Ketanserin: a novel cardiovascular drug.

Ketanserin is the archetype of a new class of cardiovascular drugs, the 5HT2 (S2) serotonergic receptor antagonists. In humans, ketanserin inhibits serotonin-induced vasoconstriction and platelet activation. In addition, it reduces platelet hyperactivity, blood viscosity and total serum cholesterol. The antihypertensive effect of ketanserin is more pronounced in older people, in whom it decreases blood pressure gradually to normal levels. It lowers systemic vascular resistance resulting in a reduction of pre- and afterload. It improves vascular compliance and reduces left ventricular hypertrophy. Ketanserin improves the microcirculation of the skin, in particular capillary blood flow. Placebo-controlled studies have established that ketanserin prevents amputations in patients with atherosclerosis, enhances ulcer healing in patients with scleroderma and reduces the frequency and duration of attacks in patients with Raynaud's disease. In a placebo-controlled trial the on-treatment analysis of 3071 patients with intermittent claudication (the PACK-trial) showed a 23% reduction of severe cardiovascular events with ketanserin, suggesting that ketanserin may prevent complications of atherosclerosis. The accumulated clinical evidence indicates that serotonergic antagonism opens new perspectives in the treatment of cardiovascular disease. Current clinical research with ketanserin further explores its potential as a vascular protective agent.