We evaluated the long-term
antihypertensive effects of
ketanserin, a selective serotonin2-receptor blocker with weak
adrenergic receptor blocker properties.
Ketanserin was given alone, 40 mg o.d. or b.i.d., for 2 years to 12 patients with
essential hypertension. Systolic and diastolic blood pressures (BPs) were significantly reduced 14 days after the start of
therapy and remained lowered during the 2-year follow-up period. In a larger group of patients who received
ketanserin monotherapy for 2 to 3 months, the response to
therapy varied considerably between subjects, with an overall response rate (BP less than 165/95 mm Hg) of 60% to 75%. During steady-state conditions, the maximum and minimum
ketanserin plasma concentrations varied from threefold to fourfold between subjects and did not correlate with individual reductions in BP, but for each individual there was a positive correlation between BP reduction and
ketanserin plasma concentration throughout a study day. In combination with beta-blockers,
ketanserin effectively reduced BP in the supine and standing positions. The plasma concentration profile was not altered as much during combination
therapy as when
ketanserin was given alone. Side effects were few and tolerable.
Ketanserin effectively reduces BP both alone and in combination with beta-blockers and may be still another
drug useful in the treatment of
essential hypertension.