Determination and metabolism of dithiol chelating agents XVI: Pharmacokinetics of 2,3-dimercapto-1-propanesulfonate after intravenous administration to human volunteers

K. M. Hurlbut, R. M. Maiorino, M. Mayersohn, R. C. Dart, D. C. Bruce, H. V. Aposhian

Research output: Contribution to journalArticle

33 Scopus citations

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 (n = .94) and the disulfide metabolites (r2 = .96).

Original languageEnglish (US)
Pages (from-to)662-668
Number of pages7
JournalJournal of Pharmacology and Experimental Therapeutics
Volume268
Issue number2
StatePublished - Jan 1 1994

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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