New Generation Calcium Channel Blockers in Hypertensive Treatment

Yuri      Ozawa; Koichi      Hayashi; Hiroyuki      Kobori

doi:10.2174/157340206776877370

Abstract

During a couple of decades, a number of antihypertensive drugs have been developed, and the choice of hypertension treatment has been expanded. Among antihypertensive drugs, calcium channel blockers, which inhibit Ltype voltage-gated calcium channels, are potent vasodilators, and have been used as a first- or second-line drug. Dihydropyridine-class calcium channel blockers are categorized into three generations according to the length of activity, and long-acting calcium channel blockers cause less activation of sympathetic nervous system, and are reported to offer beneficial action compared with short-action agents. Furthermore, novel types of calcium channel blockers have been developed that possess the blocking action on other calcium channel subtypes (T- and N-type), and exert agent-specific action apart from their class effects, such as the effects on heart rate and renin/aldosterone release. These additional benefits conferred by T/N-type calcium channel blockade are anticipated to provide organ protective actions in the treatment of hypertension, in addition to the blood pressure-lowering effect of L-type calcium channel blockade. In conclusion, novel calcium channel blockers with sustained activity and T/N-type calcium channel blocking action could provide more beneficial effects than classical blockers, and may expand the clinical utility of these agents.

Keywords: N-type calcium channels, T-type calcium channels, tachycardia, heart failure, renal protection