From Big Medical Encyclopedia

BICILLINUM (Bicillinum-1, joint venture. B; Bicillinum-1; synonym: Benzathine penicillin, Benzethacil, Duapen, Duropenin, Neolin, Permapen, Retarpen, Tardocillin) — the antibiotic of group of penicillin possessing the prolonged action. Ν,Ν1-дибензилэтилендиаминовая salt of benzylpenicillin, C 48 H 64 O 12 N 6 S 2 . B. it is received in 1951 at interaction of two molecules of potassium salt of benzylpenicillin and one molecule two-uksusnokisl oho N, N1-dibenziletilendiamina.

Bicillinum — inodorous thin white crystal powder and taste. Let's badly dissolve in water, it is alcohol-soluble, formamide, pyridine, ethylene glycol; it is insoluble on air. During the mixing with water forms thin resistant suspension. For definition biol, B.'s activities originally dissolve in formamide or dimethyl formamide. Biol, B.'s activity is defined in terms of effect of benzylpenicillin. Theoretical activity of B. is equal to 1307 PIECES/mg. B. at effect of acids, alkalis, hydroxylamine and enzyme is inactivated penicillinases (see). On a range of antibacterial action it is similar to other drugs of benzylpenicillin (see. Penicillin ). But B.'s toxicity it is similar to novocainic salt of benzylpenicillin. LD 50 Bicillinum at intraperitoneal introduction to white mice makes 460 mg/kg. At peroral introduction to white mice the dose of 4 g/kg is well transferred. Possesses mestnoanesteziruyushchy action. Does not collapse salt to - that a stomach in this connection in the first years after implementation in medical practice it was applied not only intramusculary, but also per os.

The prolonged B.'s action is caused by its bad solubility in water owing to what in an injection site the depot of drug is created, from to-rogo it is slowly soaked up in blood. After intramuscular introduction of B. the maximum concentration of benzylpenicillin in blood is 15 times lower, than after administration of novocainic salt, and 30 times below, than after administration of sodium salt of benzylpenicillin, however its advantage consists that it remains in blood for a long time. So, therapeutic concentration remains in blood after single intramuscular introduction of B. in a dose of 300 000 PIECES about a week, 600 000 PIECES — apprx. 2 weeks, 1 200 000 PIECES — apprx. 3 weeks. Increase in a dose of B. affects, first of all, duration of its circulation in an organism, but not at the level of benzylpenicillin in blood. For creation of higher concentration of benzylpenicillin in blood use the combined drugs B. with potassium (or sodium) and novocainic salt of benzylpenicillin.

Bicillinum-2 represents mix of three parts of B. and one part of potassium or sodium salt of benzylpenicillin. Bntsillin-3 — mix of equal parts B., potassium or sodium salt of benzylpenicillin and novocainic salt of benzylpenicillin. Bicillinum-5 — mix of four parts B. and one part of novocainic salt of benzylpenicillin. Bicillinum-6 — mix of three parts B., one part potassium and two parts of novocainic salt of benzylpenicillin. All listed combined drugs B. of a malotoksichna, are identical but to an antibacterial range, are stable at storage.

For to lay down. the purposes the industry Bicillinum-1, Bicillinum-3 and Bicillinum-5 are issued.

Bicillinum-1 is released in bottles on 300 000, 600 000, 1 200 000 and 2 400 000 PIECES. Bicillinum-3 — on 300 000, 600 000, 900 000 and 1 200 000 PIECES and Bicillinum-5 — on 1 500 000 PIECES. Keep with precaution at the room temperature.

B. appoint use of Bicillinum in clinic on condition of sensitivity of an infestant to benzylpenicillin. B. apply at the same indications, as benzylpenicillin, but it is especially reasonable to apply it to prevention and treatment of rheumatism, to treatment of syphilis, it is long the current infectious diseases, for prevention of infectious complications after some surgeries. Treatment and prevention of rheumatism and treatment of all stages of syphilis is carried out according to special schemes. At treatment of scarlet fever of B. it is so effective, as well as penicillin.

Bicillinum-1 is appointed by the adult in a dose of 300 000 — 600 000 PIECES once a week or in a dose of 1 200 000 PIECES by two times a month. To children Bicillinum-1 two times a month enter in a dose 5000 — 10 000 PIECES on 1 kg of weight once a week or in a dose of 20 000 PIECES on 1 kg of weight.

Bicillinum-3 is appointed the adult in a dose of 300 000 PIECES once in 3 days { the next injection to the fourth days after previous) or in a dose of 600 000 PIECES once in 6 — 7 days.

At treatment of syphilis of a dose of Bicillinum-3 increase up to 900 000 — 1 200 000 PIECES.

The greatest distribution was gained by two techniques of prevention of a recurrence of rheumatism: seasonal and year-round. At the first Bicillinum-1 is entered intramusculary on 600 000 PIECES with week intervals or on 1 200 000 PIECES once into 3 weeks; duration of a course — 6 weeks.

Apply Bicillinum-5 in a single dose of 1 500 000 PIECES with four-week intervals within a year to year-round prevention.

Bicillinum-5 the adult is entered once into 4 weeks, to children of preschool age — on 600 000 PIECES once into 3 weeks, to children 8 years — 1 200 000 PIECES once in 4 weeks are more senior.

Therapeutic concentration of penicillin for impact on a beta and hemolitic streptococcus of group A makes 0,025 PIECES/ml, and the stated above B.'s doses provide during the specified time slices concentration in blood it is not lower than 0,03 PIECES/ml. Regular use of B. promotes decrease in a vysevayemost of a streptococcus, and also reduction of indicators of a streptococcal sensitization (according to dynamics of credits of antistreptococcal antibodies). The question of B.'s use for the purpose of primary prevention of rheumatism is in recent years developed.

At acute and an aggravation hron, streptococcal infections (first of all tonsillitis) treatment by penicillin with single introduction at the end of a course B. for long maintenance of concentration of penicillin in an organism and final elimination of an infection is more shown.

B. enter only intramusculary. Suspension B. is prepared sterilely before the use. With an antibiotic enter 2 — 3 ml into a bottle sterile diets, water for injections or isotonic solution of sodium chloride. The homogeneous suspension received after hashing is entered deeply into an upper outside quadrant of a buttock, previously having convinced that the needle did not get to a blood vessel.

Fears concerning oppression of factors of natural immunity at long introduction of B. were exaggerated.

Contraindications to use of drugs B. are: hypersensitivity to benzylpenicillin and other medicines, including to antibiotics, streptocides, novocaine, allergic diseases (bronchial asthma, a small tortoiseshell, hay fever, etc.), severe forms of an idiopathic hypertensia, postinfarction conditions, diseases of closed glands and the hemopoietic system, serious illnesses of c. N of page. By-effects are same, as at use of drugs of penicillin.

During the performing prevention of a recurrence of rheumatism allergic reactions occur at children and adults in 2 — 8% of cases, including heavy — in 0,3%. For the prevention of medicinal reaction it is very important to find out portability of drug the patient earlier.

See also - Penicillin

Bibliography: Bochorishvili V. G. and d river. Comparative assessment of therapeutic effect of Bicillinum and penicillin at treatment of patients with scarlet fever, Pediatrics, No. 1, page 13, 1970; Dyurantny drugs of penicillin, under the editorship of G. E. Vladimirov, D., 1955, bibliogr.; Ermolyeva 3. B. Antibiotics, interferon, bacterial polysaccharides, M., 1968; Ermolyeva 3. Century, etc. Bicillinum (N, R-dibenziletilendiaminovaya salt of penicillin), Antibiotics, t. 1, J4» 1, page 37, 1956, bibliogr.; Labinsk A. S. and d the ruble Immuno-mikrobiolognchesky indicators at patients with rheumatism at a seasonal bitsillinoprofilaktika, Rubbed. arkh., t. 42, No. 2, page 50, 1970; Mashkovsky M. D. Pharmaceuticals, p. 2, page 258, M., 1972; Navashin S. M. and Fomina I. P. Spranochnik on antibiotics, M., 1974; Nesterov A. I. About theoretical, clinical and methodical aspects of early diagnosis and prevention of rheumatism, Vopr, revmat., No. 1, page 3, 1969; S z a b about J. L., Edwards C. D. a. Bruce W. F. N, N1-dibenzylethylenediamine penicillin, Ant-ibiot. et Chemother. (Basel), v. 1, p. 499, 1951.

L. B. Goldberg, B. A. Nasonova.