Amoxicillin of the penicillin group. Penicillin group. Inhibitor-protected, combined agents

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 a preventive measure after surgery, to maintain remission in rheumatism, chorea minor, and 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 the acidic environment of the 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 a significant number of 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. It is well tolerated by patients, but should be prescribed with caution to those taking anticoagulants (for example, people with pathologies of the cardiovascular 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 benefits should significantly exceed the 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.


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

This section provides a complete list of currently relevant antimicrobial drugs. In addition to the characteristics of the main compounds, all trade names and analogues are given.


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

The information provided is for informational purposes only and is not a guide to action. All prescriptions are made exclusively by a doctor, and therapy is carried out under his supervision.

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

The medication prescribed by the specialist should be used for antibacterial therapy. Independent attempts to find a cheap analogue and save money can lead to a worsening of the condition.

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


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

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

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

Medications based on waste products of mold fungi have become widespread in all areas of medicine due to the following properties:

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

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


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

Today, penicillin antibiotics, a full list of which is given below, are divided into 4 main groups.

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

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

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

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

These drugs are used for long-term antibiotic therapy of chronic rheumatism, syphilis, and focal streptococcal infection.
Phenoxymethylpenicillin is another form of benzylpenicillin intended for the treatment of moderate infectious diseases. Differs from those described above in its resistance to hydrochloric acid of gastric juice.

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


Read also: Instructions for using penicillin in injections and tablets

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

For a long time, penicillin was not used to treat staphylococcal infections, until oxacillin was synthesized on its basis in 1957. It inhibits the activity of beta-lactamases of the pathogen, but is ineffective against diseases caused by strains sensitive to benzylpenicillin. This group also includes cloxacillin, dicloxacillin, methicillin and others, which are almost never used in modern medical practice due to increased toxicity.

This includes two subgroups of antimicrobial agents intended for oral use and having a bactericidal effect against most pathogenic microorganisms (both gram+ and gram-).

Compared to the previous groups, these compounds have two significant advantages. Firstly, they are active against a wider range of pathogens, and secondly, they are available in tablet form, which makes them much easier to use. Disadvantages include sensitivity to beta-lactamase, that is, aminopenicillins (ampicillin and amoxicillin) are unsuitable for the treatment of staphylococcal infections.

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

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

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

According to the degree of effectiveness they are divided into:

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

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


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

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

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

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

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

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

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

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

Intestinal inflammation caused by pathogenic microflora responds well to treatment with acid-resistant medications.

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

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

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

Diseases of the urinary system that are of bacterial origin respond well to treatment only with inhibitor-protected medications. The remaining subgroups are ineffective, since pathogen strains are highly resistant to them.

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

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

The scope of application of penicillin and various drugs based on it in medicine is determined by the activity of the substance against specific pathogens. Bacteriostatic and bactericidal effects occur in relation to:

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

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

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

During pregnancy, antibiotic therapy with penicillin drugs should be treated with extreme caution. Despite the fact that they have minimal teratogenic effects, tablets and injections should be prescribed only in cases of urgent need, assessing the degree of risk to the fetus and the pregnant woman herself.

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

Among other antibacterial agents, penicillins stand out due to their low toxicity.

Undesirable consequences of use include:

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

Timely medicinal support of the body will help prevent the development of dysbiosis and avoid allergies. It is advisable to combine antibiotic therapy with the use of pre- and probiotics, as well as desensitizers (if sensitivity is increased).

Tablets and injections should be prescribed to children with caution, taking into account possible negative reactions, and the choice of a specific drug should be approached thoughtfully.

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

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

A little theory:

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

Alexander Fleming - discoverer of penicillin

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

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

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

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

Read a fascinating article: The inventor of antibiotics or the story of saving humanity!

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Mushrooms are a kingdom of living organisms. Mushrooms come in many varieties: some of them end up in our diet, some cause skin diseases, and some are so poisonous that they can cause death. But fungi of the genus Penicillium save millions of human lives from pathogenic bacteria.

Penicillin antibiotics based on this mold (mold is also a fungus) are still used in medicine.

In the 30s of the last century, Alexander Fleming conducted experiments with staphylococci. He studied bacterial infections. Having grown a group of these pathogens in a nutrient medium, the scientist noticed that there were areas in the dish around which there were no living bacteria. The investigation showed that the culprit for these stains was ordinary green mold, which likes to settle on stale bread. The mold was called Penicillium and, as it turned out, produced a substance that kills staphylococci.

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

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

For the next 10 years, an invisible war took place between pathogens that destroy penicillin, and scientists who modify this penicillin. This is how many modifications of penicillin were born, which now form the entire penicillin series of antibiotics.

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

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

The medicine is quickly eliminated from the body; after 1-3 hours, most of it exits through the kidneys.

Watch a video on this topic

All drugs are divided into: natural (short and long-acting) and semi-synthetic (antistaphylococcal, broad-spectrum drugs, antipseudomonas).

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

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

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

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

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

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

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

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

Examples of drugs: Ticarcillin, Piperacillin

Pills

Sumamed

Active ingredient: azithromycin.

Indications: respiratory tract infections.

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

Price: 300-500 rubles.

Oxacillin

Active ingredient: oxacillin.

Indications: infections sensitive to the drug.

Price: 30-60 rubles.

Amoxicillin Sandoz

Indications: respiratory tract infections (including sore throat, bronchitis), genitourinary system infections, skin infections, other infections.

Contraindications: intolerance, children under 3 years of age.

Price: 150 rubles.

Ampicillin trihydrate

Indications: pneumonia, bronchitis, tonsillitis, other infections.

Contraindications: hypersensitivity, liver failure.

Price: 24 rubles.

Phenoxymethylpenicillin

Active ingredient: phenoxymethylpenicillin.

Indications: streptococcal diseases, mild to moderate infections.

Price: 7 rubles.

Amoxiclav

Active ingredient: amoxicillin + clavulanic acid.

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

Contraindications: hypersensitivity, jaundice, mononucleosis and lymphocytic leukemia.

Price: 116 rubles.

Bicillin-1

Active ingredient: benzathine benzylpenicillin.

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

Contraindications: hypersensitivity.

Price: 15 rubles per injection.

Ospamox

Active ingredient: amoxicillin.

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

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

Price: 65 rubles.

Ampicillin

Active ingredient: ampicillin.

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

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

Price: 163 rubles.

Benzylpenicillin

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

Contraindications: intolerance.

Price: 2.8 rubles per injection.

Benzylpenicillin novocaine salt

Active ingredient: benzylpenicillin.

Indications: similar to benzylpenicillin.

Contraindications: intolerance.

Price: 43 rubles for 10 injections.

Amoxiclav, Ospamox, Oxacillin are suitable for treating children. But Before using the medicine, you must consult your doctor to adjust the dose.

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

Most often, infections of the respiratory tract and genitourinary system are treated with antibiotics.

In the case of treating children, you must follow the instructions of the doctor, who will prescribe the right antibiotic and adjust the dose.

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

There are no special guidelines for older people, although the doctor should consider the condition of the patient's kidneys and liver when prescribing treatment.

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

If side effects occur, you should immediately seek medical help, discontinue the drug and carry out symptomatic treatment.

Where does penicillin mold grow?

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

What can replace penicillin antibiotics?

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

Penicillin antibiotics are a powerful remedy against infections caused by various bacteria. There are quite a few types of them, and treatment must be selected according to the type of pathogen.

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

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Antibiotics owe their appearance to the Scottish scientist Alexander Fleming. More precisely, his sloppiness. In September 1928, he returned to his laboratory from a long trip. During this time, a moldy area grew in a Petri dish forgotten on the table, and a ring of dead microbes formed around it. It was this phenomenon that a microbiologist noticed and began to study.

The mold in the test tube contained a substance that Fleming called penicillin. However, 13 years passed before penicillin was obtained in its pure form and its effect was first tested on humans. Mass production of the new drug began in 1943, at a factory where whiskey was previously brewed.

Today, there are about several thousand natural and synthetic substances that have an antimicrobial effect. However, the most popular of them are still penicillin drugs.

Any pathogenic microorganism, entering the blood or tissues, begins to divide and grow. The effectiveness of penicillins is based on their ability to disrupt the formation of bacterial cell walls.

Antibiotics of the penicillin group block special enzymes that are responsible for the synthesis of the protective peptidoglycan layer in the bacterial shell. It is thanks to this layer that they remain insensitive to aggressive environmental influences.

The result of disrupted synthesis is the inability of the shell to withstand the difference between external pressure and pressure inside the cell itself, which is why the microorganism swells and simply bursts.

Penicillins are antibiotics that have a bacteriostatic effect, that is, they affect only active microorganisms that are at the stage of division and formation of new cell membranes.

According to the chemical classification, penicillin antibiotics are classified as β-lactam antibiotics. In their structure they contain a special beta-lactam ring, which determines their main effect. Today the list of such drugs is quite large.

The first, natural penicillin, despite all its effectiveness, had one significant drawback. It was not resistant to the enzyme penicillinase, which was produced by almost all microorganisms. Therefore, scientists have created semi-synthetic and synthetic analogues. Today, antibiotics of the penicillin group include three main types.

As many years ago, they are obtained using molds Penicillium notatum and Penicillium chrysogenum. The main representatives of this group today are benzylpenicillin sodium or potassium salt, as well as their analogues Bicillins -1, 3 and 5, which are the novocaine salt of penicillin. These drugs are not resistant to the aggressive environment of the stomach and therefore are used only by injection.

Benzylpenicillins are characterized by a rapid onset of therapeutic effect, which develops literally in 10–15 minutes. However, its duration is very short, only 4 hours. Due to its combination with novocaine, Bicillin can boast of greater stability; its action lasts for 8 hours.

Another representative included in the list of this group, phenoxymethylpenicillin, is resistant to acidic environments, therefore it is available in tablets and suspensions that can be used by children. However, it also does not differ in duration of action and can be prescribed 4 to 6 times a day.

Natural penicillins are used very rarely today due to the fact that most pathological microorganisms have developed resistance to them.

This penicillin group of antibiotics was obtained using various chemical reactions by adding additional radicals to the main molecule. A slightly modified chemical structure gave these substances new properties, such as resistance to penicillinase and a broader spectrum of action.

Semi-synthetic penicillins include:

  • Antistaphylococcal, such as Oxacillin, obtained in 1957 and still used today, and cloxacillin, flucloxacillin, and dicloxacillin, which are not used due to high toxicity.
  • Antipseudomonas, a special group of penicillins that was created to combat infections caused by Pseudomonas aeruginosa. These include Carbenicillin, Piperacillin and Azlocillin. Unfortunately, today these antibiotics are used very rarely, and due to the resistance of microorganisms to them, new drugs are not being added to their list.
  • Penicillin series of broad-spectrum antibiotics. This group acts on many microorganisms and is resistant to acidic environments, which means it is available not only in injection solutions, but also in tablets and suspensions for children. This includes the aminopenicillins that are most commonly used, such as Ampicillin, Ampiox and Amoxicillin. The drugs have a long-lasting effect and are usually used 2-3 times a day.

Of the entire group of semi-synthetic drugs, it is penicillin-broad-spectrum antibiotics that are the most popular and are used both in inpatient and outpatient treatment.

Once upon a time, injections of penicillin could cure blood poisoning. Today, most antibiotics are ineffective even for simple infections. The reason for this is resistance, that is, resistance to drugs that microorganisms have acquired. One of its mechanisms is the destruction of antibiotics using the enzyme beta-lactamase.

In order to avoid this, scientists have created a combination of penicillins with special substances - beta-lactamase inhibitors, namely clavulanic acid, sulbactam or tazobactam. Such antibiotics are called protected and today the list of this group is the most extensive.

In addition to the fact that inhibitors protect penicillins from the destructive action of beta-lactamases, they also have their own antimicrobial effect. The most commonly used of this group of antibiotics is Amoxiclav, which is a combination of amoxicillin and clavulanic acid, and Ampisid, a combination of ampicillin and sulbactam. Doctors prescribe and their analogues - the drugs Augmentin or Flemoklav. Protected antibiotics are used to treat children and adults, and they are also the first choice drugs for treating infections during pregnancy.

Antibiotics protected by beta-lactamase inhibitors are used successfully even to treat severe infections that are resistant to most other drugs.

Statistics show that in terms of prevalence of use, antibiotics are in second place after painkillers. According to the analytical company DSM Group, 55.46 million packages were sold in just one quarter of 2016. Today, pharmacies sell approximately 370 different brands of drugs produced by 240 companies.

The entire list of antibiotics, including the penicillin series, refers to strictly licensed drugs. Therefore, to purchase them you will need a prescription from a doctor.

Indications for the use of penicillins can be any infectious diseases that are sensitive to them. Doctors usually prescribe penicillin antibiotics:

  1. For diseases caused by gram-positive bacteria, such as meningococci, which can cause meningitis and gonococci, which cause the development of gonorrhea.
  2. For pathologies that are caused by gram-negative bacteria, such as pneumococci, staphylococci or streptococci, which are often the causes of infections of the upper and lower respiratory tract, genitourinary system and many others.
  3. For infections caused by actinomycetes and spirochetes.

The low toxicity of the penicillin group compared to other antibiotics makes them the most prescribed drugs for the treatment of sore throats, pneumonia, various infections of the skin and bone tissue, diseases of the eyes and ENT organs.

This group of antibiotics is relatively safe. In some cases, when the benefits of their use outweigh the risks, they are prescribed even during pregnancy. Especially when non-penicillin antibiotics are ineffective.

They are also used during lactation. However, doctors advise against breastfeeding while taking antibiotics, as they can pass into milk and can cause allergies in the baby.

The only absolute contraindication to the use of penicillin drugs is individual intolerance to both the main substance and the auxiliary components. For example, benzylpenicillin novocaine salt is contraindicated for allergies to novocaine.

Antibiotics are fairly aggressive drugs. Even though they do not have any effect on the cells of the human body, there may be unpleasant effects from their use.

Most often this is:

  1. Allergic reactions, manifested mainly in the form of skin itching, redness and rashes. Less commonly, swelling and fever may occur. In some cases, anaphylactic shock may develop.
  2. An imbalance of natural microflora, which provokes disorders, abdominal pain, bloating and nausea. In rare cases, candidiasis may develop.
  3. Negative effects on the nervous system, signs of which are irritability, excitability, and rarely convulsions may occur.

Today, of the entire variety of open antibiotics, only 5% are used. The reason for this is the development of resistance in microorganisms, which often occurs due to improper use of drugs. Antibiotic resistance already kills 700 thousand people every year.

In order for the antibiotic to be as effective as possible and not cause the development of resistance in the future, it must be taken in the dosage prescribed by the doctor and always in full course!

If your doctor has prescribed you penicillin or any other antibiotics, be sure to follow these rules:

  • Strictly observe the time and frequency of taking the drug. Try to take the medicine at the same time, this will ensure a constant concentration of the active substance in the blood.
  • If the dosage of penicillin is small and the drug must be taken three times a day, then the time between doses should be 8 hours. If the dose prescribed by the doctor is intended to be taken twice a day - up to 12 hours.
  • The course of taking the drug can range from 5 to 14 days and is determined by your diagnosis. Always drink the entire course prescribed by your doctor, even if the symptoms of the disease no longer bother you.
  • If you do not feel any improvement within 72 hours, be sure to tell your doctor. Perhaps the drug he chose was not effective enough.
  • Do not replace one antibiotic with another on your own. Do not change the dosage or dosage form. If the doctor prescribed injections, then the pills will not be effective enough in your case.
  • Be sure to follow the instructions for use. There are antibiotics that you need to drink with meals, and there are those that you drink immediately after. Take this medication only with plain, still water.
  • During antibiotic treatment, avoid alcohol, fatty, smoked and fried foods. Antibiotics are mainly eliminated by the liver, so it is not worth additionally loading it during this period.

If penicillin antibiotics are prescribed to a child, you should be especially careful when taking them. A child's body is much more sensitive to these drugs than an adult, so allergies in children may occur more often. Penicillins for children are usually produced in a special dosage form, in the form of suspensions, so you should not give tablets to your child. Take antibiotics correctly and only as prescribed by your doctor when really necessary.

Penicillin antibiotics are several types of drugs that are divided into groups. In medicine, drugs are used to treat various diseases of infectious and bacterial origin. The drugs have a minimal number of contraindications and are still used to treat various patients.

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

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

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

The discovery helped save many people's lives. It saved humanity from those diseases that previously caused panic among the population. Naturally, modern medicines are relatively similar to those drugs that were used at the end of the 19th century. But the essence of the medications and their action have not changed so dramatically.

Penicillin antibiotics were able to revolutionize medicine. But the joy of the discovery did not last long. It turned out that pathogenic microorganisms and bacteria can mutate. They change and become insensitive to drugs. This led to significant changes in antibiotics such as penicillin.

Scientists spent almost the entire 20th century “fighting” microorganisms and bacteria, trying to create the ideal drug. The efforts were not in vain, but such improvements have led to the fact that antibiotics have changed significantly.

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

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

Important: These medications have virtually no contraindications. It is not recommended to take them if you have an individual intolerance to antibiotics, or if you develop an allergic reaction.

Modern antibacterial agents differ significantly from the familiar penicillin. In addition to the fact that today you can easily purchase medications of this class in tablets, there are a great variety of them. Classification and generally accepted division into groups will help you understand the drugs.

Antibiotics of the penicillin group are conventionally divided into:

  1. Natural.
  2. Semi-synthetic.

All medicines based on mold are antibiotics of natural origin. Today, such medications are practically not used in medicine. The reason is that pathogenic microorganisms have become immune to them. That is, the antibiotic does not act on bacteria properly; the desired result in treatment can only be achieved by administering a high dose of the drug. The drugs in this group include: Benzylpenicillin and Bicillin.

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

Penicillin antibiotics of semi-synthetic origin are the result of modification of drugs produced from mold. It was possible to impart some properties to medications belonging to this group; first of all, they became insensitive to acid-base environments. This made it possible to produce antibiotics in tablets.

Medicines also appeared that acted on staphylococci. This class of drugs is different from natural antibiotics. But the improvements have significantly affected the quality of the drugs. They are poorly absorbed, do not have such a wide sector of action, and have contraindications.

Semi-synthetic drugs can be divided into:

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

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

Antibiotics belonging to the penicillin group are prescribed by a doctor. It is recommended to take the drugs if you have:

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

Information: Antibiotics are prescribed for extensive burns and deep wounds, gunshot or knife wounds.

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

What contraindications do medications have:

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

Direct contraindications for the use of antibiotics:

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

Attention! The main side effects of taking medications are long-term diarrhea and candidiasis. They are due to the fact that the drugs affect not only pathogenic microorganisms, but also beneficial microflora.

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

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

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

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

List or list of penicillin antibiotics, which are available in powder form:

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

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

Sumamed - cost varies from 300 to 500 rubles.

Amoxicillin tablets - price is about 159 rubles. per package.

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

Ampicillin in powder form, intended for injection - 170 rubles.

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

Amoxiclav - cost - 120 rubles.

Ospamox - price varies from 65 to 100 rubles.

Benzylpenicillin novocaine salt - 50 rub.

Benzylpenicillin - 30 rub.


Penicillins are the first AMPs developed based on waste products of microorganisms. They belong to the broad class of β-lactam antibiotics (β-lactams), which also includes cephalosporins, carbapenems, and monobactams. What these antibiotics have in common in their structure is a four-membered β-lactam ring. β-lactams form the basis of modern chemotherapy, as they occupy a leading or important place in the treatment of most infections.

Classification of penicillins

Natural:

Benzylpenicillin (penicillin), sodium and potassium salts

Benzylpenicillin procaine (procaine salt of penicillin)

Benzathine benzylpenicillin

Phenoxymethylpenicillin

Semi-synthetic:

isoxazolylpenicillins

aminopenicillins

Ampicillin
Amoxicillin

carboxypenicillins

Carbenicillin
Ticarcillin

ureidopenicillins

Azlocillin
Piperacillin

inhibitor-protected penicillins

Amoxicillin/clavulanate
Ampicillin/sulbactam
Ticarcillin/clavulanate
Piperacillin/tazobactam

The ancestor of penicillins (and all β-lactams in general) is benzylpenicillin (penicillin G, or simply penicillin), which has been used in clinical practice since the early 40s. Currently, the penicillin group includes a number of drugs, which, depending on their origin, chemical structure and antimicrobial activity, are divided into several subgroups. Of the natural penicillins, benzylpenicillin and phenoxymethylpenicillin are used in medical practice. Other drugs are semi-synthetic compounds obtained as a result of chemical modification of various natural AMPs or intermediate products of their biosynthesis.

Mechanism of action

Penicillins (and all other β-lactams) have a bactericidal effect. The target of their action is penicillin-binding proteins of bacteria, which act as enzymes at the final stage of the synthesis of peptidoglycan, a biopolymer that is the main component of the bacterial cell wall. Blocking peptidoglycan synthesis leads to the death of the bacterium.

To overcome the widespread acquired resistance among microorganisms associated with the production of special enzymes - β-lactamases that destroy β-lactams - compounds have been developed that can irreversibly suppress the activity of these enzymes, the so-called β-lactamase inhibitors - clavulanic acid (clavulanate), sulbactam and tazobactam. They are used to create combined (inhibitor-protected) penicillins.

Since peptidoglycan and penicillin-binding proteins are absent in mammals, β-lactams are not known to exhibit specific host toxicity.

Activity spectrum

Natural penicillins

They are characterized by an identical antimicrobial spectrum, but differ slightly in the level of activity. The MIC value of phenoxymethylpenicillin against most microorganisms is, as a rule, slightly higher than that of benzylpenicillin.

The main clinical significance is the resistance of oxacillin to staphylococcal β-lactamases. Thanks to this, oxacillin is highly active against the vast majority of strains of staphylococci (including PRSA) - causative agents of community-acquired infections. The activity of the drug against other microorganisms is of no practical importance. Oxacillin does not act on staphylococci, whose resistance to penicillins is associated not with the production of β-lactamases, but with the appearance of atypical PSB - MRSA.

The spectrum of activity of aminopenicillins has been expanded due to the action on some members of the family Enterobacteriaceae - E.coli, Shigella spp., Salmonella spp. And P.mirabilis, which are characterized by a low level of production of chromosomal β-lactamases. Ampicillin is slightly more active against Shigella than amoxicillin.

The advantage of aminopenicillins over natural penicillins is noted in relation to Haemophilus spp. The effect of amoxicillin on H. pylori.

In terms of spectrum and level of activity against gram-positive bacteria and anaerobes, aminopenicillins are comparable to natural penicillins. However, Listeria is more sensitive to aminopenicillins.

Aminopenicillins are susceptible to hydrolysis by all β-lactamases.

The antimicrobial spectrum of inhibitor-protected aminopenicillins (amoxicillin/clavulanate, ampicillin/sulbactam) has been expanded to include such gram-negative bacteria as Klebsiella spp., P.vulgaris, C.diversus, as well as anaerobes of the group B.fragilis, which synthesize class A chromosomal β-lactamases.

In addition, inhibitor-protected aminopenicillins are active against microflora with acquired resistance due to the production of β-lactamases: staphylococci, gonococci, M.catarrhalis, Haemophilus spp., E.coli, P.mirabilis.

For microorganisms whose resistance to penicillins is not associated with the production of β-lactamases (for example, MRSA, S. pneumoniae), inhibitor-protected aminopenicillins do not show any advantages.

The spectrum of action of carbenicillin and ticarcillin against gram-positive bacteria generally coincides with that of other penicillins, but the level of activity is lower.

Actinomycosis.

Since long-acting penicillins do not create high concentrations in the blood and practically do not pass through the BBB, they are not used to treat severe infections. Indications for their use are limited to the treatment of tonsillopharyngitis and syphilis (except neurosyphilis), the prevention of erysipelas, scarlet fever and rheumatism. Phenoxymethylpenicillin is used to treat mild and moderate streptococcal infections (tonsillopharyngitis, erysipelas).

Due to the increasing resistance of gonococci to penicillin, its empirical use for the treatment of gonorrhea is unjustified.

Oxacillin

Confirmed or suspected staphylococcal infections of various localizations (with confirmation of sensitivity to oxacillin or with a slight risk of spreading methicillin resistance).

Aminopenicillins and inhibitor-protected aminopenicillins

The main indications for the use of these drugs are the same. The prescription of aminopenicillins is more justified for mild and uncomplicated infections, and their inhibitor-protected derivatives for more severe or recurrent forms, as well as in the presence of data on the high incidence of β-lactamase-producing microorganisms.

The route of administration (parenteral or oral) is selected depending on the severity of the infection. For oral administration, it is more advisable to use amoxicillin or amoxicillin/clavulanate.

Additional indications for prescribing inhibitor-protected aminopenicillins are:

Carboxypenicillins and inhibitor-protected carboxypenicillins

The clinical significance of carboxypenicillins is currently decreasing. Nosocomial infections caused by sensitive strains can be considered as indications for their use. P. aeruginosa. In this case, carboxypenicillins should be prescribed only in combination with other AMPs active against Pseudomonas aeruginosa (aminoglycosides of the II-III generation, fluoroquinolones).

Indications for the use of ticarcillin/clavulanate are somewhat broader and include severe, mainly nosocomial, infections of various locations caused by multidrug-resistant and mixed (aerobic-anaerobic) microflora:

Ureidopenicillins and inhibitor-protected ureidopenicillins

Ureidopenicillins in combination with aminoglycosides are used for pseudomonas infection (in case of sensitivity P. aeruginosa).

Piperacillin/tazobactam is used to treat severe, predominantly nosocomial, mixed (aerobic-anaerobic) infections of various locations:

postpartum purulent-septic complications;

Gallbladder, bile peritonitis, liver abscesses;

Drug interactions

Penicillins cannot be mixed in the same syringe or in the same infusion system with aminoglycosides due to their physicochemical incompatibility.

When ampicillin is combined with allopurinol, the risk of ampicillin rash increases.

The use of high doses of benzylpenicillin potassium salt in combination with potassium-sparing diuretics, potassium supplements or ACE inhibitors predicts an increased risk of hyperkalemia.

Caution is required when combining penicillins active against Pseudomonas aeruginosa with anticoagulants and antiplatelet agents due to the potential risk of increased bleeding. It is not recommended to combine with thrombolytics.

The use of penicillins in combination with sulfonamides should be avoided, as this may weaken their bactericidal effect.

Cholestyramine binds penicillins in the gastrointestinal tract and reduces their bioavailability when taken orally.

Oral penicillins may reduce the effectiveness of oral contraceptives by impairing the enterohepatic circulation of estrogen.

Penicillins can slow down the elimination of methotrexate from the body by inhibiting its tubular secretion.

Patient Information

Penicillins should be taken orally with plenty of water. Ampicillin and oxacillin should be taken 1 hour before meals (or 2 hours after meals), phenoxymethylpenicillin, amoxicillin and amoxicillin/clavulanate - regardless of meals.

Prepare and take the suspension for oral administration in accordance with the attached instructions.

Strictly follow the prescribed regimen throughout the course of treatment, do not miss a dose and take it at regular intervals. If you miss a dose, take it as soon as possible; do not take if it is almost time for the next dose; do not double the dose. Maintain the duration of therapy, especially for streptococcal infections.

Do not use expired or decomposed products as they may be toxic.

Consult a doctor if improvement does not occur within a few days and new symptoms appear. If a rash, hives or other signs of an allergic reaction appear, you should stop taking the drug and consult a doctor.

Table. Penicillin group drugs.
Main characteristics and application features
INN Lekforma LS F
(inside), %
T ½, h * Dosage regimen Features of drugs
Natural penicillins
Benzylpenicillin
(potassium and sodium salt)
Por. d/in. 250 thousand units;
500 thousand units;
1 million units; 1.5 million units; 5 million units; 10 million units
into the bottle
10-20 0,5-0,7 Parenterally
Adults: 4-12 million units/day
in 4-6 injections;
for streptococcal tonsillopharyngitis - 500 thousand units every 8-12 hours for 10 days;
for meningitis and endocarditis - 18-24 million units/day
6 introductions
Children:
up to 1 month: see section “Use of AMPs in children”;
over 1 month: 50-100 thousand units/kg/day in 4 administrations;
for streptococcal tonsillopharyngitis - 25-50 thousand units/kg/day in 2 administrations for 10 days;
with meningitis -
300-400 thousand units/kg/day
in 6 injections
The main natural penicillin.
Predominant activity against gram-positive microorganisms.
High allergenicity
Benzylpenicillin procaine Por. d/in.
600 thousand units;
And
1.2 million units;
into the bottle
ND 24 V/m
Adults:
600 thousand-1.2 million units/day
in 1-2 injections
Children:
up to 1 month: see section “Use of APM in children”;
over 1 month: 50-100 thousand units/kg/day
in 1-2 injections

Indications: mild to moderate streptococcal infections, outpatient forms of pneumococcal pneumonia.
In case of overdose, mental disorders are possible.
Benzathine benzylpenicillin Por. d/in. 300 thousand units;
600 thousand units;
1.2 million units;
2.4 million units
into the bottle
ND A few days V/m
Adults: 1.2-2.4 million units
once;
for syphilis - 2.4 million units/day every 5-7 days (2-3 injections); for the prevention of rheumatism and recurrent erysipelas - 1.2-2.4 million units once a month
Children: 1.2 million units once;
for the prevention of rheumatism - 600 thousand-1.2 million units once a month
Does not create high concentrations in the blood.

Indications: syphilis, mild to moderate streptococcal infections, prevention of scarlet fever and recurrent erysipelas, year-round prevention of rheumatism
Benzylpenicillin (potassium salt)/
benzylpenicillin procaine/benzathine benzylpenicillin (1:1:1)
(Bicillin-3)
Por. d/in.
1.2 million units per bottle.
ND A few days V/m
Adults and children:
1.2 million units once
Does not create high concentrations in the blood.
Intravascular administration is not allowed.
Indications: mild to moderate streptococcal infections, year-round prevention of rheumatism.
Contraindicated if you are allergic to procaine (novocaine)
Benzathine benzylpenicillin/
benzylpenicillin procaine (4:1) ( Bicillin-5)
Por. d/in. 1.5 million units per bottle. ND A few days V/m
Adults and children: 1.5 million units once; for the prevention of rheumatism - 1.5 million units once a month
See Bicillin-3
Phenoxymethyl penicillin Table 0.1 g; 0.25 g; 0.5 g; 1.0 g; 1.5 g; 1 million units; 1.2 million IU Table. sol. 600 thousand IU;
1 million IU
Dragee 100 thousand units Port. d/susp. d/orally 0.3 g; 0.6 g; 1.2 g; 300 thousand IU/5 ml
Gran. d/susp. d/oral 125 mg/5 ml; 300 thousand IU/5 ml
Sire. 400 mg/ml; 750 thousand IU/5 ml
Cap. for oral administration 150 thousand.
IU/ml
40-60 0,5-1,0 Inside
Adults: 0.25-0.5 g every 6 hours;
for streptococcal tonsillopharyngitis - 0.25 g every 8-12 hours for 10 days;
for the prevention of rheumatism - 0.25 g every 12 hours.
Children: 30-40 mg/kg/day in 4 divided doses;
for streptococcal tonsillopharyngitis - 0.125-0.25 g every 8-12 hours for 10 days
Does not create high concentrations in the blood.
Indications: mild to moderate streptococcal infections, year-round prevention of rheumatism
Isoxazolylpenicillins
Oxacillin Caps. 0.25 g
Table 0.25 g; 0.5 g
Por. d/in. 0.25 g; 0.5 g per bottle.
25-30 0,5-0,7 Inside
Adults: 0.5-1.0 g every 6 hours 1 hour before meals
Children:
up to 1 month: see section “Use of AMPs in children”; over 1 month: 40-60 mg/kg/day in 3-4 doses (but not more than 1.5 g/day)
Parenterally
Adults: 4-12 g/day in 4-6 injections
Children: 0.2-0.3 g/kg/day in 4-6 injections
Antistaphylococcal penicillin.
When taken orally, it does not create high concentrations in the blood.
Indications: staphylococcal infections (except those caused by MRSA)
Aminopenicillins
Ampicillin Table 0.125 g; 0.25 g
Caps. 0.25 g; 0.5 g
Susp. for oral administration 0.125 g/5 ml; 0.25 g/5 ml
Por. d/in. 0.25 g; 0.5 g; 1.0 g; 2.0 g
Por. d/susp. d/orally 5 g
Sir., 0.25 g/5 ml
Por. d/cap. for oral administration for children 100 mg/ml
35-40 1,0 Inside
Adults: 0.5 g every 6 hours 1 hour before meals
Children: 30-50 mg/kg/day in 4 divided doses
Parenterally
Adults: 2-6 g/day in 4 administrations;
for meningitis and endocarditis - 8-12 g/day in 4-6 injections
Children:
up to 1 month: see section “Use of AMPs in children”; over 1 month: 50-100 mg/kg/day in 4 administrations;
for meningitis - 0.3 g/kg/day in 6 injections
The range of activity has been expanded due to E.coli, Salmonella, Shigella, non-β-lactamase-producing strains H.influenzae.
When taken orally, it does not create high concentrations in the blood. May cause non-allergic rash
Amoxicillin Table 0.125 g;
0.25 g; 0.5 g; 0.375 g; 0.75 g; 1.0 g
Table sol.
0.75 g; 1.0 g
Caps. 0.25 g; 0.5 g
Cap. d/orally 100 mg/ml
Gran. d/susp.
for oral administration 0.125 g/5 ml; 0.25 g/5 ml
75-93 ** 1-1,3 Inside
Adults: 0.25-0.5 g every 8 hours;
for the prevention of endocarditis - 3.0 g once
Children: 30-60 mg/kg/day in 3 divided doses
Bioavailability is independent of food.
Indications: infections of the DP and urinary tract of mild to moderate severity; eradication H. pylori; prevention of endocarditis
Carboxypenicillins
Carbenicillin Por. d/in. 1.0 g per bottle. 10-20 1 IV
Adults and children:
0.4-0.6 g/kg/day in 6-8 administrations
Administration is carried out by slow infusion over 30-60 minutes.
P. aeruginosa
Low activity against gram-positive cocci.
May cause electrolyte disturbances, platelet aggregation disorders, phlebitis
Ureidopenicillins
Azlocillin Por. d/in. 0.5 g; 1.0 g; 2.0 g; 4.0 g per bottle. ND 1 IV
Adults: 0.2-0.35 g/kg/day in 4-6 injections
Children:
up to 1 month: see section “Use of AMPs in children”; over 1 month: 0.2-0.3 g/kg/day in 4 administrations
The spectrum has been expanded due to Enterobacteriaceae and non-fermenting bacteria.
The main clinical significance is activity against P. aeruginosa, but now many strains are resistant.
Piperacillin Por. d/in. 1.0 g; 2.0 g; 3.0 g; 4.0 g per bottle. ND 1 IV
Adults: 0.2-0.3 g/kg/day in 4-6 injections
Children: 0.15-0.3 g/kg/day in 3-4 administrations
Administration is carried out by slow infusion over 30 minutes.
The spectrum has been expanded due to Enterobacteriaceae and non-fermenting bacteria.
The main clinical significance is activity against P. aeruginosa, but now many strains are resistant.
Better tolerated than carbenicillin
Inhibitor-protected penicillins
Amoxicillin/
clavulanate
Por. d/susp.
d/oral intake 0.156 g/5 ml for children; 0.312 g/
5 ml
Table 0.375 g; 0.625 g; 1.0 g
Por. d/cap. 0.063 g/ml
Por. liof. d/in. 0.6 g; 1.2 g
90/75 1,3/1 Inside (during meals)
Adults: 0.375-0.625 g every 8-12 hours
Children: 40-60 mg/kg/day (amoxicillin) in 3 divided doses
IV
Adults: 1.2 g every 6-8 hours.
Children: 40-60 mg/kg/day (amoxicillin) in 3 doses
H.influenzae, representatives Enterobacteriaceae And B.fragilis.
Ampicillin/
sulbactam
(Sultamicillin)

Ampicillin/
sulbactam

Table 0.375 g
Por. d/susp.
for oral administration 0.25 g/5 ml Pos. liof. d/in. 0.25 g; 0.5 g; 0.75 g; 1.0 g; 1.5 g; 3.0 g per bottle.
ND 1/1 Inside
Adults: 0.375-0.75 g every 12 hours
Children: 50 mg/kg/day in 2 divided doses
Parenterally
Adults: 1.5-12 g/day
in 3-4 injections
Children: 150 mg/kg/day
in 3-4 injections
Spectrum expanded to include PRSA, β-lactamase-producing strains H.influenzae, some representatives Enterobacteriaceae And B.fragilis.
Wider possibilities for DP and urinary tract infections. Can be used for skin and soft tissue infections, intra-abdominal infections, for prophylaxis in surgery
Ticarcillin/
clavulanate
Por. liof. d/inf. 1.6 g and 3.2 g per bottle. ND 1/1 IV
Adults: 3.1 g every 6-8 hours,
for severe infections - every 4 hours
Children: 0.2-0.3 g/kg/day in 4-6 injections
Administration is carried out by slow infusion over 30 minutes.
Spectrum expanded to include PRSA, β-lactamase-producing strains Enterobacteriaceae And B.fragilis. Used for nosocomial infections
Piperacillin/
tazobactam
Por. liof. d/inf. 2.25 g and 4.5 g per bottle. ND 1/1 IV
Adults and children over 12 years of age: 2.25-4.5 g every 6-8 hours
Administration is carried out by slow infusion over 30 minutes.
Broad spectrum, covering most gram-positive and gram-negative microorganisms, B.fragilis.
Used for nosocomial infections. Not prescribed for children under 12 years of age

* With normal kidney function

** Flemoxin solutab

Antibiotics are substances that are produced by microorganisms or synthesized using medical technologies from natural raw materials. These drugs 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 little 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. Only a doctor can select the specific dosage of a penicillin group medication; you cannot use antibiotics for treatment on your own.

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 in 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.

The most effective remedy from the ureidopenicillin group is 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 pass 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 penicillins are highly effective in eliminating infectious agents, these drugs cannot be used 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 one of the lowest toxic antibiotics, and the above side effects on the body appear 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.