Benzylpenicillin sodium salt

General characteristics. Structure:

Active ingredient: 500000 PIECES - 0,3 g or 1000000 PIECES - 0,6 g of benzylpenicillin of sodium salt.

Biosynthetic penicillinic antibiotic.

Pharmacological properties:

Pharmacodynamics. Benzylpenicillin, an antibiotic from group of biosynthetic penicillin, is active concerning gram-positive microorganisms (Staphylococcus spp., Streptococcus spp, Corynebacterium diphtheriae, anaerobic spore-forming sticks, sticks of a malignant anthrax), and also concerning Spirochaetaceae, gram-negative cocci (Neisseria gonorrhoeae, N.meningitidis), Actinomycetaceae.

The strains of stafilokokk forming a penicillinase as this enzyme destroys a benzylpenicillin molecule are steady against effect of benzylpenicillin. Drug is not active concerning the majority of gram-negative bacteria, rickettsiae (Rickettsia spp.), viruses, the elementary.

Pharmacokinetics. Benzylpenicillin is well soaked up at parenteral administration, has no cumulative action, are quickly brought out of an organism with urine. At intramuscular introduction the maximum concentration of drug in blood are created in 30-60 minutes, in 3-4 hours in blood antibiotic traces are found.

Level of concentration and duration of circulation of benzylpenicillin in blood depends on the size of the entered dose.

The antibiotic well gets into fabrics and liquids of an organism: in cerebrospinal fluid normal it is found in insignificant quantity, at an inflammation of meningeal covers its concentration in liquor increases.

Indications to use:

Route of administration and doses:

The drug is administered intramusculary, in a cavity (belly, pleural, etc.) or subcutaneously. In a cavity the drug is administered only in the conditions of a hospital!

Intramusculary: at moderately severe infections the single dose of drug makes usually 250000–500000 PIECES; daily – 1000000–2000000 PIECES; at heavy infections enter up to 10000000–20000000 PIECES a day; at gas gangrene – to 40 000 000–60 000 000 PIECES.

The daily dose for children aged till 1 year makes 50 000–100 000 PIECES/kg, 1 years – 50 000 PIECES/kg are more senior; if necessary it is possible to increase a daily dose to 200 000–300 000 PIECES/kg, according to vital indications – to 500 000 PIECES/kg. Frequency rate of administration of drug of 4-6 times a day.

For intramuscular introduction add to bottle contents 1–3 ml of sterile water for injections or 0,9% of solution of sodium of chloride, or 0,5% of solution of Procainum.

Subcutaneously drug is used for an obkalyvaniye of infiltrates in concentration 100000-200000 PIECES in 1 ml of 0,25-0,5% of solution of Procainum.

Into cavities (belly, pleural, etc.) drug solution the adult enter into concentration 10 000–20 000 PIECES in 1 ml, to children – 2 000–5 000 PIECES in 1 ml. Dissolve in sterile water for injections or 0,9% chloride sodium solution. Duration of treatment is 5–7 days with the subsequent transition to intramuscular introduction.

Features of use:

Use at pregnancy and during breastfeeding. Use at pregnancy is possible only in that case when the estimated advantage exceeds potential risk for a fruit. In need of use in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

If in 3-5 days after the beginning of use of effect it is not noted, it is necessary to pass to use of other antibiotics or a combination therapy.

Due to a possibility of development of fungal superinfection it is reasonable at prolonged treatment by benzylpenicillin if necessary to appoint antifungal drugs.

It is necessary to consider that use of insufficient doses of benzylpenicillin or too early termination of treatment often leads to emergence of resistant strains of activators.

During administration of drug it is necessary to be careful at control of vehicles, mechanisms and when performing other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Allergic reactions: a hyperthermia, urticaria, skin rash, rash on mucous membranes, an arthralgia, an eosinophilia, a Quincke's disease, intersticial nephrite, a bronchospasm, an acute anaphylaxis.

At the beginning of a course of treatment (especially at treatment of inborn syphilis) - fever, a fever, the increased sweating, an exacerbation of a disease, Yarisha-Gerksgeymer's reaction.
From cardiovascular reaction:  decrease in pumping function of a myocardium.

Local reactions: morbidity and consolidation in the place in oil of introduction.

At prolonged use: dysbacteriosis, development of superinfection.

At endolumbar introduction - neurotoxic reactions: nausea, vomiting, increase in reflex irritability, meningeal symptoms, spasms, coma.

Interaction with other medicines:

Probenetsid reduces canalicular secretion of benzylpenicillin, concentration of the last in a blood plasma thereby increases, the elimination half-life increases.

At simultaneous use with the antibiotics having bacteriostatic action (macroleads, chloramphenicol, linkozamida, tetracycline), bactericidal effect of benzylpenicillin decreases.

Increases efficiency of indirect anticoagulants (suppressing intestinal microflora, reduces a prothrombin ratio); reduces efficiency of oral contraceptives, medicines in the course of which metabolism paraaminobenzoic acid, ethinylestradiol - risk of development of bleedings of "break" is formed.

Diuretics, Allopyrinolum, blockers of canalicular secretion, phenylbutazone, nesteroydny antiinflammatory drugs, reducing canalicular secretion, increase concentration of benzylpenicillin.

Allopyrinolum increases risk of development of allergic reactions (skin rash).

Bactericidal antibiotics (including cephalosporins, Vancomycinum, rifampicin, aminoglycosides) have sinergidny effect.

Contraindications:

Hypersensitivity to benzylpenicillin and other drugs from group of penicillin and cephalosporins, the laktition period.

With care. Pregnancy, lactation period, heavy liver failure, renal failure, allergic diseases (including bronchial asthma, pollinosis).

Overdose:

Symptoms: spasms, consciousness disturbance.

Treatment: drug withdrawal, symptomatic therapy.

Storage conditions:

In the dry place at a temperature not above 20 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for intramuscular introduction of 500000 Pieces, 1000000 Pieces to bottles. On 50 bottles together with application instructions place a box from a cardboard (for hospitals).