A Comprehensive Insight on Pharmacological Properties of Cilnidipine: A Fourth-generation Calcium Channel Blocker

Preventing the development of cardiovascular problems is a key objective of antihypertensive drugs. Many of the non-pressure related coronary risk factors for hypertension are thought to be connected to an increase in sympathetic activity. The sympathetic systems have N-type calcium channels at the nerve terminals that control neurotransmitter release. Cilnidipine is a unique fourth-generation calcium channel blocker with blocking action on both L-/N- type calcium channels. Several L-type calcium channel blockers (Nilvadipine, amlodipine, azelnidipine, nifedipine, etc.) have been used to treat hypertensive patients. Cilnidipine is a novel drug that exerts a hypotensive effect through vasodilation action via blocking L-type calcium channels and potent antisympathetic activity via blocking N-type calcium channels. Inhibiting N-type calcium channels might be a new approach to treating cardiovascular disorders. Therefore, it is expected that cilnidipine may respond well to complicated hypertension. The present review aims to describe the management mechanism of hypertension, and other pharmacological and physicochemical properties of cilnidipine. Cilnidipine has various other beneficial effects such as lipid-lowering effect, reduced white coat effect, improves insulin sensitivity in essential hypertensive patients, ameliorates osteoporosis in ovariectomized hypertensive rats, reduced arterial stiffness, reduced the risk of pedal edema, antinociceptive effects, neuroprotective and renal protective effect, probably through inhibition of N-type calcium channels. Cilnidipine distinguishes itself from other calcium channel blockers due to its wide range of beneficial pharmacological effects. In conclusion, cilnidipine may be more advantageous than other dihydropyridines, such as nisoldipine, amlodipine, azelnidipine, and other antihypertensive drugs.