Peringatan Keamanan

Premature discontinuation of any oral anticoagulant, including edoxaban, in the absence of adequate alternative anticoagulation increases the risk of ischemic events. If edoxaban is discontinued for reasons other than pathological bleeding or completion of a course of therapy, consider the use of another anticoagulant. Edoxaban increases the risk of potentially fatal major bleeding such as intracranial hemorrhage and gastrointestinal bleeding. Patients should be educated on how to watch for signs of major and minor bleeding and when to seek medical help. Co-administration of other anti-coagulants, anti-platelets, or thrombolytics may increase the risk of bleeding and should therefore be avoided.

Edoxaban

DB09075

small molecule approved

Deskripsi

Edoxaban is a member of the Novel Oral Anti-Coagulants (NOACs) class of drugs, and is a rapidly acting, oral, selective factor Xa inhibitor. By inhibiting factor Xa, a key protein in the coagulation cascade, edoxaban prevents the stepwise amplification of protein factors needed to form blood clots. It is indicated to reduce the risk of stroke and systemic embolism (SE) in patients with nonvalvular atrial fibrillation (NVAF) and for the treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE) following 5-10 days of initial therapy with a parenteral anticoagulant. Traditionally, warfarin, a vitamin K antagonist, was used for stroke prevention in these individuals but effective use of this drug is limited by it's delayed onset, narrow therapeutic window, need for regular monitoring and INR testing, and numerous drug-drug and drug-food interactions. This has prompted enthusiasm for newer agents such as dabigatran, apixaban, and rivaroxaban for effective clot prevention. In addition to once daily dosing, the benefits over warfarin also include significant reductions in hemorrhagic stroke and GI bleeding, and improved compliance, which is beneficial as many patients will be on lifelong therapy.

Struktur Molekul 2D

Berat 548.06
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of edoxaban following oral administration is 10 to 14 hours.
Volume Distribusi The steady state volume of distribution is 107 L.
Klirens (Clearance) 22 L/hr

Absorpsi

Following oral administration, peak plasma edoxaban concentrations are observed within 1-2 hours. Absolute bioavailability is 62%.

Metabolisme

Edoxaban is not extensively metabolized by CYP3A4 resulting in minimal drug-drug interactions. However, it does interact with drugs that inhibit p-gp (p-glycoprotein), which is used to transport edoxaban across the intestinal wall. Unchanged edoxaban is the predominant form in plasma. There is minimal metabolism via hydrolysis (mediated by carboxylesterase 1), conjugation, and oxidation by CYP3A4. The predominant metabolite M-4, formed by hydrolysis, is human-specific and active and reaches less than 10% of the exposure of the parent compound in healthy subjects. Exposure to the other metabolites is less than 5% of exposure to edoxaban.

Rute Eliminasi

Edoxaban is eliminated primarily as unchanged drug in urine. Renal clearance (11 L/hour) accounts for approximately 50% of the total clearance of edoxaban (22 L/hour). Metabolism and biliary/intestinal excretion account for the remaining clearance.

Interaksi Makanan

2 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Additive anticoagulant activity may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 2. Take with or without food.

Interaksi Obat

1297 Data
Apixaban Apixaban may increase the anticoagulant activities of Edoxaban.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Edoxaban.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Edoxaban.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Edoxaban is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Cholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Deoxycholic acid.
Obeticholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Hyodeoxycholic Acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Taurocholic acid.
Lepirudin The risk or severity of bleeding can be increased when Edoxaban is combined with Lepirudin.
Bivalirudin The risk or severity of bleeding can be increased when Edoxaban is combined with Bivalirudin.
Alteplase The risk or severity of bleeding can be increased when Edoxaban is combined with Alteplase.
Urokinase The risk or severity of bleeding can be increased when Edoxaban is combined with Urokinase.
Reteplase The risk or severity of bleeding can be increased when Edoxaban is combined with Reteplase.
Anistreplase The risk or severity of bleeding can be increased when Edoxaban is combined with Anistreplase.
Tenecteplase The risk or severity of bleeding can be increased when Edoxaban is combined with Tenecteplase.
Abciximab The risk or severity of bleeding can be increased when Edoxaban is combined with Abciximab.
Drotrecogin alfa The risk or severity of bleeding can be increased when Edoxaban is combined with Drotrecogin alfa.
Streptokinase The risk or severity of bleeding can be increased when Edoxaban is combined with Streptokinase.
Dicoumarol The risk or severity of bleeding can be increased when Edoxaban is combined with Dicoumarol.
Argatroban The risk or severity of bleeding can be increased when Edoxaban is combined with Argatroban.
Ardeparin The risk or severity of bleeding can be increased when Edoxaban is combined with Ardeparin.
Phenindione The risk or severity of bleeding can be increased when Edoxaban is combined with Phenindione.
Fondaparinux The risk or severity of bleeding can be increased when Edoxaban is combined with Fondaparinux.
Warfarin The risk or severity of bleeding can be increased when Edoxaban is combined with Warfarin.
Pentosan polysulfate The risk or severity of bleeding can be increased when Edoxaban is combined with Pentosan polysulfate.
Phenprocoumon The risk or severity of bleeding can be increased when Edoxaban is combined with Phenprocoumon.
Dipyridamole The risk or severity of bleeding can be increased when Edoxaban is combined with Dipyridamole.
Heparin The risk or severity of bleeding can be increased when Edoxaban is combined with Heparin.
Enoxaparin The risk or severity of bleeding can be increased when Edoxaban is combined with Enoxaparin.
Epoprostenol The risk or severity of bleeding can be increased when Edoxaban is combined with Epoprostenol.
Acenocoumarol The risk or severity of bleeding can be increased when Edoxaban is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Edoxaban is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Edoxaban is combined with Coumarin.
Ximelagatran The risk or severity of bleeding can be increased when Edoxaban is combined with Ximelagatran.
Desmoteplase The risk or severity of bleeding can be increased when Edoxaban is combined with Desmoteplase.
Defibrotide The risk or severity of bleeding can be increased when Edoxaban is combined with Defibrotide.
Ancrod The risk or severity of bleeding can be increased when Edoxaban is combined with Ancrod.
Beraprost The risk or severity of bleeding can be increased when Edoxaban is combined with Beraprost.
Prasugrel The risk or severity of bleeding can be increased when Edoxaban is combined with Prasugrel.
Rivaroxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Rivaroxaban.
Sulodexide The risk or severity of bleeding can be increased when Edoxaban is combined with Sulodexide.
Semuloparin The risk or severity of bleeding can be increased when Edoxaban is combined with Semuloparin.
Idraparinux The risk or severity of bleeding can be increased when Edoxaban is combined with Idraparinux.
Cangrelor The risk or severity of bleeding can be increased when Edoxaban is combined with Cangrelor.
Astaxanthin The risk or severity of bleeding can be increased when Edoxaban is combined with Astaxanthin.
Otamixaban The risk or severity of bleeding can be increased when Edoxaban is combined with Otamixaban.
Amediplase The risk or severity of bleeding can be increased when Edoxaban is combined with Amediplase.
Danaparoid The risk or severity of bleeding can be increased when Edoxaban is combined with Danaparoid.
Dalteparin The risk or severity of bleeding can be increased when Edoxaban is combined with Dalteparin.
Tinzaparin The risk or severity of bleeding can be increased when Edoxaban is combined with Tinzaparin.
(R)-warfarin The risk or severity of bleeding can be increased when Edoxaban is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Edoxaban is combined with Ethyl biscoumacetate.
Nadroparin The risk or severity of bleeding can be increased when Edoxaban is combined with Nadroparin.
Triflusal The risk or severity of bleeding can be increased when Edoxaban is combined with Triflusal.
Ticagrelor The risk or severity of bleeding can be increased when Edoxaban is combined with Ticagrelor.
Ditazole The risk or severity of bleeding can be increased when Edoxaban is combined with Ditazole.
Vorapaxar The risk or severity of bleeding can be increased when Edoxaban is combined with Vorapaxar.
Potassium citrate Potassium citrate may increase the excretion rate of Edoxaban which could result in a lower serum level and potentially a reduction in efficacy.
Sodium citrate The risk or severity of bleeding can be increased when Edoxaban is combined with Sodium citrate.
Dextran The risk or severity of bleeding can be increased when Edoxaban is combined with Dextran.
Bemiparin The risk or severity of bleeding can be increased when Edoxaban is combined with Bemiparin.
Parnaparin The risk or severity of bleeding can be increased when Edoxaban is combined with Parnaparin.
Desirudin The risk or severity of bleeding can be increased when Edoxaban is combined with Desirudin.
Antithrombin Alfa The risk or severity of bleeding can be increased when Edoxaban is combined with Antithrombin Alfa.
Protein C The risk or severity of bleeding can be increased when Edoxaban is combined with Protein C.
Antithrombin III human The risk or severity of bleeding can be increased when Edoxaban is combined with Antithrombin III human.
Letaxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Letaxaban.
Darexaban The risk or severity of bleeding can be increased when Edoxaban is combined with Darexaban.
Betrixaban The risk or severity of bleeding can be increased when Edoxaban is combined with Betrixaban.
Nafamostat The risk or severity of bleeding can be increased when Edoxaban is combined with Nafamostat.
Monteplase The risk or severity of bleeding can be increased when Edoxaban is combined with Monteplase.
Gabexate The risk or severity of bleeding can be increased when Edoxaban is combined with Gabexate.
Fluindione The risk or severity of bleeding can be increased when Edoxaban is combined with Fluindione.
Protein S human The risk or severity of bleeding can be increased when Edoxaban is combined with Protein S human.
Brinase The risk or severity of bleeding can be increased when Edoxaban is combined with Brinase.
Clorindione The risk or severity of bleeding can be increased when Edoxaban is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Edoxaban is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding can be increased when Edoxaban is combined with Tioclomarol.
Melagatran The risk or severity of bleeding can be increased when Edoxaban is combined with Melagatran.
Saruplase The risk or severity of bleeding can be increased when Edoxaban is combined with Saruplase.
(S)-Warfarin The risk or severity of bleeding can be increased when Edoxaban is combined with (S)-Warfarin.
Tocopherylquinone The risk or severity of bleeding can be increased when Edoxaban is combined with Tocopherylquinone.
Dabigatran The risk or severity of bleeding can be increased when Edoxaban is combined with Dabigatran.
Edetic acid The risk or severity of bleeding can be increased when Edoxaban is combined with Edetic acid.
Troxerutin The risk or severity of bleeding can be increased when Edoxaban is combined with Troxerutin.
Reviparin The risk or severity of bleeding can be increased when Edoxaban is combined with Reviparin.
Dermatan sulfate The risk or severity of bleeding can be increased when Edoxaban is combined with Dermatan sulfate.
SR-123781A The risk or severity of bleeding can be increased when Edoxaban is combined with SR-123781A.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Edoxaban.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Edoxaban is combined with Obinutuzumab.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Edoxaban is combined with Sugammadex.

Target Protein

Coagulation factor X F10

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18096568
    Turpie AG: New oral anticoagulants in atrial fibrillation. Eur Heart J. 2008 Jan;29(2):155-65. Epub 2007 Dec 19.
  • PMID: 20081065
    Ogata K, Mendell-Harary J, Tachibana M, Masumoto H, Oguma T, Kojima M, Kunitada S: Clinical safety, tolerability, pharmacokinetics, and pharmacodynamics of the novel factor Xa inhibitor edoxaban in healthy volunteers. J Clin Pharmacol. 2010 Jul;50(7):743-53. doi: 10.1177/0091270009351883. Epub 2010 Jan 15.
  • PMID: 25792448
    Yeh CH, Hogg K, Weitz JI: Overview of the new oral anticoagulants: opportunities and challenges. Arterioscler Thromb Vasc Biol. 2015 May;35(5):1056-65. doi: 10.1161/ATVBAHA.115.303397. Epub 2015 Mar 19.
  • PMID: 25682085
    Senoo K, Lip GY: Comparative efficacy and safety of the non-vitamin K antagonist oral anticoagulants for patients with nonvalvular atrial fibrillation. Semin Thromb Hemost. 2015 Mar;41(2):146-53. doi: 10.1055/s-0035-1544156. Epub 2015 Feb 15.
  • PMID: 26620048
    Parasrampuria DA, Truitt KE: Pharmacokinetics and Pharmacodynamics of Edoxaban, a Non-Vitamin K Antagonist Oral Anticoagulant that Inhibits Clotting Factor Xa. Clin Pharmacokinet. 2015 Nov 30.

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