Amoxicillin belongs to the penicillin group. penicillin antibiotics. Short acting natural antibiotics

Content

The first antibiotics were penicillins. Medicines have helped save millions of people from infections. The drugs are effective in our time - they are constantly modified, improved. Many popular antimicrobial agents have been developed based on penicillins.

General information about penicillin antibiotics

The first antimicrobial drugs developed on the basis of the waste products of microorganisms are penicillins (Penicillium). Their ancestor is benzylpenicillin. Substances belong to a wide range of β-lactam antibiotics. A common feature of the beta-lactam group is the presence of a four-membered beta-lactam ring in the structure.

Penicillin antibiotics inhibit the synthesis of a special polymer - peptidoglycan. It is produced by the cell to build a membrane, and penicillins prevent the formation of a biopolymer, which leads to the impossibility of cell formation, causes lysis of the exposed cytoplasm and the death of the microorganism. The drug does not have a detrimental effect on the cellular structure of humans or animals due to the fact that peptidoglycan is absent in their cells.

Penicillins work well with other drugs. Their effectiveness weakens with complex treatment together with bacteriostatics. The penicillin series of antibiotics is effectively used in modern medicine. This is possible due to the following properties:

• Low toxicity. Among all antibacterial drugs, penicillins have the smallest list of side effects, provided that they are correctly prescribed and the instructions are followed. Medicines are approved for use in the treatment of newborns and pregnant women.
• Wide spectrum of action. Modern antibiotics of the penicillin series are active against most gram-positive, some gram-negative microorganisms. Substances are resistant to the alkaline environment of the stomach and penicillinase.
• Bioavailability. A high level of absorption ensures the ability of beta-lactams to quickly spread through tissues, penetrating even into the cerebrospinal fluid.

Classification of penicillin antibiotics

Antimicrobial agents based on penicillin are classified according to many criteria - belonging, compatibility, mechanism of action. The inability of natural penicillin substances to resist penicillinase determined the need for the creation of synthetic and semi-synthetic drugs. Based on this, the classification of this type of antibiotics according to the method of manufacture is informative for understanding the pharmacological properties of penicillins.

Biosynthetic

Benzylpenicillin is produced by the fungi Penicillium chrysogenum and Penicillium notatum. According to the molecular structure, the active substance belongs to acids. For medicine, it is chemically combined with potassium or sodium, resulting in salts. They are the basis of powders for injection solutions, which are quickly absorbed into the tissues. The therapeutic effect occurs within 10-15 minutes after administration, but after 4 hours the effect of the substance ends. This necessitates multiple injections.

The active substance quickly penetrates into the mucous membranes and lungs, to a lesser extent - into the bones, myocardium, synovial and cerebrospinal fluid. To prolong the action of drugs, benzylpenicillin is combined with novocaine. The resulting salt at the injection site forms a drug depot, from where the substance slowly and constantly enters the bloodstream. This helped to reduce the number of injections to 2 r/d while maintaining the therapeutic effect. These drugs are aimed at long-term treatment of syphilis, streptococcal infection, rheumatism.

Biosynthetic penicillins are active against most pathogens, except for spirochetes. For the treatment of moderate infections, a benzylpenicillin derivative, phenoxymethylpenicillin, is used. The substance is resistant to the effects of hydrochloric acid in the gastric juice, so it is produced in the form of tablets and taken orally.

Semi-synthetic antistaphylococcal

Natural benzylpenicillin is not active against staphylococcus strains. For this reason, oxacillin was synthesized, which inhibits the action of beta-lactamases of the pathogen. Semi-synthetic penicillins include methicillin, dicloxacillin, cloxacillin. These drugs are rarely used in modern medicine due to their high toxicity.

Aminopenicillins

This group of antibiotics includes ampicillin, amoxicillin, thalampicillin, bacampicillin, pivampicillin. Means are active to a wide range of pathogens and are available in tablets. The disadvantage of drugs is the ineffectiveness of amoxicillin and ampicillin to strains of staphylococcus aureus. For the treatment of such diseases, substances are combined with oxacillin.

Aminopenicillins are rapidly absorbed and act for a long time. For a day, 2-3 pills are prescribed according to the doctor's decision. Of the side effects, only an allergic rash is observed, which quickly disappears after the drug is discontinued. The drugs are used to treat the following conditions:

• upper respiratory and urinary tract infections;
• sinusitis;
• enterocolitis;
• otitis;
• causative agent of stomach ulcers (Helicobacter pylori).

Antipseudomonal

Antibiotics of the penicillin group have a similar effect to aminopenicillins. The exception is pseudomonads. Substances are effective in the treatment of diseases caused by Pseudomonas aeruginosa. The drugs in this group include:

Inhibitor-protected combined

Preparations of this group are artificially synthesized to increase the resistance of the active substance to most microorganisms. Medicines are obtained by combining with clavulanic acid, tazobactam, sulbactam, which provide immunity to beta-lactamases. Protected penicillins have their own antibacterial effect, enhancing the action of the main substance. Drugs are successfully used in the treatment of severe nosocomial infections.

penicillin tablets

The use of penicillins in tablets is convenient and beneficial for patients. No need to spend money on injection syringes, treatment is carried out at home on your own. Penicillin antibiotics:

Name	Active substance	Indications	Contraindications	Price, rub
Azithromycin	Azithromycin dihydrate	Acute bronchitis, impetigo, chlamydial urethritis, borreliosis, erythema	Kidney disease, component intolerance, myasthenia gravis
Oxacillin	oxacillin	Joint, bone, skin infections, sinusitis, bacterial meningitis, and endocarditis	Hypersensitivity to penicillins
Amoxicillin Sandoz	amoxicillin	Tonsillitis, bacterial pharyngitis and enteritis, community-acquired pneumonia, cystitis, endocarditis	Sensitivity to penicillin, cross-allergy with other beta-lactam agents
Phenoxymethylpenicillin	phenoxymethylpenicillin	Angina, bronchitis, pneumonia, syphilis, gonorrhea, tetanus, anthrax	Pharyngitis, aphthous stomatitis, sensitivity to penicillins
Ampicillin	ampicillin trihydrate	Infections of the gastrointestinal tract, bronchopulmonary and urinary tract, meningitis, sepsis, erysipelas	Lymphocytic leukemia, infectious mononucleosis, liver dysfunction
Amoxicillin	amoxicillin	Urethritis, pyelonephritis, pneumonia, bronchitis, listeriosis, gonorrhea, leptospirosis, Helicobacter	Allergic diathesis, hay fever, infectious mononucleosis, asthma, lymphocytic leukemia, diseases of the liver, blood and central nervous system
	azithromycin	Soft tissue infections, skin infections, respiratory tract infections, Lyme disease, cervicitis, urethritis	Azithromycin sensitivity, liver disease, combination with dihydroergotamine and ergotamine
Amoxiclav	amoxicillin, clavulanate	Acute otitis, sinusitis, bronchitis, pharyngeal abscess, pneumonia, infections of the skin, gynecological, biliary tract, connective and bone tissue	Liver disease, lymphocytic leukemia, infectious mononucleosis, hypersensitivity to penicillins

In injections

For injections, penicillin G sodium salt is used 500 thousand or 1 million units. The powder is released in glass bottles sealed with a rubber cap. Before use, the product is diluted with water. Examples of drugs:

Name	Active substance	Indications	Contraindications	Price, rub
Ampicillin	ampicillin sodium salt	Cystitis, pyelonephritis, bacterial sinusitis, intra-abdominal and female genital infections	Liver and kidney disorders, colitis, leukemia, HIV
Bicillin-1	benzathine benzylpenicillin	Syphilis, scarlet fever, bacterial skin infection	Intolerance to components, a tendency to allergies
Benzylpenicillin	benzylpenicillin	Sepsis, pyemia, osteomyelitis, meningitis, diphtheria, actinomycosis, scarlet fever, blennorrhea	Hypersensitivity to penicillins and cephalosporins
Ospamox	amoxicillin	Pneumonia, otitis media, bronchitis, prostatitis, endometritis, gonorrhea, erysipelas, typhoid fever, listeriosis	Epilepsy, acute lymphocytic leukemia, asthma, allergic diathesis, hay fever
Benzylpenicillin novocaine salt	benzylpenicillin	Croupous and focal pneumonia, syphilis, diphtheria, meningitis, septicemia, blennorrhea	Hypersensitivity to penicillins, epilepsy - for endolumbar injections

Today, no medical institution can do without an antibiotic. Successful treatment of various diseases is possible only through the appointment of effective antibiotic therapy. Antibiotic today is represented by a wide range of different drugs aimed at the death of the pathogenic environment of a bacterial nature.

The first antibiotic created was penicillin, which defeated some epidemics and deadly diseases in the 20th century. To date, antibiotics of the penicillin group are rarely used in medical practice due to the high sensitivity of patients and the risk of developing allergies.

Groups of antibiotics without penicillin

Antibacterial therapy without the use of penicillin components involves the appointment of alternative drugs of other pharmacological groups. Antibiotics without penicillin in a large assortment are available for the treatment of various diseases in hospital and outpatient practice in children or adults.

Group of cephalosporins

Cephalosporins are broad-spectrum antibiotics, which is due to the detrimental effect on many groups of microorganisms, strains and other pathogenic environments. Preparations of the cephalosporin group are available as intramuscular or intravenous injections. Antibiotics of this group are prescribed for the following conditions:

Known cephalosporins include Ceforal, Suprax, Pancef. All antibiotics of this series have similar side effects, for example, dyspeptic disorders (stool disorder, skin rashes, nausea). The main advantage of antibiotics is not only the detrimental effect on many strains, but also the possibility of treating children (including the neonatal period). Cephalosporin antibiotics are classified into the following groups:

1st generation

Antibiotics-cephalosporins include Cefadroxil and Cefalexin, Cefazolin, Cefuroxime.

They are used for inflammatory diseases caused by many anaerobic bacteria, staphylococcal infection, streptococci and others.

Forms of release of the drug are varied: from tablets to solutions for parenteral administration.

II generation

Known drugs in this group: Cefuroxime (injections), Cefaclor, Cefuroxime axetil. The drugs are particularly active against many Gram-positive and Gram-negative bacteria. The drugs are available both in the form of solutions and in tablet form.

III generation

Antibiotics of this series just belong to a wide spectrum of action. The drugs act on almost all microorganisms and are known by the following names:

• Ceftriaxone;
• Ceftazidime;
• Cefoperazone;
• Cefixime and Ceftibuten.

Release form - injections for intravenous or intramuscular administration. When the drug is administered, it is often mixed with saline or lidocaine solution to reduce pain. The drug and additional components are mixed in one syringe.

IV generation

The group is represented by only one drug - Cefepime. The pharmaceutical industry produces the drug in the form of a powder, which is diluted just before administration through the parenteral or intramuscular route.

The detrimental effect of the antibiotic is to disrupt the synthesis of the body wall of the microbial unit at the cellular level. The main advantages include the possibility of outpatient treatment, ease of use, use in young children, minimal risks of side effects and complications.

Macrolide group

Antibiotics from the group of macrolides are a new generation of drugs, the structure of which is a complete macrocyclic lactone ring. According to the type of molecular-atomic structure, this group received its name. Several types of macrolides are distinguished from the number of carbon atoms in the molecular composition:

• 14, 15-membered;
• 15 members.

Macrolides are particularly active against many gram-positive cocci bacteria, as well as pathogens acting at the cellular level (for example, mycoplasmas, legionella, campylobacter). Macrolides have the least toxicity and are suitable for the treatment of inflammatory diseases of the ENT organs (sinusitis, whooping cough, otitis media of various classifications). The list of macrolide drugs is as follows:

Numerous medical studies have confirmed the low likelihood of side effects. The main disadvantage can be considered the rapid development of resistance of various groups of microorganisms, which explains the lack of therapeutic results in some patients.

Fluoroquinolone group

Antibiotics from the fluoroquinol group do not contain penicillin and its components, but are used to treat the most acute and severe inflammatory diseases.

These include purulent bilateral otitis, severe bilateral pneumonia, pyelonephritis (including chronic forms), salmonellosis, cystitis, dysentery and others.

Fluoroquinols include the following drugs:

• Ofloxacin;
• Levofloxacin;
• Ciprofloxacin.

The very first developments of this group of antibiotics date back to the 20th century. The best-known fluoroquinols can belong to different generations and solve individual clinical problems.

1st generation

Well-known drugs from this group are Negram and Nevigramone. The basis of antibiotics is nalidixic acid. Drugs have a detrimental effect on the following types of bacteria:

• Proteus and Klebsiella;
• shigella and salmonella.

Antibiotics of this group are characterized by strong permeability, a sufficient number of negative consequences of taking. According to the results of clinical and laboratory studies, the antibiotic confirmed the absolute uselessness in the treatment of gram-positive cocci, some anaerobic microorganisms, Pseudomonas aeruginosa (including the nosocomial type).

II generation

Antibiotics of the second generation are obtained due to the combination of chlorine atoms and quinoline molecules. Hence the name - a group of fluoroquinolones. The list of antibiotics in this group is represented by the following drugs:

Second-generation antibiotics are prescribed for serious surgical situations and are used in patients of any age group. Here the main factor is the risk of death, and not the appearance of any side effects.

III, IV generation

The main pharmacological drugs of the 3rd generation include Levofloxacin (otherwise, Tavanic), used for chronic bronchitis, severe bronchial obstruction in other pathologies, anthrax, diseases of the ENT organs.

Moxifloxacin (pharmacol. Avelox), known for its inhibitory effect on staphylococcal microorganisms, is reasonably ranked as the 4th generation. Avelox is the only drug that is effective against non-spore-forming anaerobic microorganisms.

Antibiotics of various groups have special indications, indications, as well as contraindications for use. In connection with the uncontrolled use of antibiotics without penicillin and others, a law was passed on prescription dispensing from pharmacy chains.

Such introductions are very necessary for medicine due to the resistance of many pathogenic environments to modern antibiotics. Penicillins have not been widely used in medical practice for more than 25 years, so it can be assumed that this group of drugs will effectively affect new types of bacterial microflora.

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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.

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

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

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

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

Antibiotics of the penicillin group

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

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

General properties of penicillins

Antibacterial drugs from the penicillin group have the following properties:

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

Side effects of penicillin ov

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

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

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

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

Electrolyte imbalances- in patients with heart failure, with the introduction of large doses of sodium salt, edema may increase, and with hypertension, an increase in blood pressure (BP) (1 million IU contains 2.0 mmol of sodium).

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

Prevention measures

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

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

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

Indications for the use of penicillins

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

Preparations of natural penicillins

Preparations of natural penicillins include the following:

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

Phenoxymethylpenicillin

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

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

Side effects

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

Indications for use

1. Prevention of pneumococcal infections in individuals after splenectomy.

Benzathine phenoxymethylpenicillin

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

Indications for use

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

Prolonged penicillin preparations

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

Side effects long-acting penicillin preparations

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

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

Indications for use

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

Benzylpenicillin novocaine salt

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

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

Benzathine Benzylpenicillin

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

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

Combined drugs penicillins

Bicillin-3, Bicillin-5.

Isoxazolylpenicillins (anti-staphylococcal penicillins)

The drug isoxazolylpenicillins - Oxacillin.

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

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

Oxacillin

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

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

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

Side effects

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

Indications for use

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

1. bone and joint infections;
2. pneumonia;
3. infective endocarditis;
4. meningitis;
5. sepsis.

Aminopenicillins

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

Ampicillin

Differences from penicillin in the spectrum of antibacterial activity

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

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

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

Side effects

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

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

Indications for use

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

Warnings and precautions

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

Amoxicillin

It is a derivative of ampicillin with improved pharmacokinetics.

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

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

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

Side effects

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

Indications for use

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

Warnings

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

Carboxypenicillins

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

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

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

Ureidopenicillins

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

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

Inhibitor-protected penicillins

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

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

1) penicillinases that destroy penicillins;

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

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

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

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

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

Such drugs are called inhibitor-protected penicillins.

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

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

Amoxicillin + clavulanate

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

Spectrum of antibacterial activity

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

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

Side effects

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

Indications for use

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

Amoxicillin + sulbactam

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

Like amoxicillin.

Indications for use

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

Ampicillin + sulbactam

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

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

Indications for use

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

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

Warning

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

Ticarcillin + clavulanate

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

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

Side effects

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

Indications for use

Severe, predominantly nosocomial infections of various localization:

1. intra-abdominal infections;
2. infections of the pelvic organs;
3. skin and soft tissue infections;
4. bone and joint infections;
5. sepsis.

Piperacillin + tazobactam

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

Spectrum of antibacterial activity

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

Side effects

Same as Ticarcillin + clavulanate.

Indications for use

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

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

Preparations of inhibitor-protected penicillins

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

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

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

(Ticarcillin + clavulanate) - Timentin.

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

Antibiotics are substances that are produced by microorganisms or synthesized using medical technology 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 cephalosporin, fluoroquinol and other drugs, penicillin-type compounds still remain the main antibacterial drugs for stopping a huge list of infectious diseases.

A bit of history

The discovery of penicillin happened quite by accident: in 1928, a scientist working in one of the London hospitals, Alexander Fleming, discovered a mold that had grown on a nutrient medium, which was capable of destroying staphylococcus colonies.

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

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

Operating principle

The described active substance acts bactericidal and bacteriostatically on pathogens. The mechanism of the bactericidal scheme of the work 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 a temporary suppression of the ability of pathogens to reproduce.

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

Most penicillins in small doses affect microbes bacteriostatically. With an increase in the amount of the drug involved, the effect changes to bactericidal. Only a doctor can choose a specific dosage of a drug of the penicillin group; it is impossible to use antibiotics for treatment on your own.

Systematization of drugs

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

• Phenoxymethylpenicillin;
• Benzathine benzylpenicillin.

The basic principles for the classification of semi-synthetic types of penicillin are listed below.

• isoxazolyl-penicillins (Oxacillin, Nafcillin);
• amino-penicillins (Amoxicillin, Ampicillin);
• aminodi-penicillins (there are no medicines 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 description of natural medicines

Natural (natural) penicillins are drugs that have a narrow spectrum of effects on microorganisms. Due to their long (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 drugs Bicillin and Benzylpenicillin are most often used, which are sufficiently effective against certain 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) are still sensitive to natural antibiotics.

The method of using drugs to prevent 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 semi-synthetic drugs included in the penicillin antibiotic series, and united in the aminodipenicillin group, are not registered in our country. Acidocillin, Amdinocillin, Bakamdinocillin are medicines 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. Most often, the drug Oxacillin is used in therapy. The subspecies includes several more drugs (in particular, Nafcillin, Dicloxacillin, Methicillin), which are used extremely rarely due to their high toxicity.

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

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

Aminopenicillins

This group of semi-synthetic 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 effect of beta-lactamases, medicines protected from the effects of enzymes of infectious agents 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.

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

Ureidopenicillins and carboxypenicillins

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

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

The most effective remedy from the group of ureidopenicillins is Piperacillin; it is used in the fight against diseases caused by Klebsiella spp.

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

Inhibitor-protected ureidopenicillins, carboxypenicillins have a wide range of effects on most known pathogens.

Pharmacokinetics

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

Medicines are characterized by the ability to concentrate in the pleural, pericardial, synovial fluids and bile. Practically do not pass into the internal environment of the organs of vision and prostate, cerebrospinal fluid. In minimal proportions are found in breast milk. In small quantities 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.

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

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

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

Contraindications

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

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

If there is an individual intolerance to penicillin in the anamnesis, it is impossible to use medical products of this group in therapy.

Warnings

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

• bouts of nausea and vomiting;
• pain in the abdomen;
• diarrhea
• pseudomembranous colitis.

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

In addition, the use of drugs of the described series is often accompanied by the development of candidiasis, intestinal dysbacteriosis, the appearance of edema, and a violation of the level of blood pressure.

It should be noted that penicillins are among the most low-toxic antibiotics, and the above side effect on the body occurs more often with 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 media, 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 involved in making such diagnoses as:

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

It should be remembered that the use of drugs of the penicillin group is allowed only on prescription. Self-medication can provoke the development of superinfection or the occurrence of severe complications of the disease.

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