Pharmacological properties : Benzathine penicillin G is a beta-lactam antibiotic of the penicillin group of type G prolonged action. In the microbial cell bactericidal effect. It is characterized by prolonged action. It inhibits synthesis of cell walls of microorganisms. It is active against gram-positive pathogens: Staphylococcus spp. (penitsillinazoneobrazuyuschih), Streptococcus spp., including Streptococcus pneumoniae, Corynebacterium diphtheriae, anaerobic spore-forming rods, Bacillus anthracis, Clostridium spp, Actinomyces israelii.; Gram-negative organisms: Neisseria gonorrhoeae, Neisseria meningitidis, as well as against Treponema spp. By the action of the drug-resistant strains of Staphylococcus spp., Producing penicillinase, destroys testosterone enanthate.
After intramuscular administration is slowly hydrolyzed with release of penicillin. The time to reach maximum plasma concentration – 12-24 h after injection. On day 14 after administration of 2400000 IU plasma concentration is 0.12 micrograms / ml; 21 days after the administration of U 1200000 – 0.06 mg / ml. Penetration into liquid high in the tissue – is low. It overcomes the placental barrier and passes into breast milk. Relationship to plasma proteins – 40-60%. Is metabolized slightly, is derived mainly kidneys unchanged. For 8 days allocated to 33% of the administered dose.
Treatment of infections caused by susceptible microorganisms: syphilis (monotherapy), yaws, pint; acute tonsillitis, scarlet fever.
Prevention of infections caused by susceptible organisms: after repeated attacks of acute rheumatic fever, recurrent erysipelas, wound infection, infection in tonsillectomy or after tooth extraction.
Hypersensitivity (including to other beta-lactam antibiotics). Precautions : complicated by allergoanamnez, pseudomembranous colitis, chronic renal failure.
Pregnancy and lactation
Use in pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus.
It is recommended to stop breast-feeding if necessary, the appointment of the drug.
DOSAGE AND ADMINISTRATION
Inject by intramuscular injection only, can not be administered intravenously!
When the need for two injections do them in different buttocks. The drug is injected deep into the upper outer quadrant of the gluteus maximus. When the appearance of blood in the syringe, a needle indicating a hit in a vessel and should be removed to produce an injection syringe to another location.
A suspension formulation was prepared under aseptic conditions immediately prior to use. Water is introduced into a vial for injection or 0.9% sodium chloride solution at 1 ml of 5: 2 ml to 0.6 million IU dosages, 4 ml – 1.2 million units and 8 ml – to 2.4 million units. The mixture was stirred until a uniform slurry rapidly rotating bottle between your hands for at least a minute or gently shaking the vial in the direction of its longitudinal axis within 30 seconds. Presence of bubbles on the surface of the slurry in the vial walls.
Treatment of syphilis in adults and children 2-12 years old: primary seronegative syphilis -2.4 million units once; primary seropositive – 2.4 million units with an interval of 7 days, the course – 2 injection;secondary and early latent syphilis, late (tertiary and neurosyphilis) – 2.4 million units with an interval of 7 days, the course – 3 injections. Congenital syphilis in children under 2 years of age, born to untreated infected mothers – 50 thousand units / kg of body weight (dose is divided in half and inserted into different buttock) with an interval of 7 days, the course – 3 injections.; preventive treatment of children with insufficient treatment of the mother or serorezistentnosti -. 50 thousand units / kg of body weight (dose is divided in half and inserted into different buttock) with an interval of 7 days, the course – 2 injections.
Treatment of yaws and a pint: children – 1.2 million units once; adults – 2.4 million units once.
Treatment of acute tonsillitis, scarlet fever, wound infection: children up to 12 years for 0.6 million units every 3 days, or 1.2 million units every 2-4 weeks depending on the severity of the infection; adults – at 1.2-2.4 million IU 1 time per week.
Prevention of recurrent attacks after acute rheumatic fever: children weighing up to 25 kg – 0.6 million units 1, every 3 weeks, more than 25 kg – 1.2 million units 1 every 3 weeks; adults and children over 12 years – 2.4 million units 1 every 3 weeks.
Prevention of relapse faces: children – by 0.6 million units 1 every 2 weeks or 1.2 million units every 3-4 weeks; adults with seasonal recurrences – 2.4 million units 1 to 4 times a week for 3-4 months each year, with frequent relapses – 2.4 million units 1 every 3-4 weeks for 2-3 years.
Prevention of infections after tonsillectomy or tooth extraction: children – by 0.6 million units or 1.2 million units, adults – 2.4 million units every 7-14 days until complete recovery.
In chronic renal failure in creatinine clearance (CC) 10-50 ml / min – 75% of the daily dose, CC less testosterone enanthate than 10 ml / min – 25-50% of the daily dose.
SIDE EFFECTS : Allergic reactions : anaphylactic shock, anaphylactoid reactions, urticaria, fever, eosinophilia, arthralgia, angioedema, erythema multiforme exudative, exfoliative dermatitis, difficulty breathing, anaphylaxis. In the treatment of syphilis due to the release of toxins may develop Jarisch-Herxheimer. From the side of hematopoiesis : hemolytic anemia, thrombocytopenia, leukopenia. From the digestive system : stomatitis, glossitis, nausea, vomiting, diarrhea, candidiasis, pseudomembranous colitis, mild transient increase in activity of “liver” transaminases. Other : interstitial nephritis. In the long-term treatment – superinfection of resistant microorganisms and mushrooms; at high doses, especially with concurrent chronic renal failure, may develop encephalopathy (disturbance of consciousness, seizures, movement disorders). Local infusion reactions (more children) : infections of the injection site, inflammation, swelling, abscess, edema, hemorrhage , inflammation of the subcutaneous tissue, necrosis, atrophy, ecchymosis, skin ulceration.
If overdose possible substantial muscle twitching or convulsions.
Treatment is symptomatic.
INTERACTION WITH OTHER DRUGS
bactericidal antibiotics (including cephalosporin, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) – antagonistic,
increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reducing prothrombin index); reduces the effectiveness of oral contraceptives, medicines, in the process of metabolism that produce para-aminobenzoic acid, ethinylestradiol -. risk of bleeding “breakthrough”
Diuretics, allopurinol, blockers of tubular secretion, phenylbutazone, nonsteroidal anti-inflammatory drugs reduce the tubular secretion, increase the concentration of penicillin. Allopurinol increases the risk of allergic reactions (skin rash).
When any allergic reaction, immediate discontinuation of treatment is needed.
You can not be administered subcutaneously, intravenously, endolyumbalno, as well as in the body cavity. Accidental intravascular administration may experience a transient feeling of depression, anxiety, and visual impairment (Oigney syndrome). In order to avoid accidental intravascular administration is recommended prior to intramuscular injection aspirate to identify possible contamination of the needle into the vessel.
In the treatment of syphilis before treatment and then for 4 months is necessary to conduct microscopic and serological studies.
In connection with the possibility of fungal lesions in the treatment of testosterone enanthate advisable to appoint B vitamins, and if necessary -protivogribkovye infectives for systemic use.
Please note that use of the drug in inadequate dosages or discontinuation of treatment too early often leads to the emergence of resistant strains of pathogens