Bidisomide (SC-40230), a new antiarrhythmic agent: initial study of tolerability and pharmacokinetics.

Published

Journal Article

Forty-nine healthy male volunteers received the test article for bidisomide (SC-40230) in a double-blind, placebo-controlled, dose-ranging study. Intravenous doses ranged from 0.03 to 2.5 mg/kg. There was a close relationship between the dose and the peak plasma concentration. The PR, QRS, QT, RR, and QTc intervals each demonstrated a statistically significant response to the dose administered. The PR and QRS intervals lengthened and the other intervals shortened (although to a lesser degree). The compound was well tolerated, with mild symptoms only at higher doses. Bioavailability was studied in 12 male volunteers, with each receiving 2.0 mg/kg of bidisomide, both orally and intravenously, in an open-label crossover trial. After a 10-minute zero-order intravenous infusion, bidisomide plasma levels could best be described in terms of a three-compartment pharmacokinetic model with the mean half-life values of alpha, beta, and gamma phases of 0.12, 1.77, and 12.3 hours, respectively. The mean absolute oral bioavailability was 43%.

Full Text

Duke Authors

Cited Authors

  • Page, RL; Wharton, JM; Wilkinson, WE; Friedman, IM; Claypool, WD; Karim, A; Kowalski, KG; McDonald, SJ; Gardiner, P; Pritchett, EL

Published Date

  • April 1, 1992

Published In

Volume / Issue

  • 51 / 4

Start / End Page

  • 371 - 378

PubMed ID

  • 1563207

Pubmed Central ID

  • 1563207

International Standard Serial Number (ISSN)

  • 0009-9236

Digital Object Identifier (DOI)

  • 10.1038/clpt.1992.36

Language

  • eng

Conference Location

  • United States