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Journal of Pharmacology And Experimental Therapeutics, Vol. 134, Issue 1, 110-116, 1961
Copyright © 1961 by American Society for Pharmacology and Experimental Therapeutics

THE METABOLIC FATE OF THIOBARBITURATES: THIOBARBITAL IN MAN

Milton T. Bush 1, Paul Mazel 1, and John Chambers 1

1 Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee

In three human males we have injected 2 mg/kg of thiobarbital intravenously, and found that during the following 8 to 12 days some 5 to 7% of the drug was excreted in the urine as barbital, some 1 to 5% as unchanged thiobarbital. The fate of the other 90-odd% of the thio compound remains unknown.

We have also found that in vitro conversion of thiobarbital to barbital can readily be brought about by diethyl ether in the presence of air.

A method of recovery, purification, and separation of thiobarbital and barbital from urine is described. The method involves the quantitative extraction of thiobarbital with n-butyl chloride, a solvent in which it is stable, and which removes only a minor part of the barbital. The latter is subsequently recovered by extraction with ether. The sensitivity of the method is approximately 0.1 mg/liter of urine for these and related drugs.

Submitted on March 20, 1961






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