Zolmitriptan is a potent selective 5HT1B/1D receptor agonist for acute migraine 
therapy. Zolmitriptan has vasoconstrictor activity in cerebral vessels and may 
cause slight elevations of blood pressure in subjects without hypertension. 
Therefore, the pharmacokinetics and pharmacodynamics of zolmitriptan (5, 10, and 
20 mg) were evaluated in 16 patients with mild to moderate hypertension 
(controlled by hydrochlorothiazide 50 mg once daily) and 17 healthy age- and 
sex-matched control subjects in a randomized, placebo-controlled, double-blind, 
four-period crossover study. The pharmacokinetics of zolmitriptan and its 
metabolites were dose proportional. Although area under the concentration-time 
curve (AUC0-infinity) and maximum concentration (Cmax) were slightly higher in 
patients with hypertension at all doses, this was only statistically significant 
for AUC at the 20-mg dose. Differences between subjects with and without 
hypertension were not clinically significant. Zolmitriptan produced a small 
increase in blood pressure, but this was similar in subjects with and without 
hypertension and was of no clinical significance. Zolmitriptan was well 
tolerated in both groups. Zolmitriptan plasma concentrations were higher in 
women than in men, with higher values of AUC and Cmax and lower total clearance 
in women. These results indicate that zolmitriptan can be administered for 
treatment of migraine in patients with controlled hypertension without dose 
adjustment.