List of all antibiotics of the penicillin series and a sea of ​​\u200b\u200bdata on them. Penicillin series of antibiotics: classification Antibiotics of the penicillin series names of drugs in tablets

Penicillin analogues have opened up new possibilities for physicians 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 action 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, a fairly wide use and a good indicator of bactericidal action, but they are much more common than doctors would like. This is due to the organic nature of antibiotics. Another negative quality can also be attributed to the difficulty in combining them with other drugs, especially those similar in class.

Story

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

Before the Second World War, British microbiologists worked on the issue of industrial production of drugs in the required volumes. The same problem was solved in parallel in the United States. Since then, penicillin has become the most common drug. But over time, others were isolated and synthesized, which gradually replaced him from the podium. In addition, microorganisms began to develop resistance to this drug, which complicated the treatment of severe infections.

The principle of antibacterial action

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

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

Human danger

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

Action spectrum

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

Scientists invent more and more new types of penicillins, trying to prevent bacteria from getting used 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 dysbacteriosis, since the human intestine is colonized by bacteria that are sensitive to the effects of penicillin. This is worth remembering when taking medication.

Main types (classification)

Modern scientists offer 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 with resistance to penicillinase. They are 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

For example, it is worth giving a few of the most common medicines at the moment that correspond to this group. Probably the most famous of the pennicillins can be considered "Bicillin-3" and "Bicillin-5". They pioneered a group of natural antibiotics and were the flagships in their category until more advanced forms of antimicrobials came along.

1. "Extencillin". Instructions for use states that it is a long-acting beta-lactam antibiotic. Indications for its use are exacerbations of rheumatic disease and diseases caused by treponema (syphilis, yaws and pinta). Available in powders. "Extencillin" instructions for use do not recommend combining with non-steroidal anti-inflammatory drugs (NVPS), since competitive interaction is possible. This may adversely affect the effectiveness of treatment.
2. "Penicillin-Fau" refers 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 surgical interventions, to maintain remission in rheumatism, chorea minor, bacterial endocarditis.
3. Antibiotic "Ospen" is an analogue of the previous drug. It comes in the form of tablets or granules. It is not recommended to combine with NVPS and oral contraceptives. Often used in the treatment of childhood diseases.

Semi-synthetic forms

This group of drugs includes chemically modified antibiotics derived from molds.

1. The first on this list is Amoxicillin. Instructions for use (price - about a hundred rubles) indicates 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 do not idealize "Amoxicillin". Instructions for use (the price may vary in different regions) warns that the drug should not be prescribed to patients with mononucleosis, allergies 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, it can be taken orally, it is well absorbed in the intestine. It is rapidly 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 the form of tablets or in vials as a liquid for injection.
3. The last representative of semi-synthetic 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. Patients are well tolerated, but caution should be given to those who take anticoagulants (for example, people with pathology of the cardiovascular system), as the drug potentiates their action.

Solvent

Penicillins are sold in pharmacies as a powder for injection. Therefore, for intravenous or intramuscular administration, they must be dissolved in a 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 diagnoses: lobar and focal pneumonia, pleural empyema, sepsis and septicemia, septic endocarditis, meningitis, osteomyelitis. Bacterial tonsillitis, diphtheria, scarlet fever, anthrax, gonorrhea, syphilis, purulent skin infections fall into the field of action.

There are few contraindications to treatment with the penicillin group. First, the presence of hypersensitivity to the drug and its derivatives. Secondly, the established diagnosis of epilepsy, which does not make it possible to inject the drug into 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 transferred to another method of feeding, as the drug penetrates into the milk.

Side effects can be observed at several levels at once.

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

Features of use

With caution, it is necessary to prescribe to patients with impaired liver and kidney function, with 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, no changes in the patient's condition have occurred, then it is necessary to use penicillin analogues or replace the group of antibiotics. Simultaneously with the appointment, for example, the substance "Bicillin-3", care must be taken to prevent fungal superinfection. For this, antifungal drugs are prescribed.

It is necessary to clearly explain to the patient that the interruption of the medication without good reason causes the 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 open group of antibiotics, it still remains relevant for the treatment of meningitis, gonorrhea and syphilis, has a broad enough spectrum of action and mild side effects to be prescribed to children. Of course, like any medicine, penicillins have contraindications and side effects, but they are more than offset by the possibilities for use.

It would seem - what are mushrooms? Representatives of the nature of our planet, which grow in every forest and not only: they are also grown in an industrial environment; we eat them, and some of their species contain a huge amount of poisons - they can kill any adult. In addition, they are the culprits of a large group of skin diseases and lesions of the human mucous membranes.

But there is one unique representative of this species in this kingdom of living organisms - a fungus of the genus Penicillium, which, for almost a hundred years, has been saving the lives of millions and millions of people. All humanity is grateful for its discovery talented scientist from Scotland Alexander Flemming.

This world discovery happened almost by accident: the scientist, after a long trip, returned to his laboratory and found a forgotten Petri dish on his desk. In it, during his absence, mold has grown - and a ring with dead microbes has appeared around it. The microbiologist immediately began to study this phenomenon, but pure penicillin was obtained only 13 years later. At the same time, they began to use it in medical practice and put it into mass production. In the 40s of the last century, the first antibiotics were already treating a huge variety of diseases.

Scope of action of penicillin antibiotics

With bacterial pathogens, any antibiotic-penicillin fights mercilessly and effectively: drugs that work according to the bactericidal scheme of action on pathogenic microorganisms damage the structure of their cell walls, and due to the difference in pressure between the external and internal environment, they die.

Penicillins react to a specific substance in the cell walls of bacteria - peptidoglycan, due to which the process of destruction occurs. In the human body, cells do not contain such a substance in their structure, so penicillins do not have a negative effect on the building material of the cell.

Therefore, doctors and scientists from the very beginning of the use of penicillins argued that this drug does not have toxicity and harmful effects. . A bacteriostatic action antibiotics is as follows: in pathogenic microflora, the process of reproduction is temporarily inhibited, due to which human immunity is able to destroy the existing pathogenic environment. The list of pathogens with which the penicillin group of antibiotics fights is considerable. Among them, it is worth noting the most common:

• streptococci,
• meningococcus,
• staphylococci,
• gonococcus,
• pneumococci,
• tetanus stick,
• botulism stick,
• anthrax bacteria,
• diphtheria bacteria and many others

List of penicillin antibiotics

It makes no sense to ask which antibiotic is better - the active agent in each drug works in a similar way. But it just so happened that among physicians there are more prescribed drugs of this group. This may be due to the convenience of taking, and a short course of treatment, and a proven manufacturer. Therefore, among the population, such drugs are most famous and trusted in the appointment. Below you can see the list of antibiotics of the penicillin series of drugs.

The nuances of the use of antibiotics based on penicillin in pediatrics

A child's body is significantly different from an adult: many of its systems and organs are not yet fully formed and do not work with 100% efficiency. The impact of any drug on a child's body is many times stronger than on an adult. Therefore, every pediatrician approaches the appointment of antibiotics for babies and growing children with great care.

This group of drugs used in the treatment of infants with sepsis and toxic lesions; in the first 3 years after birth, they also treat otitis media, meningitis, pleurisy, and pneumonia. Amoxicillin, amoxiclav or flemoxin have the least toxic effect on the child's not yet fully formed organism - these drugs are the most effective in pediatric practice among penicillin drugs.

Prescribing and adjusting the dosage only a pediatrician is engaged, in no case should you prescribe medications yourself: this can harm the health of the child. During pregnancy, treatment with penicillins should also be carried out with extreme caution - after consulting the attending physician. In this case, the antibiotic has free access to the fetus, which can harm a small developing organism. During the feeding period, it is recommended to switch to milk formulas, since antibiotics tend to penetrate into breast milk.

Areas of medical practice where penicillin antibiotics are used

Since its inception, antibacterial therapy in the form of penicillin antibiotics has penetrated literally into all areas of modern medicine. Even though that for several decades of their use, many pathogens have developed resistance to penicillins, they are still the leading link in antibacterial therapy in many branches of medicine.

Recommendations for therapy with penicillin antibiotics

Even antibiotics of the latest generation, unfortunately, have side effects on the body of an adult and, especially, a child. They quite effectively destroy the cause of the disease - pathogenic microbes that have entered the body, but they also have a detrimental effect on their own intestinal microflora. Therefore, a common side effect the use of antibiotics is to reduce the body's defenses of immunity.

After a course of treatment with penicillin preparations, the body needs time to recover, and in the severe symptoms of such a side effect, a special diet. It consists in the use of a large amount of fermented milk products, which perfectly restores the normal functioning of the microflora of the gastrointestinal tract. For a couple of weeks, it is worth limiting the use of salty, spicy foods, as well as fatty and high-calorie foods.

While taking antibiotics and for two weeks after, doctors recommend taking prebiotics and probiotics, which will protect beneficial bacteria. gastrointestinal tract and will contribute their colonization in the stomach and intestines.

If an antibiotic of the penicillin series toxic effect on liver cells is confirmed, then a course of treatment with hepatoprotectors should be taken. They will protect the liver and restore its damaged cellular material.

The consequence of a decrease in immunity against the background of taking antibiotics is an increased predisposition to colds, so you should not expose the body to hypothermia. In this case, it is worth drinking a course of immunomodulators (immunal, echinacea preparations).

And most importantly, do not self-medicate: if you need to use penicillin antibiotics, you should consult your doctor to select and adjust the dosage of one or another antibiotic.

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

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

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

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

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

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

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

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

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

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

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

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

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

Short acting:

benzylpenicillin (sodium salt),

benzylpenicillin (potassium salt);

Long lasting:

benzylpenicillin (novocaine salt),

Bicillin-1,

Bicillin-5.

I.2.

phenoxymethylpenicillin (penicillin V).

II. Semi-synthetic penicillins

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

Penicillinase resistant:

oxacillin (sodium salt),

nafcillin;

Broad spectrum of action:

ampicillin,

amoxicillin.

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

Broad spectrum of action, including Pseudomonas aeruginosa:

carbenicillin (disodium salt),

ticarcillin,

azlocillin.

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

carbenicillin (indanyl sodium),

carfecillin.

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

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

2. Isoxazolpenicillins (oxacillin, cloxacillin, flucloxacillin).

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

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

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

6. Ureidopenicillins (azlocillin, mezlocillin, piperacillin).

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

1. Natural:

benzylpenicillin (penicillin G),

phenoxymethylpenicillin (penicillin V),

benzathine benzylpenicillin,

benzylpenicillin procaine,

benzathine phenoxymethylpenicillin.

2. Antistaphylococcal:

oxacillin.

3. Extended spectrum (aminopenicillins):

ampicillin,

amoxicillin.

4. Active towards Pseudomonas aeruginosa:

Carboxypenicillins:

ticarcillin.

Ureidopenicillins:

azlocillin,

piperacillin.

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

amoxicillin / clavulanate,

ampicillin/sulbactam,

ticarcillin/clavulanate.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Acid-resistant, effective when administered orally;

Possessing a wide spectrum of activity.

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

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

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

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

The main pharmacokinetic differences between isoxazolpenicillins and benzylpenicillin:

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

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

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

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

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

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

Penicillins with an extended spectrum of activity

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

I. Drugs that do not affect Pseudomonas aeruginosa:

Aminopenicillins: ampicillin, amoxicillin.

II. Drugs active against Pseudomonas aeruginosa:

Carboxypenicillins: carbenicillin, ticarcillin, carfecillin;

Ureidopenicillins: piperacillin, azlocillin, mezlocillin.

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

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

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

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

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

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

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

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

Possibility of appointment inside;

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

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

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

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

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

Antipseudomonal penicillins

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

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

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

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

All antipseudomonal penicillins are destroyed by beta-lactamases.

Pharmacokinetic features of ureidopenicillins:

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

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

Multiplicity of application - 3 times a day;

Secondary bacterial resistance develops rapidly.

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

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

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

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

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

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

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

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

Indications for the use of penicillins

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

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

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

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

The use of penicillins in urological practice. In urological practice, inhibitor-protected drugs are widely used from penicillin antibiotics (the use of natural penicillins, as well as the use of semi-synthetic penicillins as drugs of choice, is considered unjustified due to the high level of resistance of uropathogenic strains.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Pediatrics. When using penicillins in children, specific pediatric problems have not been registered, however, it should be borne in mind that insufficiently developed kidney function in newborns and young children can lead to cumulation of penicillins (in this regard, there is an increased risk of neurotoxicity with the development of seizures).

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

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

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

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

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

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

Thus, at present, most strains Staphylococcus spp. resistant to natural penicillins. In recent years, the frequency of detection of resistant strains has increased. Neisseria gonorrhoeae.

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

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

Antibiotics of the penicillin series are considered the first AMPs that were developed from the waste products of certain bacteria. In the general classification, they are in the class of beta-lactams. In addition to penicillins, this also includes carbapenems, cephalosporins, and monobactams. The similarity is due to the fact that there is a four-membered ring. All drugs from this group are used in chemotherapy. They play an important role in the treatment of infectious diseases.

Initially, all drugs of the penicillin group came from ordinary penicillin. It has been used in medicine since the 1940s. Many subgroups of both natural and synthetic origin have now been created:

1. natural penicillins.
2. Oxacillin.
3. Aminopenicillin.

Natural penicillin medicines are used in a number of cases. For example, drugs that belong to the natural group of penicillins are recommended only for the treatment of those infections whose etiology is already known. For example, this can be confirmed during diagnostic measures or by characteristic symptoms. Depending on the form and how severe the disease develops, medications are prescribed for internal or parenteral use. Penicillins from the natural group help in the treatment of rheumatism, scarlet fever, tonsillopharyngitis, erysipelas, sepsis, pneumonia.

In addition, such funds are prescribed for the treatment of other diseases that are provoked by streptococcus. For example, this applies to infectious-type endocarditis. For this disease, not only antibiotics from this group are used, but also drugs that have the following names: streptomycin, gentamicin, etc. Diseases that are caused by a meningococcal type infection can also be cured with natural penicillins. Indications for their use are leptospirosis, gangrene, Lyme disease, syphilis, actinomycosis.

By the way, it is necessary to take into account the fact that drugs with a prolonged effect do not have a high concentration in the blood, so they are not prescribed for the treatment of severe forms of the disease. The only exceptions are syphilis, tonsillopharyngitis, rheumatism and scarlet fever. If earlier medicines from this group were used to treat gonorrhea, now the causative agents of the disease quickly adapted and became resistant to these drugs.

As for oxacillin, it is prescribed only when the disease is caused by a staphylococcal infection, and this does not depend on its location. Infection may already be confirmed in the laboratory or only suspected.

However, in any case, before prescribing such drugs to a patient, it is necessary to check whether bacteria are susceptible to their action. Medicines from the oxacillin group are prescribed in case of sepsis, pneumonia, meningitis, endocarditis caused by a bacterial infection, as well as for various lesions of bones, skin, joints, soft tissues that are caused by infections.

Aminopenicillins are prescribed in cases where the disease proceeds in a fairly mild form, and without any complications in the form of other infections. Inhibitor-protective forms of aminopenicillins are used in the case of relapses in severe illness. There are many medicines, including antibiotics in tablets. Substances are administered either orally or parenterally. Such funds are prescribed for the acute form of cystitis, pyelonephritis, pneumonia, sinusitis, exacerbation of the chronic form of bronchitis.

In addition, indications for use are intestinal diseases that are caused by infections, endocarditis, meningitis. Sometimes inhibitor-protective derivatives are prescribed by doctors for a preoperative form of prevention and in the treatment of infectious diseases of the skin and soft tissues.

What else applies?

The following drugs are also used:

1. Carboxypenicillin. Drugs from the group of carboxypenicillins are now used less and less in medicine. They can be prescribed only in the case of infections of the nosocomial type. Such drugs should be used only in complex therapy along with drugs that can affect Pseudomonas aeruginosa. As for indications for use, carboxypenicillins are prescribed for infections on the skin, bones, soft tissues, and joints. Also, these drugs will be needed for abscess, pneumonia, sepsis, infection in the pelvic organs.
2. Ureidopenicillin. Drugs from the group of ureidopenicillins are often prescribed only together with aminoglycosides. This combination helps to cope with Pseudomonas aeruginosa. Indications for use are infectious diseases of the pelvic organs, soft tissues, skin (diabetic foot is also included). In addition, such funds will be needed for peritonitis, hepatic abscess, pneumonia, lung abscess.

Mechanism of action

Preparations from the penicillin group have a bactericidal effect. They affect the penicillin-binding proteins that are found in all bacteria. These compounds act as enzymes that are already involved in the final stage of microorganism wall synthesis. As a result, the production of the substance is blocked, and the bacterium dies. In addition, clavulonic acid, tazobactam and sulbactam have been developed to inhibit certain enzymatic substances. They are part of the drugs that belong to complex penicillins.

As for the effect on the human body, carboxypenicillins, benzylpenicillins and ureidopenicillins are destroyed in the human body due to hydrochloric acid, which is part of the gastric juice. In this regard, they can only be used parenterally. Preparations that contain oxacillin, phenoxymethylpenicillin and aminopenicillin, on the contrary, are resistant to the influence of an acidic environment, and they can be used orally. By the way, amoxicillin is best absorbed through the organs of the gastrointestinal tract. As for the worst digestibility indicators, oxacillin and ampicillin have parameters of only 30%.

Substances that are part of penicillin preparations are perfectly distributed throughout the body, affecting tissues, body fluids, and organs. High concentrations will be in the kidneys, mucous membranes, intestines, lungs, genitals, fluids. A small dose can pass through breast milk and the placenta. Practically do not get to a prostate gland. Significant transformation in the liver is characteristic of ureidopenicillins and oxacillins. Other substances from this group are excreted from the body practically unchanged. In most cases, excretion is by the kidneys. The time it takes to remove the substance is about an hour. If the patient is diagnosed with renal insufficiency, then the time will increase. Almost all types of penicillins are excreted from the body through hemodialysis.

Contraindications and side effects

Like all drugs, drugs with penicillin have their own contraindications. Basically, this only applies to allergies to penicillin. People who are at risk of an allergic reaction due to intolerance to certain components should not use these medicines. The same applies to an allergic reaction to novocaine.

As for side effects, in case of overdose or improper use of drugs, there is a risk of an allergic reaction. It can be dermatitis, rash, urticaria. In rare cases, Quincke's edema, anaphylactic shock, bronchospasm, and fever appear. If a person has an anaphylactic shock, then glucocorticoids, adrenaline, oxygen therapy will be required. It is also urgent to ensure the work of the respiratory tubular organs.

As for problems with the functioning of the central nervous system, in rare cases, tremors and mental disorders appear.

Sometimes the patient has a headache, convulsions appear.

Basically, this happens in those people who suffer from kidney failure.

More often there are problems with the work of the digestive tract. A person can feel sick, there are vomiting attacks, abdominal pain, colitis. In this case, it is necessary to refuse such drugs. Additionally, if colitis is suspected, sigmoidoscopy is prescribed. To restore health, you need to return the water and electrolyte balance to normal. Sometimes taking drugs from the penicillin group also leads to a violation of these processes.

This leads to hyperkalemia, hypernatremia. As a result, blood pressure changes, edema appears. In some cases, there may be problems in the functioning of the liver, kidneys, various hematological reactions, complications of the state of the blood vessels. In rare cases, oral or vaginal candidiasis develops.

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

The influence of the penicillin series is determined by their ability to provoke the death of pathogenic microflora. Penicillin antibiotics act bactericidal, entering into association with bacterial enzymes, disrupting the synthesis of the bacterial wall.

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

Classification

There are two main groups of penicillins:

• natural;
• semi-synthetic.

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

The spectrum of action of penicillins

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

1. Staphylococcus.
2. Streptococcus.
3. Pneumococcus.
4. Listeria.
5. Bacilli.
6. Meningococcus.
7. Gonococcus.
8. Ducrey-Unna's stick.
9. Clostridia.
10. Fusobacteria.
11. Actinomycetes.
12. Leptospiram.
13. Borrelia.
14. Pale spirochete.

The spectrum of influence of semi-synthetic penicillin antibiotics is somewhat wider than that of natural ones.

Antimicrobials from this list are classified according to the spectrum of effects, as:

• not active to Pseudomonas aeruginosa;
• antipseudomonal drugs.

When are penicillins prescribed?

Antimicrobial agents of this group are used to eliminate:

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

Aminopenicillins

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

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

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

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

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

List of names of penicillin antibiotics

The most effective drugs in the fight against ailments:

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

Drugs show resistance to staphylococcal penicillinases, which eliminate other drugs of this series. The most popular is considered - "Oxacillin".

Antipseudomonal penicillins

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

Antibiotics of the penicillin series (names):

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

Combined drugs

Inhibitor-protected penicillins include medicines that include an antibiotic and a component that blocks the activity of bacterial beta-lactamase.

The inhibitors are:

• clavulanic acid;
• tazobactam;
• sulbactam.

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

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

Combined drugs include the antimicrobial drug Ampiox and its generic Ampiox-sodium, which contains Ampicillin and Oxacillin.

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

Medicines for adults

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

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

Against prostatitis, such antimicrobial agents are not used, since they do not enter the prostate tissue. In case of allergic manifestations to penicillins, the patient may develop nettle rash, anaphylaxis, and during cephalosporin therapy.

"Ampicillin"

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

"Flemoxin Solutab"

People who are prone to allergies to drugs should be tested for sensitivity before therapy. The drug is not prescribed to patients who have already had intense adverse reactions to penicillin.

Treatment must be completed. Interruption of therapy ahead of time can lead to the development of resistance of pathogens to the active substance and the transition of the disease to the chronic stage.

"Amoxiclav"

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

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

"Augmentin"

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

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

Penicillins for the treatment of children

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

The list of penicillin antimicrobials intended for the treatment of children includes Amoxicillin and generics, Augmentin, Amoxiclav, as well as Flemoxin and Flemoklav Solutab. Medicines in the form of dispersible tablets act no less effectively than injections and cause fewer problems in treatment.

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

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

"Ospamox"

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

Daily concentration is divided into several uses. Duration of therapy: until the symptoms disappear plus five days. To make a suspension, the bottle with granules is filled with water, then shaken. Dosing of the drug to "Ospamox" will be as follows:

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

Contraindications and side effects

Restrictions for admission include an allergy to antibiotics of the penicillin series. If rashes, itching occur during therapy, it is necessary to stop using the medication and consult a doctor.

Allergy can be manifested by Quincke's edema, anaphylaxis. The list of adverse reactions in penicillins is small. The main negative phenomenon is the inhibition of beneficial intestinal microflora.

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

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

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

An extensive list of negative effects in "Oxacillin" and substitutes:

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

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

Opinions

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

But the therapy of pathological conditions using antibiotics should be carried out only after the diagnosis is established and strictly according to the doctor's prescription. Of the most effective antimicrobial agents, Amoxiclav, Ampicillin, Flemoxin Solutab are distinguished.

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