title: Determination and metabolism of dithiol chelating agents. XVI: Pharmacokinetics of 2,3-dimercapto-1-propanesulfonate after intravenous administration to human volunteers.
abstract: 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).
authors.affiliation: Department of Pharmacology and Toxicology, University of Arizona, Tucson.
authors.forename: K M
authors.initials: KM
authors.lastname: Hurlbut
authors.forename: R M
authors.initials: RM
authors.lastname: Maiorino
authors.forename: M
authors.initials: M
authors.lastname: Mayersohn
authors.forename: R C
authors.initials: RC
authors.lastname: Dart
authors.forename: D C
authors.initials: DC
authors.lastname: Bruce
authors.forename: H V
authors.initials: HV
authors.lastname: Aposhian
mesh_terms: D000328:Adult; D005260:Female; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D014494:Unithiol / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D014494:Unithiol