Peringatan Keamanan

As with any calcium channel blocker toxicity, bradycardia and hypotension may result from overdose. The treatment of patients with bradycardia and hypotension begins with supportive therapy and atropine, however, patients with severe toxicity do not have an adequate response and must be managed more aggressively.

Calcium plays an imperative role in myocardial contractility, automaticity and vascular tone. Administration of exogenous calcium is of benefit in cases of toxicity L1384.

Azelnidipine

DB09230

small molecule investigational

Deskripsi

Azelnidipine is a dihydropyridine calcium channel blocker. It is marketed by Daiichi-Sankyo pharmaceuticals, Inc. in Japan. It has a gradual onset of action and produces a long-lasting decrease in blood pressure, with only a small increase in heart rate, unlike some other calcium channel blockers L1379. It is currently being studied for post-ischemic stroke management L1380.

Struktur Molekul 2D

Berat 582.657
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 16 –28 hours [L1383].
Volume Distribusi In a Chinese study examining the pharmacokinetics of the drug, the volume of distribution was found to be 1749 +/- 964 [L1383].
Klirens (Clearance) -

Absorpsi

Oral ingestion of azelnidipine demonstrates rapid and dose-dependent absorption L1382.

Metabolisme

Like most members of its class, azelnidipine primarily undergoes first-pass hepatic metabolism. Azelnidipine is metabolized by hepatic cytochrome P450 (CYP) 3A4 and has no active metabolite product. It may interact with other drugs or compounds that are substrates for this enzyme. Azelnidipine is lipophilic and has a potent affinity for membranes of vascular smooth muscle cells L1382.

Rute Eliminasi

In one study, following a single 4mg oral dose of 14C-labeled azelnidipine in humans, about 26% of the drug was thought to br excreted in the urine and 63% in the feces during the 1 week period post administration A31944.

Interaksi Obat

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

Target Protein

Voltage-dependent L-type calcium channel subunit beta-1 CACNB1

Referensi & Sumber

Synthesis reference: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4245158/
Artikel (PubMed)
  • PMID: 2810942
    Oizumi K, Nishino H, Koike H, Sada T, Miyamoto M, Kimura T: Antihypertensive effects of CS-905, a novel dihydropyridine Ca++ channel blocker. Jpn J Pharmacol. 1989 Sep;51(1):57-64.
  • PMID: 18193691
    Nada T, Nomura M, Koshiba K, Kawano T, Mikawa J, Ito S: Clinical study with azelnidipine in patients with essential hypertension. Antiarteriosclerotic and cardiac hypertrophy-inhibitory effects and influence on autonomic nervous activity. Arzneimittelforschung. 2007;57(11):698-704. doi: 10.1055/s-0031-1296670.

Contoh Produk & Brand

Produk: 0 • International brands: 14
International Brands
  • Azelnidipine Chemipha
  • Azelnidipine FFP
  • Azelnidipine JG
  • Azelnidipine KOG
  • Azelnidipine Nichi-Iko
  • Azelnidipine Tanabe
  • Azelnidipine TCK
  • Azelnidipine Teva
  • Azelnidipine Towa
  • Azelnidipine YD

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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