Bicillin-1 – description of the drug, instructions for use, reviews

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Manufacturers: Synthesis

Active ingredients

  • Benzathine benzylpenicillin

Disease class

  • Rheumatic fever without mention of cardiac involvement
  • Rheumatic fever with cardiac involvement
  • Rheumatism, unspecified
  • Scarlet fever
  • Erysipelas
  • Syphilis, unspecified
  • Yaws
  • Leishmaniasis, unspecified
  • Post-traumatic wound infection, not elsewhere classified
  • Acute tonsillitis, unspecified
  • Inflammatory diseases of the female pelvic organs caused by syphilis (A51.4, A52.7)

Clinical and pharmacological group

  • Not indicated. See instructions

Pharmacological action

  • Antibacterial
  • Bactericidal

Pharmacological group

  • Penicillins

Powder for preparing a suspension for intramuscular administration of Bicillin-1 (Bicillin-1)

Instructions for medical use of the drug

Description of pharmacological action

Active against gram-positive microorganisms, incl. Staphylococcus spp. (except for strains that produce penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming bacilli Bacillus anthracis, some gram-negative microorganisms (including Neisseria gonorrhoeae, Neisseria meningitidis), Actinomyces israelii, as well as Treponema spp. Not effective against viruses (causative agents of influenza, polio, smallpox, etc.), mycobacterium tuberculosis, protozoa, rickettsia, fungi, as well as most gram-negative microorganisms.

Indications for use

Infectious diseases caused by microorganisms sensitive to the drug (especially when long-term maintenance of therapeutic concentration is necessary), incl. acute tonsillitis, scarlet fever, wound infections, erysipelas; rheumatism (prevention and treatment) caused by treponemes (syphilis, yaws), leishmaniasis.

Release form

powder for preparing a suspension for intramuscular administration 1.2 million units; bottle (bottle), cardboard pack 1; powder for preparing a suspension for intramuscular administration 1.2 million units; bottle (bottle), cardboard pack 10; powder for preparing a suspension for intramuscular administration 1.2 million units; bottle (bottle), cardboard pack 5; powder for preparing a suspension for intramuscular administration 1.2 million units; bottle (bottle), cardboard box (box) 50; powder for preparing a suspension for intramuscular administration 2,400,000 units; bottle (bottle), cardboard pack 10; powder for preparing a suspension for intramuscular administration 2,400,000 units; bottle (bottle), cardboard pack 5; powder for preparing a suspension for intramuscular administration 2,400,000 units; bottle (bottle), cardboard box (box) 50; powder for preparing a suspension for intramuscular administration 600,000 units; bottle (bottle), cardboard pack 10; powder for preparing a suspension for intramuscular administration 600,000 units; bottle (bottle), cardboard pack 5; powder for preparing a suspension for intramuscular administration 600,000 units; bottle (bottle), cardboard box (box) 50; powder for preparing a suspension for intramuscular administration 600,000 units; bottle (bottle); powder for preparing a suspension for intramuscular administration 2,400,000 units; bottle (bottle); powder for preparing a suspension for intramuscular administration 1.2 million units; bottle (bottle); Composition 1 bottle (Bicillin-1) with powder for preparing an injection solution for intramuscular administration contains benzathine benzylpenicillin 600,000 units or 1,200,000 units. 1 bottle (Bicillin-3) with powder for the preparation of an injection solution for intramuscular administration contains benzathine benzylpenicillin, benzylpenicillin sodium and benzylpenicillin novocaine salt, 200,000 units or 400,000 units each; in 10 ml bottles or 10 ml bottles, 50 bottles in a box. 1 bottle with a capacity of 10 ml (Bicillin-5) with powder for preparing an injection solution for intramuscular administration contains benzathine benzylpenicillin 1,200,000 units and benzylpenicillin novocaine salt 300,000 units.

Pharmacodynamics

Active against gram-positive microorganisms, incl. Staphylococcus spp. (except for strains that produce penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming bacilli Bacillus anthracis, some gram-negative microorganisms (including Neisseria gonorrhoeae, Neisseria meningitidis), Actinomyces israelii, as well as Treponema spp. Not effective against viruses (causative agents of influenza, polio, smallpox, etc.), mycobacterium tuberculosis, protozoa, rickettsia, fungi, as well as most gram-negative microorganisms.

Pharmacokinetics

When administered intramuscularly, bicillin-1 is slowly absorbed, hydrolyzed to release benzylpenicillin, and enters the bloodstream over a long period of time. Cmax is reached within 12–24 hours, therapeutic concentration is achieved within 3–6 hours. Bicillin-3 after intramuscular administration is slowly hydrolyzed to release benzylpenicillin. With a single injection, the therapeutic concentration in the blood is maintained for 6–7 days, Cmax is achieved 12–24 hours after injection. On the 14th day after administration at a dose of 2.4 million units, the serum concentration is 0.12 mcg/ml, on the 21st day after administration of 1.2 million units - 0.06 mcg/ml (1 unit = 0. 6 mcg). Binding to blood proteins is 40–60%. Penetration into liquids is high, into tissues low. Passes through the placental barrier and enters breast milk. It is biotransformed to a small extent and is excreted mainly by the kidneys. With the intramuscular administration of Bicillin-5, high concentrations in the blood are created already in the first hours after the injection. After administration of 1.2–1.5 million units in most patients (adults and children), the therapeutic concentration in plasma (0.3 units/ml) persists for 28 days or more.

Contraindications for use

Hypersensitivity (including to other penicillins and drug components). With caution - bronchial asthma, hay fever, urticaria and other allergic diseases; hypersensitivity to various drugs, incl. to antibiotics and sulfonamides (in history).

Side effects

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, Quincke's edema, anaphylactic shock. Other: headache, fever, arthralgia, stomatitis, glossitis, pain at the injection site; with long-term therapy - superinfection caused by drug-resistant microorganisms and fungi.

Directions for use and doses

IM, deep, into the upper outer quadrant of the gluteal muscle (IV administration is prohibited). Bicillin-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 a month. When treating rheumatism in adults, the dose is increased to 2.4 million units 2 times a month. To prevent relapses of rheumatism - 600,000 units once a week for 6 weeks in combination with acetylsalicylic acid or other NSAIDs. Treatment of syphilis is carried out according to special instructions. The average dose is 2.4 million units 2-3 times at intervals of 8 days. Bicillin-3 - in a dose of 300,000 units (if necessary, 2 injections are given in different buttocks). Repeated injections are carried out 4 days after the previous injection. A dose of 600,000 units is administered once every 6 days. For the treatment of primary and secondary syphilis, a single dose is 1.8 million units. The course of treatment is 7 injections. The first injection is carried out at a dose of 300,000 units, the second injection - after 1 day at the 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 is 14 injections. Bicillin-5 for adults - 1.5 million units once every 4 weeks, for children under 8 years old - 600,000 units once every 3 weeks, for children over 8 years old - 1.2–1.5 million units once every 4 weeks. The suspension is prepared under aseptic conditions immediately before use (5-6 ml of sterile distilled water, 0.9% sodium chloride solution or 0.25-0.5% novocaine solution is added to a bottle containing 1.5 million units). The mixture in the bottle is shaken for 30 s in the direction of the longitudinal axis until a homogeneous suspension (or suspension) is formed and immediately administered.

Interactions with other drugs

Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) have an antagonistic effect. Reduces the effectiveness of oral contraceptives and ethinyl estradiol (risk of breakthrough bleeding). Diuretics, allopurinol, phenylbutazone, NSAIDs reduce tubular secretion and increase concentration. Allopurinol increases the risk of allergic reactions (skin rash).

Precautions for use

If blood appears in the syringe during an intramuscular injection (indicating that the needle has entered a blood vessel), the syringe should be removed and injected elsewhere. At the end of the injection, the injection site is pressed with a cotton swab, which prevents the drug from entering the muscle tissue into the subcutaneous tissue (rubbing the buttock after the injection is not recommended). If an allergic reaction develops, treatment is stopped immediately. When the first signs of anaphylactic shock appear, it is necessary to take urgent measures to remove the patient from this state: administration of norepinephrine, glucocorticoids, etc., and, if necessary, mechanical ventilation. When treating sexually transmitted diseases, if syphilis is suspected, microscopic and serological studies are necessary before starting therapy and then for 4 months. Due to the possibility of developing fungal infections, it is advisable to prescribe B vitamins and vitamin C, and, if necessary, nystatin and levorin. It must be taken into account that using the drug in insufficient doses or stopping treatment too early often leads to the emergence of resistant strains of pathogens.

Special instructions for use

IV administration of the drug should not be allowed (possible development of Wanier syndrome - the development of a feeling of depression, anxiety and visual impairment).

Storage conditions

List B: In a dry place, at a temperature not exceeding 15 °C.

Best before date

36 months

ATX classification:

J Antimicrobials for systemic use

J01 Antimicrobials for systemic use

J01C Beta-lactam antibiotics - penicillins

J01CE Penicillins, sensitive to beta-lactamases

J01CE08 Benzathine benzylpenicillin

Bicillin-5 por. d/susp. i.m. 1.5 million units 10 ml No. 1

Benzathine benzylpenicillin* + Benzylpenicillin procaine (Benzathini benzylpenicillinum + Benzylpenicillinum-Procainum)

  • Penicillins in combinations

Pharmacological action - bactericidal, antibacterial.
Inhibits the synthesis of peptidoglycan in the cell wall of microorganisms.

Active against gram-positive microorganisms, incl. Staphylococcus spp. (except for strains that produce penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming bacilli Bacillus anthracis, some gram-negative microorganisms (including Neisseria gonorrhoeae, Neisseria meningitidis), Actinomyces israelii, as well as Treponema spp. Not effective against viruses (causative agents of influenza, polio, smallpox, etc.), mycobacterium tuberculosis, protozoa, rickettsia, fungi, as well as most gram-negative microorganisms.

When administered intramuscularly, bicillin-1 is slowly absorbed, hydrolyzed to release benzylpenicillin, and enters the bloodstream over a long period of time. Cmax is reached within 12–24 hours, therapeutic concentration is achieved within 3–6 hours.

Bicillin-3 after intramuscular administration is slowly hydrolyzed to release benzylpenicillin. With a single injection, the therapeutic concentration in the blood is maintained for 6–7 days, Cmax is achieved 12–24 hours after injection. On the 14th day after administration at a dose of 2.4 million units, the serum concentration is 0.12 mcg/ml, on the 21st day after administration of 1.2 million units - 0.06 mcg/ml (1 unit = 0. 6 mcg). Binding to blood proteins is 40–60%. Penetration into liquids is high, into tissues low. Passes through the placental barrier and enters breast milk. It is biotransformed to a small extent and is excreted mainly by the kidneys.

With the intramuscular administration of Bicillin-5, high concentrations in the blood are created already in the first hours after the injection. After administration of 1.2–1.5 million units in most patients (adults and children), the therapeutic concentration in plasma (0.3 units/ml) persists for 28 days or more.

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, Quincke's edema, anaphylactic shock.

Other:

headache, fever, arthralgia, stomatitis, glossitis, pain at the injection site; with long-term therapy - superinfection caused by drug-resistant microorganisms and fungi.

Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect, bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) have an antagonistic effect. Reduces the effectiveness of oral contraceptives and ethinyl estradiol (risk of breakthrough bleeding). Diuretics, allopurinol, phenylbutazone, NSAIDs reduce tubular secretion and increase concentration. Allopurinol increases the risk of allergic reactions (skin rash).

If blood appears in the syringe during an intramuscular injection (indicating that the needle has entered a blood vessel), the syringe should be removed and injected elsewhere. At the end of the injection, the injection site is pressed with a cotton swab, which prevents the drug from entering the muscle tissue into the subcutaneous tissue (rubbing the buttock after the injection is not recommended).

If an allergic reaction develops, treatment is stopped immediately. When the first signs of anaphylactic shock appear, it is necessary to take urgent measures to remove the patient from this state: administration of norepinephrine, glucocorticoids, etc., and, if necessary, mechanical ventilation.

When treating sexually transmitted diseases, if syphilis is suspected, microscopic and serological studies are necessary before starting therapy and then for 4 months.

Due to the possibility of developing fungal infections, it is advisable to prescribe B vitamins and vitamin C, and, if necessary, nystatin and levorin. It must be taken into account that using the drug in insufficient doses or stopping treatment too early often leads to the emergence of resistant strains of pathogens.

IV administration of the drug should not be allowed (possible development of Wanier syndrome - the development of a feeling of depression, anxiety and visual impairment).

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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use the drug Bicillin-1, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

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