pharmachologic effect
A combined antibacterial drug of the penicillin group of prolonged action, destroyed by penicillinase. The mechanism of action is based on disruption of the synthesis of peptidoglycan, a mucopeptide of the cell wall, which leads to inhibition of the synthesis of the cell wall of the microorganism, suppression of the growth and reproduction of bacteria. Active against gram-positive bacteria: Staphylococcus spp. (non-penicillinase-forming), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, Bacillus anthracis; gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Actinomyces israelii. The drug is also active against Treponema spp., anaerobic spore-forming bacilli, and Leishmania. Staphylococcus spp., which produce penicillinase, are resistant to the drug.
Bicillin®-5 (Bicillin-5)
Manufacturer: SYNTHEZ OJSC (Russia)
lyophilisate for preparation. susp. intramuscular injection 1.2 million units + 300 thousand units: vial. 1, 5, 10 or 50 pcs. Reg. No.: LS-000082
Clinical and pharmacological group:
Antibiotic of the penicillin group, destroyed by penicillinase
Release form, composition and packaging
Lyophilisate for preparing a suspension for intramuscular administration
white, odorless, bitter taste, forming a homogeneous suspension of milky turbidity when adding water, 0.9% sodium chloride solution or 0.25%-0.5% novocaine solution; with prolonged contact with water or other above-mentioned solutions, the physical and colloidal properties of the drug change, as a result of which the suspension becomes uneven and difficult to pass through the syringe needle.
| 1 fl. | |
| benzathine benzylpenicillin | 1.2 million IU |
| benzylpenicillin novocaine salt | 300 thousand units |
Bottles with a volume of 10 ml (1) - cardboard packs. 10 ml bottles (5) - cardboard packs. Bottles with a volume of 10 ml (10) - cardboard packs. 10 ml bottles (50) - cardboard boxes.
Description of the active components of the drug "Bicillin®-5"
pharmachologic effect
Antibiotic of the penicillin group of prolonged action, destroyed by penicillinase. The mechanism of action is based on disruption of the synthesis of peptidoglycan, a mucopeptide of the cell wall, which leads to inhibition of the synthesis of the cell wall of the microorganism, suppression of the growth and reproduction of bacteria. Active regarding
gram-positive bacteria: Staphylococcus spp.
(non-penicillinase-forming), Streptococcus spp. (including Streptococcus pneumoniae), as well as Corynebacterium diphtheriae, Bacillus anthracis.
Viruses, rickettsia, fungi, protozoa, and most gram-negative bacteria are resistant to the drug The drug has a prolonged effect.
Indications
- treatment of infectious diseases caused by pathogens sensitive to penicillin (especially in cases where it is necessary to create a long-term therapeutic concentration in the blood);
- year-round prevention of rheumatism in adults and children.
Dosage regimen
More frequent administration of the drug than indicated in the dosage regimen is not allowed. For adults
the drug is prescribed in a dose of 1.5 million units once every 4 weeks.
For preschool children
the drug is prescribed at a dose of 600,000 units once every 3 weeks,
for children over 8 years old
1.2-1.5 million units once every 4 weeks.
Rules for preparing and administering the solution
Bicillin-5 suspension is prepared immediately before use. 5-6 ml of sterile water for injection, or 0.9% sodium chloride solution, or 0.25-0.5% novocaine solution is injected into the bottle with the drug. The mixture in the bottle is mixed (by rotating the bottle between the palms) until a homogeneous suspension (or suspension) is formed, which is injected immediately deep into the upper outer quadrant of the buttock. Rubbing the buttock after the injection is not recommended.
Side effect
Allergic reactions:
headache, fever, urticaria, rash on the skin and mucous membranes, arthralgia, eosinophilia, angioedema.
Cases of anaphylactic shock with fatal outcome have been described. Local reactions:
possible pain at the injection site.
Contraindications
- bronchial asthma;
- urticaria;
- hay fever;
- hypersensitivity to penicillins.
Pregnancy and lactation
Data on the use of Bicillin-5 during pregnancy and lactation (breastfeeding) are not provided.
Application for children
For preschool children
the drug is prescribed in a dose of 600,000 units once every 3 weeks,
for children over 8 years old
1.2-1.5 million units once every 4 weeks.
special instructions
Bicillin-5 can only be used in cases where it is known that the patient does not have hypersensitivity reactions to penicillin, because the drug ensures a constant flow of penicillin into the blood for a long time.
Patients who have experienced reactions unusual for the drug should be under constant medical supervision until the side effects completely disappear. In severe cases, appropriate therapy is prescribed (atropine 0.1% 0.5-0.6 ml, epinephrine 0.1% 1 ml, ephedrine 5% 1 ml, caffeine sodium benzoate 10%, ammonia).
Overdose
Currently, no cases of overdose of Bicillin-5 have been reported.
Drug interactions
Drug interactions with Bicillin-5 have not been described.
Storage conditions and periods
List B. The drug should be stored in a cool, dry place at a temperature not exceeding 20°C. Shelf life: 3 years. Conditions for dispensing from pharmacies
The drug is available with a prescription.
Drug interactions
Drug interactions with Bicillin-5 have not been described.
Pharmacokinetics
Suction
With a single administration, it remains in an average therapeutic concentration for 6-7 days. Cmax in blood plasma is achieved 12-24 hours after administration.
After administration of Bicillin-3 at a dose of 2.4 million units, the concentration in the blood serum on day 14 is 0.12 mcg/ml; after administration of Bicillin-3 at a dose of 1.2 million units, the concentration in the blood serum on day 21 is 0.06 mcg/ml.
Distribution and metabolism
After intramuscular administration, it is slowly hydrolyzed to release benzylpenicillin.
Slightly undergoes biotransformation.
Binding to blood plasma proteins is 40-60%. Passes through the placental barrier and enters breast milk.
It is well distributed in liquids, while the distribution in tissues is low.
Removal
It is excreted primarily by the kidneys.
Bicillin-5 1,500,000 units powder for the preparation of a suspension for intramuscular administration
Bicillin-5 1500000 units for injection
Bicillin-5 is an antibiotic (biosynthetic penicillin).
Release form and composition
The drug is produced in the form of a powder for the preparation of a suspension for intramuscular administration: a white or white with a yellowish tint, a powdery mass prone to clumping, with the addition of water it forms a stable suspension (10 ml in bottles; in a cardboard pack 1, 5, 10 or 50 bottles) .
Powder composition (per 1 bottle):
benzylpenicillin procaine (benzylpenicillin novocaine salt) – 300,000 units; benzathine benzylpenicillin – 1,200,000 units. Pharmacological properties Pharmacodynamics Bicillin-5 is a bactericidal combination antibiotic containing two long-acting benzylpenicillin salts. Inhibits the synthesis of the cell wall of pathogenic microorganisms. Active against the following microbes: gram-positive: Streptococcus spp. (including Streptococcus pneumoniae), Staphylococcus spp. (non-penicillinase-forming), Bacillus anthracis, Clostridium spp., Corynebacterium diphtheriae, anaerobic spore-forming rods, Actinomyces israelii; gram-negative: Treponema spp., Neisseria gonorrhoeae, Neisseria meningitidis. Penicillinase-producing strains of Staphylococcus spp. are resistant to the drug. Pharmacokinetics Bicillin-5 is a long-acting antibiotic; its high concentration in the blood persists for 4 weeks. Benzathine benzylpenicillin hydrolyzes very slowly after intramuscular injection, releasing benzylpenicillin. The maximum concentration (Cmax) in the blood serum is achieved 12–24 hours after administration. The long half-life ensures a long and stable concentration of the drug in the blood: on the 14th day after injection of 2,400,000 IU, the drug concentration in serum is 0.12 μg/ml; on the 21st day after administration - 1,200,000 IU, the concentration is 0.06 μg/ml (1 IU = 0.6 μg). Diffusion of the substance in tissue is very weak, in liquid it is complete. Plasma protein binding is 40–60%. Benzathine benzylpenicillin passes in small volumes through the placental barrier and also passes into breast milk. Biotransformation is insignificant, mainly excreted unchanged by the kidneys, up to 33% of the administered dose is excreted in 8 days. Benzylpenicillin reaches its maximum concentration in blood plasma when administered intramuscularly after 20–30 minutes. The half-life is 0.5–1 hour; in the presence of renal failure, this figure increases to 4–10 hours or more. Plasma protein binding ~ 60%. The substance penetrates into tissues, organs and biological fluids, except for eye tissue, cerebrospinal fluid and prostate gland. Passes through the blood-brain barrier during inflammation of the meningeal membranes. Penetrates the placenta and enters breast milk. It is excreted unchanged by the kidneys.
Indications for use Bicillin-5
used for the treatment of the following infectious and inflammatory diseases/conditions provoked by pathogens sensitive to the drug: rheumatism - for year-round long-term prevention of relapses; syphilis; yaws; streptococcal infections (except for infections caused by group B streptococci) - scarlet fever, acute tonsillitis, erysipelas, wound infections.
Absolute contraindications:
breastfeeding period; hypersensitivity to any components of the drug and other beta-lactam antibiotics. Relative: bronchial asthma; burdened allergy history; pregnancy; renal failure; pseudomembranous colitis. Instructions for use of Bicillin-5: method and dosage A suspension prepared from powder is administered intramuscularly (i.m.). Recommended dosages of Bicillin-5: children under 8 years of age: 480,000 units + 120,000 units once every 3 weeks; children over 8 years old: 960,000 units + 240,000 units once every 4 weeks; adults: 1,200,000 units + 300,000 units once every 4 weeks. When preparing the suspension, it is recommended to use a 0.25–0.5% solution of novocaine (procaine), isotonic sodium chloride solution or sterile water for injection. The suspension is prepared under aseptic conditions, immediately before use (ex tempore): 5-6 ml of solvent is slowly introduced into a bottle with Bicillin-5 under pressure (at a rate of 5 ml in 20-25 seconds). The contents are mixed and shaken along the longitudinal axis of the bottle until a homogeneous suspension is formed. There may be bubbles near the walls of the bottle on the surface of the suspension. The finished drug must be injected deep intramuscularly into the upper outer quadrant of the gluteal muscle immediately after preparation. It is not recommended to rub the gluteal muscle after the injection. If administration is delayed after preparation, the colloidal and physical properties of the suspension change, as a result of which its movement through the syringe needle may be difficult. Side effects: allergic reactions: anaphylactoid reactions, fever, urticaria, angioedema, arthralgia, exfoliative dermatitis, exudative erythema multiforme, anaphylactic shock; laboratory parameters: leukopenia, thrombocytopenia, anemia, hypocoagulation; others: glossitis, stomatitis. Overdose There is no information about overdose. Special instructions Intravenous, endolumbar and subcutaneous administration of the suspension, as well as injections into body cavities, are not allowed. With unintentional intravascular administration, a transient feeling of anxiety, depression and visual disturbances (Wanier syndrome) may occur. To avoid inadvertent intravascular injection of the drug, aspiration should be performed before intramuscular injection in order to identify possible needle entry into the vessel. When treating syphilis, serological and microscopic studies should be carried out before starting treatment and for 4 months. Due to the development of fungal infections, it is advisable to prescribe vitamin C and B vitamins at a time, and if necessary, prescribe antifungal agents for systemic use. It is important to consider that stopping therapy too early or using an insufficient dosage of Bicillin-5 can lead to the emergence of resistant strains of pathogens.
Use during pregnancy and lactation
According to the instructions, Bicillin-5 penetrates into mother's milk and through the placental barrier in small quantities. Its use during pregnancy is allowed only when the expected benefit to the mother outweighs the potential risk to the fetus. If it is necessary to prescribe the drug during lactation, breastfeeding should be discontinued.
Drug interactions: bactericidal antimicrobial drugs, including vancomycin, cephalosporins, aminoglycosides, rifampicin: have a synergistic effect; bacteriostatic antimicrobial drugs, including chloramphenicol, macrolides, tetracyclines, lincosamides: have an antagonistic effect; indirect anticoagulants: their effectiveness increases due to the inhibition of intestinal microflora and a decrease in the prothrombin index; oral contraceptives, drugs whose metabolism occurs with the formation of para-aminobenzoic acid, ethinyl estradiol: the antibiotic reduces their effectiveness, increasing the risk of breakthrough bleeding; blockers of tubular secretion, diuretics, allopurinol, non-steroidal anti-inflammatory drugs, phenylbutazone: reduce tubular secretion, increase the concentration of benzylpenicillin in tissues and blood; allopurinol: increases the risk of allergic reactions such as skin rash. Analogues Analogues of Bicillin-5 are: Benzylpenicillin, Benzylpenicillin sodium salt, Benzylpenicillin sodium salt-Vial, Benzylpenicillin novocaine salt.
Terms and conditions of storage
Store at a temperature not exceeding 25 °C.
Shelf life – 3 years.
Conditions for dispensing from pharmacies
Dispensed by prescription.
Dosage
Bicillin-3 is injected deep into the upper outer quadrant of the buttock in a dose of no more than 1.2 million units. If 2 injections are necessary, they are given in different buttocks. Repeated injections are carried out 4 days after the previous injection. The drug in a dose of 600,000 units is administered once every 6 days. In the treatment of primary and secondary syphilis, a single dose of the drug 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 (1.8 million units). 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. Intravenous administration of the drug is prohibited. Rules for preparing and administering the solution Bicillin-3 suspension is prepared immediately before use. 2-3 ml of sterile water for injection or isotonic sodium chloride solution is injected into the bottle with the drug. The mixture in the bottle is shaken for 30 seconds (in the direction of the longitudinal axis) until a homogeneous suspension (or suspension) is formed, which is injected deep intramuscularly into the upper outer quadrant of the buttock. Rubbing the buttock after the injection is not recommended.
Side effects of the drug Bicillin-5
Some patients, especially those with hypersensitivity to penicillins and procaine, experience headache, fever, urticaria, rash on the skin and mucous membranes, joint pain, eosinophilia, angioedema, anaphylactic shock and other allergic reactions. After injection of the drug (like other long-acting penicillin preparations), pain at the injection site is possible. Patients who have experienced unusual reactions to the drug should be under constant and direct medical supervision until the reactive phenomena completely disappear. In severe cases, 0.5–0.6 ml of 0.1% atropine solution is administered, injections of 1 ml of 0.1% epinephrine solution or 1 ml of 5% ephedrine solution, injection of 1–2 ml of 2% solution -ra chloropyramine.
Drug interactions
When used simultaneously with bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides), a synergistic effect is observed; with bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonism.
Bicillin-3 reduces the effectiveness of oral contraceptives and ethinyl estradiol (risk of breakthrough bleeding).
With the simultaneous use of Bicillin-3 with allopurinol, the risk of developing allergic reactions increases.
Pharmacokinetic interaction
With simultaneous use of diuretics, allopurinol, phenylbutazone, NSAIDs, they reduce tubular secretion and increase the concentration of penicillin.
special instructions
If allergic reactions develop, treatment should be stopped immediately.
With the development of anaphylactic shock, anti-shock therapy is indicated (administration of norepinephrine, corticosteroids, mechanical ventilation).
Intravenous and endolumbar administration is not allowed, because possible development of Wannier syndrome (depression, anxiety, paresthesia, visual impairment).
When treating sexually transmitted diseases, if syphilis is suspected, before starting therapy and then for 4 months, microscopic and serological studies are necessary.
In connection with the possible development of fungal infections, it is advisable to prescribe antifungal drugs (nystatin, levorin), as well as ascorbic acid and B vitamins.
It must be taken into account that the use of the drug in insufficient doses or early cessation of treatment leads to the emergence of resistant strains of pathogens.
