TRIFTAZYN (Triftazinum; synonym: Stelazinum, Fluperin, Parstelin, Ter-fluzine, Trifluoperazini Hydrochlori-dum, Trifluperazine, Triperazine, etc.; GFH, joint venture. B) — neuroleptic. 2-Triftormetil-10-[3-(1-me-tilpiperazinil - 4) - propyl] - a fenotia-zina dihydrochloride; C2iH24F3N3S’
Crystal powder of white or inodorous slightly greenish-yellowish color. Let's easily dissolve in water, we will dissolve in 95% alcohol; g°pl 232 — 240 °; pier. weight (weight) 480,41.
On a chemical structure it is close to Metherazinum, from to-rogo differs only in presence of the trifluoromethyl radical in the 2nd provision of a fenotiazino-vy ring instead of chlorine atom. Together with Metherazinum, Thioproperazinum, ftorfenaziny (see) and etaperaziny (see) treats group of so-called piperazinovy derivatives of a feno-tiazin, to-rye along with high antipsychotic and antiemetic activity exert the expressed impact on striopallidal system of a brain. It is shown by the high frequency of the extrapyramidal disturbances arising at a wedge, use of drug (see. Extrapyramidal system). In an experiment Triphtazinum causes block, decrease in a physical activity, a katalepsy in animals. Besides, in small doses oppresses conditional defensive reflexes, prevents exciting effect of Phenaminum and has antiemetic effect. On these indicators Triphtazinum is about 10 — 20 times more active than aminazine (see). On antiinflammatory and antiserotoninovy activity it is close to aminazine, on and - adrenobloki-ruyushchey and hypotensive activity, and also on ability to exponentiate effect of anesthetics concedes to it.
According to a wedge, to observations of T. has high antipsychotic activity and exerts the expressed impact on the main displays of psychoses (nonsense, hallucinations, mental avtomatizm). At the same time T. does not cause in patients of aminazine of a condition of block, typical for action, depression and emotional slackness that is caused, apparently, by smaller expressiveness at T. sedative
properties. Besides, T. less often and to a lesser extent, than aminazine, causes hypotension.
Mechanism of action of T., as well as other neuroleptics, connect with ability to interact with dopamine receptors of neurons of a striatum and limbic system of a brain owing to what metabolic turnover of dopamine (see Catecholamines) in these educations accelerates and pulse activity of dofaminergi-chesky neurons in the field of a mesencephalon increases.
T. apply hl. obr. in psychiatry for treatment of various forms of schizophrenia (see). It is especially effective T. at a paranoid and hallucinatory form of schizophrenia. Sometimes T. use for premedication (in a combination with Promedolum or other narcotic analgetics), and also as an antiemetic.
Appoint inside (after food) or intramusculary. Inside in an initiation of treatment appoint 0,001 — 0,005 g to reception 2 — 4 times a day, gradually increasing a single dose by 0,005 g on reception to a daily dose of 0,03 — 0,08 g (sometimes to 0,1 — 0,12 g). Intramusculary 2 — 3 times a day enter on 0,5 — 1 ml 0,2% of solution. As antiemetic of T. usually appoint inside 0,001 — 0,004 g a day.
The most characteristic manifestation of side effect of T. consider extrapyramidal frustration (constraint, a zatrudnennost of the speech, restlessness, dyskinesia, hyperkinesias), to-rye weaken after reduction of a dose of drug, and also under the influence of protivoparkins.o-nichesky means (see), e.g., Cyclodolum, etc. Dyskinesia, the caused T., stop also caffeine-sodium benzoate.
Forms of release: tablets, on
covered by a cover, on 0,001; 0,005 and 0,01 g and ampoules on 1 ml of 0,2% of solution. Store in well corked container protecting from effect of light.
See also Neuroleptics.
Bibliography: And in r at c to and y, I. and to Ned va A. A. Treatment mentally sick, with * 52, M., 1981; The Medicines used in psychiatry under the editorship of G. Ya. Avrutsky, page 50, M., 1980;
K. S. Pharmakologiya's Rajevski of neuroleptics, page 178, M., 1976; The pharmacological basis of therapeutics, ed. by A. G. Gilman and. o., N, Y., 1980.
K. S. Rayevsky.