Treatment of arterial hypertension with ketanserin in mono‐ and combination therapy

We evaluated the long‐term antihypertensive effects of ketanserin, a selective serotonin 2 ‐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 < 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 β‐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 β‐blockers and may be still another drug useful in the treatment of essential hypertension. Clinical Pharmacology and Therapeutics (1985) 38, 188–194; doi: 10.1038/clpt.1985.157