Metabolism of the prostaglandin fertility regulator sulprostone in monkeys.

F C Falkner

Index: Prostaglandins 24(3) , 341-50, (1982)

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Abstract

The prostaglandin imide analog sulprostone (I) was labeled with tritium in the phenoxy ring to trace the fate of the prostanoic acid portion of the molecule and with carbon-14 in the methanesulfonimide moiety to trace the fate of that portion of the molecule. Disposition was studied after intravenous administration to female cynomolgus monkeys. The excretion and plasma pharmacokinetics of total radioactivity indicated that the prostanoic acid and methanesulfonimide moieties were disposed of differently, implying that hydrolysis of sulprostone was extensive and that the hydrolysis products were treated independently. The urinary excretion of tritium (prostanoic acid) was consistent with that observed for other prostaglandins. The urinary excretion and plasma pharmacokinetics of carbon-14 were consistent with those expected for methanesulfonamide. Urinary metabolites identified in 0-2 hr urine included a trace amount of unchanged drug, methanesulfonamide, and two products of beta-oxidation - the tetranor and dihydrotetranor prostanoic acids.