Penicillin tablets are antibiotics that are actively used to combat a number of bacterial diseases that arise as a result of the pathological activity of pathogens characterized by sensitivity to penicillin. Let us consider in more detail the principle of action and features of the use of the presented drug.

Penicillin is an antibacterial agent obtained from the waste products of a special mold fungus called Penicillium. The presented antibiotic drug is characterized by a wide spectrum of action, helping to destroy pathogens such as spirochetes, gonococcus, staphylococcus and others. Modern analogues of this medication (for example, Phenoxymethylpenicillin) have identical properties. The drug is available in the form of a solution for injection, as well as in tablets intended for resorption and for oral administration.

Indications for use

These medications are actively used in the field of modern medicine to combat a number of different diseases that are bacterial in nature. Experts identify the following indications for the use of the tablet form of penicillins:

1. Sepsis.
2. Brain abscess.
3. Cholecystitis.
4. Infectious lesions of the upper respiratory tract.
5. Otitis in acute or chronic form.
6. Burn lesions in the third and fourth degrees.
7. Furunculosis.
8. Pneumonia.
9. Gonorrhea.
10. Extensive wound surfaces localized in the skin area.
11. Syphilis.
12. Gas gangrene.
13. Angina.
14. Anthrax.
15. Scarlet fever.
16. Diphtheria.
17. Septicemia.
18. Purulent and inflammatory diseases of a gynecological nature.
19. Actinomycosis.
20. Septic endocarditis in acute form.
21. Infectious lesions of the urinary tract.
22. Meningitis.
23. Acute or chronic form of osteomyelitis.
24. Purulent diseases of an infectious nature, affecting mucous membranes and soft tissues.
25. Empyema of the pleura.
26. Tetanus.
27. Laryngitis and tonsillitis.
28. Sinusitis.
29. Inflammatory lesions of the lymph nodes.

Penicillin preparations are well tolerated by pediatric patients. In the field of pediatrics, the medications presented are used in cases where there is:

1. Otitis.
2. Pneumonia in newborns.
3. Septicopyemia.
4. Meningitis.
5. Pleurisy of a purulent nature.
6. A septic process localized in the umbilical region.

Contraindications for use

Despite the high degree of effectiveness in combating infectious diseases of a bacterial nature, the use of penicillin tablets in some cases is highly discouraged and can be dangerous for the patient. The following contraindications to the use of drugs of this pharmacological group, as well as their analogues, are identified:

1. Tendency to allergic reactions.
2. Bronchial asthma.
3. Hay fever.
4. Hives.
5. Ulcerous colitis.
6. Increased individual sensitivity to the drug.
7. Infectious mononucleosis.
8. Regional enteritis.
9. Serious disturbances in the functioning of the digestive system.
10. Pharyngitis.
11. Diarrhea.
12. Severe diseases of the gastrointestinal tract.
13. Aphthous stomatitis.
14. Kidney pathologies.
15. Acute heart failure.

Side effects

In some cases, the use of penicillin drugs may cause the development of undesirable reactions, such as:

1. Nausea.
2. Attacks of vomiting.
3. Allergic reactions.
4. Diarrhea.
5. Increased body temperature.
6. Coma.
7. Cramps.
8. Swelling.
9. Hives.
10. Eosinophilia.
11. Candidiasis of the vagina and oral cavity.

In some particularly severe cases, taking these drugs can lead to the development of anaphylactic shock and death of the patient.

However, only a few such incidents have been recorded in medical practice. In addition, it must be emphasized that in most cases, the development of side effects is observed with prolonged and uncontrolled use of medications.

In order to avoid possible complications and minimize risks, it is recommended to take medications exclusively as prescribed by a doctor, strictly observing his instructions and following the instructions for use. The choice of a specific drug, its dosage and the duration of the therapeutic course are determined by a specialist, taking into account the disease, its severity, age and individual characteristics of the patient.

Principles of application

The instructions for the use of drugs of the penicillin group state that the optimal dosage of the drug depends on the therapeutic regimen prescribed by the attending physician. The dosage for children is calculated individually, depending on the age and body weight of the child.

The tablets must be taken every 8 hours. It is recommended to strictly follow this rule in order to achieve the optimal concentration of the active substance. The medicine is taken either half an hour before a meal, or 2 hours after a meal.

The average duration of treatment is from 5 to 14 days. The first results become noticeable after 3-4 days. If no visible effect is observed, you should contact your doctor to prescribe another antibiotic drug.

Advantages of the tablet form of the drug

Recently, the use of tablet form of penicillin preparations has become especially widespread, which is associated with its undoubted advantages. Firstly, the patient can save on the purchase of syringes and special solutions needed for injections. Secondly, the therapeutic course can be completed on an outpatient basis, without the help of medical personnel. In addition, the tablets include so-called antacid substances that help reduce the effect of gastric juice on the main active ingredient, providing maximum therapeutic effect.

1. Flemoxin.
2. Amoxicillin.
3. Ospamox.
4. Amoxil KMP.

Penicillin preparations are an extremely effective and efficient remedy that helps cure numerous infectious diseases. Compliance with medical recommendations and basic rules of use allows you to achieve extremely fast and favorable results, while avoiding the occurrence of unwanted reactions and side effects.

Penicillin refers to 4 generations of antibiotics that are similar in structure, mechanism of action, contraindications and side effects. All of them belong to beta-lactam antibacterial drugs. The instructions for use of Penicillin describe its properties, release form, features of use, and possible negative consequences.

Bactericidal drug.

Antibiotic properties:

• high activity against sensitive strains of bacteria;
• low toxicity;
• Possibility of use during pregnancy.

The drug is compatible with other bactericidal agents.

Compound

The active substance is 6-aminopenicillanic acid, the main components of which are a molecule of 3 carbon atoms and 1 nitrogen atom (beta-lactam) and a thiazolidine ring. Changes in antibacterial properties and the creation of new variants of Penicillin are associated with modification of the active substance.

Release form

The antibiotic is highly soluble in water and is available in the form of powder for injection, ready-made solutions and tablets.

Injections in ampoules

Sealed glass ampoules with a capacity of 1-3 milliliters can be sold complete with or without solvent. Concentration: 1 milliliter of the finished solution contains 5000 units.

Pills

The pressed form is available in two versions: standard and for resorption. The concentration of penicillin in a standard tablet is 250, 500 milligrams, for resorption - 5000 units.

Powder

White powder with a specific aroma is available in transparent bottles, under a rubber cap sealed with a metal lid. The dose of the drug in one bottle is from 50,000 to 300,000 units.

Pharmacological characteristics

Penicillin is an acid from which salts are obtained to impart chemical stability and produce new drugs.

Pharmacological group

Penicillin is a natural antibiotic. A drug whose original form is a waste product of moldy fungi.

Pharmacodynamics

When administered intramuscularly, the antibiotic penetrates from the bloodstream into tissues, joints, and muscles, creating a therapeutic dose within a short period of time. It is excreted from the body by the kidneys after 4 hours.

Pharmacokinetics

The inhibitory qualities of the antibiotic are manifested in a destructive effect on the bacterial membrane, as a result of which the microorganism dies.

When administered orally, the medicinal properties are reduced by the influence of gastric juice, since the drug is not acid-resistant.

Diseases for which antibiotics are prescribed

The medicine has a therapeutic effect during therapy:

• lungs and bronchi;
• nasopharynx, oropharynx;
• genitourinary system;
• inflammation of the heart muscle;
• gallbladder;
• purulent lesions of the skin and soft tissues;
• venereal diseases;
• erysipelas;
• diphtheria and scarlet fever;
• purulent-necrotic inflammation of bones, bone marrow.

Instructions for use, dosage

The tablet dose is determined by the doctor. The daily norm is most often 750-1500 milligrams per day, divided into 3 parts, every 8 hours. In severe forms of infection, the dosage is increased 3 times. Rule for taking Penicillin: 30 minutes before meals or 120 after.

Antibiotic injections can be given:

• intravenously;
• intramuscularly;
• subcutaneously;
• into the spinal canal;
• in the cavity.

The norm is calculated based on the patient’s weight: the therapeutic dose should be constantly maintained at 0.1-0.3 units per milliliter of blood. To fulfill this condition, injections are given every 4 hours.

For pneumonia and sexually transmitted diseases, the specific dosage is determined by the doctor.

Preparation of solutions using powder

Physiological solution, Novocaine, and water for injection are used as a solvent. The main requirement concerns the temperature of the liquid: it should be within 18-20 degrees.

Using ampoules for injections

The powder in ampoules is diluted with a solvent in the same way as in bottles.

Treatment of children

The medication should be taken while monitoring the condition of the hematopoietic system, kidneys and liver.

During pregnancy and lactation

The possibility of use during pregnancy should be determined by a doctor, since Penicillin overcomes the placental barrier. Breast milk during antibiotic therapy is not suitable for feeding a baby.

For patients with liver and kidney failure

The bactericidal agent is excreted by the kidneys. In case of renal failure, penicillin is used under medical supervision. Intravenous administration of a drug containing potassium salts can cause hyperkalemia.

Contraindications

The drug is not prescribed for hypersensitivity to penicillins and other antibiotics, bronchospasms, urticaria, polyps.

Cases of excess doses

Oral intake in excess of the norm will cause gastrointestinal disorders: diarrhea, nausea, vomiting.

Undesirable effects

A side effect is an allergy to the drug, which can develop during the first long course of treatment. But it occurs more often with repeated use. Hypersensitivity to antibiotics manifests itself in the form of rash, swelling, and fever. Anaphylactic shock can be fatal.

Possible negative side effects:

• gag reflex;
• frequent bowel movements;
• involuntary muscle contractions;
• headache with vomiting, hypersensitivity to light and auditory stimuli;
• loss of consciousness;
• fungal infection of the mucous membranes in the mouth, vagina.

Before prescribing a medicine, it is necessary to test for an allergic reaction.

To stop a fungal infection, it is necessary to take antifungal agents simultaneously with a bactericidal drug.

A low therapeutic dose and cessation of treatment before complete recovery will cause the emergence of varieties of microorganisms resistant to penicillin.

When taken orally, take the medicine with a sufficient amount of liquid.

The drug dosage regimen should not be disrupted to maintain a therapeutic dose of the antibiotic in the blood.

High doses, when administered intravenously, can provoke the development of acute drug-induced epilepsy.

Interaction with other drugs

Bactericidal drugs enhance the effect of penicillin, while bacteriostatic drugs weaken it. Do not use simultaneously with thrombolytic, potassium-sparing diuretics, or anticoagulants. Concomitant use with oral contraceptives reduces their effectiveness.

Terms and storage

Penicillins retain their properties for 60 months at a temperature not exceeding 25 degrees, in a dry place.

Vacation and cost

Treatment requires a doctor's appointment with a prescription. The price of tablets is from 30 rubles per package, ampoules – from 60 rubles per piece, bottles – from 6 rubles, depending on the unit.

Drug substitutes

The first generation of penicillins are penicillins obtained from the acid produced by molds. To impart stability, it is converted into salts: sodium, potassium, novocaine.

Depending on the type of salt, natural penicillins, in turn, are divided into subgroups, for example, penicillin G (Benzylpenicillin), penicillin V (Phenoxymethylpenicillin).

The second generation is analogues of natural penicillins, obtained artificially, for example, Oxacillin.

Third, aminopenicillins, semisynthetic drugs that have an advantage over biosynthetic forms in affecting a larger number of pathogens. The third generation includes Amoxicillin and Ampicillin.

The fourth generation of bactericidal drugs has protection against the effects of beta-lactose bacteria. They are effective against most types of bacteria.

V-Penicillin

Phenoxymethylpenicillin is available in the form of tablets and powder for suspension. The drug is not prescribed for severe forms of the inflammatory process; it has a therapeutic effect on gram-positive bacteria and a narrow range of gram-negative ones.

The drug is effective against bacterial infections of the oral cavity, lungs, bronchi, and skin. It is recommended to take it for infections with anthrax, tetanus, syphilis and gonorrhea, for preventive purposes in the postoperative period.

Contraindications for use: vomiting, diarrhea, allergies to penicillins, severe inflammatory processes.

The solution is used in the form of injections and infusions, without age restrictions, including premature babies.

Contraindications for use:

• allergy to penicillins;
• liver, kidney failure;
• inflammation of the large intestine.

Treatment is as prescribed by a doctor, with the duration of therapy extended by 2-3 days after the disappearance of the main symptoms.

According to the chemical composition, the drug is potassium, sodium, novocaine salt. Available in powder form for the preparation of intramuscular, intravenous injections, as well as into the spinal canal.

The purpose and method of administration depend on the course of the inflammatory process. Potassium and sodium salts have high penetrating ability. Used for acute forms of infection. The therapeutic effect occurs a quarter of an hour after administration.

Potassium salt is used for intramuscular injection, sodium salt - for intravenous and intramuscular injection. To maintain the required concentration in the blood, injections are required 6 times a day, observing time intervals.

The novocaine salt of benzylpenicillin, after intramuscular administration, forms a capsule from which the medicine enters the blood for a long time. The drug is effective for the treatment of chronic infections.

Streptococci are sensitive to benzylpenicillin, and to a lesser extent staphylococci, as well as bacteria that cause:

• anthrax;
• sexually transmitted diseases;
• diphtheria;
• meningococcus;
• gas gangrene.

Trade names of benzylpenicillin depend on the chemical composition:

• Benzylpenicillin, sodium salt;
• Benzylpenicillin, potassium salt;
• Benzylpenicillin, novocaine salt;

Currently, 6 groups of penicillins are known:

1. Natural penicillins;
2. Isoxazolepenicillins;
3. Amidinopenicillins;
4. Aminopenicillins;
5. Carboxypenicillins;
6. Ureidopenicillins.

All penicillins have fundamentally the same pharmacodynamics. They disrupt the formation of the microbial wall during mitosis, as they are competitive inhibitors of transpeptidases, enzymes that catalyze the formation of interpeptide bridges in the cell wall. In addition, they can disrupt the synthesis of adhesins - proteins that cover the microbe like hairs and ensure its binding to the cells of the macroorganism. Only in this way is a fixed microbial cell capable of reproduction. The pharmacological effect is bactericidal.

Differences between the named groups of penicillins

Each penicillin drug has its own characteristics. The differences are mainly due to the characteristics of their spectrum of action, pharmacokinetics and undesirable effects.

Natural penicillins - antibiotics of the penicillin group

Natural penicillins (benzylpenicillins, bicillins, phenoxymethylpenicillin). These are narrow-spectrum antibiotics. They mainly affect Gr. “+” bacteria (corynebacteria, anthrax bacilli, clostridia, spirochetes) and cocci (staphylococci, streptococci, pneumococci). It should be noted that the sensitivity of microorganisms to natural penicillins is very high (MIC = 0.0X - 0.00X μg/ml), it is significantly greater than to other groups of penicillins.

Penicillin for children - instructions for use

Benzylpenicillin sodium salt (penicillin G) can be administered intramuscularly (IM), intravenously (IV), endolumbarally and into various cavities. Potassium and novocaine salts of benzylpenicillin are used only intramuscularly.

With intramuscular injection of therapeutic doses, the average therapeutic concentration (ATC) in the blood plasma occurs after 15 minutes (after 30-40 minutes when using novocaine salt). Moreover, only 40-60% of the drug is bound to blood proteins, and the remaining 50% is free. Therefore, benzylpenicillin is an emergency medicine.

From the blood, penicillin penetrates into the mucous membranes, lungs, kidneys, heart, intestinal wall, pleural and synovial fluids, in which its concentration is 25-50% of the concentration in the blood plasma. Benzylpenicillin penetrates poorly through the blood-brain barrier, even with inflammation of the meninges, the maximum the concentration in the cerebrospinal fluid is 10% of the level in the blood.

The time for maintaining therapeutic concentration in the blood ranges from 3 to 4 hours. Therefore, the frequency of administration of benzylpenicillin is 6 times a day (in practice, it is more often prescribed 4 times a day, the continuation of the drug’s effect is ensured by increasing the dose, this possibility of dosing benzylpenicillin is explained by its very large breadth of therapeutic action) after a month of life. The exception is the novocaine salt of the drug (benzylpenicillin procaine), which is administered 2 times a day.

The half-life of elimination is 30 minutes, but in case of renal failure it can increase to 6-20 hours, since the main route of excretion is filtration in the glomeruli of the kidneys in an unchanged form. Therefore, when the clearance of endogenous creatinine decreases to less than 30 ml/min, adjustment of the dosage regimen is required. In newborns, the frequency of administration for benzylpenicillin is: up to 1 week of life - 2 times a day, up to 1 month - 3-4 times a day. This is due to the anatomical and physiological characteristics of the kidneys of young children. Penicillins are effective in acidic urine.

Pharmacokinetic features of penicillin:

Penicillin can only be administered parenterally (intramuscularly, intravenously). Piperacillin is bound to plasma proteins by only 16%.

Not only the kidneys, but also the liver take part in the excretion of drugs.

The frequency of administration is 3 times a day.

Secondary resistance to the listed groups of penicillins (except carboxy- and ureidopenicillins) develops slowly. Interaction of penicillins with drugs from other groups. Penicillins are incompatible with many substances: bases, solutions of salts of heavy and alkaline earth metals, heparin, gentamicin, lincomycin, chloramphenicol, tetracyclines, amphotericin B, immunoglobulins, barbiturates, aminophylline, etc. Therefore, penicillins should be administered with a separate syringe.

Penicillins are pharmacodynamically incompatible with macrolides, tetracyclines, polymyxin M (mutual decrease in effectiveness). The combination of penicillins with aminoglycosides, cephalosporins, and monobactams is synergistic. For meningitis caused by meningococcus, pneumococcus or Haemophilus influenzae type "b" - aminopeaicillins are synergists of chloramphenicol, which has a bactericidal effect on these microbes. Penicillins are pharmacokinetically incompatible with butadione, furosemide and glucocorticoids, since the latter accelerate the elimination of the former from the body.

Side effects of penicillins

Natural penicillins, isoxazolepenicillins, amidinopenicillins, aminopenicillins are low-toxic antibiotics with a wide range of therapeutic effects, so they can be administered in large doses. The most common undesirable effects with the administration of these drugs are allergic reactions (both immediate and delayed types). It should be noted that when ampicillin is used, relatively often (in 5-10% of patients) a peculiar “ampicillin” macular nodular rash (of non-allergic origin) appears, localized first on the skin of the torso, then the limbs and head, accompanied by itching and increased body temperature.

This side effect most often occurs on the 5th to 10th day of treatment with ampicillin, when treating children with lymphadenopathy and viral infections with large doses of the drug or when taking allopurinol concomitantly, as well as in almost all patients with infectious mononucleosis. To a certain extent, this complication is associated with the release of endotoxins from dead microorganisms, especially those that are part of the normal intestinal microflora.

When high concentrations of drugs are created in the blood plasma, they penetrate into the cerebrospinal fluid and brain, which leads to neurotoxic effects: hallucinations, delirium, disorders of blood pressure regulation, and seizures. All these phenomena are the result of antagonism with gamma-aminobutyric acid (a mediator of inhibition in the central nervous system).

When using ampicillin, cases of pseudomembranous colitis have been described.

Local infiltrates and vascular complications in the form of Aune syndrome (ischemia and gangrene of the limbs when accidentally introduced into an artery) or Nikolaou syndrome (embolism of pulmonary and cerebral vessels when it enters a vein).

Carboxypenicillins and ureidopenicillins are drugs with a small breadth of therapeutic action. Their use may be accompanied by the appearance of: allergic reactions, symptoms of neurotoxicity, acute interstitial nephritis, intestinal dysbiosis, thrombocytopenia, neutropenia, leukopenia, eosinophilia, hypokalemia and hypocaligistia, hypernatremia (the last two complications are usually not caused by ureidopenicillins).

Combination drugs containing clavulanic acid can cause acute liver damage.

Isoxazolepenicillins - antibiotics of the penicillin group

Oxacillin, cloxacillin, flucloxacillin are isoxazolepenicillins. This group of penicillins also includes methicillin, nafcillin and dicloxacillin, which are practically not used due to high toxicity and/or low effectiveness. These are the so-called antistaphylococcal penicillins.

It must be emphasized that isoxazolepenicillins for children, like all other beta-lactam antibiotics, do not affect the so-called methicillin-resistant staphylococci. Their spectrum of action is similar to that of natural penicillins, but the greatest activity of these drugs is manifested in their effect on staphylococci, including staphylococci that produce beta-lactamase.

Pharmacokinetic differences between isoxazolepenicillins and benzylpenicillin:

Isoxazolepenicillins can be administered either parenterally (IM, IV) or orally 1-1.5 hours before meals. Compliance with the rules for taking the drug in relation to food intake is mandatory, since these antibiotics have low resistance to hydrochloric acid. In particular, for this reason, their bioavailability ranges from 30 to 50%.

These drugs have a high ability to bind to blood plasma proteins, it is more than 90%, they cannot be removed from the body by hemodialysis.

Excretion occurs in large quantities (especially oxacillin) by the liver. Therefore, in cases of mild renal failure, their use does not require adjustment of the dosage regimen.

Amidinopenicillins - antibiotics of the penicillin group

Amdinocillin, pivamdinocillin, bacamdinocillin, acidocillin are narrow-spectrum antibiotics, but their spectrum of action lies in the Gr region. “-” enterobacteria (Escherichia, Shigella, Salmonella, Klebsiella, Proteus).

Pharmacokinetic differences between amidinopenicillins and benzylpenicillin:

All drugs (except amdinocillin) can be administered orally. They have sufficient bioavailability (about 40%). It should be noted that enteral forms of the drug are inactive in the lumen of the gastrointestinal tract; they practically do not cause dysbacteriosis.

Larger volume of distribution. The drugs penetrate better through the blood-brain barrier and into cells.

Microorganisms practically do not develop secondary resistance to amidinopenicillins.

In order to increase the spectrum of action, amidinopenicillins for children can be combined with isoxazolepenicillins, natural penicillins and other antibiotics.

Aminopenicillins - antibiotics of the penicillin group

Ampicillin, amoxicillin, talampicillin, bacampicillin, pivampicillin are broad-spectrum antibiotics. Their spectrum of action covers that of all the above-mentioned groups of narrow-spectrum penicillins, and they additionally affect Listeria, Enterococci, Haemophilus influenzae, Bordetella, Helicobacter pylori and actinomycetes. Gr. is more sensitive to aminopenicillins. "+" bacteria than Gr. "-".

However, it should be noted that aminopenicillins for children do not affect staphylococci that produce beta-lactamase. In other words, they do not solve the problem of hospital infections, where staphylococcus and other beta-lactamase-producing microbes play an important role. Therefore, combination drugs have been created: ampiox (ampicillin + oxacillin), clonacom-R (ampicillin + cloxacillin), unasin and its oral analogues sulacillin, sultamicillin (ampicillin + sulbactam, which is a beta-lactamase inhibitor), clonacom X (amoxicillin + cloxacillin) and augmentin and its analogue amoxiclav (amoxicillin + clavulanic acid, which is also a beta-lactamase inhibitor).

Pharmacokinetic differences between aminopenicillins and benzylpenicillin:

All drugs in this group can be prescribed internally. However, ampicillin must be taken 1-1.5 hours before meals, its bioavailability is about 40%; amoxicillin is taken regardless of food intake, its bioavailability is 70-80%. Amoxicillin in a special dosage form, Flemoxin Solutab, has a bioavailability of 93%. Such high bioavailability reduces the load on the flora of the gastrointestinal tract several times, and this reduces the risk of dysbacteriosis.

In addition, the time of contact of the drug with the intestinal mucosa is reduced to a minimum, therefore, dyspeptic disorders appear less frequently. Finally, the dose of the drug taken orally is almost equal to the dose of the same drug administered parenterally. A modified amoxicillin tablet, Flemoxin Solutab, can be broken, chewed and dissolved, which makes it easier to swallow the drug, and, therefore, compliance with the dosage regimen (or, as they say now, compliance).

It is known that 30% of patients who regularly take medications have difficulty swallowing tablets and capsules; 25% of patients (usually children, elderly people) prefer dissolved forms of drugs. It should be emphasized that non-compliance with the antibiotic regimen leads to treatment failure, relapse or chronicity of the disease and the spread of resistant infection. Tal-, bak and pavampicillins have sufficient bioavailability, are not active in the intestinal lumen, and therefore rarely cause dysbiosis and dyspeptic disorders.

Aminopenicillins in the blood remain in free form, about 80%. The drugs penetrate better into many tissues and liquids. With meningitis, the concentration of drugs in the cerebrospinal fluid can be 70-95% of their concentration in the blood plasma.

The frequency of administration of combined drugs is 2-3 times a day.

Carboxypenicillins - antibiotics of the penicillin group

Carbenicillin, carfecillin, carindacillin, ticardillin - carboxypenicillins. These are so-called antipseudomonas antibiotics, since these microbes are most sensitive to them. Although their spectrum of action includes many other microorganisms (streptococci, pneumococci, neisseria, clostridia, corynebacteria, anthrax bacilli, spirochetes, Escherichia, Shigella, Salmonella, Klebsiella, Proteus, Bacteroides).

However, it should be noted that the spectrum of influence of carboxypenicillins does not include staphylococci. Therefore, in some cases, carboxypenicillins for children must be combined with isoxazolepenicillins; A special combination drug, timentin, has also been created. (ticarcillin + clavulanic acid).

Pharmacokinetic differences between carboxypenicillins and benzylpenicillin:

Carfecillin and carindacillin are the phenyl and indanyl esters of carbenicillin. These drugs are used orally, their bioavailability is about 40%. Carbenicillins and ticarcillins are practically not absorbed from the gastrointestinal tract.

The drugs hardly penetrate the blood-brain barrier.

The frequency of administration is 4 times a day.

Secondary microbial resistance develops rapidly.

Cephalosporin group

There are 4 generations of cephalosporins. Their division is based not on chronological criteria, but mainly on the features of the spectrum of action and pharmacokinetics. At the same time, all cephalosporins are characterized by resistance to varying degrees to some beta-lactamases of staphylococci, so they suppress most benzylpenicillin-resistant strains of these microorganisms.

For all cephalosporins, there is a risk of cross-allergy with other beta-lactam antibiotics (penicillins, carbapenems, monobactams). Finally, all cephalosporins have the same pharmacodynamics. They, like penicillins, disrupt the synthesis of the microbial wall at the time of mitosis. The pharmacological effect is bactericidal. Cephalosporins are broad-spectrum antibiotics. Different generations of cephalosporins differ significantly from each other.

Group of 1st generation cephalosporins:

For parenteral administration - cephaloridine (ceporin), cephalothin (keflin), cefazolin (kefzol), cefapirin, cefacitril (cephalospor).

For oral administration - cephalexin (Keflex, Ospexin, Ceporex), cefadroxil (Ultracef, Duracef), cefradine (Velotsef). The latter drug can also be administered parenterally.

The spectrum of action of first generation cephalosporins is quite wide. They affect Gr. "+" and Gr. “-” cocci (except enterococci and methicillin-resistant staphylococci), corynebacteria, anthrax bacilli, spirochetes, Escherichia, Shigella, Salmonella, Moraxella, Klebsiella, Proteus, Haemophilus influenzae, Bordetella, Yersinia. The greatest sensitivity to first generation cephalosporins is in Gr. “+” bacteria and cocci (except for enterococci and methicillin-resistant staphylococci), significantly less in Gr. "-" bacteria. To increase efficiency or expand the spectrum (due to the effect on pseudomonads), these antibiotics can be combined with amidinopenicillins or with monobactams, aminoglycosides, etc.

Group II generation cephalosporins:

For parenteral administration - cefuroxil (ketocef, zinacef), cefamandol (mandol, lekacef), cefoxitin (mefoxin, mefoxitin), cefotetan (cetophan), cefotiam (halospor), cefonicide (monocide), ceforanide (precef), cefmetazole, cefatidime, cephaloglycin , cefatrizine.

For oral administration – cefuroxime (zinnate), cefaclor (ceclor, ceflor, vercef, alfacet), cefaprozil, loracarbef.

The spectrum of action of second generation cephalosporins coincides with the spectrum of first generation cephalosporins, but antimicrobial activity against Gr. “-” flora is most pronounced in second generation cephalosporins. At the same time, second generation cephalosporins are resistant to some Gr beta-lactamases. "-" bacteria. In addition, cefoxitin and cefotetan showed activity against bacteroids; for cefamandole - to methicillin-resistant staphylococci. To expand the spectrum of action or increase the effectiveness of use, these antibiotics can be combined with isoxazolepenicillins, aminoglycosides, etc.

Group of III generation cephalosporins:

For parenteral administration - cefotaxime (claforan), ceftazidine (fortum, cefadim, tazidine, tizacef), deftriaxone (rodefin, longacef), cefoperazone (defobid), ceftizoxime (epoceline, cefisox), moxalactam (moxam, lamoxef), cefmenoxime (cefmax) , cefsulodin (cefomonide), cefodizime (modispecies), latamoxef.

For oral administration – ceftibuten (Cedex), cefixime (Cefspan), cefetamet pivoxil, cefpodoxime proxetil.

The spectrum of action of third-generation cephalosporins is greater than that of the previous two generations. It additionally includes: pseudomonads, morganella, serrations, clostridia (except CI. difficile) and bacteroides. Moreover, the activity of third-generation cephalosporins is even more, compared to second-generation cephalosporins, shifted towards Gr. "-" flora. III generation cephalosporins are also resistant to some Gr beta-lactamases. "-" bacteria. It should be noted that most antibiotics in this group have moderate activity against pseudomonas, serrations, morganella and anaerobes.

The exceptions are the following drugs: pseudomonas are highly sensitive to ceftazidime and cefoperazone; in anaerobes - to latamoxef, cefotaxime and ceftriaxone. To expand the spectrum of action or increase the effectiveness of the use of third-generation cephalosporins, they can be combined with natural penicillins, isoxazolepenicillins (to increase the effect on Gr. “+” bacteria, cocci and clostridia), aminopenicillins (to expand the spectrum due to the effect on enterococci, listeria), carboxy- and ureidopenicillins, aminoglycosides (to increase the effect on pseudomonas, serrations, anaerobes), a synthetic anti-infective drug - metronidazole (to increase the effect on anaerobes), etc.

IV generation cephalosporins:

Cefepime (Maxipim), cefpirome (Keyten), cefclidine, cefquin, cefozopran, cefoselyse. All drugs are administered only parenterally (i.m., i.v.). The spectrum of action of IV generation cephalosporins is very wide. It is larger than previous generations.

IV generation cephalosporins affect the same microorganisms as III cephalosporins and, in addition, citro-, entero- and acinetobacter. Moreover, they are equally highly active in relation to Gr. “+”, and in relation to Gr. "-" flora. IV generation cephalosporins affect multidrug-resistant microorganisms resistant to extended-spectrum beta-lactamases. This is due to the ability of drugs to easily penetrate the cell membrane, due to their high affinity for penicillin-binding proteins (PBPs), and create high concentrations in the periplasmic space.

All this determines the high activity of cefepime (maxipim) and similar drugs against strains of microorganisms resistant to other cephalosporins and, sometimes, even to carbapenems. However, bacteroids fall out of the zone of influence of these drugs, so to expand the spectrum they can be combined with carboxy- and ureidopenicillins, metronidazole, etc. Secondary resistance of microorganisms to all cephalosporins develops slowly.

Ureidopenicillins - antibiotics of the penicillin group

Azlocillin, mezlocillin, piperacillin - ureidopenicillins. These are also antipseudomonas antibiotics. Their spectrum of action coincides with carboxypenicillins. The most active drug from this group is piperacillin. Its combined drug is tazocin (piperacillin + tazabactam, the latter is a beta-lactamase inhibitor).

Penicillin is one of the most commonly used bactericidal drugs, available in tablet form and as a powder for injection. The medicine has a wide range of applications and is actively used to eliminate many pathologies of a bacterial nature. The most effective form of using the drug is injections.

Description and composition of the drug

Penicillin is the first bactericidal agent obtained from the waste products of microorganisms. Its inventor is called Alexander Fleming, who discovered the antibiotic by accident, discovering its antimicrobial effect.

The first samples of the drug were obtained in the USSR by scientists Balezina and Ermolyeva in the mid-twentieth century. After this, the medicine began to be produced on an industrial scale. At the end of the fifties of the twentieth century, synthetic penicillins were also obtained.

Currently, four groups of penicillins are used in medicine:

• natural origin;
• semi-synthetic compounds;
• broad-spectrum aminopenicillins;
• broad-spectrum bactericidal penicillins.

For injection use penicillin G sodium salt 500 thousand units or 1 million units. In pharmacy chains, such powder can be purchased in glass bottles sealed with a rubber stopper. Before direct administration, the powder is diluted with water. The drug can be obtained from a pharmacy with a doctor's prescription.

Pharmacological characteristics

In terms of its chemical composition, Penicillin is an acid for producing salts. Its biosynthetic products act on anaerobic spore-forming bacilli, gram-positive and gram-negative bacteria, inhibiting the synthesis of their walls. Benzylpenicillin is considered the most active and relevant drug today.

The penicillin drug is administered intramuscularly and immediately after direct use it enters the bloodstream and quickly concentrates in muscles and joints, and tissue lesions. The highest degree of concentration of the composition is observed half an hour to an hour after the procedure.

The concentration of the drug in the cerebrospinal fluid and abdominal cavity is minimal. The composition is excreted through the kidneys and bile. The half-life is up to one and a half hours.

Indications for use

Penicillin treatment with injections is carried out for the development of bacterial infections, including:

• focal and lobar pneumonia;
• chronic and acute osteomyelitis;
• pleural empyema;
• blood poisoning;
• acute and subacute types of endocarditis;
• tonsillitis;
• scarlet fever;
• infectious inflammatory processes of the brain;
• erysipelas;
• anthrax;
• furunculosis and its complications;
• acute cholecystitis;
• gonorrhea;
• rheumatism;
• inflammatory bacterial pathologies of the urinary tract and reproductive organs;
• diphtheria;
• ENT pathologies;
• purulent dermatological lesions;
• pyemia;
• actinomycosis.

Important: Penicillin is used not only to treat human diseases, but also to eliminate pathologies in animals and is one of the most inexpensive drugs of its kind.

Methods of treatment using Penicillin

According to the instructions for use, the drug is allowed to be administered in four main ways, depending on the type and extent of the lesion:

• into the spinal canal;
• intravenously;
• intramuscularly;
• subcutaneously

Injections are given every three to four hours, maintaining the content of the composition so that for each milliliter of the patient’s blood there is a concentration of 0.1-0.3 units. In most cases, the treatment regimen is selected individually for each patient. The same applies to the course of treatment.

Special instructions for use

In order for treatment to be as effective and safe as possible, it is necessary to take into account the following therapy problems:

1. Before starting to use the medicine, it is necessary to test for possible intolerance to antibiotics.
2. The medication must be replaced if three to five days later, if the therapy shows insufficient effectiveness.
3. To prevent the occurrence of mycotic superinfection, it is necessary to take antifungal medications during treatment. It is also important to pay attention to the likelihood of colonization of the body with resistant strains of bacteria.
4. It is possible to dilute the medicine for injection only with water for injection, strictly following the proposed proportions.
5. It is not recommended to skip injections. If missed, it is necessary to administer the drug as soon as possible and restore the regimen.
6. After the expiration date, the medicine becomes toxic and dangerous to use.

Limitations and main contraindications

Penicillin has relatively few contraindications. The main one is hypersensitivity to the antibiotic itself and other drugs in its group. In addition, the medication is not recommended for use if:

• manifestations of allergies in the form of urticaria, asthma and hay fever;
• manifestations of intolerance to antibiotics and sulfonamides.

It is necessary to use the medicine under the supervision of a doctor for pathologies of the kidneys and cardiovascular system.

Side effects and complications

An overdose of medication does not pose a threat to the patient’s life. In this case, nausea and vomiting and a general deterioration in health may occur. In addition, the development of hyperkalemia is likely with the simultaneous use of potassium supplements. In rare cases, epileptic seizures are possible. Exceeding the prescribed dosage is treated symptomatically.

With prolonged use of the antibiotic, allergic reactions are likely to occur (urticaria, swelling, rash formation, anaphylactic manifestations, and, extremely rarely, death). Treatment in this situation is symptomatic. Typically, adrenaline is administered intravenously. In other situations the following are also possible:

• disturbance of digestive processes and stool;
• dysbacteriosis;
• fungal diseases of the oral cavity and vagina;
• neurotoxic manifestations, seizures, coma.

Important: In order to reduce the likelihood of negative reactions to therapy, it is recommended not to exceed the established dosages and not to extend the course of treatment without the consent of the doctor.

Interaction of Penicillin with other drugs

Concomitant treatment with Probenecid increases the half-life of the antibiotic components. The use of Tetracycline and sulfonamides significantly reduces the effectiveness of Penicillin. Cholistyramine seriously reduces the bioavailability of the antibiotic.

Due to incompatibility, you cannot give an injection of Penicillin and any aminoglycoside at the same time. The combined use of thrombolytics is also prohibited.

The risk of bleeding increases with the simultaneous use of anticoagulants and Penicillins against Pseudomonas aeruginosa. Therefore, treatment in this case should be supervised by a specialist.

Antibiotic therapy slows down the elimination of methotrexate and also reduces the effectiveness of oral contraceptives.

Penicillin analogues

1. Cefazolin. A drug from the group of cephalosporins, which can be used in case of intolerance to penicillin medications. It is used for intramuscular and intravenous administration and retains its therapeutic properties after the procedure for ten hours.
2. Ceftriaxone. The cephalosporin medication is most often used in a hospital setting. Intended for the treatment of inflammatory processes caused by bacterial pathogens, it is active against gram-negative bacteria and anaerobic infections.
3. Extensillin. It is one of the long-acting beta-lactam antibiotics. The medication is available in powders and is not recommended for use simultaneously with non-steroidal drugs against inflammatory processes.

Among the drugs for oral administration containing a similar active ingredient are:

• Ampicillin trihydrate;
• Amoxicillin;
• Flemoxin Solutab;
• Amosin;
• Amoxicar;
• Ecobol.

Important: Replacement is made in case of impossibility of giving injections, intolerance to penicillins, as well as in case of insufficient effectiveness of the latter.

Conclusion

Penicillin is a first-generation antibiotic that has been tested over the years and through long-term trials. Currently, the drug is used to treat many bacterial infections in a modernized form and is relatively safe for humans. Penicillins are actively used in veterinary medicine and have several varieties, which are selected for therapy depending on the type of disease and the individual characteristics of the patient.

In modern medicine, antibiotics of the penicillin group are widely used for standard forms of inflammatory diseases. Although semi-synthetic penicillins have recently been used more often, a simple version of this drug is often indispensable for otitis, cystitis and sore throats in children.

The antibiotic penicillin is one of the first forms of targeted antibacterial agents invented by man. At the time of its discovery, it was a powerful drug that helped save the lives of patients with pneumonia and. Before the invention of penicillin, pneumonia was a fatal disease in almost 90% of cases. But, a few years later, doctors began to notice a decrease in the activity of the antibiotic penicillin against the vast majority of pathogens. This provided the impetus for the development of new antibacterial agents.

However, with each new generation, antibiotics acquired not only powerful antibacterial properties, but also severe side effects. At the same time, simple, completely natural penicillin was gradually forgotten. Today, the use of first generation penicillin is recommended by all foreign microbiologists. The point is simple. Immediately after the invention of penicillin, a gradual decrease in its activity began to appear due to bacterial mutations. They began to adapt to this antibiotic and develop a kind of immunity against it. Subsequently, this process progressed. Man invented new bacteria - new forms of adaptation.

According to recent microbiological studies, resistance to the antibiotic penicillin in bacteria is low. This means that it can be successfully used in the treatment of bacterial infections caused by bacteria sensitive to this drug.

The main pharmacological action of penicillin is aimed at disrupting protein synthesis in bacterial cells. As a result of disruption of the permeability of the cell membrane, it causes destruction and death of bacteria. This determines its rapid bactericidal effect. Unlike other antibiotics, it does not slow down the reproduction of pathogens, but provokes their disappearance.

Low resistance to penicillin has been experimentally proven in:

1. gram-positive bacteria that cause inflammation of the respiratory system and urinary system;
2. gram-negative bacteria of the cocci group, including those causing meningitis, gonorrhea, syphilis;
3. bacteria of the actinomycete group.

The maximum concentration in the biological media of the human body is achieved with intramuscular administration of the drug. In this case, the increase in percentage begins 5 minutes after the injection of penicillin and reaches its maximum after 30 minutes. The antibiotic penicillin freely penetrates into the blood, urine, and bile, binding to blood plasma proteins. Cerebrospinal fluid, tissue in the eye area and the prostate gland are inaccessible to him. Therefore, in the treatment of gonorrhea in men, penicillin is used in combination with other drugs.

The antibiotic penicillin is available in tablets and vials for injection in the form of a dry powder. Before use, it is diluted with physiological sodium chloride solution or novocaine.

Where is penicillin used?

Penicillin is used in the treatment of inflammatory bacterial infections of the upper respiratory tract. In particular, it gives good results in the treatment of catarrhal and lacunar tonsillitis. The drug is effective in combination with sulfonamides in the treatment of uncomplicated forms of pneumonia. Used in the treatment of pyelonephritis, consequences of urolithiasis, cystitis in combination with nitrofuran drugs.

Other indications for the use of penicillin include:

• inflammation and purulent lesions of the epidermis, including erysipelas;
• otitis and sinusitis;
• chronic and acute forms of pleurisy with effusion;
• endocarditis, pericarditis, rheumatic heart defects;
• some sexually transmitted infections (syphilis, ureaplasmosis, toxicoplasmosis);
• infectious diseases, among which scarlet fever and anthrax are most successfully treated with penicillin.

Penicillin is not effective for intestinal infections, in particular dysentery and salmonellosis. This drug is not stable in an acidic environment and is quickly destroyed in the intestine by penicillinase.

Treatment of inflammatory diseases with penicillin

For effective treatment of inflammatory diseases with penicillin, two factors are important. This is the correct selection of the method of administration and the exact determination of the daily and single dosage. It is recommended that the course of treatment for acute conditions and severe diseases begin with intramuscular administration. The half-life of penicillin in human tissues and body fluids is just over 4 hours. Therefore, to maintain maximum concentration, injections should be given at intervals of 4 hours. Those. 6 times daily administration of penicillin is necessary to obtain a high-quality treatment result.

The dosage is calculated based on the patient’s weight, the severity of his condition and the type of pathogen. Approximate dosages can be seen in the table below; the course of treatment is at least 10 days.

Can children take penicillin?

Penicillin can be prescribed to children from 1 year of age. At an earlier age, this drug can have an otogenic effect, which in the future will negatively affect the development of hearing in the baby. Penicillin injections to children can only be given in a hospital setting. At home, only oral administration of the drug is allowed.

Use of penicillin during pregnancy and lactation

During pregnancy, penicillin is strictly prohibited for intramuscular and internal use. Can be used as an ointment on limited areas of the skin.

Penicillin should also be avoided during breastfeeding. It easily passes into breast milk and has an extremely negative effect on the infant.

Allergy to penicillin

Allergies to penicillin are quite common. In this case, an allergic reaction after intramuscular injection often develops like anaphylactic shock, which is dangerous for the patient’s life. Therefore, before prescribing penicillin, a skin test is mandatory.

To do this, the nurse makes a small scratch on the inside of the patient's forearm. A penicillin solution prepared for injection is applied to the wound surface. After 30 minutes the reaction is checked. If there is even slight redness at the scratch site, penicillin cannot be used in this patient.

To reduce the level of local irritation, penicillin should be diluted with a solution of novocaine before injection. Although dilution with sodium chloride solution is usually recommended.