Peringatan Keamanan

The percentage of reports of cilnidipine that express drug toxicity reported as side effects are 5.26%.L1454

Cilnidipine

DB09232

small molecule investigational

Deskripsi

Cilnidipine is a dihydropyridine calcium antagonist. It was jointly developed by Fuji Viscera Pharmaceutical Company, Japan and Ajinomoto, Japan and approved 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. This drug is approved in China, Japan, Korea, India, and several countries in the European Union.A31970

Struktur Molekul 2D

Berat 492.528
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of the hypotensive effect for cilnidipine is of about 20.4 min.[A32004]
Volume Distribusi Drugs on the group of dihydropyridines such as cilnidipine tend to have a large volume of distribution.[T119]
Klirens (Clearance) -

Absorpsi

Cilnidipine presents a very rapid absorption with a maximum peaked concentration after 2 hours. Its distribution tends to be higher in the liver as well as in kidneys, plasma and other tissues. Cilnidipine does not present a high accumulation in the tissue after repeated oral administration.L1444 Cilnidipine is reported to present very low bioavailability determined to be approximately 13%. This low bioavailability is suggested to be due to its low aqueous solubility and high permeability. Hence, efforts have been made in order to find an innovative formulation that can significantly improve the bioavailability of this drug. One of these formulations corresponds to the generation of polymeric nanoparticles which enhance the bioavailability by 2.5-3-fold.L6124

Metabolisme

Cilnidipine is metabolized by both liver and kidney. It is rapidly metabolized by liver microsomes by a dehydrogenation process. The major enzymatic isoform involved in cilnidipine dehydrogenation of the dihydropyridine ring is CYP3A.L1440

Rute Eliminasi

Cilnidipine gets eliminated through the urine in a proportion of 20% of the administered dose and 80% is eliminated by the feces.L1440

Interaksi Obat

909 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Cilnidipine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Cilnidipine is combined with Levodopa.
Risperidone Cilnidipine may increase the hypotensive activities of Risperidone.
Ceritinib Cilnidipine may increase the bradycardic activities of Ceritinib.
Ivabradine Cilnidipine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Cilnidipine.
Cimetidine The serum concentration of Cilnidipine can be increased when it is combined with Cimetidine.
Clopidogrel The therapeutic efficacy of Clopidogrel can be decreased when used in combination with Cilnidipine.
Efavirenz The serum concentration of Cilnidipine can be decreased when it is combined with Efavirenz.
Melatonin The therapeutic efficacy of Cilnidipine can be decreased when used in combination with Melatonin.
Nafcillin The therapeutic efficacy of Cilnidipine can be decreased when used in combination with Nafcillin.
Nitroprusside Cilnidipine may increase the hypotensive activities of Nitroprusside.
Dantrolene The risk or severity of hyperkalemia can be increased when Dantrolene is combined with Cilnidipine.
Lithium citrate The risk or severity of adverse effects can be increased when Cilnidipine is combined with Lithium citrate.
Lithium carbonate The risk or severity of adverse effects can be increased when Cilnidipine is combined with Lithium carbonate.
Lithium hydroxide The risk or severity of adverse effects can be increased when Cilnidipine is combined with Lithium hydroxide.
Boceprevir The serum concentration of Cilnidipine can be increased when it is combined with Boceprevir.
Nicorandil Nicorandil may increase the hypotensive activities of Cilnidipine.
Ibutilide Ibutilide may increase the arrhythmogenic activities of Cilnidipine.
Hyoscyamine Hyoscyamine may increase the arrhythmogenic activities of Cilnidipine.
Atropine Atropine may increase the arrhythmogenic activities of Cilnidipine.
Adenosine Adenosine may increase the arrhythmogenic activities of Cilnidipine.
Moricizine Moricizine may increase the arrhythmogenic activities of Cilnidipine.
Procainamide Procainamide may increase the arrhythmogenic activities of Cilnidipine.
Tocainide Tocainide may increase the arrhythmogenic activities of Cilnidipine.
Flecainide Flecainide may increase the arrhythmogenic activities of Cilnidipine.
Encainide Encainide may increase the arrhythmogenic activities of Cilnidipine.
Ajmaline Ajmaline may increase the arrhythmogenic activities of Cilnidipine.
Aprindine Aprindine may increase the arrhythmogenic activities of Cilnidipine.
Azimilide Azimilide may increase the arrhythmogenic activities of Cilnidipine.
Tedisamil Tedisamil may increase the arrhythmogenic activities of Cilnidipine.
Vernakalant Vernakalant may increase the arrhythmogenic activities of Cilnidipine.
Cariporide Cariporide may increase the arrhythmogenic activities of Cilnidipine.
Xylometazoline Xylometazoline may increase the arrhythmogenic activities of Cilnidipine.
Sparteine Sparteine may increase the arrhythmogenic activities of Cilnidipine.
Fasudil Fasudil may increase the arrhythmogenic activities of Cilnidipine.
Melperone Melperone may increase the arrhythmogenic activities of Cilnidipine.
Carteolol Cilnidipine may increase the arrhythmogenic activities of Carteolol.
Metipranolol Cilnidipine may increase the arrhythmogenic activities of Metipranolol.
Tropisetron Cilnidipine may increase the arrhythmogenic activities of Tropisetron.
Simendan Cilnidipine may increase the arrhythmogenic activities of Simendan.
Spiradoline Cilnidipine may increase the arrhythmogenic activities of Spiradoline.
Pilsicainide Cilnidipine may increase the arrhythmogenic activities of Pilsicainide.
Cibenzoline Cilnidipine may increase the arrhythmogenic activities of Cibenzoline.
Nizofenone Cilnidipine may increase the arrhythmogenic activities of Nizofenone.
Prajmaline Cilnidipine may increase the arrhythmogenic activities of Prajmaline.
Tiracizine Cilnidipine may increase the arrhythmogenic activities of Tiracizine.
Ethacizine Cilnidipine may increase the arrhythmogenic activities of Ethacizine.
Lorajmine Cilnidipine may increase the arrhythmogenic activities of Lorajmine.
Bunaftine Cilnidipine may increase the arrhythmogenic activities of Bunaftine.
Lorcainide Cilnidipine may increase the arrhythmogenic activities of Lorcainide.
Hydroquinine Cilnidipine may increase the arrhythmogenic activities of Hydroquinine.
Bioallethrin Cilnidipine may increase the arrhythmogenic activities of Bioallethrin.
Fosfructose Cilnidipine may increase the arrhythmogenic activities of Fosfructose.
Hydroquinidine Cilnidipine may increase the arrhythmogenic activities of Hydroquinidine.
SOR-C13 Cilnidipine may increase the arrhythmogenic activities of SOR-C13.
Digoxin Digoxin may increase the arrhythmogenic activities of Cilnidipine.
Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Cilnidipine.
Deslanoside Deslanoside may increase the arrhythmogenic activities of Cilnidipine.
Cymarin Cilnidipine may increase the arrhythmogenic activities of Cymarin.
Metildigoxin Cilnidipine may increase the arrhythmogenic activities of Metildigoxin.
Acetyldigoxin Cilnidipine may increase the arrhythmogenic activities of Acetyldigoxin.
Niguldipine Cilnidipine may increase the arrhythmogenic activities of Niguldipine.
Levosimendan Levosimendan may increase the arrhythmogenic activities of Cilnidipine.
Isradipine Isradipine may increase the arrhythmogenic activities of Cilnidipine.
Diltiazem Diltiazem may increase the arrhythmogenic activities of Cilnidipine.
Trimethadione Trimethadione may increase the arrhythmogenic activities of Cilnidipine.
Amlodipine Amlodipine may increase the arrhythmogenic activities of Cilnidipine.
Nimodipine Nimodipine may increase the arrhythmogenic activities of Cilnidipine.
Lercanidipine Lercanidipine may increase the arrhythmogenic activities of Cilnidipine.
Lamotrigine Lamotrigine may increase the arrhythmogenic activities of Cilnidipine.
Cinnarizine Cinnarizine may increase the arrhythmogenic activities of Cilnidipine.
Nicardipine Nicardipine may increase the arrhythmogenic activities of Cilnidipine.
Verapamil Verapamil may increase the arrhythmogenic activities of Cilnidipine.
Losartan Losartan may increase the arrhythmogenic activities of Cilnidipine.
Levomenthol Levomenthol may increase the arrhythmogenic activities of Cilnidipine.
Zonisamide Zonisamide may increase the arrhythmogenic activities of Cilnidipine.
Nitrendipine Nitrendipine may increase the arrhythmogenic activities of Cilnidipine.
Perhexiline Perhexiline may increase the arrhythmogenic activities of Cilnidipine.
Bepridil Bepridil may increase the arrhythmogenic activities of Cilnidipine.
Nimesulide Nimesulide may increase the arrhythmogenic activities of Cilnidipine.
Prenylamine Prenylamine may increase the arrhythmogenic activities of Cilnidipine.
Cyclandelate Cyclandelate may increase the arrhythmogenic activities of Cilnidipine.
Flunarizine Flunarizine may increase the arrhythmogenic activities of Cilnidipine.
Fluspirilene Fluspirilene may increase the arrhythmogenic activities of Cilnidipine.
Clevidipine Clevidipine may increase the arrhythmogenic activities of Cilnidipine.
Methsuximide Methsuximide may increase the arrhythmogenic activities of Cilnidipine.
Seletracetam Seletracetam may increase the arrhythmogenic activities of Cilnidipine.
Nylidrin Nylidrin may increase the arrhythmogenic activities of Cilnidipine.
Ziconotide Ziconotide may increase the arrhythmogenic activities of Cilnidipine.
Dotarizine Dotarizine may increase the arrhythmogenic activities of Cilnidipine.
Nilvadipine Nilvadipine may increase the arrhythmogenic activities of Cilnidipine.
Tranilast Tranilast may increase the arrhythmogenic activities of Cilnidipine.
Agmatine Agmatine may increase the arrhythmogenic activities of Cilnidipine.
Fendiline Fendiline may increase the arrhythmogenic activities of Cilnidipine.
Eperisone Eperisone may increase the arrhythmogenic activities of Cilnidipine.
Trimebutine Trimebutine may increase the arrhythmogenic activities of Cilnidipine.
Pinaverium Pinaverium may increase the arrhythmogenic activities of Cilnidipine.
Barnidipine Barnidipine may increase the arrhythmogenic activities of Cilnidipine.
Aranidipine Aranidipine may increase the arrhythmogenic activities of Cilnidipine.

Target Protein

Voltage-dependent N-type calcium channel subunit alpha-1B CACNA1B
Voltage-dependent L-type calcium channel CACNA1C

Referensi & Sumber

Artikel (PubMed)
  • PMID: 1881002
    Yoshimoto R, Dohmoto H, Yamada K, Goto A: Prolonged inhibition of vascular contraction and calcium influx by the novel 1,4-dihydropyridine calcium antagonist cinaldipine (FRC-8653). Jpn J Pharmacol. 1991 Jun;56(2):225-9.
  • PMID: 25336921
    Lee J, Lee H, Jang K, Lim KS, Shin D, Yu KS: Evaluation of the pharmacokinetic and pharmacodynamic drug interactions between cilnidipine and valsartan, in healthy volunteers. Drug Des Devel Ther. 2014 Oct 8;8:1781-8. doi: 10.2147/DDDT.S68574. eCollection 2014.
  • PMID: 10408255
    Uneyama H, Uchida H, Konda T, Yoshimoto R, Akaike N: Selectivity of dihydropyridines for cardiac L-type and sympathetic N-type Ca2+ channels. Eur J Pharmacol. 1999 May 28;373(1):93-100.
Textbook
  • Henrich W. (2012). Principles and practice of dialysis. Lippincott, Williams & Wilkins.

Contoh Produk & Brand

Produk: 0 • International brands: 2
International Brands
  • Atelec — Ajinomoto Pharmaceuticals Co. Ltd
  • Cilogard — Cipla Ltd

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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