Description
Efonidipine hydrochloride ethanol was first launched in Japan for the treatment of
essential severe and renal hypertension. As the fourteenth dihydropyridine (DHP)
calcium channel blocker to reach the market, it functions by binding to the DHP
receptors on voltage-dependent calcium channels to cause diuretic and natriuretic
actions in patients with essential hypertension. Its vasodilating and calcium
antagonist effects are very slow in onset and long-lasting in all types of
experimentally hypertensive models and the agent is reported to exhibit an improved
side effect profile compared with other drugs of the same class. This may be
explained by the slow and long-lasting inhibition of transmembrane Ca
+2 uptake,
which is accompanied by its very slow binding to and dissociation from the DHP
receptors. A recent study in cholesterol-fed rabbits suggested that efonidipine may
suppress the development of atherosclerosis without affecting the plasma lipids.
Clinical trials for angina, peetoris, and for cerebrovasodilatory disorders have been
reported.
Biological Activity
Selective blocker of L-type and T-type Ca 2+ channels. Displays minimal inhibition of N- and P/Q-type channels and no inhibition of R-type channels. R (-) and S (+)-enantiomers displays different channel selectivity; S (+)-Efonidipine blocks L-type and T-type channels whereas R (-)-Efonidipine displays selectivity for T-type channels. Exhibits antihypertensive activity.
