ETAPERAZIN

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ETAPERAZYN (Aethaperazinum; synonym: Chlorpiprozine, Decentan, Fen-tazin, Neuropax, Perphenan, Per-phenazini Hydrochloridum, Perphenazine Hydrochloride, Trilafon, Trilifan, etc.; joint venture. B) — antipsychotic and antiemetic. 2-Hlor-10-{ 3-[-pi-perazinit 1 (R-hydroxyethyl) - 4] - propyl } - a fenotiazina dihydrochloride; C21H26C1N3OS • 2HC1:

Crystal powder, white or white with a scarcely noticeable grayish shade. Let's easily dissolve in water, it is not enough — in alcohol, it is practically not ether-soluble also chloroform. It is hygroscopic. Under the influence of light powder and water solutions decay; g°pl 217 — 223 °; pier. weight (weight) 476,9.

AA. treats neuroleptics (see) a fenotiazinovy row. On structure and pharmacological properties E. treats so-called piperazinovy group of fenotiazin (see), in to-ruyu also enter Metherazinum (see), Triphtazinum (see), ftorfenazin (see) and Thioproperazinum. Feature of drugs of this group is the combination of high antipsychotic and antiemetic activity to the expressed influence on striopallidal system of a brain that is shown by the high frequency of extrapyramidal disturbances at patients (see. Extrapyramidal system).

AA. possesses the range of neurotropic activity characteristic and for other drugs of piperazinovy group of fenotiazin. In an experiment E. causes a condition of block, decrease in motor and approximate performance, a katalepsy, moderate synchronization of EEG in animals. In high doses renders myshechno the weakening effect and breaks coordination of movements.

On oppression of uslovnooboronitelny reflexes E. surpasses aminazine (see) by 4 — 8 times, and in expressiveness of antiemetic action — by 5 — 10 times, sedation at E. it is expressed more. Like other drugs of piperazinovy group of fenotiazin, AA. shows selective antagonism concerning the dofaminomimetichesky effects (motive excitement, a stereotypy) caused by Phenaminum (see) and Apomorphinum (see). On ability to exponentiate narcotic effect of barbiturates E. it is close to aminazine. Hypotensive and and - adrenoblokiruyu-shchee action is expressed at E. to a lesser extent. The m-holinoblokiruyu-shchiye, antihistaminic and spasmolytic properties are expressed poorly. In comparison with aminazines E. is less toxic.

Mechanism of action E., as well as other neuroleptics, it is accepted to connect with their ability to interact with dopamine receptors of neurons mezolimbi-chesky and other systems of a brain. As a result of blockade of receptors at prolonged use of neuroleptics acceleration of a metabolic turnover of dopamine of a feedback mechanism develops.

In a wedge, conditions E. shows high antipsychotic activity of broad range. AA. apply to treatment of various forms of schizophrenia (see) and other mental diseases, neurosises with the phenomena of alarm and emotional pressure, at vomiting the pregnant and other states which are followed by vomiting and a hiccups and also at a skin itch. Most often E. appoint at schizophrenia. It is shown to patients, at to-rykh along with nonsense and hallucinations are observed motive block up to a catatonic stupor and the depressive phenomena.

Apply E. inside after food. Treatment of psychoses begin with a dose 0,004 — 0,01 g of 1 — 2 time a day, gradually increasing it. For patients, the Crimea neuroleptics are appointed for the first time, a daily dose E. makes 0,05 — 0,08 g. At hron. the course of a disease daily doses make 0,1 — 0,15 g; in some cases — 0,25 — 0,4 g. For a maintenance therapy E. appoint 0,01 — 0,06 g a day. As an antiemetic E. apply 0,004 — 0,008 and 3 — 4 times a day.

AA. can cause the same side effects, as well as other neuroleptics. However extrapyramidal disturbances and especially an akathisia arise more often than at use of aminazine. For their correction use protivoparkinsoniche-sky means (see).

Form of release: tablets, coated, on 0,004; 0,006 and 0,01 g. Storage: in the dry, protected from light place.

See also Neuroleptics.

Bibliography: Avrutsky G. Ya. and to Ned in and A. A. Treatment mentally sick, M., 1981; The Medicines used in psychiatry under the editorship of G. Ya. Avrutsky, page 76, M., 1980; K. S. Pharmakologiya's Rajevski of neuroleptics, page 170, M., 1976; The pharmacological basis of therapeutics, ed. by A. Gilman

and. lake, N. Y., 1980. K. S. Rayevsky.

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