Bitsillin-5 powder d / prig.susp. d / v / m introduction 1500000ED, No. 1

Inflammatory diseases caused by sensitive pathogens:

-Long-term (year-round) prevention of recurrence of rheumatism;

-syphilis, yaws;

- streptococcal infections (excluding infections caused by group B streptococci) - acute tonsillitis, scarlet fever, wound infections, erysipelas.

Intramuscularly.

Adults 1.2 million units + 300 thousand units 1 time in 4 weeks. Children of preschool age - 480 thousand units + 120 thousand units once every 3 weeks, children over 8 years old - 960 thousand units + 240 thousand units once every 4 weeks.

To prepare the suspension, use sterile water d / i, isotonic sodium chloride solution or 0.25-0.5% solution of procaine (novocaine).

Suspension BicillinЃ-5 is prepared aseptically, immediately before use (ex tempore): 5-6 ml of solvent is slowly introduced into the vial with the drug under pressure (at a rate of 5 ml in 20-25 seconds). The contents of the vial are mixed and shaken along the longitudinal axis of the vial until a homogeneous suspension is formed.

The presence of bubbles on the surface of the suspension at the walls of the bottle is allowed. Suspension BicillinЃ-5 is injected deep intramuscularly into the upper outer quadrant of the gluteus muscle immediately after preparation. Rubbing the gluteus maximus muscle after injection is not recommended. If the introduction is delayed immediately after preparation, the physical and colloidal properties of the suspension change, as a result of which its movement through the syringe needle may be impeded.

Powder for preparing a suspension for intramuscular administration is white or white with a slightly yellowish tinge, prone to clumping, forming a stable suspension when water is added.

1 fl.

benzathine benzylpenicillin 1.2 million units

benzylpenicillin novocaine salt (benzylpenicillin procaine) 300 thousand units

• Hypersensitivity to the drug, benzylpenicillin and other beta-lactam antibiotics;

• lactation period.

• With care: pregnancy, renal failure, aggravated allergic anamnesis, bronchial asthma, pseudomembranous colitis.

pharmachologic effect

Combined bactericidal antibiotic consisting of two long-acting benzylpenicillin salts. Suppresses the synthesis of the cell wall of the microorganism. Active against gram-positive microorganisms: Staphylococcus spp. (non-forming penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming rods, Bacillus anthracis, Clostridium spp., Actinomyces israelii; gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Treponema spp. Strains of Staphylococcus spp., Producing penicillinase, are resistant to the action of the drug.

Pharmacokinetics

BicillinЃ-5 is a long-acting drug, a high concentration of antibiotic in the blood lasts up to 4 weeks. Benzathine benzylpenicillin After an intramuscular injection of benzathine, benzylpenicillin is very slowly hydrolyzed, releasing benzylpenicillin. The maximum concentration of the drug in the blood serum is reached 12-24 hours after injection. The long half-life provides a stable and long-term concentration of the drug in the blood: on the 14th day after the excretion of 2,400,000 IU of the drug, the serum concentration is 0.12 ?g / ml; on the 21st day after the injection of 1200000 IU of the drug - 0.06 ?g / ml (1 IU = 0.6 ?g). Diffusion of the drug in the liquid is complete, diffusion in the tissue is very weak. Communication with plasma proteins 40-60%. Benzathine benzylpenicillin passes in small amounts across the placental barrier,and also passes into the mother's breast milk. The biotransformation of the drug is insignificant. It is excreted mainly by the kidneys unchanged. For 8 days, up to 33% of the administered dose is released. Benzylpenicillin The maximum concentration in blood plasma with intramuscular administration is achieved after 20-30 minutes. The half-life of the drug is 30-60 minutes, with renal failure 4-10 hours or more. Communication with plasma proteins - 60%. Penetrates into organs, tissues and biological fluids, except for cerebrospinal fluid, eye tissue and prostate gland. With inflammation of the meningeal membranes, it penetrates the blood-brain barrier. Passes through the placenta and enters breast milk. Excreted by the kidneys unchanged.For 8 days, up to 33% of the administered dose is released. Benzylpenicillin The maximum concentration in blood plasma with intramuscular administration is achieved after 20-30 minutes. The half-life of the drug is 30-60 minutes, with renal failure 4-10 hours or more. Communication with plasma proteins - 60%. Penetrates into organs, tissues and biological fluids, except for cerebrospinal fluid, eye tissue and prostate gland. With inflammation of the meningeal membranes, it penetrates the blood-brain barrier. Passes through the placenta and enters breast milk. Excreted by the kidneys unchanged.For 8 days, up to 33% of the administered dose is released. Benzylpenicillin The maximum concentration in blood plasma with intramuscular administration is achieved after 20-30 minutes. The half-life of the drug is 30-60 minutes, with renal failure 4-10 hours or more. Communication with plasma proteins - 60%. Penetrates into organs, tissues and biological fluids, except for cerebrospinal fluid, eye tissue and prostate gland. With inflammation of the meningeal membranes, it penetrates the blood-brain barrier. Passes through the placenta and enters breast milk. Excreted by the kidneys unchanged.tissues and biological fluids, except for cerebrospinal fluid, eye and prostate tissues. With inflammation of the meningeal membranes, it penetrates the blood-brain barrier. Passes through the placenta and enters breast milk. Excreted by the kidneys unchanged.tissues and biological fluids, except for cerebrospinal fluid, eye and prostate tissues. With inflammation of the meningeal membranes, it penetrates the blood-brain barrier. Passes through the placenta and enters breast milk. Excreted by the kidneys unchanged.

Side effect

Allergic reactions: anaphylactic shock, anaphylactoid reactions, urticaria, fever, arthralgia, angioedema, exudative erythema multiforme, exfoliative dermatitis. Laboratory indicators: anemia, thrombocytopenia, leukopenia, hypocoagulation. Others: stomatitis, glossitis.

Application during pregnancy and lactation BitsillinЃ-5

in small quantities, it penetrates the placental barrier and into the mother's milk. Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. It is recommended that breastfeeding be discontinued if the drug is prescribed.

Application for impaired renal function

With caution in renal failure.

Application in children

Apply according to indications

special instructions

Cannot be administered subcutaneously, intravenously, endolumbar, and also in the body cavity. Inadvertent intravascular administration may result in a transient feeling of depression, anxiety, and visual impairment (Wanier syndrome). In order to avoid accidental intravascular injection of the drug, it is recommended to aspirate before intramuscular injection in order to identify possible needle penetration into the vessel. When treating syphilis, microscopic and serological examinations are necessary before starting therapy and then within 4 months. In connection with the development of fungal infections, it is advisable to simultaneously prescribe B vitamins and vitamin C, and, if necessary, antifungal drugs for systemic use. Should be considered,that the use of insufficient doses or too early discontinuation of treatment often leads to the emergence of resistant strains of pathogens.

Drug interactions

Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic. Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the prothrombin index); reduces the effectiveness of oral contraceptives, drugs, in the process of metabolism of which para-aminobenzoic acid is formed, ethinylestradiol - the risk of bleeding 'breakthrough'. Diuretics, allopurinol, tubular secretion blockers, phenylbutazone, NSAIDs, by reducing tubular secretion, increase the concentration of benzylpenicillin in the blood and tissues. Allopurinol increases the risk of developing allergic reactions (skin rash).