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Abstract
1. The pharmacokinetics of bucindolol and its major metabolite, 5-hydroxybucindolol, have been studied in eight patients with mild/moderate hypertension.
2. The mean terminal elimination half-life of bucindoiol following acute oral dosing was 8·0 · 4·5 h, while the elimination half-life of the metabolite was 0·15 · 0·13 h.
3. Because of the large intraindividual variation in the pharmacokinetics of the drug and metabolite, no significant differences in the kinetics following acute or chronic dosing were seen.
4. There was very wide interindividual variability in the pharmacokinetics of bucindoiol and 5-hydroxybucindolol, and large interindividual differences in the metabolic profiles as assessed by the areas under drug and metabolite concentration-time curves. This latter observation might be associated with a genetic polymorphism of drug metabolism.