Cilnidipine

Cilnidipine

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Systematic (IUPAC) name
3-(E)-3-Phenyl-2-propenyl 5-2-methoxyethyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Clinical data
Trade names	Atelec (アテレック), Cilogard
AHFS/Drugs.com	International Drug Names
Identifiers
CAS Number	132203-70-4
ATC code	C08CA14 (WHO)
PubChem	CID: 5282138
IUPHAR/BPS	7767
ChemSpider	4445338
UNII	97T5AZ1JIP Y
KEGG	D01173
Chemical data
Formula	C27H28N2O7
Molecular mass	492.52 g/mol
SMILES O=C(OCCOC)\C2=C(\N/C(=C(/C(=O)OC\C=C\c1ccccc1)C2c3cccc([N+]([O-])=O)c3)C)C

Cilnidipine (INN) is a calcium channel blocker. Cilnidipine 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, cilnidipine 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.

Cilnidipine is approved for use in Japan, China,India, Korea and some European countries.

Medical uses

Cilnidipine due to its blocking action at N-type and L type calcium channel dilates both arterioles and venules as a result the pressure in the capillary bed is reduced. It is used for hypertension management.

Adverse effects

Peripheral edema a common side effect of the use of amlodipine was found to be reduced when patients were shifted to cilnidipine.

Clinical Benefits

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 produced blood pressuree reduction for 24-hour period. 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.

As catecholamines induce platelet activation via α₂-receptor on platelet membrane, decrease in norepinephrine level by cilnidipine causes attenuation of platelet activation.

Brand names

In India it is marketed by J.B. Chemicals and Pharmacists Ltd under the brand name Cilacar.

External links

• http://www.mcyy.com.cn/e-product2.asp
• 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