Bicillinum-1

General characteristics. Structure:

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

Active ingredient:                1 фл.
benzatina benzylpenicillin     of 2.4 million. Piece

Pharmacological properties:

Antibiotic of group of the penicillin of the prolonged action collapsing a penicillinase. Has bactericidal effect. 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: Streptococcus spp. (including Streptococcus pneumoniae, Streptococcus pyogenes of group A), Staphylococcus spp. (not forming a penicillinase), Corynebacterium diphtheriae; gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis; anaerobic bacteria: Bacillus anthracis, Clostridium spp., Actinomyces israelii; also concerning Treponema spp.
Staphylococcus spp are steady against drug., forming a penicillinase.

 

Pharmacokinetics. Absorption

After an injection of a benzatin in oil benzylpenicillin is very slowly hydrolyzed, releasing benzylpenicillin.
Cmax in blood serum is reached in 12-24 h after an injection.

Distribution and metabolism

The long elimination half-life provides stable and long concentration of drug in blood: for the 14th day after introduction of 2.4 million. Drug piece concentration in serum makes 0.12 mkg/ml; for the 21st day after introduction of 1.2 million. Piece - 0.06 mkg/ml (1 ED=0.6 mkg). Diffusion of drug in liquid full, diffusion in fabric very weak.

Linkng with proteins of plasma - 40-60%.

Benzatina benzylpenicillin gets in small amounts through a placental barrier, and also is allocated with chest in milk.

Drug biotransformation insignificant.

Removal

It is removed preferential by kidneys in not changed look. For 8 days about 33% of the entered dose are allocated.

Indications to use:

For treatment of the infections caused by microorganisms, sensitive to drug:

— syphilis (as monotherapy);

— frambeziya;

— pint;

— acute tonsillitis;

— scarlet fever.

For prevention of the infections caused by microorganisms, sensitive to drug:

— the repeated attacks after acute rheumatic fever;

— ugly face recurrence;

— wound fever;

— postoperative complications.

Route of administration and doses:

The drug is administered by buttocks, only deeply in oil in an upper outside quadrant. At emergence of blood in the syringe, a needle, testimonial of hit, in a vessel, it is necessary to take the syringe and to make an injection to other place. In need of two injections the drug should be administered in different buttocks.

The drug cannot be administered in/in!

The adult at preventive treatment of syphilis appoint once 2.4 million. Piece; at primary syphilis - on 1 injection (2.4 million. Piece) in oil with an interval of 7 days (a course - 2 injections); at the secondary and early latent syphilis - on 1 injection (2.4 million. Piece) in oil with an interval of 7 days (a course - 3 injections).

For preventive treatment of the child born by mother with not treated syphilis - on 1 injection (50 000 PIECES/kg of body weight) in oil with an interval of 7 days (a course - 3 injections), the dose is halved and entered into different buttocks.

At preventive treatment of the child in connection with insufficient treatment of mother or a serorezistentnost of syphilis - on 1 injection (50 000 PIECES/kg of body weight) in oil with an interval of 7 days (a course - 2 injections).

At treatment of a frambeziya and pints (local treponematoza) to children - 1.2 million. Piece once; adult - 2.4 mln units once.

At acute tonsillitis, scarlet fever, an ugly face, wound fevers in an acute phase to children up to 12 years - 0.6 million. To piece there are each 3 days or 1.2 million. To piece there are each 2-4 weeks depending on weight of an infection; adult - 1.2-2.4 million. Piece once a week.

For prevention of the repeated attacks after the postponed acute rheumatic fever to children with body weight <25 kg - 0.6 million. Piece of 1 times in 3 weeks; to children with body weight> 25 kg - 1.2 million. Piece of 1 times in 3 weeks; to teenagers and adults - 2.4 million. Piece of 1 times in 3 weeks. Duration of prevention is established individually.

For prevention of a recurrence of an ugly face to children - 0.6 PIECES of 1 times in 2 weeks or 1.2 million. To piece there are each 3-4 weeks; the adult at a seasonal recurrence - 2.4 million. Piece of 1 times in 4 weeks for 3-4 months annually; at a frequent recurrence - 2.4 million. Piece of 1 times in 3-4 weeks for 2-3 years.

For prevention of postoperative infections to children - 0.6 million. Piece or 1.2 million. Piece; adult - 2.4 million. To piece there are each 7-14 days to an absolute recovery.

At a renal failure of a dose decrease according to KK: at KK from 10 to 50 ml/min. enter 75% of a daily dose of drug, at KK <10 ml/min. enter 25-50% of a daily dose of drug.

Rules of preparation of solution
Suspension of drug is prepared in aseptic conditions just before use: enter 3-5 ml of water for injections into a bottle or 0.9% of solution of sodium of chloride. Mix is mixed before receiving a uniform suspension, quickly rotating a bottle between palms within not less than 1 min. or carefully stirring up a bottle in the direction of its longitudinal axis during 30 pages.

Features of use:

At emergence of any allergic reactions it is necessary to stop administration of drug and to appoint the corresponding treatment. Fatal allergic reactions up to development of an acute anaphylaxis can be observed heavy and sometimes.

When collecting the anamnesis it is necessary to pay attention to portability of the treatment which is carried out earlier penicillin. At instructions in the anamnesis on an allergy to penicillin drug is categorically contraindicated. Allergic reactions to penicillin can be cross with allergic reactions to cephalosporins. In this regard at instructions in the anamnesis on allergic reactions to cephalosporins purpose of penicillin is contraindicated.

It is impossible to administer the drug п / to, in/in, endolyumbalno, and also in a perigastrium. At accidental intravascular introduction the passing feeling of alarm and a vision disorder (Uanye's syndrome) can be noted. To avoid accidental intravascular administration of drug, it is recommended to make before carrying out in oil an injection aspiration for the purpose of identification of possible hit of a needle in a vessel.

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

Due to a possibility of development of fungal infections it is reasonable to appoint at treatment drug vitamins of group B and vitamin C, and if necessary - nystatin and levorinum.

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

Side effects:

Allergic reactions: acute anaphylaxis, small tortoiseshell, fever, joint pains, Quincke's disease, exfoliative dermatitis, polymorphic erythema, breath difficulty. At therapy of syphilis because of release of endotoxins Yarisha-Gerksgeymer's reaction can develop.

From system of a hemopoiesis: reversible anemia, leukopenia, thrombocytopenia.

From the alimentary system: stomatitis, a glossitis, nausea, vomiting, diarrhea, candidiasis, were described separate cases of development of pseudomembranous colitis at drug use; seldom moderate tranzitorny increase in level of serumal transaminases.

From an urinary system: seldom - acute intersticial nephrite.

At long therapy development of superinfection by steady microorganisms and mushrooms is possible.

Use of high doses beta лактамных antibiotics, especially at a renal failure, can cause development of encephalopathy (including consciousness disturbance, motive disturbances, spasms).

At children development of local reactions to administration of drug is possible.

Interaction with other medicines:

At co-administration of Bicillinum-1 with NPVS (indometacin, phenylbutazone, salicylates), Allopyrinolum, probenetsidy it must be kept in mind a possibility of competitive inhibition of removal of drugs from an organism.

At simultaneous use with Bicillinum-1 of bactericidal antibiotics (including cephalosporins, Cycloserinum, Vancomycinum, rifampicin, aminoglycosides) an action synergism is noted; bacteriostatic antibiotics (including macroleads, chloramphenicol, linkozamid, tetracyclines) - antagonism of action.

Bicillinum-1 increases efficiency of indirect anticoagulants (suppressing intestinal microflora, reduces a prothrombin ratio).

Bicillinum-1 reduces efficiency of oral contraceptives and medicines in the course of which metabolism paraaminobenzoic acid is formed.

At simultaneous use of Bicillinum-1 with ethinylestradiol the risk of development of breakthrough bleedings increases.

At simultaneous use of Bicillinum-1 and Allopyrinolum the risk of development of allergic reactions (skin rash) increases.

Contraindications:

— hypersensitivity to a beta laktamnym to antibiotics (penicillin and cephalosporins).

With care it is necessary to appoint at tendency to allergic reactions, pseudomembranous colitis, a renal failure.

 

Use of the drug BITSILLIN®-1 at pregnancy and feeding by a breast

Benzatina benzylpenicillin in small amounts gets through a placental barrier and into mother's milk. Use at pregnancy is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit.
It is recommended to stop feeding by a breast in need of purpose of drug.

 

Use at renal failures

At a renal failure of a dose decrease according to KK: at KK from 10 to 50 ml/min. enter 75% of a daily dose of drug, at KK less than 10 ml/min. enter 25-50% of a daily dose of drug.

Overdose:

Now about cases of overdose of the drug Bicillinum-1 it was not reported.

Storage conditions:

List B. Drug should be stored in unavailable to children, the dry, cool place at a temperature not above 15 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Bottles of 10 ml (1) - packs cardboard.
Bottles of 20 ml (1) - packs cardboard.