Cilnidipine (INN) is a calcium channel blocker. It is sold as Atelec in Japan, as CILACAR (Cilnidipine 5mg, 10mg, 20mg) in India by JB CHEMICALS & PHARMACEUTICALS LTD., since 2007. If you are in INDIA, ask for CILACAR.
Cilnidipine is a dual blocker of L-type voltage-gated calcium channels in vascular smooth muscle and N-type calcium channels in sympathetic nerve terminals that supply blood vessels. However, the clinical benefits of cilnidipine and underlying mechanisms are incompletely understood.
Clinidipine is the novel calcium antagonist accompanied with L-type and N-type calcium channel blocking function. It was jointly developed by Fuji Viscera Pharmaceutical Company, Japan and Ajinomoto, Japan and approved to come into market for the first time and used for high blood pressure treatment in 1995. Compared with other calcium antagonists, clinidipine can act on the N-type calcium-channel that existing sympathetic nerve end besides acting on L-type calcium-channel that similar to most of the calcium antagonists. Due to its N-type calcium-channel blocking properties, it has more advantages compared to conventional calcium-channel blockers. It has lower incidence of Pedal edema, one of the major adverse effects of other calcium channel blockers. Cilnidipine has similar blood pressure lowering efficacy as compared to amlodipine. One of the distinct property of cilnidipine from amlodipine is that it does not cause reflex tachycardia.
CILNIDIPINE (Cilacar) ADVANTAGES OVER AMLODIPINE
One of the main advantage of CILNIDIPINE is it REDUCES THE INCIDENCE OF PEDAL EDEMA UNLIKE AMLODIPINE
L-type calcium channel blocker (Amlodipine) dilates the only arterioles & not the venules, hence blood pressure increases in the capillary bed and are thought to cause leg edema.
CILNIDIPINE (Cilacar) due to its blocking action at N-type calcium channel dilates both arteriole & venules as a result the pressure in the capillary bed is reduces. The accumulated fluid in the tissues flows back to veins & thus Cilacar minimizes the incidence of pedal edema.
Superior Clinical Benefits
Cilnidipine controls hypertension for 24 hours with once daily dose. Cilnidipine has enhanced lipophilicity leading to prolonged antihypertensive effect correlated with occupancy of the binding site. In 24 hour clinical assessment, once-daily administration of cilnidipine (5–20 mg) produced BP reduction for 24 hour period. This indicates that once-daily cilnidipine exerts a sufficient and prolonged reduction of BP.2 Cilnidipine has 50 times higher selectivity for N-type of calcium channels than amlodipine. The inhibitory effect on the N-type Ca2+channel may bestow an additional clinical advantage for the treatment of hypertension, such as suppression of reflex tachycardia.3
As catecholamines induce platelet activation via alpha 2-receptors on platelet membrane, decrease in norepinephrine level by cilnidipine (absent in amlodipine) causes attenuation of platelet activation.
Cilnidipine significantly decreased urinary albumin excretion without affecting serum creatinine concentration in hypertensive patients.11 Cilnidipine is superior to amlodipine in preventing the progression of proteinuria in patients with hypertension and chronic renal disease.1 Cilnidipine suppresses the development of proteinuria greater than amlodipine through inhibiting N-type calcium channel-dependent podocyte injury.12 Cilnidipine leads to less activation of the RAS compared with amlodipine for the first time in human clinical patients and therefore cilnidipine might be expected to be superior in organ protection in addition to the antialbuminuric effect.13 Cilnidipine inhibits proliferation of vascular smooth muscle cells through inhibition of DNA/ RNA synthesis induced by growth-promoting factors released during atherosclerosis.
"PLEIOTROPIC EFFECTS of CILNIDIPINE (CILACAR"
Improves baroreflex sensitivity
Improves NO availability
Ensures Antiproliferative effect
Inhibition of platelet activity
Exerts Antiarrhythmic effect
Reduction in Serum uric acid