Cilnidipine
Clinical data | |
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Trade names | Atelec (アテレック), Cilacar |
AHFS/Drugs.com | International Drug Names |
ATC code | C08CA14 (WHO) |
Identifiers | |
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CAS Number | 132203-70-4 |
PubChem (CID) | 5282138 |
IUPHAR/BPS | 7767 |
ChemSpider | 4445338 |
UNII | 97T5AZ1JIP |
KEGG | D01173 |
ECHA InfoCard | 100.162.338 |
Chemical and physical data | |
Formula | C27H28N2O7 |
Molar mass | 492.52 g/mol |
3D model (Jmol) | Interactive image |
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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 Bangladesh it is marketed by The ACME Laboratories Ltd. under the brand name DUOCARD, available as both 5 mg & 10 mg and Opsonin Pharma Ltd. under the brand name CILDIP and is available in the two strengths 5 mg & 10 mg Tablet. In India it is marketed by JBCPL under the brand name CILACAR and is available in the three strengths, 5 mg, 10 mg, 20 mg & combinations also availlable CILACAR T, CILACAR T80, CILACAR M, CILACAR C12.5, CILACAR C6.25, CILACAR TC12.5, CILACAR TC6.25. In Japan it is marketed BY Ajinomoto Pharmaceuticals Co., Ltd.under the brand name Atelec. In usa it is available in different brands whose central ingredients are CILNIDIPINE like-ATELEC & CILACAR (Ref: 20)
References
External links
- 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 20. http://buymedicinesx.com/buycilacarpricesideeffects2/