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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/12/08 06:53:45」(JST)

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

References

External links

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

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English Journal

L/N-type calcium channel blocker cilnidipine added to Renin-Angiotensin inhibition improves ambulatory blood pressure profile and suppresses cardiac hypertrophy in hypertension with chronic kidney disease.

Kanaoka T, Tamura K, Wakui H, Ohsawa M, Azushima K, Uneda K, Kobayashi R, Fujikawa T, Tsurumi-Ikeya Y, Maeda A, Yanagi M, Toya Y, Umemura S.SourceDepartment of Medical Science and Cardiorenal Medicine, Graduate School of Medicine, Yokohama City University, 3-9 Fukuura, Kanazawa-ku, Yokohama 236-0004, Japan. tamukou@med.yokohama-cu.ac.jp.
International journal of molecular sciences.Int J Mol Sci.2013 Aug 16;14(8):16866-81. doi: 10.3390/ijms140816866.
Ambulatory blood pressure (BP) and heart rate (HR) profile are proposed to be related to renal deterioration and cardiovascular complication in hypertension and chronic kidney disease (CKD). In this study, we examined the beneficial effects cilnidipine, a unique L/N-type calcium channel blocker (CCB
PMID 23959116

Comparison of the Antialbuminuric Effects of L-/N-type and L-type Calcium Channel Blockers in Hypertensive Patients with Diabetes and Microalbuminuria: The Study of Assessment for Kidney Function by Urinary Microalbumin in Randomized (SAKURA) Trial.

Ando K, Ueshima K, Tanaka S, Kosugi S, Sato T, Matsuoka H, Nakao K, Fujita T.Source1. Department of Nephrology and Endocrinology, University of Tokyo Graduate School of Medicine, Tokyo, Japan.
International journal of medical sciences.Int J Med Sci.2013 Jul 30;10(9):1209-16. doi: 10.7150/ijms.5508. Print 2013.
Objective: To clarify whether the L-/N-type calcium channel blocker (CCB) cilnidipine is more renoprotective than the L-type CCB amlodipine in patients with early-stage diabetic nephropathy. Methods: In this prospective, multicenter, open-labeled, randomized trial, the antialbuminuric effects of cil
PMID 23935398

Effects of cilnidipine on sympathetic outflow and sympathetic arterial pressure and heart rate regulations in rats.

Yamamoto H, Kawada T, Shimizu S, Kamiya A, Miyazaki S, Sugimachi M.SourceDivision of Cardiology, Department of Medicine, Faculty of Medicine, Kinki University, Osaka 589-8511, Japan.
Life sciences.Life Sci.2013 Jul 10;92(24-26):1202-7. doi: 10.1016/j.lfs.2013.05.004. Epub 2013 May 18.
AIMS: Cilnidipine is a unique Ca(2+) channel blocker that inhibits both L-type and N-type Ca(2+) channels. The present study aimed to assess the effects of intravenous cilnidipine on sympathetic outflow and sympathetic arterial pressure (AP) and heart rate (HR) regulations.MAIN METHODS: Carotid sinu
PMID 23688866

Japanese Journal

Industrial Info. L/N型カルシウムチャネルブロッカー

細胞 47(7), 340-343, 2015-07
NAID 40020568881

The organ-protective effect of N-type Ca(2+) channel blockade.

Pharmacology & therapeutics 151, 1-7, 2015-07
NAID 120005663276

Development and Characterization of Solid Self-emulsifying Drug Delivery System of Cilnidipine

Chemical and Pharmaceutical Bulletin 63(6), 408-417, 2015
NAID 130005072106

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リンク元

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Cilnidipine
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
PubChem	CID: 5282138
IUPHAR/BPS	7767
ChemSpider	4445338
UNII	97T5AZ1JIP
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 ;

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英: cilnidipine
商: アテレック、シスカード、シナロング、アテディオ配合

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案内

cilnidipine