensable in modern medicine. Although this is the earliest discovered group of antibiotics, it still remains relevant for the treatment of meningitis, gonorrhea and syphilis, and has a wide enough spectrum of action and mild side effects that it can be prescribed to children. Of course, like any medicine, penicillins have contraindications and side effects, but they are more than compensated for by the possibilities for use.

Antimicrobial drugs of the penicillin series are characterized by low toxicity and a wide spectrum of influence. They have an antibacterial effect on a large number of both gram-positive and gram-negative bacteria.

The influence of the penicillin series is determined by their ability to provoke the death of pathogenic microflora. Penicillin antibiotics have a bactericidal effect by interacting with bacterial enzymes, disrupting the synthesis of the bacterial wall.

The target for such antimicrobial agents is considered to be proliferating bacterial cells. These drugs are safe for humans, since the membranes of human cells do not have bacterial peptidoglycan.

Classification

There are two main groups of penicillins:

• natural;
• semi-synthetic.

A number of penicillins, which are obtained from the Penicillium microfungus, are not resistant to bacterial enzymes that have the ability to break down beta-lactam substances. Because of this, the spectrum of action of the natural penicillin series is reduced compared to the group of semi-synthetic drugs. What names of antibiotics belong to the penicillin series?

Spectrum of action of penicillins

Natural antimicrobial agents of this group exhibit increased activity against the following bacteria:

1. Staphylococcus.
2. Streptococcus.
3. Pneumococcus.
4. Listeria.
5. Bacilli.
6. Meningococcus.
7. Gonococcus.
8. Ducray-Unna's wand.
9. Clostridia.
10. Fusobacteria.
11. Actinomycetes.
12. Leptospira.
13. Borrelia.
14. Spirochete pallidum.

The spectrum of influence of semisynthetic penicillin antibiotics is somewhat wider than that of natural ones.

Antimicrobial drugs from this list are classified according to their spectrum of effects as:

• not active against Pseudomonas aeruginosa;
• antipseudomonas drugs.

When is penicillin prescribed?

Antimicrobial agents of this group are used to eliminate:

1. Pneumonia (acute inflammation of the lungs, usually of infectious origin, which affects all elements of the organ structure).
2. Bronchitis (damage to the respiratory system, in which inflammatory process bronchi are involved).
3. Otitis (inflammatory process in different parts of the ear).
4. Sore throat (an infectious and allergic process that affects the pharyngeal lymphoid ring).
5. Tonsillopharyngitis (acute infectious lesion pharynx and palatine tonsils).
6. Scarlet fever (an acute illness characterized by intoxication of the body, rashes throughout the body, as well as fever and redness of the tongue).
7. Cystitis (defeat Bladder).
8. Pyelonephritis (nonspecific inflammation with damage to the renal tubular system).
9. Gonorrhea (a sexually transmitted disease that causes damage to the mucous membranes of organs).
10. Syphilis (chronic damage to the skin, as well as mucous membranes, internal organs).
11. Skin infections.
12. Osteomyelitis (an infectious disease that affects not only the bone and bone marrow, but the entire body).
13. Blennorea of ​​newborns (a disease characterized by purulent conjunctivitis, hyperemia of the eyelids and suppuration from them).
14. Bacterial lesions of the mucous membranes, connective tissue.
15. Leptospirosis (an acute infectious disease caused by bacteria of the genus Leptospira).
16. Actinomycosis ( chronic illness from the group of mycoses, which is characterized by the formation of granulomatous foci).
17. Meningitis (a disease that is caused by damage to the membranes of the brain and spinal cord).

Aminopenicillins

Antibacterial agents from the list of aminopenicillins show increased effectiveness against a large number of infections that are caused by enterobacteria bacteria, as well as Helicobacter pylori and Haemophilus influenzae. Names of penicillin antibiotics, list of medications:

1. "Ampicillin."
2. "Amoxicillin."
3. "Flemoxin Solutab".
4. "Ospamox".
5. "Amosin".
6. "Ecoball".

The action of antibacterial drugs from the list of ampicillins and amoxicillins, the effects of these medications are similar.

Antimicrobial agents of the ampicillin series have a much lesser effect on pneumococci, but the activity of "Ampicillin" and its generics with the following drug names - penicillin antibiotics "Ampicillin Akos", "Ampicillin trihydrate" is somewhat stronger in eliminating Shigella.

The amoxicillin series is more effective against Pseudomonas aeruginosa, but some members of the group are eliminated by bacterial penicillinases.

List of names of penicillin antibiotics

The most effective drugs in the fight against ailments:

1. "Oxacillin."
2. "Dicloxacillin."
3. "Nafcillin."
4. "Methicillin."

The drugs exhibit resistance to staphylococcal penicillinases, which eliminate other drugs in this series. The most popular is Oxacillin.

Antipseudomonas penicillins

Drugs of this drug group have a wide spectrum of action; they are effective against Pseudomonas aeruginosa, which provokes cystitis, as well as tonsillitis and skin infections. What names are included in the list of drugs?

Penicillin antibiotics (names):

1. "Karbetzin".
2. "Piopen."
3. "Timentin."
4. "Securopen".
5. "Picillin."

Combination drugs

Inhibitor-protected penicillins include medications that contain an antibiotic and a component that blocks the activity of bacterial beta-lactamases.

The inhibitors are:

• clavulanic acid;
• tazobactam;
• sulbactam.

To eliminate respiratory and genitourinary infections, as a rule, the following names of penicillin antibiotics are used:

1. "Augmentin".
2. "Amoxiclav".
3. "Amoxil".
4. "Unazin."

Medicines with combined effects include the antimicrobial drug Ampiox and its generic Ampiox-sodium, which contains Ampicillin and Oxacillin.

"Ampioks" is produced in tablet form and in the form of powder for injections. The drug is used in the treatment of children and adult patients for sepsis, as well as septic endocarditis.

Medicines for adults

The list of semi-synthetic drugs that are good for tonsillitis, as well as otitis, pharyngitis, sinusitis and pneumonia, diseases of the genitourinary system includes tablets and injections:

1. "Hiconcil."
2. "Ospamox".
3. "Amoxiclav".
4. "Amoxicar".
5. "Ampicillin."
6. "Augmentin".
7. "Flemoxin Solutab".
8. "Amoxiclav".
9. "Piperacillin"
10. "Ticarcillin."

Such antimicrobial agents are not used against prostatitis, since they do not enter the prostate tissue. In case of allergic manifestations to penicillins, the patient may develop a nettle rash, anaphylaxis, and during therapy with cephalosporins.

"Ampicillin"

The drug inhibits the connection of bacterial cell walls, which is due to its antimicrobial effect. The drug affects coccal microorganisms and a large number of gram-negative bacteria. Under the influence of penicillinase, Ampicillin is destroyed, so it is not effective against penicillinase-forming pathogens.

"Flemoxin Solutab"

People prone to allergies to medications need a sensitivity test before therapy. The medication is not prescribed to patients who have already had severe adverse reactions to penicillin.

Treatment must be completed to the end. Interruption of therapy ahead of schedule may lead to the development of pathogen resistance to active substance and the transition of the disease to the chronic stage.

"Amoxiclav"

The drug also contains amoxicillin, which is considered a penicillin antibiotic; its molecule contains a beta-lactam ring. It is active against many bacteria and also has a bactericidal effect due to disruption of cell wall synthesis. "Amoxiclav" is a new penicillin antibiotic.

To maintain the activity of the antimicrobial agent in the drug, the second active ingredient is clavulanic acid. This compound irreversibly neutralizes the β-lactamase enzyme, thereby making such pathogens sensitive to amoxicillin.

"Augmentin"

The drug has a prolonged effect, which is significantly different from other drugs based on amoxicillin. With this help, the medication can be used to eliminate pneumonia that is resistant to penicillins.

After penetration, the active components - amoxicillin and clavulanic acid - quickly dissolve and are absorbed into the stomach and intestines. The maximum pharmacological effect is manifested in the situation if the patient takes the drug before meals.

Penicillins for the treatment of children

Penicillin antibiotics are practically non-toxic, which is why they are usually recommended for children with infectious diseases. In most cases, preference is given to inhibitor-protected penicillins, which are intended for oral use.

The list of penicillin antimicrobial drugs intended for the treatment of children includes Amoxicillin and generics, Augmentin, Amoxiclav, as well as Flemoxin and Flemoclav Solutab. Medicines in the form of dispersible tablets are no less effective than injections and cause fewer problems during treatment.

From birth, Ospamox and a number of its substitutes, which are available in soluble tablets, as well as granules and powder for making a suspension, are used to treat children. The dosage is prescribed by the doctor, based on the age and body weight of the child.

In children, accumulation of penicillins in the body is possible, which is caused by anemia of the urinary system or kidney damage. An increased content of an antimicrobial substance in the blood has a toxic effect on nerve cells, which is manifested by spasms. If such signs occur, therapy is stopped and the penicillin antibiotic is replaced with a medication from another group.

"Ospamox"

The medicine is produced in two dosage forms- tablets and granules. The dosage of the drug according to the instructions for use depends on the location of the infectious process. "Ospamox" is a modern penicillin antibiotic for children.

The daily concentration is divided into several uses. Duration of therapy: until symptoms disappear plus five days. To make a suspension, a bottle with granules is filled with water and then shaken. The dosage of the medication for Ospamox will be as follows:

• infants under one year of age are prescribed a suspension at a concentration of 125 mg/5 ml - 5 milliliters (1 spoon) twice a day;
• for children from one to six years old - a suspension from 5 to 7.5 milliliters (1-1.5 spoons) twice a day;
• children from six to ten years old - a suspension of 7.5 to 10 ml twice a day;
• patients from ten to fourteen years old are already prescribed a tablet form of the drug - 1 tablet of 500 milligrams twice a day;
• adolescents - 1.5 tablets of 500 mg twice a day.

Contraindications and side effects

Restrictions for use include allergies to penicillin antibiotics. If rashes occur during therapy, itchy skin, you need to stop using the medications and consult a doctor.

Allergies can manifest as angioedema and anaphylaxis. The list of adverse reactions for penicillins is small. The main negative phenomenon is the inhibition of beneficial intestinal microflora.

Diarrhea, thrush, skin rashes are the main negative reactions when using penicillins. The following effects occur less frequently:

1. Nausea.
2. Vomit.
3. Migraine.
4. Pseudomembranous colitis.
5. Edema.

The use of benzylpenicillins, as well as carbenicillins, can provoke electrolyte imbalance with the development of hyperkalemia or hypernatremia, which increases the likelihood of a heart attack and increased blood pressure.

An extensive list of negative effects of Oxacillin and substitutes:

1. The appearance of blood in urine.
2. Temperature.
3. Vomiting.
4. Nausea.

To prevent the occurrence of negative effects, it is important to follow the instructions for use, and also use the drug in the dosage prescribed by the doctor.

Opinions

According to reviews, penicillin antibiotics have become a real salvation for many people. Thanks to them, you can cope with most diseases, for example: pneumonia, as well as tuberculosis, sepsis and other ailments.

But treatment of pathological conditions using antibiotics should be carried out only after a diagnosis has been established and strictly as prescribed by the doctor. The most effective antimicrobial agents include Amoxiclav, Ampicillin, and Flemoxin Solutab.

Reviews from medical specialists and people usually contain positive opinions about the drugs of these groups. It is noted that antimicrobial agents are effective in the treatment of respiratory diseases, and they are suitable for both adults and children. The responses mention the increased effectiveness of the drugs for sinusitis, otitis media, and genital tract infections.

Antibiotics are substances that are produced by microorganisms or synthesized using medical technologies from natural raw materials. These medicines are used to suppress the growth and development of colonies of pathogenic agents that have entered the human body.

Antibiotics of the penicillin group are the first drugs from this area that were used in clinical practice. And, despite the fact that almost 100 years have passed since their discovery, and the list of antimicrobial agents has been replenished with drugs of the cephalosporin, fluoroquinol and other series, penicillin-type compounds still remain the main antibacterial drugs for stopping a huge list of infectious diseases.

A bit of history

The discovery of penicillin happened completely by accident: in 1928, scientist Alexander Fleming, working in one of the London hospitals, discovered mold growing on a nutrient medium, which was capable of destroying colonies of staphylococci.

The researcher named the active substance of the microscopic mold filamentous fungus Penicillium notatum penicillin. Just 12 years later, the first antibiotic was isolated in its pure form, and in 1942, Soviet microbiologist Zinaida Ermolyeva obtained a drug from another type of fungus - Penicillium crustosum.

Since the second half of the 20th century, unlimited quantities of penicillin G (or benzylpenicillin) have become available to combat a wide variety of diseases.

Operating principle

The described active substance has a bactericidal and bacteriostatic effect on pathogens. The mechanism of the bactericidal scheme of action of drugs included in the penicillin type (series) is associated with damage to the cell walls (violation of the integrity of the structure) of infectious agents, which leads to the death of microorganisms.

The bacteriostatic principle of action on pathogens is characterized by temporary suppression of the ability of pathogenic organisms to reproduce.

The type of drug exposure is selected taking into account the severity of the disease.

Most penicillins in small doses affect microbes bacteriostatically. As the amount of the drug used increases, the effect changes to bactericidal. Specific dosage of the medication penicillin group Only a doctor can select it; you cannot use antibiotics for treatment yourself.

Systematization of drugs

Natural penicillins, in addition to benzylpenicillin (and its various salts - sodium, potassium), also include:

• Phenoxymethylpenicillin;
• Benzathine benzylpenicillin.

The basic principles for classifying semisynthetic types of penicillin are listed below.

• isoxazolyl penicillins (Oxacillin, Nafcillin);
• amino-penicillins (Amoxicillin, Ampicillin);
• aminodi-penicillins (no medications registered in the Russian Federation);
• carboxy-penicillins (Carbenicillin);
• ureido-penicillins (Piperacillin, Azlocillin);
• inhibitor-protected penicillins (Piperacillin in combination with tazobactam, Ticarcillin in combination with clavulanate, Ampicillin in combination with sulbactam).

Brief characteristics of natural medicines

Natural (natural) penicillins are drugs that have a narrow spectrum of action on microorganisms. Due to their long-term (and often uncontrolled) use for medical purposes, most pathogens have managed to acquire immunity to these types of antibiotics.

Today, in the treatment of diseases, the medications Bicillin and Benzylpenicillin are most often used, which are quite effective against some anaerobic agents, spirochetes, a number of cocci and gram-positive pathogens.

Gram-negative bacteria H.ducreyi, P.multocida, Neisseria spp., as well as Listeria, varieties of corynebacteria (in particular, C.diphtheriae) remain sensitive to natural antibiotics.

The method of using medications to suppress the development of these pathogens is injection.

Natural penicillins, according to experts, have one major drawback: they are destroyed under the influence of beta-lactamases (enzymes that are produced by certain microorganisms). That is why natural antibiotics belonging to the penicillin group are not used to treat ailments caused by staphylococcal infections.

Description of synthesized types of drugs

A number of semisynthetic drugs included in the penicillin antibiotic series and combined into the group of aminodipenicillins are not registered in our country. Acidocillin, Amdinocillin, Bacamdinocillin are medications with a narrow spectrum of action and are effective against gram-negative enterobacteria.

The remaining synthesized groups of drugs are widely used in medical institutions Russia and require more detailed consideration.

Antistaphylococcal (penicillinase-stable) drugs

Another name for this group of antibiotics is isoxazolylpenicillins. The drug most often used in therapy is Oxacillin. The subtype includes several more drugs (in particular, Nafcillin, Dicloxacillin, Methicillin), which are used extremely rarely due to their high toxicity.

In terms of its spectrum of effects on pathogens, Oxacillin is similar to medications included in the natural penicillin series, but is slightly inferior to them in the level of activity (in particular, it is less effective against microbes sensitive to the effects of benzylpenicillin).

The main difference between the drug and other penicillins is its resistance to beta-lactamases produced by staphylococci. The practical use of Oxycillin has been found in the fight against strains of this microorganism, which is the causative agent of community-acquired infections.

Aminopenicillins

This group of semisynthetic penicillins is characterized by a wide range of effects on pathogens. The ancestor of aminopenicillins is the drug Ampicillin. In a number of parameters it is superior to Oxycillin, but inferior to Benzylpenicillin.

Close in scope to this medication is the drug Amoxicillin.

Since these representatives of the group are susceptible to the destructive effects of beta-lactamases, medications protected from the effects of infectious agent enzymes by inhibitors (for example, Amoxicillin in combination with clavuanic acid, Ampicillin in combination with sulbactam) were introduced into medical practice.

The expansion of the antimicrobial spectrum of inhibitor-protected aminopenicillins occurred due to the manifestation of their activity against:

• gram-negative bacteria (C.diversus, P.vulgaris, Klebsiella spp.);
• gonococci;
• staphylococci;
• anaerobes of the species B.fragilis.

Inhibitor-protected aminopenicillins do not affect the growth and development of microorganisms whose resistance to penicillin-type antibiotics is not associated with the production of beta-lactamases.

Ureidopenicillins and carboxypenicillins

Representatives of these groups are semi-synthetic penicillin antibiotics that relieve Pseudomonas aeruginosa; The list of these drugs is quite wide, but in modern medicine they are rarely used (pathogens lose sensitivity to them in a short time).

Medicines of the carboxypenicillin type Carbenicillin, Ticarcillin (the latter is not registered in the Russian Federation) suppress the development of colonies of gram-positive bacteria and microorganisms of the P.aeruginosa, Enterobacteriaceae family.

Most effective remedy from the group of ureidopenicillins - Piperacillin; it is involved in the fight against diseases caused by Klebsiella spp.

The described antibiotics, as well as natural penicillins, are susceptible to the negative influence of beta-lactamases. A solution to the problem was found in the synthesis of fundamentally new antimicrobial agents, into which, in addition to the already mentioned active substances, inhibitors were introduced.

Inhibitor-protected ureidopenicillins and carboxypenicillins have a wide spectrum of effects on most known pathogens.

Pharmacokinetics

When taken orally, the antibiotic, which is part of the penicillin series of drugs, is absorbed quite quickly and, penetrating into liquid media and tissues of the body, begins to affect colonies of pathogens.

Medicines are characterized by the ability to concentrate in pleural, pericardial, synovial fluids and bile. They practically do not penetrate into the internal environments of the organs of vision, prostate, or cerebrospinal fluid. Found in minimal proportions in breast milk. In small quantities they penetrate the placental barrier.

If necessary (for example, when meningitis is detected in a patient), therapeutic concentrations in the cerebrospinal fluid are achieved by administering significant doses of drugs.

Some penicillins in tablet form are destroyed under the influence of gastrointestinal enzymes, and therefore are used parenterally.

The main indicators of the process of transporting active substances from the digestive system into the blood of commonly used medications (in tablets) are shown in the table.

Excretion of penicillins mainly (more than 60%) occurs through the kidneys; some medications are excreted in bile. Almost all drugs of the described group are removed during hemodialysis.

Contraindications

Despite the fact that most representatives of penicillins are characterized high efficiency in the elimination of infectious agents, it is impossible to use these drugs to treat all patients without exception.

One of the disadvantages of this type of medication is the frequent occurrence of allergic reactions to them in patients (according to statistics, the percentage of skin rashes, swelling and itching reaches 10 units).

If the patient has a history of individual intolerance to penicillin, medical products of this group cannot be used in therapy.

Warnings

Antibiotics of the penicillin group can cause toxic side effects of non-allergic etiology, in particular:

• attacks of nausea and vomiting;
• painful sensations in the abdomen;
• diarrhea;
• pseudomembranous colitis.

When using high doses of drugs, seizures, headaches, hallucinations and fever may occur.

In addition, the use of drugs of the described series is often accompanied by the development of candidiasis, intestinal dysbiosis, the appearance of edema, and impaired blood pressure levels.

It should be noted that penicillins are among the lowest toxic antibiotics, and the above side effect on the body manifests itself more often with the independent, uncontrolled use of medications (without prior consultation with a doctor).

Indications

Mostly antibiotics of the penicillin group are used to eliminate the symptoms of upper tract infections, tonsillitis, otitis, as well as to stop the growth of colonies of infectious agents that cause inflammation of the urinary tract, the development of scarlet fever, syphilis and gonorrhea; for the prevention of rheumatism.

In addition, penicillin antibiotic therapy is used when making diagnoses such as:

• erysipelas;
• sepsis;
• Lyme disease;
• meningitis;
• tonsilopharyngitis;
• leptospirosis;
• actinomycosis

It should be remembered that the use of drugs from the penicillin group is allowed only as prescribed by a doctor. Self-medication can provoke the development of superinfection or the occurrence of severe complications of the disease.

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

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

Properties of penicillin and its discovery

Before the discovery of antibiotics, many diseases seemed simply incurable; scientists and doctors all over the world wanted to find a substance that could help defeat pathogenic microorganisms without causing harm to human health. People died from sepsis, wounds infected with bacteria, gonorrhea, tuberculosis, pneumonia and other dangerous and serious diseases.

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

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

Properties of antibiotics of the penicillin group

Antibiotic penicillin suppresses the emergence and development pathogenic organisms such as:

This is only a small list of those pathogenic bacteria whose vital activity is suppressed by penicillin and all penicillin-type drugs.

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

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

Cell membranes in the human body do not contain peptidoglycan and therefore antibiotics of the penicillin group do not have a negative effect on our body. Also, we can talk about the slight toxicity of these products.

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

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

List of drugs and classification of penicillins

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

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

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

To date, the Federal Guidelines for Use medicines This classification of penicillins is given.

Natural short-acting antibiotics

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

Benzylpenicillin is active during treatment:

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

Restrictions for use and contraindications: hay fever, allergy to penicillin, renal impairment, arrhythmia, bronchial asthma.

Natural antibiotics with prolonged action

Benzylpenicillin benzathine is used in cases of:

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

It is also used to prevent complications after operations.

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

Contraindications: hay fever, bronchial asthma, penicillin allergies.

Benzylpenicillin procaine is used in the treatment of:

Used for relapses of erysipelas and rheumatism.

Side effects: convulsions, nausea, allergic reaction.

Contraindications: hypersensitivity to procaine and penicillin.

Antistaphylococcal agents

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

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

Contraindications: allergic reactions for penicillin.

Broad-spectrum drugs

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

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

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

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

Side effects: dysbacteriosis, dyspeptic disorders, allergies, candidiasis, superinfection, central nervous system disorders.

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

Antipseudomonas antibiotics

Carboxypenicillins contain active ingredient – ​​carbenicillin. In this case, the name of the antibiotic coincides with the active ingredient. Used in the treatment of diseases caused by Pseudomonas aeruginosa. Today, they are almost never used in medicine due to the availability of stronger drugs.

Ureidopenicillins include: Azlocillin, Piperacillin, Mezlocillin.

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

Contraindications: pregnancy, high sensitivity to penicillin.

Features of the use of penicillin antibiotics in children

Use of antibiotics in pediatric treatment Much attention is constantly paid, since the child’s body has not yet fully formed and most organs and systems are not working fully yet. Therefore, doctors need to take the choice of antibiotics for infants and growing children with great responsibility.

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

For sore throat, ARVI, cystitis, bronchitis, sinusitis, as a rule, children are prescribed Flemoxin, Amoxicillin, Augmentin, Amoxiclav. These antibiotics are the least toxic and most effective for the child’s body.

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

In infants, the excretory function of the kidneys is not sufficiently developed and there is likely to be an accumulation of penicillin in the body. The result of this is the appearance of seizures.

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

The use of probiotics and prebiotics (Bifidumbacterin, Linex, Bifiform, Acipol, etc.) is mandatory. The start of administration must occur simultaneously with the start of using the antibacterial agent. Moreover, after a course of antibiotics, prebiotics and probiotics must be used for about 14 more days to populate the stomach with beneficial bacteria.

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

Since immunity decreases, the body is especially susceptible to colds. Therefore, you need to take care of yourself and not get too cold. Use immunomodulators, preferably of plant origin (Echinacea purpurea, Immunal).

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

To use antibiotics less often and get sick less often, it is necessary to healthy image life. The most important thing is not to overdo it with use. antibacterial agents to prevent bacteria from developing resistance to them. Otherwise, it will be impossible to cure any infection. Therefore, always consult your doctor before using any antibiotic.