TsIKLOSERYN (Cycloserinum; synonym: Oxamycin, Seromycin, etc.) — the antitubercular antibiotic produced by various streptomi-tseta or received by chemical synthesis. D-4-amino-Z-izoksa-zolidinon. A total formula of Cycloserinum C3H6N202, molecular weight (weight) — 102,09
Powder of white color, well water soluble. C. possesses a wide range of antimicrobic action, including nek-ry spirochetes, and also rickettsiae and viruses. Growth of the majority of microorganisms is suppressed at high levels of concentration of an antibiotic (10 — 300 mkg! ml) which are not reached in blood serum at usual schemes of its introduction. Therefore practical value has action of C. on nek-ry microorganisms, hl. obr. on a mycobacterium of tuberculosis (the minimum overwhelming concentration on various environments 3 — 25 mkg! ml and more). C. affects bacteriostatically both on extracellular, and the microorganisms located intracellularly. Mechanism of action of C. it is connected with competitive antagonism of synthesis of D-alanine. Though C. is less active, than other antituberculous remedies, to it stability of mycobacteria develops more slowly. It also has no cross resistance to various tuberkulostatika.
At introduction in C. it is quickly and completely soaked up from went. - kish. a path therefore there is no need for its parenteral administration. The maximum concentration of an antibiotic in blood is created on average in 2 hours and remains within 8 — 10 hour. At prolonged use the cumulation of drug which is not constituting danger to the patient at norkhmalny function of kidneys can be observed. The daily dose of 10 — 20 mg/kg provides therapeutic concentration of C. in blood serum. It well gets into fabrics and liquids, including through a blood-brain barrier; in high concentration drug is found in pulmonary fabric and limf, nodes. C. it is allocated with kidneys in not changed look and comes to light in urine in high concentration.
C. apply at hron. a destructive pulmonary tuberculosis at adult, severe forms of primary and secondary tuberculosis at children, at medicinal resistance of mycobacteria to other antituberculous remedies or their intolerance. C. use at vnele-gochny forms hron. tubercular process, especially at severe forms of tuberculosis of urinogenital system. Lech. effect of C. it is observed at other inflammatory diseases of the bodies of urinogenital system which are not giving in to influence of other germicides. It is applied also at treatment of a leprosy.
At tuberculosis of C. appoint inside 0,25 g 3 times a day to food.
Average daily doses for adult 0,75 g, for persons are more senior than 60 years and is powerful (weighing) less than 50 kg — 0,5 g. To children appoint at the rate of 0,01 — 0,02 g! kg a day (no more than 0,75 g). The highest doses for adults: one-time — 0,25 g, daily — 1 g. For the purpose of definition of portability of drug it is recommended to raise gradually in the first 5 — 7 days a daily dose to optimum and not to combine Cycloserinum with other pharmaceuticals. Further for prevention of development of bacterial resistance to C. and strengthenings of therapeutic action combine it with other antitubercular drugs. At activation of the accompanying microflora at suffering from tuberculosis lungs treatment of C. it is necessary to carry out together with other antibiotics, effective concerning this flora.
Side effect of C. it is shown by a headache, dizziness, sleeplessness or drowsiness, concern, irritability, a memory impairment, a tremor, paresthesias. Occasionally there are disturbances of mentality, epileptiform attacks, etc. In an initiation of treatment temperature sometimes increases, cough amplifies, there is a pneumorrhagia, the quantity of a phlegm increases, rattles and inflammatory changes in lungs amplify. These phenomena usually pass after a break in treatment. Heartbeat and pains are seldom watched a breast, a hypoglycemia, passing anemia. C. has weak allergenic properties. For prevention and weakening of neurotoxic action of C. appoint glutaminic to - that, drugs of rat anti-acrodynia factors, Vkh and B12, ATP, sedative and tranquilizing means, antidepressants.
It is impossible to apply C. in combination with terizidony, an isoniazid (at intravenous jet administration of 10% of solution), with care apply along with corticosteroid hormones. C. it is contraindicated at organic diseases of c. N of page and peripheral nervous system, epilepsy, mental disorders, hron. alcoholism, drug addiction, before an operative measure and in the first week after it. With care persons should appoint it with unstable mentality, at a renal failure, severe forms of a diabetes mellitus.
Form of release: tablets or capsules on 0,25 g
See also Antituberculous remedies.
Bibliography: N and in and sh and S. M. N and F about m and - N and I. P. Rational antibioticotherapia, M., 1982; At t to and N V. V. Tsikloserin in therapy of a pulmonary tuberculosis, M., 1968, bibliogr.
S. M. Navashin, V. V. Utkin.