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{{short description|Antihypertensive drug of the calcium channel blocker class}}
{{Drugbox
{{Drugbox
| IUPAC_name = 3-(''E'')-3-Phenyl-2-propenyl 5-2-methoxyethyl 2,6-dimethyl-4-(''m''-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
| IUPAC_name = 3-(''E'')-3-Phenyl-2-propenyl 5-2-methoxyethyl 2,6-dimethyl-4-(''m''-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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<!--Clinical data-->
<!--Clinical data-->
| tradename = Atelec (アテレック), Cilacar
| tradename = Atelec (アテレック), Cilaheart, Cilacar
| Drugs.com = {{drugs.com|international|cilnidipine}}
| Drugs.com = {{drugs.com|international|cilnidipine}}
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
Line 39: Line 40:
| chemical_formula =
| chemical_formula =
| C=27 | H=28 | N=2 | O=7
| C=27 | H=28 | N=2 | O=7
| molecular_weight = 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
| smiles = O=C(OCCOC)\C2=C(\N/C(=C(/C(=O)OC\C=C\c1ccccc1)C2c3cccc([N+]([O-])=O)c3)C)C
}}
}}
<!-- Definition and medical uses -->
<!-- Definition and medical uses -->
'''Cilnidipine''' is a [[calcium channel blocker]]. Cilnidipine is approved for use in Japan, China, India, Korea, and some European countries to treat [[hypertension]].
'''Cilnidipine''' is a [[calcium channel blocker]]. Cilnidipine is approved for use in Japan, China, India, Nepal, and Korea for [[hypertension]].


<!-- Side effects and mechanisms -->
<!-- Side effects and mechanisms -->
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<!-- Society and culture -->
<!-- Society and culture -->
It was patented in 1984 and approved for medical use in 1995.<ref>{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=466 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA466 |language=en}}</ref>
It was patented in 1984 and approved for medical use in 1995. Cilnidipine is currently being repurposed and developed for use in patients with Raynaud's Phenomenon and Systemic Sclerosis by Aisa Pharma, a US biopharma development company.<ref>{{cite book | vauthors = Fischer J, Ganellin CR |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=466 |url=https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA466 |language=en}}</ref>


== Medical uses ==
== Medical uses ==
Cilnidipine decreases blood pressure and is used to treat hypertension and its [[Comorbidity|comorbidities]]. Due to its blocking action at the <small>N</small>-type and <small>L</small>-type calcium channel, cilnidipine dilates both [[arteriole]]s and [[venule]]s, 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.
Cilnidipine decreases blood pressure and is used to treat hypertension and its [[Comorbidity|comorbidities]]. Due to its blocking action at the <small>N</small>-type and <small>L</small>-type calcium channel, cilnidipine dilates both [[arteriole]]s and [[venule]]s, 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.<ref>{{Cite journal | doi=10.1080/10641963.2016.1235183| pmid=28448181|title = Blood pressure control with cilnidipine treatment in Japanese post-stroke hypertensive patients: The CA-ATTEND study| journal=Clinical and Experimental Hypertension| volume=39| issue=3| pages=225–234|year = 2017|last1 = Aoki|first1 = Shiro| last2=Hosomi| first2=Naohisa| last3=Nezu| first3=Tomohisa| last4=Teshima| first4=Tsukasa| last5=Sugii| first5=Hitoshi| last6=Nagahama| first6=Shinobu| last7=Kurose| first7=Yoshiki| last8=Maruyama| first8=Hirofumi| last9=Matsumoto| first9=Masayasu}}</ref>
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.<ref>{{cite journal | vauthors = Aoki S, Hosomi N, Nezu T, Teshima T, Sugii H, Nagahama S, Kurose Y, Maruyama H, Matsumoto M | display-authors = 6 | title = Blood pressure control with cilnidipine treatment in Japanese post-stroke hypertensive patients: The CA-ATTEND study | journal = Clinical and Experimental Hypertension | volume = 39 | issue = 3 | pages = 225–234 | year = 2017 | pmid = 28448181 | doi = 10.1080/10641963.2016.1235183 | doi-access = free }}</ref>
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.<ref>{{cite journal|title=The Effects of the L / N‐Type Calcium Channel Blocker (Cilnidipine) on Sympathetic Hyperactive Morning Hypertension: Results From ACHIEVE‐ONE* |first1=Kazuomi |last1=Kario |first2=Shin‐ichi |last2=Ando |first3=Hidenori |last3=Kido|first4=Jin |last4=Nariyama |first5=Shin |last5=Takiuchi |first6=Tetsuo|last6=Yagi |first7=Toshiki|last7=Shimizu|first8=Kazuo|last8=Eguchi|first9=Minoru|last9=Ohno|first10=Osamu|last10=Kinoshita|first11=Takahisa|last11=Yamada|date=1 February 2013|journal=The Journal of Clinical Hypertension|volume=15|issue=2|pages = 133–142|doi=10.1111/jch.12042|pmid=23339732 }}</ref>
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. Cilnidipine is currently being studied in the RECONNOITER study in Australia for its effect on Raynaud's and other manifestations of disease in patients with Systemic Sclerosis. <ref>{{cite journal | vauthors = Kario K, Ando S, Kido H, Nariyama J, Takiuchi S, Yagi T, Shimizu T, Eguchi K, Ohno M, Kinoshita O, Yamada T | display-authors = 6 | title = The effects of the L/N-type calcium channel blocker (cilnidipine) on sympathetic hyperactive morning hypertension: results from ACHIEVE-ONE | journal = Journal of Clinical Hypertension | volume = 15 | issue = 2 | pages = 133–42 | date = February 2013 | pmid = 23339732 | doi = 10.1111/jch.12042 | pmc = 8034443 }}</ref><ref>{{cite web | url=https://www.anzctr.org.au/Trial/Registration/TrialReview.aspx?id=380810&isReview=true | title=ANZCTR - Registration }}</ref>


== Side effects ==
== 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.
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.<ref>{{Cite journal|last=Minami|first=Junichi|last2=Kawano|first2=Yuhei|last3=Makino|first3=Yuriko|last4=Matsuoka|first4=Hiroaki|last5=Takishita|first5=Shuichi|date=2017-05-01|title=Effects of cilnidipine, a novel dihydropyridine calcium antagonist, on autonomic function, ambulatory blood pressure and heart rate in patients with essential hypertension|journal=British Journal of Clinical Pharmacology|volume=50|issue=6|pages=615–620|doi=10.1046/j.1365-2125.2000.00299.x|issn=0306-5251|pmc=2015014|pmid=11136301}}</ref>
[[Peripheral edema]], a common side effect from the use of [[amlodipine]], was reduced when patients were shifted to cilnidipine.<ref>{{cite journal | vauthors = Minami J, Kawano Y, Makino Y, Matsuoka H, Takishita S | title = Effects of cilnidipine, a novel dihydropyridine calcium antagonist, on autonomic function, ambulatory blood pressure and heart rate in patients with essential hypertension | journal = British Journal of Clinical Pharmacology | volume = 50 | issue = 6 | pages = 615–20 | date = December 2000 | pmid = 11136301 | pmc = 2015014 | doi = 10.1046/j.1365-2125.2000.00299.x }}</ref>

== Brand Name ==
In India, it is sold under the brand name Cinod, cilacar, clinblue, cilaheart among others at doses of 5mg/10mg/20mg.<ref>{{cite web | url=https://medicaldialogues.in/partner/jbcpl/cilacar-cilnidipine | title=Cilacar (Cilnidipine): Uses, Side Effects, Dosage - Medical Dialogues | publisher=[[Medical Dialogues]] | date=3 March 2021 | access-date=3 March 2021}}</ref>


==History==
==History==
It was jointly developed by [[Fuji Viscera Pharmaceutical Company]] and [[Ajinomoto]],<nowiki/> and was approved to enter the market and be used as an [[anti-hypertensive]] in 1995.{{citation needed|date=August 2017}}
It was jointly developed by [[Fuji Viscera Pharmaceutical Company]] and [[Ajinomoto]],<nowiki/> and was approved to enter the market and be used as an [[anti-hypertensive]] in 1995.{{citation needed|date=August 2017}}


== Brand names ==
== References ==
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==
{{Reflist}}
{{Reflist}}


== Further reading ==
==External links==
{{refbegin}}
*{{cite journal |vauthors=Löhn M, Muzzulini U, Essin K |title=Cilnidipine is a novel slow-acting blocker of vascular L-type calcium channels that does not target protein kinase C |journal=J. Hypertens. |volume=20 |issue=5 |pages=885–93 |date=May 2002 |pmid=12011649 |doi= 10.1097/00004872-200205000-00023|url=|display-authors=etal}}
* {{cite journal | vauthors = Löhn M, Muzzulini U, Essin K, Tsang SY, Kirsch T, Litteral J, Waldron P, Conrad H, Klugbauer N, Hofmann F, Haller H, Luft FC, Huang Y, Gollasch M | display-authors = 6 | title = Cilnidipine is a novel slow-acting blocker of vascular L-type calcium channels that does not target protein kinase C | journal = Journal of Hypertension | volume = 20 | issue = 5 | pages = 885–93 | date = May 2002 | pmid = 12011649 | doi = 10.1097/00004872-200205000-00023 | s2cid = 30765257 }}
* 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.
{{refend}}
{{Calcium channel blockers}}


[[Category:Aldosterone synthase inhibitors]]
[[Category:Calcium channel blockers]]
[[Category:Calcium channel blockers]]
[[Category:Dihydropyridines]]
[[Category:Dihydropyridines]]
[[Category:Nitro compounds]]
[[Category:3-Nitrophenyl compounds]]
[[Category:Carboxylate esters]]
[[Category:Carboxylate esters]]
[[Category:Ethers]]
[[Category:Ethers]]

Latest revision as of 05:58, 3 December 2024

Cilnidipine
Clinical data
Trade namesAtelec (アテレック), Cilaheart, Cilacar
AHFS/Drugs.comInternational Drug Names
ATC code
Identifiers
  • 3-(E)-3-Phenyl-2-propenyl 5-2-methoxyethyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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 mass492.528 g·mol−1
3D model (JSmol)
  • O=C(OCCOC)\C2=C(\N/C(=C(/C(=O)OC\C=C\c1ccccc1)C2c3cccc([N+]([O-])=O)c3)C)C

Cilnidipine is a calcium channel blocker. Cilnidipine is approved for use in Japan, China, India, Nepal, and Korea for 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. Cilnidipine is currently being repurposed and developed for use in patients with Raynaud's Phenomenon and Systemic Sclerosis by Aisa Pharma, a US biopharma development company.[1]

Medical uses

[edit]

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.[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. Cilnidipine is currently being studied in the RECONNOITER study in Australia for its effect on Raynaud's and other manifestations of disease in patients with Systemic Sclerosis. [3][4]

Side effects

[edit]

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.[5]

Brand Name

[edit]

In India, it is sold under the brand name Cinod, cilacar, clinblue, cilaheart among others at doses of 5mg/10mg/20mg.[6]

History

[edit]

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]

References

[edit]
  1. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 466. ISBN 9783527607495.
  2. ^ Aoki S, Hosomi N, Nezu T, Teshima T, Sugii H, Nagahama S, et al. (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 K, Ando S, Kido H, Nariyama J, Takiuchi S, Yagi T, et al. (February 2013). "The effects of the L/N-type calcium channel blocker (cilnidipine) on sympathetic hyperactive morning hypertension: results from ACHIEVE-ONE". Journal of Clinical Hypertension. 15 (2): 133–42. doi:10.1111/jch.12042. PMC 8034443. PMID 23339732.
  4. ^ "ANZCTR - Registration".
  5. ^ Minami J, Kawano Y, Makino Y, Matsuoka H, Takishita S (December 2000). "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): 615–20. doi:10.1046/j.1365-2125.2000.00299.x. PMC 2015014. PMID 11136301.
  6. ^ "Cilacar (Cilnidipine): Uses, Side Effects, Dosage - Medical Dialogues". Medical Dialogues. 3 March 2021. Retrieved 3 March 2021.

Further reading

[edit]
  • Löhn M, Muzzulini U, Essin K, Tsang SY, Kirsch T, Litteral J, et al. (May 2002). "Cilnidipine is a novel slow-acting blocker of vascular L-type calcium channels that does not target protein kinase C". Journal of Hypertension. 20 (5): 885–93. doi:10.1097/00004872-200205000-00023. PMID 12011649. S2CID 30765257.
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