PMID: 7547086Jan 1, 1995Paper

Single and multiple dose pharmacokinetics of tenidap sodium in healthy subjects

British Journal of Clinical Pharmacology
M J GardnerG F McMahon

Abstract

1. The absorption, protein binding, clearance and absolute bioavailability of tenidap sodium were studied after single and multiple dosing. 2. Thirteen healthy male volunteers received a single 120 mg oral dose of tenidap sodium and a 20 mg intravenous infusion of deuterated tenidap ([D3]-tenidap) on day 1. This was followed by a 6-day washout period (days 2-7) and then further daily doses of oral tenidap sodium 120 mg for 21 consecutive days (days 8-28) with an additional 20 mg intravenous infusion of [D3]-tenidap on day 28. Twelve subjects were eligible for pharmacokinetic evaluation. 3. Following multiple oral doses, the half-life of tenidap is approximately 23 h. 4. Following single and multiple dose administration, the absolute bioavailability is 85%. 5. Systemic clearance of [D3]-tenidap was 29% greater on day 28 than on day 1 indicating a significant increase in intrinsic clearance (CLint) of tenidap since protein binding of tenidap in plasma did not change during the study. Consistent with the increase in systemic clearance, the half-life of [D3]-tenidap decreased and the ratio of AUC(0,24h) day 28/AUC day 1 following oral dosing was less than one. Tenidap is subject to extensive hepatic metabolism, so the increase in C...Continue Reading

References

Feb 1, 1990·The Biochemical Journal·P C HeinrichT Andus
Mar 1, 1990·Proceedings of the National Academy of Sciences of the United States of America·M HattoriG H Fey
Jun 1, 1984·Journal of Pharmaceutical Sciences·F D Boudinot, W J Jusko
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Apr 1, 1993·Annals of the Rheumatic Diseases·J T DingleJ J Martindale

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Citations

Dec 20, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·A G ThombreS C Sutton
Jan 1, 1995·British Journal of Clinical Pharmacology·P M DewlandP E Coates
Jan 7, 1999·The Annals of Pharmacotherapy·N V DahlR A Sherman
Aug 6, 1998·Journal of Chemical Information and Computer Sciences·M D WesselS M Muskal
Nov 1, 1995·Baillière's Clinical Rheumatology·C E Richardson, P Emery

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