Title:A Comprehensive Insight on Pharmacological Properties of Cilnidipine: A
Fourth-generation Calcium Channel Blocker
Volume: 22
Issue: 1
Author(s): Renu Kadian and Arun Nanda*
Affiliation:
- Department of Pharmaceutical Sciences, MDU, Rohtak, Haryana, India
Keywords:
Calcium channel blocker, cilnidipine, dihydropyridine, fourth generation calcium channel blocker, hypertension, metabolism, N-type calcium channel blocker.
Abstract: 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.