Benzylpenicillin

Benzylpenicillin is a natural antibiotic that belongs to the penicillin category. It is resistant to acids but can be destroyed by penicillinase.

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Indications Benzylpenicillin

The drug is indicated for the elimination of infectious and inflammatory pathologies caused by bacteria sensitive to it:

• respiratory system: bronchitis, ambulatory pneumonia, and pyothorax;
• ENT diseases;
• organs of the urogenital system: cystitis, cervicitis and pyelonephritis, as well as pyelitis and urethritis;
• biliary tract organs: cholecystitis or cholangitis;
• soft tissues and skin: infections that have entered the wound, impetigo and erysipelas, as well as dermatoses that have become re-infected;
• eye diseases: acute conjunctivitis caused by gonococcus, as well as corneal ulcer;
• bacterial endocarditis (subacute or acute form), and in addition sepsis;
• development of osteomyelitis, meningitis or peritonitis;
• the occurrence of syphilis or gonorrhea;
• anthrax, scarlet fever, and also diphtheria and ray fungal disease.

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Release form

Available in powder form (for intramuscular and subcutaneous solutions) in volumes of 500,000 and 1,000,000 U. One bottle contains 10 ml. The package may contain 1 bottle. A cardboard box contains 10 bottles. For stationary use, a cardboard box contains 50 bottles.

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Pharmacodynamics

Medicinal properties – bactericidal and antibacterial. The drug prevents the process of peptide synthesis inside the cell walls, and also promotes the lysis of microbes.

It is active against gram-positive microorganisms (strains of staphylococci that do not produce penicillinase, and streptococci, including pneumococcus), diphtheria corynebacteria, anaerobic bacteria that form spores and anthrax bacilli. In addition, it is also effective against actinomycetes, gram-negative cocci (meningococci and gonococci), pale treponema and Spirochaeta spp.

It has no effect on most gram-negative microbes, fungi with viruses, as well as protozoa and rickettsia.

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Pharmacokinetics

After intramuscular administration of the active component, the peak concentration in the blood is observed after 0.5-1 hour, and after 3-4 hours, traces of the antibiotic appear in it. The absorption of the substance is quite low, the drug has a prolonged effect.

After a single injection of the drug, penicillin in a medicinal concentration is contained in the blood for a maximum of 12 hours. Synthesis with proteins inside the plasma is 60%. The active component quickly penetrates tissues with organs, and in addition, biological fluids (except for the prostate, as well as cerebrospinal fluid). If inflammation of the meninges occurs, the substance penetrates the BBB.

After instillation into the conjunctival sac, the medicinal concentration of the drug is observed in the main substance of the cornea (with local use, it almost does not enter the moisture in the anterior eye chamber). The medicinally significant indicator in the moisture of the anterior eye chamber and the cornea is achieved as a result of the introduction of the drug subconjunctivally (but the concentration inside the Corpus vitreum is not clinically significant).

Following intravitreal administration, the half-life is approximately 3 hours.

Excretion is mainly carried out through the kidneys by glomerular filtration (about 10%), and also by tubular secretion (about 90%) - unchanged substance. In infants and newborns, the excretion process slows down, and if the patient has renal failure, the half-life increases to 4-10 hours.

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Dosing and administration

The medicine is administered intramuscularly and intravenously (except for novocaine salt). In addition, subcutaneously and endolumbarly (exclusively sodium salt), intratracheally and into cavities. In the treatment of ophthalmological pathologies, instillations are performed inside the conjunctival sac, and in addition, administration is carried out by the subconjunctival and intravitreal method.

Adults daily doses intramuscularly and intravenously - 2-12 million units for 4-6 injections. For the treatment of outpatient pneumonia - 8-12 million units per day for 4-6 administration procedures. To eliminate endocarditis, meningitis or myonecrosis - a dosage of 18-24 million units is administered for 6 injections per day.

The duration of the treatment course depends on the severity of the disease, as well as its form, and can last from 7-10 days to 2 months or more (for example, when treating sepsis or infective endocarditis).

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Use Benzylpenicillin during pregnancy

Use during pregnancy is permitted only in situations where the potential benefit to the patient outweighs the likelihood of adverse effects on the fetus. Breastfeeding is prohibited during treatment with the drug.

Contraindications

Use during pregnancy is permitted only in situations where the potential benefit to the patient outweighs the likelihood of adverse effects on the fetus. Breastfeeding is prohibited during treatment with the drug.

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Side effects Benzylpenicillin

The use of the drug can cause the following side effects:

• allergy: urticaria, angioedema, anaphylaxis, fever/chills, joint pain, headaches, and skin rashes. In addition, bronchospasms and the development of eosinophilia or tubulointerstitial nephritis;
• others: for sodium salt – disorder of the myocardial contractility process; for potassium salt – development of hyperkalemia or arrhythmia, and in addition cardiac arrest.

As a result of the introduction of the drug by the endolumbar method, neurotoxic effects may occur: nausea with vomiting. In addition, the appearance of convulsions and meningeal symptoms, as well as increased reflex excitability and a state of coma.

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Overdose

An overdose of the drug manifests itself in the form of the following symptoms: impaired consciousness and the appearance of convulsions.

If these symptoms occur, it is necessary to stop using Benzylpenicillin and then carry out therapy aimed at eliminating the disorders.

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Interactions with other drugs

Synergism is observed with antibiotics from the bactericidal group (such as rifampicin and vancomycin, as well as cephalosporins with aminoglycosides), and antagonism is observed with antibiotics from the bacteriostatic group (such as lincosamides, macrolides, as well as chloramphenicol and tetracyclines).

NSAIDs, diuretics, allopurinol and drugs that block tubular secretion increase the concentration of the active component of Benzylpenicillin and reduce the severity of tubular secretion. In combination with allopurinol, the likelihood of skin allergies increases - in the form of rashes.

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Storage conditions

The medicine should be kept in normal conditions for medicines - in a place protected from sunlight and moisture. Temperature - no more than 30°C.

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Special instructions

Benzylpenicillin sodium salt is a bitter-tasting finely crystalline white powder. It has weak hygroscopic properties. It dissolves easily in water. It also dissolves quickly in methanol, and in addition, in ethanol. It is quickly destroyed when exposed to alkalis, acids, and oxidizers. The substance is administered intravenously, intramuscularly and subcutaneously, and also intratracheally and endolumbarly.

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Shelf life

Benzylpenicillin is suitable for use for 4 years. At the same time, the ready-made injection solution may be stored for no more than 24 hours (in the refrigerator - a maximum of 72 hours), and the infusion solution - a maximum of 12 hours (in the refrigerator - no more than 24 hours).

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