MEPROTANUM (Meprotanum; synonym: meprobamate, Andaxin, Miltown etc.; joint venture. B, GFH) — tranquilizing means. Dicarbamate of a 2-methyl-2-spilled-pro-pan-diol-1,3; With 9 H 18 N 2 O 4 :
Inodorous white crystal powder or with a slight smell; we will dissolve in water and ether a little, we will easily dissolve in 95% alcohol and acetone. Pier. weight (weight) 218,25; t ° pl 103-107 °.
In experiments on animal M., like other tranquilizers, depending on a dose suppresses aggression, oppresses a spontaneous physical activity and conditioned-reflex activity, breaks coordination of movements, reduces a tone of skeletal muscles. In high doses causes muscle relaxation. Relaxation of skeletal muscles is connected with M.'s influence on c. N of page, in neuromuscular synapses it does not influence momentum transfer. The m warns and eliminates the spasms caused by Corazolum and strychnine, strengthens action of somnolent and analgetic means, reduces standard metabolism and body temperature of animals.
Like barbiturates, M. oppresses paradoxical phasa of a dream. In therapeutic doses does not exert impact on a vegetative innervation; in rare instances causes decrease in the ABP. Respiratory depression is observed only at M.'s introduction in toxic doses.
The m is well soaked up from went. - kish. a path and in the maximum concentration collects in a blood plasma in 2 — 3 hours after reception; biological half-life — apprx. the 10th hour. In fabrics it is distributed rather evenly. Out of an organism it is brought by kidneys of hl. obr. in the form of oxymeprotanum and glucuronides; apprx. 10% of the accepted dose it is excreted in not changed look. The m activates microsomal enzymes of a liver what decrease it pharmakol, activities can be connected at prolonged use with.
Apply M at the neurosises and neurosis-like states which are characterized by irritability, excitement, alarm, fear, affective tension, sleep disorders. At acute psychotic states with productive psychopathological symptomatology of M. it is inefficient. Sometimes M. apply to stopping of the abstinent phenomena at the persons having alcoholism, drug addiction and also at smokers.
At M.'s epilepsy apply to suppression of dysphorias and correction personal psikhopatol, the reactions inherent to this category of patients. At this M. it is necessary to appoint only in a complex with antiepileptic means.
The m renders therapeutic effect at sleeplessness, vegetative dystonias, a premenstrual syndrome, climax, a skin itch, in initial stages of an idiopathic hypertensia, at stenocardia, a peptic ulcer of a stomach and a duodenum, and also at the diseases which are followed by increase in a tone of skeletal muscles, napr at damages of joints with spasms of muscles, to Littl's disease, etc. In M.'s anesthesiology apply by preparation for operations.
M. appoint inside on 0,2 — 0,4 g 2 — 3 times a day. If necessary it is possible to increase a daily dose to 2 — 3 g.
Treatment of neurosises is begun usually with a daily dose of 0,4 — 0,8 g, if necessary gradually increasing it before obtaining therapeutic effect. Duration of treatment at neurosises on average 1,5 — 2 months. It is necessary to stop treatment gradually since sudden cancellation of M. can lead to resuming of neurosis.
At sleeplessness accept 0,2 — 0,6 g before going to bed.
The highest doses for adults inside: one-time 0,8 g, daily 3 g. To M. children appoint in doses: at the age of 3 — 8 years — on 0,1 — 0,2 g 2 — 3 times a day, 8 — 14 years — on 0,2 g 2 — 3 times a day.
The persons accepting M. shall not be allowed to driving of motor transport and performance of other types of the works demanding bystry mental and motor reactions.
Side effect The m can be shown by the increased drowsiness, feeling of an oglushennost, lacks of coordination of movements, muscular weakness, allergic reactions, the dispeptic phenomena. At prolonged use development of accustoming and physical medicinal dependence is possible. The withdrawal is shown in the form of a delirium and spasms. Medicinal dependence develops in most cases at persons with psychopathic traits of character, and also at the persons abusing other psychotropic drugs or alcohol.
At acute poisoning M are observed coma, falloff of the ABP, respiratory depression; the fluid lungs can develop. Acute management at poisoning includes methods of an active detoxication (a gastric lavage with the subsequent giving salt laxative, an artificial diuresis without alkalization of plasma, peritoneal dialysis, a hemodialysis, a haemo sorption detoxication) and means of symptomatic therapy.
Forms of release: tablets on 0,2 and 0,4 g. Store in well corked container.
Bibliography: Aleksandrovsky Yu. A. Clinical pharmacology of tranquilizers, M., 1973; Psychotropic drugs in medical practice, under the editorship of G. Ya. Avrutsky, page 129, M., 1971; Ludwig B. J. a. P about t t e of f i e 1 d J. R. The pharmacology of propanediol carbamates, Advanc. Pharmacol. Chemother., v. 9, p. 173, 1971, bibliogr.; The pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, p. 188, N. Y., 1975.
V. V. Churyukanov.