Cilnidipine

Cilnidipine is a calcium channel blocker. Cilnidipine is approved for use in Japan, China, India, Korea, and some European countries to treat hypertension.

Cilnidipine
Clinical data
Trade namesAtelec (アテレック), Cilacar
AHFS/Drugs.comInternational Drug Names
ATC code
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard100.162.338
Chemical and physical data
FormulaC27H28N2O7
Molar mass492.528 g·mol−1
3D model (JSmol)

It is a calcium antagonist accompanied with L-type and N-type calcium channel blocking functions. Unlike other calcium antagonists, cilnidipine can act on the N-type calcium channel in addition to acting on the L-type calcium channel.

It was patented in 1984 and approved for medical use in 1995.[1] In India, the No 1 brand is CILACAR Marketed and manufactured by JB CHEMICALS AND PHARMACEUTICALS.[2] It is also available with a combination of Telmisartan by the name of CILACAR-T manufactured by the same company.[3]

Medical uses

Cilnidipine decreases blood pressure and is used to treat hypertension and its comorbidities. Due to its blocking action at the N-type and L-type calcium channel, cilnidipine dilates both arterioles and venules, reducing the pressure in the capillary bed. Cilnidipine is vasoselective and has a weak direct dromotropic effect, a strong vasodepressor effect, and an arrhythmia-inhibiting effect. Blood pressure control with cilnidipine treatment in Japanese post-stroke hypertensive patients [The CA-ATTEND study] - the results of a large-scale prospective post-marketing surveillance study of post-stroke hypertensive patients (n = 2667, male 60.4%, 69.0 ± 10.9 years) treated with cilnidipine indicate that cilnidipine was effective in treating uncontrolled blood pressure and was well tolerated in post-stroke hypertensive patients.[4] The Ambulatory Blood Pressure Control and Home Blood Pressure (Morning and Evening) Lowering By N-Channel Blocker Cilnidipine (ACHIEVE-ONE) trial is a large-scale (n=2319) clinical study on blood pressure (BP) and pulse rate (PR) in the real world with use of cilnidipine - this study revealed that Cilnidipine significantly reduced BP and PR in hypertensive patients at the clinic and at home, especially with higher BP and PR in the morning.[5]

Side effects

The side effects could be severe dizziness, fast heartbeat, and swelling of face, lips, tongue, eyelids, hands and feet. Lesser side effects include stomach pain, diarrhea and hypotension.

Peripheral edema, a common side effect from the use of amlodipine, was reduced when patients were shifted to cilnidipine.[6]

History

It was jointly developed by Fuji Viscera Pharmaceutical Company and Ajinomoto, and was approved to enter the market and be used as an anti-hypertensive in 1995.

Brand names

In India, the No 1 brand is CILACAR Marketed and manufactured by JB CHEMICALS AND PHARMACEUTICALS.

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References
  1. Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 466. ISBN 9783527607495.
  2. "Cilacar (Cilnidipine)- Physician Information Page". Medical Dialogues. 1 July 2020. Retrieved 1 July 2020.
  3. "Cilacar T (Cilnidipine-Telmisartan)-Physician Information Page". Medical Dialogues. 1 July 2020. Retrieved 1 July 2020.
  4. Aoki, Shiro; Hosomi, Naohisa; Nezu, Tomohisa; Teshima, Tsukasa; Sugii, Hitoshi; Nagahama, Shinobu; Kurose, Yoshiki; Maruyama, Hirofumi; Matsumoto, Masayasu (2017). "Blood pressure control with cilnidipine treatment in Japanese post-stroke hypertensive patients: The CA-ATTEND study". Clinical and Experimental Hypertension. 39 (3): 225–234. doi:10.1080/10641963.2016.1235183. PMID 28448181.
  5. Kario, Kazuomi; Ando, Shin‐ichi; Kido, Hidenori; Nariyama, Jin; Takiuchi, Shin; Yagi, Tetsuo; Shimizu, Toshiki; Eguchi, Kazuo; Ohno, Minoru; Kinoshita, Osamu; Yamada, Takahisa (1 February 2013). "The Effects of the L / N‐Type Calcium Channel Blocker (Cilnidipine) on Sympathetic Hyperactive Morning Hypertension: Results From ACHIEVE‐ONE*". The Journal of Clinical Hypertension. 15 (2): 133–142. doi:10.1111/jch.12042. PMID 23339732.
  6. Minami, Junichi; Kawano, Yuhei; Makino, Yuriko; Matsuoka, Hiroaki; Takishita, Shuichi (2017-05-01). "Effects of cilnidipine, a novel dihydropyridine calcium antagonist, on autonomic function, ambulatory blood pressure and heart rate in patients with essential hypertension". British Journal of Clinical Pharmacology. 50 (6): 615–620. doi:10.1046/j.1365-2125.2000.00299.x. ISSN 0306-5251. PMC 2015014. PMID 11136301.
  • 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. Hyper tens 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.
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