DETERMINATION AND METABOLISM OF DITHIOL CHELATING-AGENTS .XVI. PHARMACOKINETICS OF 2,3-DIMERCAPTO-1-PROPANESULFONATE AFTER INTRAVENOUS ADMINISTRATION TO HUMAN VOLUNTEERS

The pharmacokinetics of 2,3-dimercaptopropane-1-sulfonate (DMPS), an e ffective 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. D MPS and its metabolites were eliminated primarily by the kidneys. By 9 6 hr after administration, 12% of the total DMPS found in the urine wa s excreted as the parent drug (10% of the administered dose) and 88% w as excreted as disulfide metabolites (74% of the administered dose). T he disposition of parent drug was described by a biexponential equatio n with an elimination half-life of 1.8 hr. By contrast, the eliminatio n half-life of total DMPS was 20 hr. The oral bioavailability of the p arent drug was found in a separate study to be 39%. Mercury excretion in healthy volunteers correlated well with the urinary excretion of bo th the parent drug (r(2) = .94) and the disulfide metabolites (r(2) = .96).