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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
Nosological classification (ICD-10)
- A38 Scarlet fever
- A46 Erysipelas
- A53.9 Syphilis, unspecified
- A66 Yaws
- B55.9 Leishmaniasis, unspecified
- I00 Rheumatic fever without mention of cardiac involvement
- I01 Rheumatic fever with cardiac involvement
- I05-I09 Chronic rheumatic heart disease
- J03.9 Acute tonsillitis, unspecified (angina agranulocytic)
- M79.0 Rheumatism, unspecified
- N74.2 Inflammatory diseases of the female pelvic organs caused by syphilis (A51.4+, A52.7+)
- T79.3 Post-traumatic wound infection, not elsewhere classified
Indications for use
"Bicillin - 3" is usually prescribed for the treatment of various kinds of infectious diseases that are caused by microorganisms sensitive to the action of the antibiotic.
An antibacterial drug is prescribed for:
- Acute or chronic tonsillitis
- Infection of wound surfaces
- Scarlet fever
- Rheumatoid arthritis and arthrosis
- Sore throat
- Prevention of rheumatism
- Erysipelas
- Syphilis, as well as yaws.
The drug can be used to treat infectious diseases in poultry (including chickens) and cattle.
Composition and release form
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.
Characteristic
Bicillin-1 is a white, odorless or almost odorless powder that forms a stable suspension when water is added.
Bicillin-3 is a white or white powder with a slightly yellowish tint that forms a stable suspension when water is added.
Bicillin-5 is a white, odorless powder with a bitter taste, which forms a homogeneous suspension of milky turbidity when adding water, saline or 0.25–0.5% novocaine solution. 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 syringe needle).
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.
Medicinal properties
The mechanism of action of "Bicillin - 3" is based on inhibition of the growth and reproduction of pathogenic microorganisms: gram-positive, gram-negative and anaerobic. The activity of the drug against pathogens of fungal infections, smallpox, poliomyelitis, influenza and penicillinase has not been detected.
When Bicillin-3 enters the body, hydrolysis occurs with a gradual release of the main active substance. With a one-time administration of the antibiotic, it is possible to maintain its therapeutic concentration for 6-7 days, the highest concentration is observed after 12-24 hours from the injection. The penetration of benzathine benzylpenicillin into physiological fluids is significantly higher than into tissue. The drug crosses the placenta and is detected in breast milk. The medicine is partially transformed and excreted by the genitourinary system.
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.
Interaction
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).
Analogs
"Phenoxymethylpenicillin"
Sintez, Russia Price from 19 to 40 rubles.
"Phenoxymethylpenicillin" is an antibacterial drug of the penicillin group. The drug is used to treat diseases of the oral cavity, skin, and soft tissues of an infectious nature. "Phenoxymethylpenicillin" is available in the form of powder for oral administration and tablets, the active ingredient of the drug is phenoxymethylpenicillin.
Pros:
- Low price
- Good drug tolerance
- Can be prescribed to children.
Minuses:
- Available with prescription
- May provoke the development of superinfection
- An allergy to the main component of the drug is possible.
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.
Bicillin-3
Release form, composition and packaging
The powder for preparing a suspension for intramuscular administration is white or white with a slightly yellowish tint, forming a stable suspension when water is added. 1 fl. a mixture of benzathine benzylpenicillin, benzylpenicillin sodium (or potassium) salt and benzylpenicillin novocaine salt 600 thousand units - "- 1.2 million units
Clinical and pharmacological group: Antibiotic of the penicillin group, destroyed by penicillinase.
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.
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.
Indications
- treatment of infectious diseases caused by penicillin-sensitive pathogens (especially in cases where it is necessary to create a long-term therapeutic concentration in the blood);
- syphilis;
- yaws;
- streptococcal infections (acute tonsillitis, scarlet fever, wound infections, erysipelas), with the exception of infections caused by group B streptococci;
- prevention of rheumatism;
- leishmaniasis.
Dosage regimen
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 effect
Allergic reactions: urticaria, angioedema, erythema multiforme, anaphylactic shock, arthralgia, fever, exfoliative edema.
- From the digestive system: stomatitis, glossitis.
- From the blood coagulation system: anemia, thrombocytopenia, leukopenia, hypocoagulation. Other: with long-term use - superinfection, mycoses.
Contraindications
- hypersensitivity to penicillins and procaine (novocaine);
- bronchial asthma;
- hay fever;
- other allergic diseases.
Pregnancy and lactation
Data on the use of Bicillin-3 during pregnancy and lactation (breastfeeding) are not provided.
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.
Overdose
Currently, no cases of overdose of Bicillin-3 have been reported.
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.
Storage conditions and periods
List B. The drug should be stored in a dry place at a temperature of 8-15°C. Shelf life: 3 years.
Precautionary measures
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.
Treatment for rheumatoid arthritis and arthrosis
"Bicillin - 3" is recommended for use as part of complex therapy for arthritis and arthrosis. The antibiotic helps eliminate the infectious focus, thanks to its prolonged action it is possible to achieve visible treatment results.
The dosage of the drug is selected by the doctor purely individually, taking into account the nature of the disease and the presence of concomitant pathologies. How long treatment will last in a particular case is determined by a specialist, taking into account the therapeutic effectiveness of the drug.
