Pharmacokinetic and pharmacological properties of doxazosin mesilate in Japanese healthy adult volunteers.

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Pharmacokinetic and pharmacological effects and safety profile of doxazosin mesilate, a new quinazoline α1-adrenoceptor blocking agent, were studied in six Japanese healthy adult male volunteers. Doxazosin 0.5 mg, 1 mg, or 2 mg was orally administered at two-week intervals. The pharmacokinetic data were well fitted to a two-compartment model. Peak plasma concentrations of doxazosin were dosed-ependent and attained at 1 .6-1.7 hr after dosing. Mean terminal elimination half-lives were 15. 62±5. 12 hr for the 1 mg and 10. 14±3.32hr for the 2 mg. Blood pressure and pulse rate were determined in the sitting, supine, and 50° tilt positions. The maximal reduction of blood pressure was observed during 4-8 hr after adminis-tration, with a corresponding increase in heart rate. With the postural change from supine to 50° tilt position, the fall of systolic blood pressure was more pronounced in the tilt posture than in the supine position at 4-6 hr after dosing. During exercise with a bicycle ergometer, the exerciseinduced increases in heart rate and systolic blood pressure were attenuated with doxazosin. Three hours after administration, one of the six volunteers complained of dizziness while taking 0.5 mg and 2 mg tablets. Except for elevated serum triglyceride noticed, in one volunteer, notable abnormalities were not observed in laboratory findings .
一般社団法人日本臨床薬理学会の論文