Mibefradil: A New Selective T-Channel Calcium Antagonist for Hypertension and Angina Pectoris.

Abstract

Calcium antagonists are an established therapy for patients with hypertension and angina pectoris, but their current usage is often limited by their pharmacologic profilers and side effects. Mibefradil is a recently developed calcium antagonist with a unique chemical structure, site of action, and set of pharmacologic effects. Unlike currently available calcium channels as well as L-type channels. It is further distinguished from the other calcium antagonists in that it is the first member of a new class of calcium antagonists, the tetralol derivatives. With chronic oral dosing, mibefradil attains steady-state plasma concentrations within 3-4 days, has a bioavailability of approximately 90%, and a plasma half-life of 17-25 hours. It has a gradual onset of action and can be administered once daily without regard to food intake. It increases coronary blood flow and lowers peripheral vascular resistance. The vasodilatory effects of mibefradil are associated with a lack of inotropic effect on myocardium, lack of neurohormonal activation, and a reduction in heart rate. In clinical trials it has been demonstrated to be an effective agent in the treatment of patients with hypertension and angina pectoris, with a good safety and tolerability profile regardless of age, gender, or race.