HLORDIAZEPOKSYD (Chlordiaze-poxidum; synonym librium, Elenium, Chlozepidum, Chlozepidum, Elenium, Librium, Methaminodiazepoxide, Radepur, Napoton, etc.; joint venture. B) — tranquilizing means. 7-Hlor-2-metilamino-5-fenil-ZN-
White crystal powder, not water soluble.
In an experiment has the calming effect on animals, normalizes behavior at an emotional stress and in a conflict situation, has rastormazhivayushchy effect, weakens aggressive reactions, exponentiates effect of somnolent substances and anesthetics, warns the spasms caused by Corazolum, strychnine, thiosemicarbazide, bikukul-liny and an electroshock. In high doses reduces a physical activity, oppresses approximate and research behavior and uslovnoreflektorny activity, weakens skeletal muskulatu-RU-
According to a wedge, to observations chlordiazepoxide causes the expressed anxiolytic effect (eliminates sensation of fear and alarms) in the person, drowses and lowers a tone of skeletal muscles. Like diazepam (see), to Phenazepamum (see) and to other tranquilizers of a benzodiazepine row strengthens processes of the synoptic braking caused at - amino - butyric acid (DIN To). With GAMK-pozitivnym action connect anticonvulsant, the muscular weakening and anxiolytic effects of chlordiazepoxide. Besides, drug exerts impact on exchange of monoamines: reduces the speed of a circulation of noradrenaline and serotonin and increases their contents in c. N of page. Assume that in the mechanism of effect of chlordiazepoxide its ability to contact specific (benzodiazepine) receptors in a brain of the person and animals matters. It is followed by change of conformation of receptors DIN To and increase in conductivity of chloric channels in membranes of neurons.
Chlordiazepoxide is well soaked up from went. - kish. a path and in the maximum concentration collects in a blood plasma in 2 — 4 hours after intake. The hl is allocated. obr. kidneys partially through went. - kish. path. The main metabolites of chlordiazepoxide in a human body and animals are dezmetilkhlordiazepoksid and dezmetilaminokhlordiazepoksid (-moksepam), and also to dezoksidemok-sepa and параоксифенилдемог^сепам.
Chlordiazepoxide is applied at the neurotic and neurosis-like conditions of various genesis which are followed by alarm, fear, emotional tension, frustration of a dream. Drug is effective at senestoipokhondriche-sky frustration, persuasive states, vegetative drgsfunktsi-yakh. Chlordiazepoxide is used for stopping of an abstinence syndrome at alcoholism (see an alcoholism). Chlordiazepoxide surpasses Trioxazinum in efficiency (see) and Meprotanum (see) t but concedes to diazepam and Phenazepamum. Chlordiazepoxide is widely applied not only in psychiatry and neurology, but also in other fields of medical practice, napr, at therapy of patients with various somatopathies, and also in surgery and obstetrics as the means calming and relaxing muscles. Besides, it is used for potentiation of action of hypnagogues (see), analgetics and anesthetics (see).
Appoint inside the adult 0,005 — 0,01 g once a day, then gradually raise a dose to 0,03 — 0,05 g (in 3 — 4 receptions). Maximum daily dose of 0,06 g. In the conditions of a hospital chlordiazepoxide is appointed sometimes to 0,1 — 0,12 g a day. To children appoint in doses, components 1/4 — V2 of a dose for adults.
Chlordiazepoxide can cause side effects: an ataxy, a sl
Bost, drowsiness, dizziness, to-rye usually arise at its use in high doses. It is contraindicated at a heavy myasthenia and disturbances of functions of a liver and kidneys. It is not recommended to apply chlordiazepoxide at pregnancy and to persons, production activity to-rykh demands bystry and exact reactions. Persons of advanced and senile age need to appoint drug with care in the reduced doses.
Form of release: tablets, coated, on 0,005; 0,01 and 0,025 g. Storage: in the place protected from light.
See also Tranquilizers. Bibliography: Aleksandrovsky
Yu. A. Clinical pharmacology of tranquilizers, M., 1973; Benzodiazepines, Today and tomorrow, ed. by R. G. Priest, Lancaster, 1980. T. A. Voronina.