|Systematic (IUPAC) name|
|O3-(2-methoxyethyl) O5-[(E)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine- 3,5-dicarboxylate|
|Mol. mass||492.52 g/mol|
Cilnidipine (INN) is a calcium channel blocker. It is sold as Atelec in Japan, & as CILACAR 5/10/20mg in India by JB CHEMICALS & PHARMACEUTICALS LTD (JBCPL) - UNIQUE since 2007. 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. JBCPL first introduced Cilnidipine in India as CILACAR 5/10/20mg way back in 2007. Effects of Cilnidipine CILACAR 5/10/20mg compels to rethink on hypertension management. CILNIDIPINE (CILACAR) ADVANTAGES OVER AMLODIPINE
The main advantages of CILNIDIPINE (Unlike Amlodipine) are
1) CILNIDIPINE REDUCES THE INCIDENCE OF PROTEINURIA - There by reduces chances of kidney damage. 2) CILNIDIPINE reduced PEDAL EDEMA due to its action on both arterioles and venules. (Amlodipine is L type only acts partially and not on both)
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 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 Cilnidipine minimizes the incidence of pedal edema.
SUPERIOR CLINICAL BENEFITS of CILNIDIPINE
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 CILACAR 5/10/20mg 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 RAAS compared with amlodipine and therefore cilnidipine might be expected to be superior in organ protection in addition to the anti-albuminuric 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 CILNIDIPINE COMPELS TO RETHINK ON HYPERTENSION MANAGEMENT Cilnidipine Improves baroreflex sensitivity, Improves NO availability, Ensures Antiproliferative effect, Inhibition of platelet activity, Exerts Antiarrhythmic effect, Reduction in Serum uric acid
- http://www.mcyy.com.cn/e-product2.asp[dead link]
- Löhn M, Muzzulini U, Essin K, et al. (May 2002). "Cilnidipine is a novel slow-acting blocker of vascular L-type calcium channels that does not target protein kinase C". J. Hypertens. 20 (5): 885–93. PMID 12011649.
- 1. Cardiovascular Therapeutics 27 (2009) 2. Cardiovascular Drugs and Therapy 1997 3. Can J Anesth. 2002. 4. Clinical and Experimental Hypertension,2009. 5. J Clin Hypertens (Greenwich). 2013 6. Hypertens Res 2003; 7. Journal of Diabetes Investigation; 2012.8 .Journal of Cardiology (2009) . 9 J Cardiovasc Pharmacol; 2007 10.J Cardiovasc Pharmacol 2004, 11 Antihypertensive Drug 2012, 12 J Hypertens. 2010 May. 13 J Hypertens. 2010 14 Hypertens Res. 2012 15 Diabetes Res Clin Pract. 2012 16 Neurochem Int. 2012 , 17 J. Neurochem. (2009) 18 Geriatr Gerontol Int 2008; , 19 Biol. Pharm. Bull. (2004), 20 Clin Calcium. 2010