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Journal of Pharmacology And Experimental Therapeutics, Vol. 118, Issue 1, 46-54, 1956
Copyright © 1956 by American Society for Pharmacology and Experimental Therapeutics


PHYSIOLOGICAL DISPOSITION AND FATE OF CHLORPROMAZINE AND A METHOD FOR ITS ESTIMATION IN BIOLOGICAL MATERIAL

Norman P. Salzman 1 and Bernard B. Brodie 1

1 Laboratory of Chemical Phmacology, National Heart Institute, National Institutes of Health, Public Health Service, U. S. Department of Health, Education and Welfare, Bethesda, Md.

A method is described for the estimation of chlorpromazine and chlorpromazine sulfoxide in biological material.

In the dog, chlorpromazine is metabolized almost completely but, partly because of its extensive localization in various tissues, especially brain, relatively slowly. At least three metabolic products are formed.

The main metabolic product has been isolated from the urine of dogs receiving chlorpromazine and identified as the sulfoxide. It is also formed in man. The sulfoxide undergoes metabolism to an unidentified product.

The sulfoxide although less active than chlorpromazine exerts a sedative action at dosage levels that do not produce postural hypotension in dog or man.

Submitted on April 27, 1956




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Copyright © 1956 by the American Society for Pharmacology and Experimental Therapeutics.