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Cilnidipine

Cilnidipine
Cilnidipine.svg
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 Edit this at Wikidata
Chemical and physical data
FormulaC27H28N2O7
Molar mass492.52 g/mol g·mol−1
3D model (JSmol)

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

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]

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 ilnidipine was effective in treating uncontrolled blood pressure and was well tolerated in post-stroke hypertensive patients.[2] 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.[3]

Side effects

The side effects could be severe diziness, 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.[4]

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.[citation needed]

Brand names

In India, cilnidipine is marketed by Systopic Laboratories Pvt. Ltd. under the brand name CILDAY, available as both 5mg and 10mg. In India, Systopic Laboratories Pvt. Ltd. provides most economical choice for the patients of hypertension. CILDAY is available at most affordable prices as INR 2.7/tab for 5mg and INR 4.3/tab for 10mg.

References

  1. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 466. ISBN 9783527607495.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.

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.
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