Bicillin-5 - instructions for use, dose, side effects, contraindications

Combined bactericidal antibiotic, consisting of two long-acting benzylpenicillin salts. Suppresses the synthesis of the cell wall of the microorganism. It is active against gram-positive microorganisms: Staphylococcus spp. (non-treating penicillinase), Streptococcus spp. (incl. Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming rods, Bacillus anthracis, Clostridium spp., Actinomyces israelii; Gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Treponema spp.

To the action of the drug resistant strains Staphylococcus spp., producing penicillinase.

Pharmacokinetics:

Bicillin®-5 is a prolonged-release drug, a high concentration of antibiotic in the blood persists up to 4 weeks.

Benzathine benzylpenicillin.

After intramuscular injection benzathine benzylpenicillin very slowly hydrolyses, releasing benzylpenicillin. The maximum concentration of the drug in the blood serum is reached 12-24 hours after the injection. A long half-life provides a stable and long-term concentration of the drug in the blood: on day 14 after the administration of 2,400,000 ME the concentration in the serum is 0.12 μg / ml; on the 21st day after the introduction of 1200000 ME The preparation was 0.06 μg / ml (1 ME = 0.6 μg). Diffusion of the drug in the liquid is complete, the diffusion in the tissue is very weak. Connection with plasma proteins 40-60%. Benzathine benzylpenicillin passes in small amounts through the placental barrier, and also penetrates into the mother's breast milk.Biotransformation of the drug is insignificant. It is excreted mainly by the kidneys in an unchanged form. Within 8 days, up to 33% of the administered dose is allocated.

Benzylpenicillin.

The maximum concentration in blood plasma with intramuscular injection is achieved in 20-30 minutes. The half-life of the drug is 30-60 minutes, with renal failure 4-10 hours or more. Connection with plasma proteins - 60%. Penetrates into organs, tissues and biological fluids, except for CSF, eye and prostate gland tissues. Inflammation of meningeal membranes penetrates the blood-brain barrier. Passes through the placenta and penetrates into breast milk. It is excreted by the kidneys unchanged.

Indications:

Infectious-inflammatory diseases caused by susceptible pathogens: prolonged (year-round) prevention of relapses rheumatism; syphilis, yaws; streptococcal infections (excluding infections caused by Group B Streptococcus) - acute tonsillitis, scarlet fever, wound infections, erysipelas.

Contraindications:

Hypersensitivity to the drug, benzylpenicillin and other beta-lactam antibiotics. Lactation period.

Carefully:

Pregnancy, renal failure, weighed allergic anamnesis, bronchial asthma, pseudomembranous colitis.

Pregnancy and lactation:

Bicillin®-5 penetrates in small amounts through the placental barrier and into the mother's milk. Use in pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

It is recommended to stop breastfeeding when it is necessary to prescribe the drug.

Dosing and Administration:

Intramuscularly.

Adults - 120000 ED + 300000 ED every 4 weeks.

Preschool children - 480000 ED + 120000 ED every 3 weeks, children older than 8 years - 960000 ED + 240000 ED 1 every 4 weeks.

To prepare the suspension use sterile water for injection, isotonic sodium chloride solution or 0.25-0.5% solution of procaine (novocaine).

A suspension of Bicillin®-5 is prepared aseptically, just before use (ex tempore): in the vial with the drug under pressure slowly (at a rate of 5 ml for 20-25 seconds), 5-6 ml of solvent are introduced. The contents of the vial are mixed and shaken along the longitudinal axis of the vial to form a homogeneous suspension. Bubbles are allowed on the surface of the suspension near the walls of the vial.Suspension of Bicillin®-5 immediately after preparation is injected deeply intramuscularly into the upper outer quadrant of the gluteus muscle. Rubbing the gluteus muscle after injection is not recommended. When the administration is delayed, the physical and colloidal properties of the suspension change immediately after preparation, as a result of which the movement through the syringe needle may be impeded.

Side effects:

Allergic reactions: anaphylactic shock, anaphylactoid reactions, urticaria, fever, arthralgia, angioedema, multiforme exudative erythema, exfoliative dermatitis.

Laboratory indicators: anemia, thrombocytopenia, leukopenia, hypocoagulation. Other: stomatitis, glossitis.

Interaction:

Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic. Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the prothrombin index); reduces the effectiveness of oral contraceptives, drugs,in the process of metabolism of which parahaminobenzoic acid is formed, ethinyl estradiol - the risk of bleeding "breakthrough". Diuretics, allopurinol, tubular secretion blockers, phenylbutazone, non-steroidal anti-inflammatory drugs, reducing tubular secretion, increase the concentration of benzylpenicillin in the blood and tissues. Allopurinol increases the risk of allergic reactions (skin rashes).

Special instructions:

Do not administer subcutaneously, intravenously, endolumbally, or in the body cavity. With a random intravascular injection, there may be a transient sense of depression, anxiety, and visual impairment (Ouenier syndrome). In order to avoid accidental intravascular administration of the drug, it is recommended to perform aspiration before intramuscular injection in order to detect a possible needle drop into the vessel.

In the treatment of syphilis before the start of therapy and then within 4 months, it is necessary to conduct microscopic and serological studies. In connection with the development of fungal infections, it is advisable to simultaneously assign vitamins of group B and vitamin C, and if necessary - antifungal agents for systemic use.It should be borne in mind that the use of insufficient doses or too early cessation of treatment often leads to the emergence of resistant strains of pathogens.

Form release / dosage:

Powder for the preparation of suspension for intramuscular injection 1200000 ED + 300000 units.

Packaging:

1200000 ED + 300000 units per bottle with a capacity of 10 ml.

1, 5 or 10 bottles with instructions for use are placed in a pack of cardboard. 50 bottles with 5 instructions for use are placed in a carton box for delivery to hospitals.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000082

Date of registration:30.09.2009

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp16.02.2017

Illustrated instructions

Instructions

Bicillin®-5 (Bicillin®-5)