Clinical pharmacology of nicorandil in patients with congestive heart failure

Nicorandil is a nicotinamide derivative with a potential role in human therapeutics because of its potent vasodilating properties. The pharmacokinetics of oral nicorandil administration and the relationships between plasma nicorandil concentration and hemodynamic responses were examined in 25 patien...

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Bibliographic Details
Published in:	Clinical pharmacology and therapeutics Vol. 52; no. 5; p. 496
Main Authors:	Tice, F D, Jungbluth, G L, Binkley, P F, MacKichan, J J, Mohrland, J S, Wolf, D L, Leier, C V, Bindley, P F
Format:	Journal Article
Language:	English
Published:	United States 01-11-1992
Subjects:	Administration, Oral Adult Aged Analysis of Variance Cardiovascular System - drug effects Double-Blind Method Female Half-Life Heart Failure - blood Heart Failure - drug therapy Humans Least-Squares Analysis Male Middle Aged Niacinamide - administration & dosage Niacinamide - analogs & derivatives Niacinamide - pharmacokinetics Niacinamide - therapeutic use Nicorandil Vasodilator Agents - administration & dosage Vasodilator Agents - pharmacokinetics Vasodilator Agents - therapeutic use
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Summary:	Nicorandil is a nicotinamide derivative with a potential role in human therapeutics because of its potent vasodilating properties. The pharmacokinetics of oral nicorandil administration and the relationships between plasma nicorandil concentration and hemodynamic responses were examined in 25 patients with moderate to severe congestive heart failure. The dose range from 10 to 60 mg was studied. Elimination half-life for this dose range was substantially longer than that previously reported in normal volunteers. Total area under the curve increased in a curvilinear fashion with progressive dose increments, indicating a disproportionate increase in systemically available drug at higher doses. Hemodynamic responses generally correlated well with plasma nicorandil concentration, with rapid loss of cardiovascular activity corresponding to the efficient clearance of nicorandil.
ISSN:	0009-9236
DOI:	10.1038/clpt.1992.177