Cilnidipine

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Cilnidipine
Cilnidipine.svg
Systematic (IUPAC) name
O3-(2-methoxyethyl) O5-[(E)-3-phenylprop-2-enyl] 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine- 3,5-dicarboxylate
Clinical data
AHFS/Drugs.com International Drug Names
Legal status
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Identifiers
CAS number 132203-70-4
ATC code C08CA14
PubChem CID 5282138
ChemSpider 4445338
UNII 97T5AZ1JIP YesY
KEGG D01173
Chemical data
Formula C27H28N2O7 
Mol. mass 492.52 g/mol

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 yet to be approved by US FDA with Extensive studies and patient data still needing to be published on this molecule.

Medical uses[edit]

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 reduced. It is used for hypertension management.

Adverse effects[edit]

Common: peripheral edema was seen in 16% of the patients currently under treatment with Cilnidipine.[1] Cases of Cilnidipine induced Ankle Edema were also reported.

Clinical Benefits[edit]

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. 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 alpha 2-receptors on platelet membrane, decrease in norepinephrine level by cilnidipine causes attenuation of platelet activation.

References[edit]

External links[edit]

  • 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. doi:10.1097/00004872-200205000-00023. 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