DIAZEPAM (Diazepam; synonym: Seduxenum, Apaurin, Relanium, Ansiolin, Eridan, Lembrol, Pacitrin, Quetinil, Valium etc.; joint venture. B) — tranquilizing means. 7-Хлор-1,3-дигидро-1-метил-5-фенил-2Н-1,4-бензодиазепин-2-он, C 16 H 13 ClN 2 O:
Colourless crystal powder, water-insoluble. On a structure and pharmakol, to properties it is close To to chlordiazepoxide (see). In D.'s experiment shows the expressed calming action, reduces a physical activity and an orientation response, it is selectively antagonistic in relation to convulsive effects of Corazolum and strychnine, at increase in a dose causes muscle relaxation of the central origin. Influence on cardiovascular system and a vegetative innervation is poorly expressed.
Is most active at a conflict situation, and also at external inhibition of conditioned reflexes, and the last are not oppressed by D. Osobennostyyu of drug it is necessary to consider the activating efficiency of small doses. The neurotropic effect of D. is result, apparently, of its influence not only on limbic structures, but also on a cerebral cortex.
Reduces the psychoemotional tension, alarm, fear, concern, an acrimony. The calming D.'s action is not followed by considerable influence on mental and physical. working capacity. As a rule, at the same time drowsiness, an adynamia and the block arising at reception of neuroleptics is not noted. The antipsychotic effect of D. is expressed poorly and the hl is shown. obr. reduction of affective frustration — fear, alarm.
Drug is widely used in psychiatry, neuropathology, anesthesiology, therapy, pediatrics, dermatology.
In neuropathology and D.'s psychiatry appoint hl. obr. at neurosises, including at neurosises of persistence. Drug is effective at the psychopathies, reactive states, diencephalic (hypothalamic) frustration which are followed by various vegetative manifestations (increase in the ABP, disturbance of thermal control, a plentiful diuresis, abdominal crises, the phenomena of stenocardia, a Bouveret's disease). Is applied also to treatment of patients with the residual phenomena of organic lesion of a brain with the accompanying neurosis-like symptomatology, at alcoholic and narcotic abstinence, at the neurosis-like schizophrenia which is followed by affective frustration. Can be applied at treatment of epilepsy and to stopping of the epileptic status.
At treatment of coronary insufficiency, a myocardial infarction and attacks of stenocardia of D. combine with vasodilators (see).
In D.'s anesthesiology apply during the training of patients for operation, during operation in combination with narcotic analgetics (a so-called ataralgeziya), in the postoperative period. With success use for the purpose of premedication at small operational or diagnostic interventions in stomatology, otorhinolaryngology, at a bronkhoskopiya and various endoscopic researches.
The dosage and ways of administration of drug depend on a form and the nature of a disease. Apply inside, intramusculary and intravenously (enter slowly into 40% solution of glucose). In the conditions of a hospital treatment is usually begun with 0,005 g, gradually the dose is increased to 0,015 — 0,06 g a day. In out-patient conditions it is not recommended to appoint more than 0,03 g of drug a day. For stopping of the epileptic status enter into a vein 8 — 12 ml of 0,5% of solution D. (0,04 — 0,06 g) in 20 ml of 40% of solution of glucose. In some cases D. can be combined with neuroleptics or antidepressants. Small doses of D. (0,005 g) allow to gain the activating effect at patients with the asthenic phenomena, high doses (0,015 — 0,03 g) cause the expressed sedation.
D.'s toxicity is small, the by-effects caused by it are rather rare. Muscular weakness, slackness, drowsiness, an ataxy, sometimes a dysarthtia are most characteristic; the allergic reactions connected with individual intolerance of drug — dryness in a mouth, dermatitis, dispeptic frustration are noted.
it is contraindicated at acute diseases of a liver and kidneys, a heavy myasthenia and glaucoma. It is not necessary to appoint D. at pregnancy up to 3 months, and also in operating time, the demanding bystry and exact mental and motor reaction (e.g., to drivers of transport). Alcohol exponentiates effect of drugs of this group therefore during their use it is necessary to abstain from consumption of alcoholic drinks.
Forms of release: tablets on 0,005 g, 0,5% solution in ampoules on 2 ml.
See also Tranquilizers .
Bibliography Aleksandrovsky Yu. A. Clinical pharmacology of tranquilizers, M., 1973, bibliogr.
K. S. Rayevsky.