Bitsillin-1
Bitsillin-1: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Bicillin-1
ATX code: J01CE08
Active ingredient: benzathine benzylpenicillin (Benzathine Benzylpenicillin)
Producer: JSC Sintez (Russia)
Description and photo updated: 30.11.2018
Bicillin-1 is an antibiotic that breaks down by penicillinase from the group of biosynthetic penicillins.
Release form and composition
The preparation is produced in the form of a powder for preparing a suspension for intramuscular (i / m) administration: a powdery mass of white or white with a slightly yellow tinge, prone to clumping, forming a stable suspension when water is added [600,000, 1,200,000, or 2,400,000 units of action (ED) in a vial with a capacity of 10 or 20 ml; in a cardboard box 1, 5 or 10 bottles and instructions for the use of Bitsillin-1; for hospitals - 50 bottles in a cardboard box].
The composition of the powder contained in 1 bottle: benzathine benzylpenicillin - 600,000, 1,200,000 or 2,400,000 units.
Pharmacological properties
Pharmacodynamics
Benzathine benzylpenicillin is a beta-lactam antibiotic that belongs to the group of long-acting type G penicillins. The active substance has a long-term effect, acts bactericidal on the cell of microbes, suppressing the synthesis of its walls.
Bicillin-1 demonstrates activity against the following microorganisms:
- gram-positive pathogens: Staphylococcus spp. (penicillinase-forming), Corynebacterium diphtheriae, Streptococcus spp. including. Streptococcus pneumoniae;
- anaerobic spore-forming bacteria: Bacillus anthracis, Clostridium spp., Actinomyces israelii;
- gram-negative microorganisms: Neisseria meningitidis, Neisseria gonorrhoeae, as well as Treponema spp.
Strains of Staphylococcus spp., Which produce penicillinase that destroy benzylpenicillin, are resistant to the antibiotic.
Pharmacokinetics
After the suspension is injected into the muscle tissue, it is slowly hydrolyzed to release benzylpenicillin. The maximum concentration of the drug (C max) in plasma after injection is reached after 12-24 hours.
The plasma concentration of the active substance in the blood after the introduction of 2,400,000 IU on the 14th day is 0.12 μg / ml; after the introduction of 1,200,000 IU on day 21 - 0.06 μg / ml. Benzylpenicillin has a high penetration rate into liquids and low penetration into tissues. It binds to plasma proteins by 40-60%, passes the placental barrier and is excreted in breast milk.
The drug is slightly biotransformed, excreted mostly by the kidneys unchanged. Up to 33% of the administered dose is eliminated within 8 days.
Indications for use
Bicillin-1 is recommended for the prevention / treatment of infections caused by antibiotic-sensitive microorganisms:
- treatment: yaws, scarlet fever, pint, acute tonsillitis, syphilis (monotherapy);
- prevention: repeated attacks after acute rheumatic fever (ARF), wound infections, relapses of erysipelas, infections after tooth extraction or tonsillectomy.
Contraindications
Bicillin-1 therapy is contraindicated during breastfeeding and in the presence of hypersensitivity to benzathine benzylpenicillin or other drugs included in the group of beta-lactam antibiotics (including cephalosporins).
The agent should be used with caution for the following diseases / conditions:
- pregnancy;
- pseudomembranous colitis;
- complicated allergic anamnesis;
- chronic renal failure (CRF).
Bitsillin-1, instructions for use: method and dosage
Bicillin-1 is intended only for intramuscular injection, the drug cannot be administered intravenously (intravenously)!
Injections are made deep into the gluteus maximus muscle, into the upper outer quadrant. If, during the injection, the needle of the syringe got into the vessel, as evidenced by the blood that appears in the cylinder, it is required to remove it and inject the suspension into another place. If two injections are necessary, they should be done in different buttocks.
The suspension must be prepared immediately before use under aseptic conditions. A 0.9% sodium chloride solution or water for injection should be introduced into the vial in the following quantities: for a dosage of 0.6 million U - 2 ml, for 1.2 million U - 4 ml, for 2.4 million U - 8 ml. The infusion rate is 1 ml / 5 seconds. To form a uniform suspension, stir the mixture by gently shaking the bottle in the direction of its longitudinal axis for 1/2 minute or by quickly rotating the bottle between your palms for at least 1 minute. On the surface of the resulting suspension, bubbles are allowed near the walls of the bottle.
Recommended dosage regimen of Bitsillin-1:
- yaws and pint (treatment): once, adults - at a dose of 2.4 million units, children - 1.2 million units;
- syphilis (treatment of adults and children 2–12 years old): primary seronegative syphilis - once in a dose of 2.4 million units; primary seropositive - with an interval of 7 days, 1 injection at a dose of 2.4 million units, course - 2 injections; secondary and latent early syphilis, late (tertiary and neurosyphilis) - with an interval of 7 days, 1 injection at a dose of 2.4 million units, course - 3 injections;
- congenital syphilis in children under 2 years of age, born to mothers with untreated syphilis (treatment): with an interval of 7 days at a dose of 50 thousand U / kg (½ dose is administered in different buttocks), course - 3 injections; for the purpose of prophylactic therapy of children with insufficient treatment of the mother or seroresistance of syphilis: with an interval of 7 days at a dose of 50 thousand U / kg (½ dose is administered in different buttocks), the course is 2 injections;
- scarlet fever, acute tonsillitis, wound infection (treatment): adults - once a week at a dose of 1.2–2.4 million units; children under 12 years old - every 3 days, 0.6 million IU or every 2-4 weeks, 1.2 million IU (depending on the severity of the infection);
- relapses of erysipelas (prevention): adults with seasonal relapses - once every 4 weeks at a dose of 2.4 million units annually for 3-4 months, with frequent relapses - once every 3-4 weeks at a dose of 2.4 million units per for 2-3 years; children - once every 2 weeks at a dose of 0.6 million IU, or every 3-4 weeks at a dose of 1.2 million IU;
- repeated attacks after suffering ARF (prevention): adults and adolescents over 12 years old - once every 3 weeks at a dose of 2.4 million units; children - once every 3 weeks, with a body weight of less than 25 kg at a dose of 0.6 million units, more than 25 kg - 1.2 million units; the duration of Bitsillin-1 application is set individually;
- infections after tooth extraction or tonsillectomy (prophylaxis): every 7-14 days adults - at a dose of 2.4 million units, children - 0.6 or 1.2 million units until the symptoms are completely removed.
Side effects
- hematopoietic organs: thrombocytopenia, hemolytic anemia, leukopenia;
- allergic reactions: arthralgia, eosinophilia, fever, urticaria, difficulty breathing, exfoliative dermatitis, exudative erythema multiforme, anaphylaxis, angioedema, anaphylactoid reactions, anaphylactic shock; when treating syphilis, as a result of the release of toxins, the Jarisch-Herxheimer reaction may occur;
- digestive system: glossitis, stomatitis, candidiasis, vomiting, nausea, diarrhea, transient moderate increase in the level of hepatic transaminases, pseudomembranous colitis;
- local reactions to Bicillin-1 injections (most often observed in children): infections at the injection site, swelling, inflammation, edema, inflammation of the subcutaneous tissue, hemorrhage, abscess, ecchymosis, atrophy, necrosis, skin ulceration;
- others: interstitial nephritis; with a long course - superinfection with resistant microorganisms and fungi; in the case of using high doses, especially against the background of chronic renal failure, encephalopathy (movement disorders, convulsions, impaired consciousness) is possible.
Overdose
In severe overdose, muscle twitching or cramps may occur. Against the background of this condition, symptomatic treatment is prescribed.
special instructions
If any allergic reaction develops, it is necessary to immediately stop the administration of Bicillin-1 and conduct appropriate therapy.
When taking anamnesis, it is necessary to take into account the tolerability of previous treatment with penicillins or other beta-lactam antibiotics.
Bicillin-1 is contraindicated to be administered intravenously, endolumbally, subcutaneously, and in the body cavity. If intravascular injection of the drug was accidentally made, a transient feeling of anxiety, depression and visual impairment (Wanier syndrome) may occur. In order to prevent intravascular injection of the drug, before carrying out the procedure, it is recommended to carry out aspiration to detect the possible penetration of the syringe needle into the vessel.
When treating syphilis, microscopic and serological studies must be carried out before the start of the course and during treatment for 4 months.
In view of the existing risk of fungal infections during therapy, it is advisable to take vitamins of group B and vitamin C, as well as, if necessary, levorin and nystatin.
It is required to take into account that when using Bicillin-1 in insufficient doses or against the background of too early termination of therapy, the likelihood of the appearance of resistant strains of pathogens increases.
Application during pregnancy and lactation
The use of Bicillin-1 during pregnancy is allowed only if the expected benefit of treatment for the mother significantly outweighs the possible risk to the health of the fetus.
If necessary, drug therapy during lactation is recommended to transfer the child to artificial feeding.
Pediatric use
The use of Bitsillin-1 in children is possible according to the dosage regimen.
With impaired renal function
Bicillin-1 should be used with caution in the presence of chronic renal failure. Patients with chronic renal failure with creatinine clearance (CC) below 10 ml / min are prescribed 25-50% of the daily dose of the drug, with CC 10-50 ml / min - 75%.
Drug interactions
- allopurinol, probenecid, nonsteroidal anti-inflammatory drugs (salicylates, phenylbutazone, indomethacin), diuretics, tubular secretion blockers: the concentration of penicillins increases due to a decrease in tubular secretion;
- macrolides, tetracyclines, lincosamide, chloramphenicol and other bacteriostatic antibiotics: there is an antagonism of the action of these drugs with benzathine benzylpenicillin;
- cycloserine, cephalosporins, aminoglycosides, rifampicin, vancomycin and other bactericidal antibiotics: synergistic action is demonstrated;
- allopurinol: the threat of allergic reactions (including skin rash) is aggravated;
- indirect anticoagulants: the effectiveness of these drugs increases, as a result of suppression of the intestinal microflora, the prothrombin index decreases;
- drugs, during the biotransformation of which para-aminobenzoic acid occurs, oral contraceptives: the effect of these drugs is weakened;
- ethinyl estradiol: increased risk of breakthrough bleeding.
Analogs
Bitsillin-1 analogs are Retarpen, Bitsillin-3, Bitsillin-5, etc.
Terms and conditions of storage
Store out of the reach of children, protected from moisture penetration, at a temperature not exceeding 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Bitsillin-1
According to a few reviews, Bicillin-1 in most cases has demonstrated a good result in the treatment of infections caused by bacteria sensitive to the drug. However, according to some doctors, it should also be borne in mind that many microorganisms have already developed immunity to the drug. Bicillin-1 is recommended to be used only as directed by a specialized specialist, as well as in combination with taking pro- and prebiotics.
The disadvantages of patients mainly include pain in / m injections and the appearance of adverse reactions.
Price for Bitsillin-1 in pharmacies
There is no reliable information on the price of Bitsillin-1, since the drug is currently not available in the pharmacy network.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
