NEUROLEPTIC, ANTI-MUSCARINIC, AND ANTIADRENERGIC ACTIVITY OF CHLORPROMAZINE, THIORIDAZINE, AND THEIR METABOLITES

被引：72

作者：

COHEN, BM

HERSCHEL, M

AOBA, A

机构：

[1] Bruce M. Cohen, M.D., Ph.D., is Instructor, and Michael Herschel, M.D., and Anri Aoba, M.D., are Research Fellows, Department of Psychiatry, Harvard Medical School, and Mailman Research Center, McLean Hospital, 115 Mill St., Belmont

来源：

PSYCHIATRY RESEARCH | 1979年 / 1卷 / 02期

关键词：

Chlorpromazine; metabolites; radioreceptor assays; thioridazine;

D O I：

10.1016/0165-1781(79)90062-3

中图分类号：

R749 [精神病学];

学科分类号：

100205 ;

摘要：

Chlorpromazine and thioridazine are widely used antipsychotic agents that are extensively metabolized. Parent compounds and metabolites have diverse pharmacologic activities, and differences in patterns of metabolism may explain differences in therapeutic and side effects from individual to individual. Radio-receptor assays were used to determine the neuroleptic, antimuscarinic, and anti-α- noradrenergic potency of chlorpromazine, thioridazine, and their metabolites. The results indicate that these metabolites show a wide range of potencies. The spectrum of activity of a metabolite may be quite different from that of its parent compound. The clinical relevance of these findings to individual differences in drug response is discussed. The combined use of radioreceptor assays and chemical assays in future clinical research is proposed. © 1979.

引用

页码：199 / 208

页数：10

共 23 条

[1]

Axelsson, On the serum concentrations and antipsychotic effects of thioridazine, thioridazine side-chain sulfoxide and thioridazine side-chain sulfone, in chronic psychotic patients, Current Therapeutic Research, 21, (1977)

[2]

Baldessarini, Chemotherapy in Psychiatry, (1977)

[3]

Barry, Steenberg, Manian, Buckley, Effects of chlorpromazine and three metabolites on behavioral responses in rats, Psychopharmacologia, 34, (1974)

[4]

Bunney, Aghajanian, A comparison of the effects of chlorpromazine, 7-hydroxychlorpromazine, and chlorpromazine sulfoxide on the activity of central dopaminergic neurons, Life Sciences, 15, (1974)

[5]

Burt, Creese, Snyder, Properties of [<sup>3</sup>H] haloperidol and [<sup>3</sup>H] dopamine binding associated with dopamine receptors in calf brain membranes, Molecular Pharmacology, 12, (1976)

[6]

Clark, Kaul, A preliminary report on clinical response and blood levels of chlorpromazine and its sulfoxide during chlorpromazine therapy in chronic schizophrenic patients, Pharmacokinetics of Psychoactive Drugs, (1976)

[7]

Creese, Burt, Snyder, Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs, Science, 192, (1976)

[8]

Fuller, Pharmacogenetics, Principles of Psychopharmacology, (1970)

[9]

Lader, Monitoring plasma concentrations in neuroleptics, Pharmakopsychiatrie, 9, (1976)

[10]

Lal, Sourkes, Effect of various metabolites on amphetamine-induced stereotyped behavior in the rat, European Journal of Pharmacology, 17, (1972)

← 1 2 3 →