Pharmacological, pharmacokinetic, and clinical properties of benidipine hydrochloride, a novel, long-acting calcium channel blocker.
Benidipine is a dihydropyridine-derived calcium channel blocker developed in Japan, with several unique mechanisms of action, that is, triple calcium channels (L, N, and T) blocking action with a membrane approach. Benidipine has relatively high vascular selectivity and is expected to show protective effects on vascular endothelial cells. Renal protective effects of benidipine also have been shown in several basic and clinical studies. Moreover, anti-oxidative action and enhancing nitric oxide production have been noted with this drug, following its cardio-protective effects in patients with ischemic heart diseases. In fact, benidipine exerted a better prognostic effect than other calcium channel blockers in the therapy for patients with vasospastic angina. In addition, benidipine showed reliable antihypertensive, renoprotective effects if used in combination with angiotensin II type 1 receptor blockers (ARBs) when adequate anti-hypertensive effects are not achieved by ARBs alone, indicating that benidipine is an useful calcium channel blocker in combination therapy for hypertension. Benidipine was launched on the Japanese market 14 years ago, but few severe side effects have been reported, suggesting that this is a drug with established safety and long-acting pharmacological effects.
Department of Pharmacology and Molecular Biology, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd., Japan.
Kozo
K
Yao
Ken
K
Nagashima
Hiroyuki
H
Miki
D000787:Angina Pectoris / Q000188:drug therapy; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects*; D002121:Calcium Channel Blockers / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D020746:Calcium Channels, L-Type / Q000187:drug effects; D020864:Calcium Channels, N-Type / Q000187:drug effects; D020747:Calcium Channels, T-Type / Q000187:drug effects; D002986:Clinical Trials as Topic; D003928:Diabetic Nephropathies / Q000188:drug therapy; D004095:Dihydropyridines / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D042783:Endothelial Cells / Q000187:drug effects; D006321:Heart / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000188:drug therapy; D007668:Kidney / Q000098:blood supply / Q000187:drug effects; D012079:Renal Circulation; D014665:Vasodilator Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use
D002121:Calcium Channel Blockers; D020746:Calcium Channels, L-Type; D020864:Calcium Channels, N-Type; D020747:Calcium Channels, T-Type; D004095:Dihydropyridines; D014665:Vasodilator Agents; C061004:benidipine