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Journal of Pharmacology And Experimental Therapeutics, Vol. 131, Issue 1, 130-134, 1961
Copyright © 1961 by American Society for Pharmacology and Experimental Therapeutics

ANTIEMETIC ACTION OF FLUPHENAZINE (PROLIXIN): A COMPARISON WITH OTHER PHENOTHIAZINES

Robert J. Laffan 1, Dimitris P. Papandrianos 1, John C. Burke 1, and Bradford N. Craver 1

1 The Squibb Institute for Medical Research, New Brunswick, New Jersey

The antiemetic activities of fluphenazine, perphenazine, triflupromazine and chlorpromazine have been determined in dogs and the durations of their protective effects against 20 µg/kg of apomorphine hydrochloride, intravenously, have been established.

Estimations of the relative potency of each of the compounds on the basis of protectionduration indicate that subcutaneously adminis- tered fluphenazine is 34 to 124 times as potent as chlorpromazine, and 4.2 to 7.5 and 16.7 to 19.0 times as potent as perphenazine and triflupromazine, respectively, in reducing the emetic susceptibility of dogs to apomorphine hydrochloride.

None of the four phenothiazines offered significant protection against the emetic effects of lanatoside, nicotine, veratrurn or nitrogen mustard.

The greater antiemetic potency of fluphenazine as compared to tniflupromazine was not accompanied by a correspondingly greater sedative action since pretreatment with over 30 times the threshold antiemetic dose of fluphenazine did not alter pentobarbital-induced sleeping time whereas an equivalent dose of triflupromazine extended sleeping time almost two-fold.

Submitted on June 1, 1960






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Copyright © 1961 by the American Society for Pharmacology and Experimental Therapeutics.