PT - JOURNAL ARTICLE AU - K M Hurlbut AU - R M Maiorino AU - M Mayersohn AU - R C Dart AU - D C Bruce AU - H V Aposhian TI - Determination and metabolism of dithiol chelating agents. XVI: Pharmacokinetics of 2,3-dimercapto-1-propanesulfonate after intravenous administration to human volunteers. DP - 1994 Feb 01 TA - Journal of Pharmacology and Experimental Therapeutics PG - 662--668 VI - 268 IP - 2 4099 - http://jpet.aspetjournals.org/content/268/2/662.short 4100 - http://jpet.aspetjournals.org/content/268/2/662.full SO - J Pharmacol Exp Ther1994 Feb 01; 268 AB - The pharmacokinetics of 2,3-dimercaptopropane-1-sulfonate (DMPS), an effective chelating agent for mercury, were determined in five healthy adults after i.v. administration of 3.0 mg/kg of DMPS. DMPS is rapidly transformed to disulfide forms; 15 min after administration, only 12% of the total DMPS detected in blood was present as the parent drug. DMPS and its metabolites were eliminated primarily by the kidneys. By 96 hr after administration, 12% of the total DMPS found in the urine was excreted as the parent drug (10% of the administered dose) and 88% was excreted as disulfide metabolites (74% of the administered dose). The disposition of parent drug was described by a biexponential equation with an elimination half-life of 1.8 hr. By contrast, the elimination half-life of total DMPS was 20 hr. The oral bioavailability of the parent drug was found in a separate study to be 39%. Mercury excretion in healthy volunteers correlated well with the urinary excretion of both the parent drug (r2 = .94) and the disulfide metabolites (r2 = .96).