Peringatan Keamanan

Ivabradine may cause fetal toxicity when administered to pregnant women. Animal studies in pregnant rats have shown embryo-fetal toxicity and cardiac teratogenic effects. Effective contraception in women is recommended while using ivabradine.

Ivabradine

DB09083

small molecule approved

Deskripsi

Ivabradine is a novel heart rate lowering medicine for the symptomatic management of stable angina pectoralis and symptomatic chronic heart failure. Ivabradine, brand name Corlanor, was approved by the FDA in April 2015 for the treatment of chronic heart failure in patients with an ejection fraction of ?35%, in sinus rhythm with resting heart rate ?70 beats per minute, who are not on beta-blockers due to contraindications or already receiving maximum beta-blocker dose. Recently a new indication was added to treat symptomatic heart failure from dilated cardiomyopathy for patients 6 months or more in ageLabel. Ivabradine acts by selectively inhibiting the "funny" channel pacemaker current (If) in the sinoatrial node in a dose-dependent fashion, resulting in a lower heart rate and thus more blood to flow to the myocardium. Although non-dihydropyridine calcium channel blockers and beta blockers also effectively lower heart rate, they exhibit adverse events due to their negative ionotropic effects. Therefore, as ivabradine is designed as a "pure" heart rate-lowering drug by selectively acting on the If channels, it may offer a more favorable side effect profile due to its lower likelihood of causing serious adverse effects.

Struktur Molekul 2D

Berat 468.594
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2 hours.
Volume Distribusi ~100 L.
Klirens (Clearance) Total clearance is about 400ml/min; renal clearance about 70ml/min. About 4% is excreted unchanged in urine.

Absorpsi

It is recommended to take ivabradine with food to reduce variability in systemic exposure. Administration with food slows absorption by 1 hour, but increases systemic absorption by 20-30%. Ivabradine's oral bioavailability is about 40%.

Metabolisme

Ivabradine is extensively metabolized by oxidation in the gut and liver by cytochrome P450 3A4 enzyme. Its active metabolite, N-desmethylated derivative, is also metabolized by CYP 3A4. Ivabradine's affinity for CYP 3A4 is low, making it unlikely to affect the metabolism of other drugs; however potent inhibitors or inducers of CYP 3A4 may affect ivabradine's plasma concentration and pharmacodynamic effects and should not be co-administered.

Rute Eliminasi

Metabolites are equally excreted in feces and urine.

Interaksi Makanan

1 Data
  • 1. Avoid grapefruit products.

Interaksi Obat

539 Data
Leuprolide Ivabradine may increase the QTc-prolonging activities of Leuprolide.
Goserelin Ivabradine may increase the QTc-prolonging activities of Goserelin.
Azithromycin Ivabradine may increase the QTc-prolonging activities of Azithromycin.
Moxifloxacin Ivabradine may increase the QTc-prolonging activities of Moxifloxacin.
Ranolazine Ivabradine may increase the QTc-prolonging activities of Ranolazine.
Sulfisoxazole Ivabradine may increase the QTc-prolonging activities of Sulfisoxazole.
Amitriptyline Ivabradine may increase the QTc-prolonging activities of Amitriptyline.
Methadone Ivabradine may increase the QTc-prolonging activities of Methadone.
Sulpiride Ivabradine may increase the QTc-prolonging activities of Sulpiride.
Promazine Ivabradine may increase the QTc-prolonging activities of Promazine.
Prochlorperazine Ivabradine may increase the QTc-prolonging activities of Prochlorperazine.
Droperidol Ivabradine may increase the QTc-prolonging activities of Droperidol.
Imipramine Ivabradine may increase the QTc-prolonging activities of Imipramine.
Chlorpromazine Ivabradine may increase the QTc-prolonging activities of Chlorpromazine.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Ivabradine.
Fluorouracil Ivabradine may increase the QTc-prolonging activities of Fluorouracil.
Perflutren Ivabradine may increase the QTc-prolonging activities of Perflutren.
Atropine Ivabradine may increase the QTc-prolonging activities of Atropine.
Chloroquine Ivabradine may increase the QTc-prolonging activities of Chloroquine.
Efavirenz Ivabradine may increase the QTc-prolonging activities of Efavirenz.
Adenosine Ivabradine may increase the QTc-prolonging activities of Adenosine.
Pentamidine Ivabradine may increase the QTc-prolonging activities of Pentamidine.
Gadobenic acid Ivabradine may increase the QTc-prolonging activities of Gadobenic acid.
Carbinoxamine Ivabradine may increase the QTc-prolonging activities of Carbinoxamine.
Dolasetron Ivabradine may increase the QTc-prolonging activities of Dolasetron.
Roxithromycin Ivabradine may increase the QTc-prolonging activities of Roxithromycin.
Nalidixic acid Ivabradine may increase the QTc-prolonging activities of Nalidixic acid.
Cinoxacin Ivabradine may increase the QTc-prolonging activities of Cinoxacin.
Granisetron Ivabradine may increase the QTc-prolonging activities of Granisetron.
Ondansetron Ivabradine may increase the QTc-prolonging activities of Ondansetron.
Levosimendan Ivabradine may increase the QTc-prolonging activities of Levosimendan.
Mesoridazine Ivabradine may increase the QTc-prolonging activities of Mesoridazine.
Desloratadine Ivabradine may increase the QTc-prolonging activities of Desloratadine.
Telithromycin Ivabradine may increase the QTc-prolonging activities of Telithromycin.
Lomefloxacin Ivabradine may increase the QTc-prolonging activities of Lomefloxacin.
Dimenhydrinate Ivabradine may increase the QTc-prolonging activities of Dimenhydrinate.
Papaverine Ivabradine may increase the QTc-prolonging activities of Papaverine.
Chlorpheniramine Ivabradine may increase the QTc-prolonging activities of Chlorpheniramine.
Levofloxacin Ivabradine may increase the QTc-prolonging activities of Levofloxacin.
Gemifloxacin Ivabradine may increase the QTc-prolonging activities of Gemifloxacin.
Ofloxacin Ivabradine may increase the QTc-prolonging activities of Ofloxacin.
Flecainide Ivabradine may increase the QTc-prolonging activities of Flecainide.
Clarithromycin Ivabradine may increase the QTc-prolonging activities of Clarithromycin.
Levacetylmethadol Ivabradine may increase the QTc-prolonging activities of Levacetylmethadol.
Saquinavir Ivabradine may increase the QTc-prolonging activities of Saquinavir.
Clomipramine Ivabradine may increase the QTc-prolonging activities of Clomipramine.
Probucol Ivabradine may increase the QTc-prolonging activities of Probucol.
Aceprometazine Ivabradine may increase the QTc-prolonging activities of Aceprometazine.
Terlipressin Ivabradine may increase the QTc-prolonging activities of Terlipressin.
Lofexidine Ivabradine may increase the QTc-prolonging activities of Lofexidine.
Azimilide Ivabradine may increase the QTc-prolonging activities of Azimilide.
Pracinostat Ivabradine may increase the QTc-prolonging activities of Pracinostat.
Technetium Tc-99m ciprofloxacin Ivabradine may increase the QTc-prolonging activities of Technetium Tc-99m ciprofloxacin.
Garenoxacin Ivabradine may increase the QTc-prolonging activities of Garenoxacin.
Tedisamil Ivabradine may increase the QTc-prolonging activities of Tedisamil.
Tucidinostat Ivabradine may increase the QTc-prolonging activities of Tucidinostat.
Telavancin Ivabradine may increase the QTc-prolonging activities of Telavancin.
Pazopanib Ivabradine may increase the QTc-prolonging activities of Pazopanib.
Nemonoxacin Ivabradine may increase the QTc-prolonging activities of Nemonoxacin.
Panobinostat Ivabradine may increase the QTc-prolonging activities of Panobinostat.
Antazoline Ivabradine may increase the QTc-prolonging activities of Antazoline.
Bedaquiline The risk or severity of QTc prolongation can be increased when Ivabradine is combined with Bedaquiline.
Butriptyline Ivabradine may increase the QTc-prolonging activities of Butriptyline.
Lenvatinib Ivabradine may increase the QTc-prolonging activities of Lenvatinib.
Melperone Ivabradine may increase the QTc-prolonging activities of Melperone.
Dexchlorpheniramine maleate Ivabradine may increase the QTc-prolonging activities of Dexchlorpheniramine maleate.
Amifampridine Ivabradine may increase the QTc-prolonging activities of Amifampridine.
Mocetinostat Ivabradine may increase the QTc-prolonging activities of Mocetinostat.
Entinostat Ivabradine may increase the QTc-prolonging activities of Entinostat.
Gilteritinib Ivabradine may increase the QTc-prolonging activities of Gilteritinib.
CUDC-101 Ivabradine may increase the QTc-prolonging activities of CUDC-101.
Simendan Ivabradine may increase the QTc-prolonging activities of Simendan.
Ricolinostat Ivabradine may increase the QTc-prolonging activities of Ricolinostat.
Mizolastine Ivabradine may increase the QTc-prolonging activities of Mizolastine.
Abexinostat Ivabradine may increase the QTc-prolonging activities of Abexinostat.
Oxatomide Ivabradine may increase the QTc-prolonging activities of Oxatomide.
Sitafloxacin Ivabradine may increase the QTc-prolonging activities of Sitafloxacin.
Sultopride Ivabradine may increase the QTc-prolonging activities of Sultopride.
Nizofenone Ivabradine may increase the QTc-prolonging activities of Nizofenone.
Bunaftine Ivabradine may increase the QTc-prolonging activities of Bunaftine.
Lorcainide Ivabradine may increase the QTc-prolonging activities of Lorcainide.
Dexchlorpheniramine Ivabradine may increase the QTc-prolonging activities of Dexchlorpheniramine.
Ivosidenib The risk or severity of QTc prolongation can be increased when Ivabradine is combined with Ivosidenib.
Quetiapine Ivabradine may increase the QTc-prolonging activities of Quetiapine.
Encorafenib The risk or severity of QTc prolongation can be increased when Encorafenib is combined with Ivabradine.
Emedastine Ivabradine may increase the QTc-prolonging activities of Emedastine.
Ceritinib Ivabradine may increase the bradycardic activities of Ceritinib.
Esmolol Esmolol may increase the bradycardic activities of Ivabradine.
Betaxolol Betaxolol may increase the bradycardic activities of Ivabradine.
Pregabalin Pregabalin may increase the bradycardic activities of Ivabradine.
Atenolol Atenolol may increase the bradycardic activities of Ivabradine.
Trimethadione Trimethadione may increase the bradycardic activities of Ivabradine.
Amlodipine Amlodipine may increase the bradycardic activities of Ivabradine.
Nimodipine Nimodipine may increase the bradycardic activities of Ivabradine.
Nisoldipine Nisoldipine may increase the bradycardic activities of Ivabradine.
Sotalol Sotalol may increase the bradycardic activities of Ivabradine.
Lercanidipine Lercanidipine may increase the bradycardic activities of Ivabradine.
Lamotrigine Lamotrigine may increase the bradycardic activities of Ivabradine.
Cinnarizine Cinnarizine may increase the bradycardic activities of Ivabradine.
Propranolol Propranolol may increase the bradycardic activities of Ivabradine.

Target Protein

Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 HCN2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20167941
    DiFrancesco D: The role of the funny current in pacemaker activity. Circ Res. 2010 Feb 19;106(3):434-46. doi: 10.1161/CIRCRESAHA.109.208041.
  • PMID: 16451297
    Sulfi S, Timmis AD: Ivabradine -- the first selective sinus node I(f) channel inhibitor in the treatment of stable angina. Int J Clin Pract. 2006 Feb;60(2):222-8.
  • PMID: 15301560
    DiFrancesco D, Camm JA: Heart rate lowering by specific and selective I(f) current inhibition with ivabradine: a new therapeutic perspective in cardiovascular disease. Drugs. 2004;64(16):1757-65.
  • PMID: 25839989
    Nawarskas JJ, Bowman BN, Anderson JR: Ivabradine: A Unique and Intriguing Medication for Treating Cardiovascular Disease. Cardiol Rev. 2015 Jul-Aug;23(4):201-11. doi: 10.1097/CRD.0000000000000070.
  • PMID: 24377458
    Rosa GM, Ferrero S, Ghione P, Valbusa A, Brunelli C: An evaluation of the pharmacokinetics and pharmacodynamics of ivabradine for the treatment of heart failure. Expert Opin Drug Metab Toxicol. 2014 Feb;10(2):279-91. doi: 10.1517/17425255.2014.876005. Epub 2013 Dec 31.

Contoh Produk & Brand

Produk: 124 • International brands: 2
Produk
  • Corlanor
    Tablet, film coated • 5 mg/1 • Oral • US • Approved
  • Corlanor
    Tablet, film coated • 7.5 mg/1 • Oral • US • Approved
  • Corlanor
    Solution • 5 mg/5mL • Oral • US • Approved
  • Corlanor
    Tablet, film coated • 5 mg/1 • Oral • US • Approved
  • Corlentor
    Tablet, film coated • 5 mg • Oral • EU • Approved
  • Corlentor
    Tablet, film coated • 5 mg • Oral • EU • Approved
  • Corlentor
    Tablet, film coated • 5 mg • Oral • EU • Approved
  • Corlentor
    Tablet, film coated • 5 mg • Oral • EU • Approved
Menampilkan 8 dari 124 produk.
International Brands
  • Bradia — Biocon
  • Ivabid

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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