Pharmacological, pharmacokinetic, and clinical properties of benidipine hydrochloride, a novel, long-acting calcium channel blocker.

Article Details

Citation

Yao K, Nagashima K, Miki H

Pharmacological, pharmacokinetic, and clinical properties of benidipine hydrochloride, a novel, long-acting calcium channel blocker.

J Pharmacol Sci. 2006 Apr;100(4):243-61. Epub 2006 Mar 25.

PubMed ID
16565579 [ View in PubMed
]
Abstract

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.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
BenidipineVoltage-dependent L-type calcium channel (Protein Group)Protein groupHumans
Yes
Antagonist
Details
BenidipineVoltage-dependent N-type calcium channel subunit alpha-1BProteinHumans
Yes
Antagonist
Details
BenidipineVoltage-dependent T-type calcium channel (Protein Group)Protein groupHumans
Yes
Antagonist
Details
Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
BenidipineCytochrome P450 3A4ProteinHumans
No
Substrate
Inhibitor
Details
BenidipineCytochrome P450 3A5ProteinHumans
No
Substrate
Details