Expiration date: 06/2025
Composition and form of issue:
1 bottle (Bicillin-1) with powder for preparation of injection solution for I/m injection contains the benzathine benzylpenicillin 600000 1200000 ED or ED.
1 bottle (Bicillin-3) with powder for preparation of injection solution for I/m injection contains benzatin benzylpenicillin, benzylpenicillin sodium and benzylpenicillin novocaine salt of 200,000 UNITS or 400,000 UNITS in 10 ml bottles or 10 ml bottles, in a box of 50 bottles.
1 bottle with a capacity of 10 ml (Bicillin-5) with powder for preparation of injection solution for I/m injection contains the benzathine penicillin 1200000 IU benzylpenicillin procaine salt of 300,000 UNITS.
Characteristic:
Bicillinum-1 - white powder odorless or almost odorless, forming a stable suspension when adding water.
Bicillinum-3-white or white with a slightly yellowish tint powder, forming a stable suspension when adding water.
Bicillinum-5 - white powder odorless, bitter taste, forming with the addition of water, saline or 0, 25-0.5% solution of novocaine homogeneous suspension of milk turbidity. With prolonged contact with water or other solutions, the physical and colloidal properties of the drug change (the suspension becomes uneven and difficult to pass through the needle syringe).
Pharmacological action:
Inhibits synthesis of peptidoglycan of the cell wall of microorganisms.
Pharmacokinetics:
Bicillinum-1 with the/m introduction slowly absorbed, hydrolyzed with the release of benzylpenicillin and for a long time enters the bloodstream. Cmax is achieved in 12-24 hours, therapeutic concentration-in 3-6 hours.
Bicillinum-3 after the/m introduction is slowly hydrolyzed with release of benzylpenicillin. With a single administration therapeutic concentration in the blood is maintained for 6-7 days, C Max achieved through 12-24 h after injection. On the 14th day after administration at a dose of 2, 4 million ED serum concentrations of 0, 12 mg/ml, on the 21st day after the introduction of 1, 2 million ED-0, 06 mcg/ml (1 ED=0, 6 mcg). Binding to blood proteins-40-60%. The penetration of the liquid is high, in the tissue is low. Passes through the placental barrier, penetrates into breast milk. Slightly biotransformiroetsa, kidneys predominantly displayed.
With the/m introduction of Bicillin-5 high blood concentrations are created in the first hours after injection. After the introduction of 1, 2-1, 5 million UNITS in most patients (adults and children) therapeutic plasma concentration (0, 3 U/ml) is maintained for 28 days or more.
Description of the pharmacological action:
Active against gram-positive microorganisms, including Staphylococcus spp. (with the exception of strains producing penicillinase), Streptococcus spp.(including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming Bacillus anthracis, some gram-negative microorganisms (including Neisseria gonorrhoeae, Neisseria meningitidis), Actinomyces israelii, and Treponema spp. Not effective against viruses (pathogens of influenza, polio, smallpox, etc.), Mycobacterium tuberculosis, protozoa, Rickettsia, fungi, as well as most gram-negative microorganisms.
Indications:
Infectious diseases caused by sensitive microorganisms (especially the long-term maintenance of therapeutic concentrations), including acute tonsillitis, scarlet fever, wound infections, erysipelas rheumatism (prevention and treatment), caused by treponemes (syphilis, yaws), leishmaniasis.
Contraindications:
Hypersensitivity (including to other penicillins and the drug component). Caution with bronchial asthma, pollinosis, urticaria and other allergic diseases are hypersensitivity to various drugs, including antibiotics and sulfonamides (in history).
Side effect:
From the cardiovascular system and blood (hematopoiesis, hemostasis): anemia, thrombocytopenia, leukopenia, hypocoagulation.
Allergic reactions: rash on the skin and mucous membranes, urticaria, eosinophilia, joint pain, erythema multiforme, exfoliative dermatitis, angioedema, anaphylactic shock.
Other: headache, fever, arthralgia, stomatitis, glossitis, pain at the injection site during prolonged therapy — superinfection caused by drug-resistant microorganisms and fungi.
Drug interaction:
Bactericidal antibiotics (including cephalosporins, cycloserine, Vancouver, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) — antagonistic. Reduces the effectiveness of oral contraceptives and ethinyl estradiol (the risk of bleeding "breakthrough"). Diuretics, allopurinol, phenylbutazone, NSAIDs reduce tubular secretion and increase concentration. Allopurinol increases the risk of allergic reactions (skin rashes).
Method of application and doses:
In/m deep in the upper outer quadrant of the gluteus Maximus (in/in the introduction is prohibited).
Bicillinum-1 for the prevention and treatment of infectious diseases in adults — 300,000 UNITS and 600,000 UNITS once a week or 1, 2 million UNITS 2 times per month. In the treatment of rheumatism in adults, the dose is increased to 2, 4 million IU 2 times per month. To prevent relapse of rheumatism-600,000 UNITS 1 time in the week for 6 weeks in combination with taking acetylsalicylic acid or other NSAIDs.
Treatment of syphilis is carried out according to special instructions. The average dose-2, 4 million UNITS 2-3 times at intervals of 8 days.
Bicillinum-3-at a dose of 300,000 UNITS (if necessary, 2 injections are made into different buttocks). Repeated injections are carried out on 4 days after the previous injection. At a dose of 600,000 IU administered once every 6 days.
In the treatment of primary and secondary syphilis single dose — 1, 8 million ED. The course of treatment — 7 injections. The first injection is carried out at a dose of 300,000 UNITS, the second injection-after 1 day in full dose, subsequent injections are carried out 2 times a week.
In the treatment of secondary recurrent and latent early syphilis, a dose of 300,000 UNITS is used for the first injection, and 1, 8 million UNITS for subsequent injections. Injections are carried out 2 times a week. The course of treatment — 14 injections.
Bicillinum-5 adults-1, 5 million MEALS 1 time in 4 weeks, children under 8 years-600,000 MEALS 1 time in 3 weeks, children over 8 years-1, 2-1, 5 million MEALS 1 time in 4 weeks.
The suspension is prepared in aseptic conditions immediately before use (in a bottle containing 1, 5 million UNITS, enter 5-6 ml of sterile distilled water, 0, 9% sodium chloride solution or 0, 25-0, 5% novocaine solution). The mixture in the bottle is shaken for 30 s in the direction of the longitudinal axis to form a homogeneous suspension (or suspension) and immediately injected.
Precautionary measures:
When blood appears in the syringe during the/m injection (indicates a needle in the blood vessel) should extract the syringe and inject to another place. At the end of the injection, the injection site is pressed with a cotton swab, which prevents the Ls from entering the muscle tissue into the subcutaneous tissue (rubbing the buttocks after the injection is not recommended).
With the development of an allergic reaction, treatment is immediately discontinued. When the first signs of anaphylactic shock, it is necessary to take urgent measures to remove the patient from this condition: the introduction of norepinephrine, glucocorticoids, etc., if necessary — IVL.
In the treatment of venereal diseases, if there is a suspicion of syphilis, before starting therapy and then for 4 months it is necessary to conduct microscopic and serological studies.
In connection with the possibility of fungal lesions, it is advisable to appoint b vitamins and vitamin C, and if necessary, nystatin and levorin. 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 appearance of resistant strains of pathogens.
Special instruction:
Do not allow on/in the introduction of the drug (possible development of uanie syndrome — the development of a feeling of depression, anxiety and visual impairment).
