A randomized, open-label, two-way crossover study of 24 normotensive, healthy male volunteers with nocturia was conducted to compare morning and evening administration of doxazosin in terms of pharmacokinetics and tolerance. In both the morning and evening phases, participants received doxazosin 1 mg once daily for 10 days, followed by 2 mg once daily for 5 days. Pharmacokinetic data were evaluated from blood samples serially collected for 72 hours after drug administration on the last day of each phase. Vital signs and adverse events were recorded throughout the study. Mean peak plasma concentrations (C(max)) were 16.98 and 15.76 ng/mL after morning and evening administration, respectively. Corresponding mean values of area under the plasma concentration-time curve (AUC0-24) were 227.90 and 253.66 ng.hr/mL, respectively. Statistical analysis of the log-transformed values for C(max) and AUC0-24 indicated that morning and evening administration of doxazosin were bioequivalent. There were no statistically or clinically significant differences between phases for mean apparent half-life (t1/2) or total body clearance. There were no clinically relevant differences in blood pressure or in pulse rate between phases, and no occurrences of orthostatic hypotension. The incidence of adverse experiences during morning and evening administration was similar. Morning and evening administration of doxazosin are equivalent and have similar tolerance profiles.