Pharmacokinetics of levosimendan and its circulating metabolites in patients with heart failure after an extended continuous infusion of levosimendan
Authors: Antila S.1; Kivikko M.1; Lehtonen L.; Eha J.2; Heikkilä A.1; Pohjanjousi P.1; Pentikäinen P.J.3
Source: British Journal of Clinical Pharmacology, Volume 57, Number 4, April 2004 , pp. 412-415(4)
Publisher: Blackwell Publishing
- Free Content
- New Content
- Subscribed Content
- Free Trial Content
Abstract:
Aims The purpose of the study was to characterize the pharmacokinetics of levosimendan and its metabolites OR-1855 and OR-1896 in patients with congestive heart failure. Methods Levosimendan was administered as a continuous intravenous infusion for 7 days. Twelve subjects received the drug at an infusion rate of 0.05 µg kg-1 min-1 and 12 at a rate 0.1 µg kg-1 min-1. Results Steady state concentrations of levosimendan were achieved within 4 h. Peak concentrations of the metabolites occurred after termination of the infusion. The mean (± SD) half-life of the active metabolite OR-1896 was 81 ± 37 h after the lower dose and 81 ± 28 h after the higher dose (P = 0.992, 95% confidence interval on the difference -27.5, 27.7). Conclusions The metabolites of levosimendan, OR-1855 and OR-1896, were formed and eliminated slowly, their peak concentrations occurring after termination of the 7-day infusion of the drug.Keywords: levosimendan; pharmacokinetics; metabolism; calcium sensitizer
Document Type: Research article
DOI: 10.1111/j.1365-2125.2003.02043.x
Affiliations: 1: Orion Pharma, Research Centre, Espoo, Finland, 2: Mustamae Hospital, Tallinn, Estonia and 3: Helsinki University Central Hospital, Department of Internal Medicine, Helsinki, Finland
- Free Content
- New Content
- Subscribed Content
- Free Trial Content
Click here for Page Help