Benzylpenicillin

Benzylpenicillin is a natural antibiotic that belongs to the category of penicillins. Resistant to acids, but can be destroyed by penicillinase.

[1], [2], [3], [4], [5]

Indications Benzylpenicillin

The medicine is indicated for the elimination of infectious-inflammatory pathologies, which are caused by bacteria sensitive to it:

• organs of the respiratory system: bronchitis, outpatient pneumonia, and also piothorax;
• diseases of ENT organs;
• organs of the urogenital system: cystitis, cervicitis and pyelonephritis, as well as pyelitis and urethritis;
• organs ZHVP: cholecystitis or cholangitis;
• soft tissues and skin: wound infections, impetigo and erysipelas, and also dermatoses infected repeatedly;
• eye diseases: gonococcal-induced acute form of conjunctivitis, as well as corneal ulcer;
• bacterial endocarditis (subacute or acute form), and in addition to this sepsis;
• development of osteomyelitis, meningitis or peritonitis;
• the emergence of syphilis or gonorrhea;
• anthrax, scarlet fever, and in addition diphtheria and radiation sickness.

[6], [7], [8],

Release form

It is produced in powder form (for in / m and n / to solutions) with a volume of 500,000 and 1,000,000 units. One bottle holds 10 ml. Packaging can contain 1 bottle. The carton contains 10 bottles. For stationary use - in a cardboard box contains 50 bottles.

[9], [10], [11]

Pharmacodynamics

Medicinal properties - bactericidal and antibacterial. The drug interferes with the process of peptidoglycan synthesis inside the cell walls, and also facilitates the lysis of microbes.

Actively acts against gram-positive microorganisms (strains of staphylococci that do not produce penicillinase, and streptococci, including pneumococcus), diphtheria corynebacterium, anaerobic bacteria that form spores and anthrax rods. In addition, also against actinomycetes, gram-negative cocci (meningococci and gonococci), pale treponema and Spirochaeta spp.

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

[12], [13], [14], [15], [16]

Pharmacokinetics

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

After a single injection of the drug, penicillin in the drug 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 (other than the prostate, as well as cerebrospinal fluid). If there is an inflammation of the membranes of the brain, the substance penetrates through the BBB.

After instillation inside the conjunctival sac, the medicinal concentration of the drug is observed in the core substance of the cornea (with local use almost does not get into the moisture in the anterior eye chamber). The medicinally significant index in the moisture of the anterior ocular chamber and the cornea as a result of the administration of the drug is subconjunctival (but the concentration inside the Corpus vitreum is not clinically significant).

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

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

[17], [18], [19], [20], [21], [22]

Dosing and administration

The drug is administered intramuscularly, as well as intravenously (except novocaine salt). In addition, subcutaneously and endolumbly (exclusively sodium salt), intratracheal and in the cavity. In the treatment of ophthalmic pathologies, instillations are made inside the conjunctival sac, and in addition, subconjunctival and intravitreal injection.

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

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, in the treatment of sepsis or infective endocarditis).

[25], [26],

Use Benzylpenicillin during pregnancy

Use during pregnancy is allowed only in situations where the possible benefit to the patient exceeds the probability of the fetus having negative consequences. During the treatment, the drug is not allowed to breast-feed.

Contraindications

Use during pregnancy is allowed only in situations where the possible benefit to the patient exceeds the probability of the fetus having negative consequences. During the treatment, the drug is not allowed to breast-feed.

[23],

Side effects Benzylpenicillin

The use of the drug can cause such side effects:

• allergies: urticaria, angioedema, anaphylaxis, fever / chills, joint pain, headaches, and rashes on the skin. In addition, spasms of the bronchi and the development of eosinophilia or tubulointerstitial nephritis;
• other: for sodium salt - a disorder of the process of myocardial contractility; for potassium salt - the development of hyperkalemia or arrhythmia, and in addition, cardiac arrest.

As a result of the introduction of the drug with the endolumbic method, neurotoxic effects can arise: nausea with vomiting. In addition, the appearance of seizures and meningeal symptoms, as well as increased reflex excitability and the state of coma.

[24],

Overdose

An overdose of a medicine manifests itself in the form of such symptoms: a disorder of consciousness and the appearance of seizures.

If these symptoms occur, it is necessary to abolish the use of benzylpenicillin, and then conduct therapy aimed at eliminating the violations.

[27], [28]

Interactions with other drugs

With antibiotics from the bactericidal group (such as rifampicin and vancomycin, as well as cephalosporins with aminoglycosides), synergism is observed, and antagonism is observed with antibiotics from the bacteriostatic group (such as lincosamides, macrolides, and 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 increases the likelihood of allergies on the skin - in the form of rashes.

[29], [30], [31], [32]

Storage conditions

Keep the medication in the usual conditions for medicines - in a place that is closed from sunlight and moisture. Temperature - no more than 30 ° C.

[33], [34], [35]

Special instructions

Benzylpenicillin sodium salt is a bitter-tasting, fine-grained white powder. It has weak hygroscopic properties. Easily soluble in water. It also dissolves rapidly in methanol, and in addition, in ethanol. Rapidly destroyed by the influence on it of alkalis, acids, and with it oxidants. The substance is administered intravenously, intramuscularly and subcutaneously, and in addition it is intratracheal and endolumbular.

[36], [37], [38]

Shelf life

Benzylpenicillin is suitable for use for 4 years. In this case, the ready-made injection solution can be stored no more than 24 hours (in a refrigerator - a maximum of 72 hours), and a solution for infusions - a maximum of 12 hours (in a refrigerator - no more than 24 hours).

[39],