Peringatan Keamanan

Common adverse effects include lethargy, back pain, chest pain, infection, feeling of weakness. In the cardiovascular system, hypotension, increased heart rate in higher doses, palpitations, worsened angina pectoris and vasodilation/flush may be observed. Dyspepsia, nausea, and vomiting may occur as gastrointestinal disorders. Headaches may arise from vasodilation. Other common side effects include myalgia, bronchitis, dyspnoea, and respiratory disorder L887. Nicorandil does not affect fertility of male or female rats, and shows no potential in carcinogenic, mutagenic or genotoxic studies L887. Oral LD50 values in mouse, rat and dog are 626 mg/kg, 1220 mg/kg and 62.5 mg/kg, respectively MSDS.

Nicorandil

DB09220

small molecule approved investigational

Deskripsi

Nicorandil is an orally efficacious vasodilatory drug and antianginal agent marketed in the UK, Australia, most of Europe, India, Philippines, Japan, South Korea, and Taiwan. It is not an approved drug by FDA. It is a niacinamide derivative that induces vasodilation of arterioles and large coronary arteries by activating potassium channels. It is often used for patients with angina who remain symptomatic despite optimal treatment with other antianginal drugs T28. Nicorandil is a dual-action potassium channel opener that relaxes vascular smooth muscle through membrane hyperpolarization via increased transmembrane potassium conductance and increased intracellular concentration of cyclic GMP. It is shown to dilate normal and stenotic coronary arteries and reduces both ventricular preload and afterload A20325.

Struktur Molekul 2D

Berat 211.177
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life is approximately 1 hour [A20328].
Volume Distribusi After oral (and i.v.) administration of the drug, the apparent volume of distribution is approximately 1.0-1.4 L/kg body weight [A20328].
Klirens (Clearance) The total body clearance is approximately 1.15 L/min [A20328].

Absorpsi

Following oral administration, nicorandil is well absorbed from the gastrointestinal tract with the oral bioavailability of 75% with the maximum peak plasma concentration (Cmax) reached within 30-60 minutes. The mean Cmax is Cmax then is approximately 300 ng/ml A20328. Steady-state plasma concentrations of nicorandil usually are reached within approximately 96-120 h after twice daily dosing (10 or 20mg) L887.

Metabolisme

Nicorandil undergoes extensive hepatic metabolism L887. The main biotransformation pathways of nicorandil are denitration, followed by subsequent nicotinamide metabolism. The main pharmacologically inactive denitrated metabolite 2-nicotinamidoethanol can be detected in the urine. The derivatives formed from the nicotinamide metabolism of denitrated products are nicotinuric acid, nicotinamide, N-methylnicotinamide and nicotinic acid L887.

Rute Eliminasi

The main route of elimination is the kidney with more than 60% of the administered dose was eliminated in the urine 24 hours after dosing L887. Only approximately 1% of nicorandil is excreted unchanged in the urine, and the remaining compounds are mainly the denitrated metabolite (9%) and its derivatives (e.g. nicotinuric acid 6%, nicotinamide 1%, N-methylnicotinamide < 1% and nicotinic acid < 1%) L887. Less than 2% of administered dose is excreted through the biliary system A20328.

Interaksi Obat

1313 Data
Alfuzosin Alfuzosin may increase the hypotensive activities of Nicorandil.
Amifostine Nicorandil may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Nicorandil.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Nicorandil.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Nicorandil.
Obinutuzumab Nicorandil may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Nicorandil.
Rituximab Nicorandil may increase the hypotensive activities of Rituximab.
Phentermine Phentermine may decrease the antihypertensive activities of Nicorandil.
Midodrine Midodrine may decrease the antihypertensive activities of Nicorandil.
Eletriptan Eletriptan may decrease the antihypertensive activities of Nicorandil.
Isoetharine Isoetharine may decrease the antihypertensive activities of Nicorandil.
Methysergide Methysergide may decrease the antihypertensive activities of Nicorandil.
Cabergoline Cabergoline may decrease the antihypertensive activities of Nicorandil.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Nicorandil.
Dihydroergotamine Dihydroergotamine may decrease the antihypertensive activities of Nicorandil.
Methylergometrine Methylergometrine may decrease the antihypertensive activities of Nicorandil.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Nicorandil.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Nicorandil.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Nicorandil.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Nicorandil.
Promazine Promazine may decrease the antihypertensive activities of Nicorandil.
Droperidol Droperidol may decrease the antihypertensive activities of Nicorandil.
Doxapram Doxapram may decrease the antihypertensive activities of Nicorandil.
Lisuride Lisuride may decrease the antihypertensive activities of Nicorandil.
Metaraminol Metaraminol may decrease the antihypertensive activities of Nicorandil.
Trazodone Trazodone may decrease the antihypertensive activities of Nicorandil.
Epinephrine Epinephrine may decrease the antihypertensive activities of Nicorandil.
Ergotamine Ergotamine may decrease the antihypertensive activities of Nicorandil.
Nicergoline Nicergoline may decrease the antihypertensive activities of Nicorandil.
Methoxamine Methoxamine may decrease the antihypertensive activities of Nicorandil.
Risperidone Risperidone may decrease the antihypertensive activities of Nicorandil.
Propiomazine Propiomazine may decrease the antihypertensive activities of Nicorandil.
Alfentanil Alfentanil may decrease the antihypertensive activities of Nicorandil.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Nicorandil.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Nicorandil.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Nicorandil.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Nicorandil.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Nicorandil.
Ritodrine Ritodrine may decrease the antihypertensive activities of Nicorandil.
Flupentixol Flupentixol may decrease the antihypertensive activities of Nicorandil.
Bitolterol Bitolterol may decrease the antihypertensive activities of Nicorandil.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Nicorandil.
Salmeterol Salmeterol may decrease the antihypertensive activities of Nicorandil.
Naratriptan Naratriptan may decrease the antihypertensive activities of Nicorandil.
Formoterol Formoterol may decrease the antihypertensive activities of Nicorandil.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Nicorandil.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Nicorandil.
Ergoloid mesylate Ergoloid mesylate may decrease the antihypertensive activities of Nicorandil.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Nicorandil.
Arbutamine Arbutamine may decrease the antihypertensive activities of Nicorandil.
Dutasteride Dutasteride may decrease the antihypertensive activities of Nicorandil.
Pergolide Pergolide may decrease the antihypertensive activities of Nicorandil.
Finasteride Finasteride may decrease the antihypertensive activities of Nicorandil.
Ergometrine Ergometrine may decrease the antihypertensive activities of Nicorandil.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Nicorandil.
Fenoterol Fenoterol may decrease the antihypertensive activities of Nicorandil.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Nicorandil.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Nicorandil.
Ephedrine Ephedrine may decrease the antihypertensive activities of Nicorandil.
Mephentermine Mephentermine may decrease the antihypertensive activities of Nicorandil.
Procaterol Procaterol may decrease the antihypertensive activities of Nicorandil.
Yohimbine Yohimbine may decrease the antihypertensive activities of Nicorandil.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Nicorandil.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Nicorandil.
Bambuterol Bambuterol may decrease the antihypertensive activities of Nicorandil.
MMDA MMDA may decrease the antihypertensive activities of Nicorandil.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Nicorandil.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Nicorandil.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Nicorandil.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Nicorandil.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Nicorandil.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Nicorandil.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Nicorandil.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Nicorandil.
Solifenacin Solifenacin may decrease the antihypertensive activities of Nicorandil.
Periciazine Periciazine may decrease the antihypertensive activities of Nicorandil.
Acepromazine Acepromazine may decrease the antihypertensive activities of Nicorandil.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Nicorandil.
Zuclopenthixol Zuclopenthixol may decrease the antihypertensive activities of Nicorandil.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Nicorandil.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Nicorandil.
Lysergic acid diethylamide Lysergic acid diethylamide may decrease the antihypertensive activities of Nicorandil.
Flibanserin Flibanserin may decrease the antihypertensive activities of Nicorandil.
Iloperidone Iloperidone may decrease the antihypertensive activities of Nicorandil.
Indacaterol Indacaterol may decrease the antihypertensive activities of Nicorandil.
Amibegron Amibegron may decrease the antihypertensive activities of Nicorandil.
Naluzotan Naluzotan may decrease the antihypertensive activities of Nicorandil.
Cariprazine Cariprazine may decrease the antihypertensive activities of Nicorandil.
Mianserin Mianserin may decrease the antihypertensive activities of Nicorandil.
Pizotifen Pizotifen may decrease the antihypertensive activities of Nicorandil.
Solabegron Solabegron may decrease the antihypertensive activities of Nicorandil.
Asenapine Asenapine may decrease the antihypertensive activities of Nicorandil.
Esmirtazapine Esmirtazapine may decrease the antihypertensive activities of Nicorandil.
Vilazodone Vilazodone may decrease the antihypertensive activities of Nicorandil.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Nicorandil.
Isometheptene Isometheptene may decrease the antihypertensive activities of Nicorandil.
Levonordefrin Levonordefrin may decrease the antihypertensive activities of Nicorandil.
Naphazoline Naphazoline may decrease the antihypertensive activities of Nicorandil.
Tetryzoline Tetryzoline may decrease the antihypertensive activities of Nicorandil.

Target Protein

ATP-binding cassette sub-family C member 9 ABCC9

Referensi & Sumber

Artikel (PubMed)
  • PMID: 1282168
    Kukovetz WR, Holzmann S, Poch G: Molecular mechanism of action of nicorandil. J Cardiovasc Pharmacol. 1992;20 Suppl 3:S1-7.
  • PMID: 12770942
    Russ U, Lange U, Loffler-Walz C, Hambrock A, Quast U: Binding and effect of K ATP channel openers in the absence of Mg2+. Br J Pharmacol. 2003 May;139(2):368-80.
  • PMID: 15102948
    Yamada M, Kurachi Y: The nucleotide-binding domains of sulfonylurea receptor 2A and 2B play different functional roles in nicorandil-induced activation of ATP-sensitive K+ channels. Mol Pharmacol. 2004 May;65(5):1198-207.
  • PMID: 22622455
    Tamura Y, Tanabe K, Kitagawa W, Uchida S, Schreiner GF, Johnson RJ, Nakagawa T: Nicorandil, a K(atp) channel opener, alleviates chronic renal injury by targeting podocytes and macrophages. Am J Physiol Renal Physiol. 2012 Aug 1;303(3):F339-49. doi: 10.1152/ajprenal.00158.2012. Epub 2012 May 23.
  • PMID: 8982500
    Fujiwara T, Angus JA: Analysis of relaxation and repolarization mechanisms of nicorandil in rat mesenteric artery. Br J Pharmacol. 1996 Dec;119(8):1549-56.
  • PMID: 15953614
    Jahangir A, Terzic A: K(ATP) channel therapeutics at the bedside. J Mol Cell Cardiol. 2005 Jul;39(1):99-112.
  • PMID: 15910878
    Kane GC, Liu XK, Yamada S, Olson TM, Terzic A: Cardiac KATP channels in health and disease. J Mol Cell Cardiol. 2005 Jun;38(6):937-43. Epub 2005 Apr 25.
  • PMID: 1281076
    Frampton J, Buckley MM, Fitton A: Nicorandil. A review of its pharmacology and therapeutic efficacy in angina pectoris. Drugs. 1992 Oct;44(4):625-55.
Menampilkan 8 dari 10 artikel.
Textbook
  • ISBN: 978-0-7020-3471-8
    21. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 261). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 0 • International brands: 27
International Brands
  • Adancor — Merck
  • Angedil — Egis Pharmaceuticals
  • Angicor — Sanofi-Aventis
  • Aprior — OEP Phils
  • Av-Cor — Strides Arcolab
  • Corangi — Unimed & Unihealth
  • Cordinik — PIQ-Farma
  • Corflo — Wockhardt
  • Dancor — Merck
  • Ikorel — Sanofi

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul