Bicillinum-3

General characteristics. Structure:

Powder for preparation of suspension for introduction in oil white or white with slightly yellowish shade, forming resistant suspension at water addition.

Active ingredient: mix бензатин benzylpenicillin, benzylpenicillin sodium (or potassium) salt and benzylpenicillin of novocainic salt of 600 thousand. Piece

Pharmacological properties:

The combined antibacterial drug of group of the penicillin of the prolonged action collapsing a penicillinase. Disturbance of synthesis of a peptidoglikan - a mukopeptid of a cellular cover is the cornerstone of the mechanism of action that leads to inhibition of synthesis of a cell wall of a microorganism, suppression of growth and reproduction of bacteria.
It is active concerning gram-positive bacteria: Staphylococcus spp. (not forming a penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis; gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Actinomyces israelii.
Drug is also active concerning Treponema spp., anaerobic spore-forming sticks, leyshmaniye.
Staphylococcus spp are steady against drug., producing a penicillinase.

 

Pharmacokinetics. Absorption

At single introduction remains in average therapeutic concentration during 6-7 Cmax in a blood plasma it is reached in 12-24 h after introduction.

After introduction of Bicillinum-3 in a dose of 2.4 million. Piece concentration in blood serum for the 14th day makes 0.12 mkg/ml; after introduction of Bicillinum-3 in a dose of 1.2 million. Piece concentration in blood serum for 21 days makes 0.06 mkg/ml.

Distribution and metabolism

After introduction in oil it is slowly hydrolyzed with benzylpenicillin release.

In insignificant degree is exposed to biotransformation.

Linkng with proteins of a blood plasma - 40-60%. Passes through a placental barrier, gets into breast milk.

Distribution in fabrics - low is well distributed in liquids, at the same time.

Removal

It is removed preferential by kidneys.

Indications to use:

— treatment of the infectious diseases caused by activators, sensitive to penicillin (especially when it is necessary to create long therapeutic concentration in blood);

— syphilis;

— frambeziya;

— streptococcal infections (acute tonsillitis, scarlet fever, wound fevers, an ugly face), except for the infections caused by group B streptococci;

— prevention of rheumatism;

— leushmaniosis.

Route of administration and doses:

Bicillinum-3 is entered deeply into an upper outside quadrant of a buttock in a dose no more than 1.2 million In need of 2 injections do them in different buttocks. Repeated injections carry out on 4 days after the previous injection.
Drug in a dose of 600 000 PIECES is entered 1 time in 6 days.
At treatment of primary and secondary syphilis the single dose of drug makes 1.8 million. Pieces. A course of treatment - 7 injections. The first injection is carried out in a dose of 300 000 PIECES, the second injection - in 1 days in a full dose (1.8 million. Piece). The subsequent injections carry out 2 times a week.
At treatment of the secondary recurrent and latent early syphilis for the first injection the dose of 300 000 PIECES, for the subsequent an injection - 1.8 million is used. Injections carry out 2 times a week. A course of treatment - 14 injections.
It is forbidden in/in administration of drug.
Rules of preparation and administration of solution
Suspension of Bicillinum-3 is prepared just before the use. With drug enter 2-3 ml of sterile water for injections into a bottle or isotonic solution of sodium of chloride. Mix in a bottle is stirred up during 30 sec. (in the direction of a longitudinal axis) before formation of homogeneous suspension (or suspensions) which is entered by buttocks, deeply in oil in an upper outside quadrant. Grinding of a buttock after an injection is not recommended.

Features of use:

At development of allergic reactions it is necessary to stop treatment immediately.

At development of an acute anaphylaxis performing antishock therapy is shown (introduction of Norepinephrinum, GKS, IVL carry out).

Intravenous and endolumbar administration since development of a syndrome of Uanye is possible (depression, alarm, paresthesias, vision disorder) is not allowed.

At treatment of venereal diseases, at suspicion of syphilis, before therapy and then within 4 months carrying out microscopic and serological examinations is necessary.

Due to the possible development of fungal infections, purpose of antifungal drugs (nystatin, levorinum), and also ascorbic acid and vitamins of group B is reasonable.

It is necessary to consider that use of drug in insufficient doses or the early termination of treatment leads to emergence of resistant strains of activators.

Side effects:

Allergic reactions: small tortoiseshell, Quincke's disease, multiformny erythema, acute anaphylaxis, arthralgia, fever, exfoliative hypostasis.

From the alimentary system: stomatitis, glossitis.

From coagulant system of blood: anemia, thrombocytopenia, leukopenia, hypocoagulation.

Others: at prolonged use - superinfection, mycoses.

Interaction with other medicines:

At simultaneous use with bactericidal antibiotics (including cephalosporins, Cycloserinum, Vancomycinum, rifampicin, aminoglycosides) an action synergism is noted; with bacteriostatic antibiotics (including macroleads, chloramphenicol, linkozamida, tetracyclines) - antagonism.

Bicillinum-3 reduces efficiency of oral contraceptives and ethinylestradiol (risk of development of breakthrough bleedings).

At simultaneous use of Bicillinum-3 with Allopyrinolum the risk of development of allergic reactions increases.

Pharmacokinetic interaction

At simultaneous use diuretics, Allopyrinolum, phenylbutazone, NPVS reduce canalicular secretion and increase concentration of penicillin.

Contraindications:

— hypersensitivity to penicillin and Procainum (novocaine);

— bronchial asthma;

— hay fever;

— other allergic diseases.

 

Use of the drug BITSILLIN®-3 at pregnancy and feeding by a breast

Data on use of the drug Bicillinum-3 at pregnancy and in the period of a lactation (breastfeeding) are not provided.

Overdose:

Now about cases of overdose of the drug Bicillinum-3 it was not reported.

Storage conditions:

List B. Drug should be stored in the dry place at a temperature of 8-15 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Bottles of 10 ml (10) - packs cardboard.
Bottles of 10 ml (50) - boxes cardboard.