Bicillin®-1 (Bicillin®-1)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Active substanceBenzathine benzylpenicillinBenzathine benzylpenicillin
Dosage form: & nbspPowder for suspension for intramuscular administration
Composition:Active substance: Benzathine benzylpenicillin - 600000 ED, 1200000 ED, 2400000ED.
Description:White or white with a slightly yellowish tint powder, prone to clumping, forming a stable suspension with the addition of water.
Pharmacotherapeutic group:Antibiotic - penicillin biosynthetic
ATX: & nbsp

J.01.C.E.08   Benzathine benzylpenicillin

Pharmacodynamics:

Benzathine benzylpenicillin is a beta-lactam antibiotic from the penicillin type group G prolonged action. The microbial cell is bactericidal. Characterized by long-term action. Suppresses the synthesis of the cell wall of microorganisms. It is active against gram-positive pathogens: Staphylococcus spp. (penicillinase-forming), Streptococcus spp., in t.ch. Streptococcus pneumoniae, Corynebacterium diphtheriae, anaerobic spore-forming sticks, Bacillus anthracis, Clostridium spp., Actinomyces israelii; Gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, as well as Treponema spp. To the action of the drug resistant strains Staphylococcus spp., producing penicillinase, destroying benzylpenicillin.

Pharmacokinetics:After intramuscular injection slowly hydrolyzed with the release of benzylpenicillin. Time to reach the maximum concentration in the plasma - 12-24 hours after the injection. On day 14 after the administration of 2,400,000 units, the concentration in the blood plasma is 0.12 μg / ml; on day 21 after the administration of 1200,000 units, 0.06 μg / ml. Penetration in the liquid is high, in the tissue - low. Overcomes the placental barrier and penetrates into breast milk. The connection with plasma proteins is 40-60%. Metabolized slightly, excreted mainly by the kidneys unchanged. For 8 days, up to 33% of the dose administered is released.
Indications:

Treatment of infections caused by sensitive microorganisms: syphilis (monotherapy), yaws, pint; acute tonsillitis, scarlet fever.

Prevention of infections caused by sensitive microorganisms: repeated attacks after acute rheumatic fever, recurrence of erysipelas, wound infections, infections in tonsillectomy or after extraction of the tooth.

Contraindications:

Hypersensitivity (including to other beta-lactam antibiotics).

Carefully:Complicated allergic anamnesis, pseudomembranous colitis, chronic renal failure.
Pregnancy and lactation:

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:

Enter only intramuscularly, can not be administered intravenously!

If necessary, two injections are done in different buttocks. The drug is injected deep into the upper outer quadrant of the gluteus muscle. When blood appears in the syringe, indicating the needle is in the vessel, you need to remove the syringe and inject it elsewhere.

The suspension of the preparation is prepared in aseptic conditions immediately before use. Water is injected into the vial. For injection or 0.9% solution of sodium chloride at a rate of 1 ml for 5 s: 2 ml for a dosage of 0.6 million units, 4 ml for 1.2 million units and 8 ml for 2.4 million units. The mixture is stirred until a uniform suspension is obtained, quickly rotating the bottle between the palms for at least a minute or gently shaking the bottle in the direction of its longitudinal axis for 30 seconds. Bubbles are allowed on the surface of the suspension near the walls of the vial.

Treatment of syphilis in adults and children 2-12 years: primary seronegative syphilis - 2.4 million units once; primary seropositive - 2.4 million units with an interval of 7 days,course - 2 injections; secondary and latent early syphilis, late (tertiary and neurosyphilis) - 2.4 million units with an interval of 7 days, the course - 3 injections. Congenital syphilis in children under 2 years old, born with an untreated mother, with syphilis - 50 thousand ED / kg of body weight (the dose is divided in half and injected into different buttocks) with an interval of 7 days, the course - 3 injections; preventive treatment of children with insufficient treatment of the mother or serosurprising - 50 thousand units / kg of body weight (the dose is divided in half and injected into different buttocks) with an interval of 7 days, the course - 2 injections.

Treatment of yaws and pints: children - 1.2 million units once; adults - 2.4 million units once.

Treatment of acute tonsillitis, scarlet fever, wound infection: children under 12 years of 0.6 million units every 3 days or 1.2 million units every 2-4 weeks, depending on the severity of the infection; adults - for 1.2-2.4 million units once a week.

Prevention of repeated attacks after acute rheumatic fever: children weighing up to 25 kg - 0.6 million units every 3 weeks, more than 25 kg - 1.2 million units every 3 weeks; adults and children over 12 years - 2.4 million units every 3 weeks.

Preventing relapse of erysipelas: children - 0.6 million units once every 2 weeks or 1.2 million units every 3-4 weeks; adults with seasonal relapses - 2.4 million units every 4 weeks for 3-4 months annually, with frequent relapses - 2.4 million units once every 3-4 weeks for 2-3 years.

Prevention of infections after tonsillectomy or tooth extraction: children - 0.6 million units or 1.2 million units, adults - 2.4 million units every 7-14 days until complete recovery.

In chronic renal failure with the clearance of creatinine (CC) 10-50 ml / min - 75 % daily dose, CC less than 10 ml / min - 25-50% of the daily dose.

Side effects:

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

In the treatment of syphilis, due to the release of toxins, the Yarisch-Gerxheimer reaction may develop.

On the part of the organs of hematopoiesis: hemolytic anemia, thrombocytopenia, and leukopenia.

From the digestive system: stomatitis, glossitis, nausea, vomiting, diarrhea, candidiasis, pseudomembranous colitis, moderate transient increase in the activity of "liver" transaminases.

Other: interstitial nephritis.

With long-term therapy - superinfection with resistant microorganisms and fungi; when high doses are used, especially against the background of concomitant chronic renal failure, the development of encephalopathy (impaired consciousness, convulsions, motor disorders) is possible.

Local reactions to the administration of the drug (more often in children): infections of the injection site, inflammation, swelling, abscess, swelling, hemorrhage, inflammation of the subcutaneous tissue, necrosis, atrophy, ecchymosis, skin ulceration.

Overdose:

With a significant overdose, there may be muscle twitching or convulsions.

Treatment is symptomatic.

Interaction:

Bactericides antibiotics (including cephalosporins, cycloserine, 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 which produces paraaminobenzoic acid, 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 penicillins. Allopurinol increases the risk of allergic reactions (skin rashes).

Special instructions:

If any allergic reaction occurs, immediate cessation of treatment is required.

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 possibility of developing fungal lesions, it is advisable in the treatment of benzylpenicillin to prescribe B vitamins, and if necessary, antifungal agents for systemic use.

It should be borne in mind that the use of the drug in insufficient doses or too early cessation of treatment often leads to the emergence of resistant strains of pathogens.
Form release / dosage:Powder for suspension for intramuscular injection 600,000 units, 1200,000 units, 2,400,000 units.
Packaging:

Powder for suspension for intramuscular injection 600,000 units, 1200000 units, 2,400,000 units in vials of 10 ml or 20 ml capacity.

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:

List B. In a dry place, at a temperature of no higher than 15 ° 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:P N003970 / 01
Date of registration:18.01.2010 / 31.05.2010
Expiration Date:Unlimited
The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia
Manufacturer: & nbsp
Information update date: & nbsp16.02.2017
Illustrated instructions
    Instructions
    Up