Peringatan Keamanan

No human studies involving pregnancy, labor and delivery, nursing, or pediatricsLabel. Geriatric patients are at higher risk of adverse effects than younger patients but the risk to benefit ratio is generally still favourable for older patientsLabel. Patients with a creatinine clearance of 15-30mL/min should have their doses of dabigatran etexilate reduced, and no data is available for patients with a creatinine clearance below 15mL/minLabel.

In animal studies, dabigatran increases the rates of dead offspring and causes uterine and vaginal bleeding close to birthLabel. Dabigatran may or may not be excreted in breast milk so the risk and benefit of stopping the drug or stopping breast feeding must be consideredLabel.

Dabigatran etexilate

DB06695

small molecule approved

Deskripsi

Dabigatran etexilate is an oral prodrug that is hydrolyzed to the competitive and reversible direct thrombin inhibitor dabigatran.A177463, A6970, L34675, L34680 Dabigatran etexilate may be used to decrease the risk of venous thromboembolic events in patients in whom anticoagulation therapy is indicated.A177463 In contrast to warfarin, because its anticoagulant effects are predictable, lab monitoring is not necessary.A177463 Dabigatran etexilate was approved by the FDA in 2010.L6022

Struktur Molekul 2D

Berat 627.7332
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Dabigatran has a half-life of 12-17 hours in adult patients and 12-14 hours in pediatric patients.[L34675, L34680]
Volume Distribusi Dabigatran has a volume of distribution of 50-70L.[L34675, L34680]
Klirens (Clearance) Following intravenous administration, renal clearance constitutes ~80% of total dabigatran clearance.[L34675, L34680]

Absorpsi

Oral dabigatran has a bioavailability of 3-7%, although the relative bioavailability of dabigatran pellets is 37% higher than that for capsules and the bioavailability increases to 75% when the capsule shell is removed; dabigatran capsules should not be tampered with in any way prior to administration. The Cmax is achieved by one hour following oral dosing, which is extended to two hours if accompanied by a high-fat meal. Dabigatran can be taken with or without food. Dabigatran pharmacokinetics are approximately linear over a range of 10-400 mg in healthy adults and adult patients and it has an accumulation factor of two in adult and pediatric patients.L34675, L34680

Metabolisme

Dabigatran is administered as the orally available prodrug dabigatran etexilate that is subsequently metabolized to the active form.A236225, L34675, L34680 In vitro studies and observations regarding the oral bioavailability and levels of plasma prodrug suggest extensive first-pass metabolism by carboxylesterases, first by intestinal CES2 to form BIBR0951 (also known as M2) and then subsequently by hepatic CES1 to form dabigatran. Dabigatran etexilate can also first undergo CES1-mediated hydrolysis to BIBR1087 (M1) followed by CES2-mediated hydrolysis to dabigatran, though it is hypothesized that the former pathway accounts for most of the active form in plasma.A17923, A236195 Dabigatran can undergo 1-O-acyl glucuronidation by UGT1A9, UGT2B7, and UGT2B15 followed by acyl migration to form the corresponding 2-O-, 3-O-, and 4-O-acyl glucuronides; all of these acyl glucuronides exhibit activity similar to dabigatran but account for a small fraction of recovered metabolites.A236225, A17924, L34675, L34680 In addition to these better characterized metabolic pathways, detailed LC/MS characterization suggests a wide variety of possible metabolites following oral or intravenous administration, most of which are present in only trace amounts in plasma, urine, or feces. These include a variety of oxidation, hydrolysis, and conjugation products, including through the addition of mannitol.A236225

Rute Eliminasi

Dabigatran is primarily eliminated in the urine. Following oral administration of radiolabeled dabigatran, 7% of the radioactivity is recovered in urine and 86% is recovered in feces.L34675, L34680

Interaksi Makanan

4 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 2. Avoid St. John's Wort. This herb induces PGP which may reduce the serum levels of dabigatran.
  • 3. Take with a full glass of water.
  • 4. Take with or without food.

Interaksi Obat

1342 Data
Apixaban Apixaban may increase the anticoagulant activities of Dabigatran etexilate.
Lepirudin Dabigatran etexilate may increase the anticoagulant activities of Lepirudin.
Bivalirudin Dabigatran etexilate may increase the anticoagulant activities of Bivalirudin.
Alteplase Dabigatran etexilate may increase the anticoagulant activities of Alteplase.
Urokinase Dabigatran etexilate may increase the anticoagulant activities of Urokinase.
Reteplase Dabigatran etexilate may increase the anticoagulant activities of Reteplase.
Anistreplase Dabigatran etexilate may increase the anticoagulant activities of Anistreplase.
Tenecteplase Dabigatran etexilate may increase the anticoagulant activities of Tenecteplase.
Abciximab Dabigatran etexilate may increase the anticoagulant activities of Abciximab.
Drotrecogin alfa Dabigatran etexilate may increase the anticoagulant activities of Drotrecogin alfa.
Streptokinase Dabigatran etexilate may increase the anticoagulant activities of Streptokinase.
Dicoumarol Dabigatran etexilate may increase the anticoagulant activities of Dicoumarol.
Argatroban Dabigatran etexilate may increase the anticoagulant activities of Argatroban.
Ardeparin Dabigatran etexilate may increase the anticoagulant activities of Ardeparin.
Phenindione Dabigatran etexilate may increase the anticoagulant activities of Phenindione.
Fondaparinux Dabigatran etexilate may increase the anticoagulant activities of Fondaparinux.
Warfarin Dabigatran etexilate may increase the anticoagulant activities of Warfarin.
Pentosan polysulfate Dabigatran etexilate may increase the anticoagulant activities of Pentosan polysulfate.
Phenprocoumon Dabigatran etexilate may increase the anticoagulant activities of Phenprocoumon.
Dipyridamole Dabigatran etexilate may increase the anticoagulant activities of Dipyridamole.
Heparin Dabigatran etexilate may increase the anticoagulant activities of Heparin.
Enoxaparin Dabigatran etexilate may increase the anticoagulant activities of Enoxaparin.
Epoprostenol Dabigatran etexilate may increase the anticoagulant activities of Epoprostenol.
Acenocoumarol Dabigatran etexilate may increase the anticoagulant activities of Acenocoumarol.
4-hydroxycoumarin Dabigatran etexilate may increase the anticoagulant activities of 4-hydroxycoumarin.
Coumarin Dabigatran etexilate may increase the anticoagulant activities of Coumarin.
Ximelagatran Dabigatran etexilate may increase the anticoagulant activities of Ximelagatran.
Desmoteplase Dabigatran etexilate may increase the anticoagulant activities of Desmoteplase.
Defibrotide Dabigatran etexilate may increase the anticoagulant activities of Defibrotide.
Ancrod Dabigatran etexilate may increase the anticoagulant activities of Ancrod.
Beraprost Dabigatran etexilate may increase the anticoagulant activities of Beraprost.
Prasugrel Dabigatran etexilate may increase the anticoagulant activities of Prasugrel.
Rivaroxaban Dabigatran etexilate may increase the anticoagulant activities of Rivaroxaban.
Sulodexide Dabigatran etexilate may increase the anticoagulant activities of Sulodexide.
Semuloparin Dabigatran etexilate may increase the anticoagulant activities of Semuloparin.
Idraparinux Dabigatran etexilate may increase the anticoagulant activities of Idraparinux.
Cangrelor Dabigatran etexilate may increase the anticoagulant activities of Cangrelor.
Astaxanthin Dabigatran etexilate may increase the anticoagulant activities of Astaxanthin.
Otamixaban Dabigatran etexilate may increase the anticoagulant activities of Otamixaban.
Amediplase Dabigatran etexilate may increase the anticoagulant activities of Amediplase.
Danaparoid Dabigatran etexilate may increase the anticoagulant activities of Danaparoid.
Dalteparin Dabigatran etexilate may increase the anticoagulant activities of Dalteparin.
Tinzaparin Dabigatran etexilate may increase the anticoagulant activities of Tinzaparin.
(R)-warfarin Dabigatran etexilate may increase the anticoagulant activities of (R)-warfarin.
Ethyl biscoumacetate Dabigatran etexilate may increase the anticoagulant activities of Ethyl biscoumacetate.
Nadroparin Dabigatran etexilate may increase the anticoagulant activities of Nadroparin.
Triflusal Dabigatran etexilate may increase the anticoagulant activities of Triflusal.
Ditazole Dabigatran etexilate may increase the anticoagulant activities of Ditazole.
Vorapaxar Dabigatran etexilate may increase the anticoagulant activities of Vorapaxar.
Edoxaban Dabigatran etexilate may increase the anticoagulant activities of Edoxaban.
Potassium citrate Potassium citrate may increase the excretion rate of Dabigatran etexilate which could result in a lower serum level and potentially a reduction in efficacy.
Sodium citrate Dabigatran etexilate may increase the anticoagulant activities of Sodium citrate.
Dextran Dabigatran etexilate may increase the anticoagulant activities of Dextran.
Bemiparin Dabigatran etexilate may increase the anticoagulant activities of Bemiparin.
Parnaparin Dabigatran etexilate may increase the anticoagulant activities of Parnaparin.
Desirudin Dabigatran etexilate may increase the anticoagulant activities of Desirudin.
Antithrombin Alfa Dabigatran etexilate may increase the anticoagulant activities of Antithrombin Alfa.
Protein C Dabigatran etexilate may increase the anticoagulant activities of Protein C.
Antithrombin III human Dabigatran etexilate may increase the anticoagulant activities of Antithrombin III human.
Letaxaban Dabigatran etexilate may increase the anticoagulant activities of Letaxaban.
Darexaban Dabigatran etexilate may increase the anticoagulant activities of Darexaban.
Betrixaban Dabigatran etexilate may increase the anticoagulant activities of Betrixaban.
Nafamostat Dabigatran etexilate may increase the anticoagulant activities of Nafamostat.
Monteplase Dabigatran etexilate may increase the anticoagulant activities of Monteplase.
Gabexate Dabigatran etexilate may increase the anticoagulant activities of Gabexate.
Fluindione Dabigatran etexilate may increase the anticoagulant activities of Fluindione.
Protein S human Dabigatran etexilate may increase the anticoagulant activities of Protein S human.
Brinase Dabigatran etexilate may increase the anticoagulant activities of Brinase.
Clorindione Dabigatran etexilate may increase the anticoagulant activities of Clorindione.
Diphenadione Dabigatran etexilate may increase the anticoagulant activities of Diphenadione.
Tioclomarol Dabigatran etexilate may increase the anticoagulant activities of Tioclomarol.
Melagatran Dabigatran etexilate may increase the anticoagulant activities of Melagatran.
Saruplase Dabigatran etexilate may increase the anticoagulant activities of Saruplase.
(S)-Warfarin Dabigatran etexilate may increase the anticoagulant activities of (S)-Warfarin.
Tocopherylquinone Dabigatran etexilate may increase the anticoagulant activities of Tocopherylquinone.
Dabigatran Dabigatran etexilate may increase the anticoagulant activities of Dabigatran.
Edetic acid Dabigatran etexilate may increase the anticoagulant activities of Edetic acid.
Troxerutin Dabigatran etexilate may increase the anticoagulant activities of Troxerutin.
Reviparin Dabigatran etexilate may increase the anticoagulant activities of Reviparin.
Dermatan sulfate Dabigatran etexilate may increase the anticoagulant activities of Dermatan sulfate.
SR-123781A Dabigatran etexilate may increase the anticoagulant activities of SR-123781A.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Dabigatran etexilate.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Dabigatran etexilate is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Glycochenodeoxycholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Deoxycholic acid.
Obeticholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Hyodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Cholic Acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Taurocholic acid.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Dabigatran etexilate.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Dabigatran etexilate is combined with Obinutuzumab.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Dabigatran etexilate is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Dabigatran etexilate.

Target Protein

Prothrombin F2

Referensi & Sumber

Synthesis reference: Christian Filser, Wolfgang Dersch, Rainer Hamm, Arndt Hausherr, Gunter Koch, Ulrich Scholz, Georg Zerban, "METHOD FOR PRODUCING AN INTERMEDIATE PRODUCT OF DABIGATRAN ETEXILATE." U.S. Patent US20110118471, issued May 19, 2011.
Artikel (PubMed)
  • PMID: 17764540
    Eriksson BI, Dahl OE, Rosencher N, Kurth AA, van Dijk CN, Frostick SP, Kalebo P, Christiansen AV, Hantel S, Hettiarachchi R, Schnee J, Buller HR: Oral dabigatran etexilate vs. subcutaneous enoxaparin for the prevention of venous thromboembolism after total knee replacement: the RE-MODEL randomized trial. J Thromb Haemost. 2007 Nov;5(11):2178-85.
  • PMID: 17869635
    Eriksson BI, Dahl OE, Rosencher N, Kurth AA, van Dijk CN, Frostick SP, Prins MH, Hettiarachchi R, Hantel S, Schnee J, Buller HR: Dabigatran etexilate versus enoxaparin for prevention of venous thromboembolism after total hip replacement: a randomised, double-blind, non-inferiority trial. Lancet. 2007 Sep 15;370(9591):949-56.
  • PMID: 23292752
    Scaglione F: New oral anticoagulants: comparative pharmacology with vitamin K antagonists. Clin Pharmacokinet. 2013 Feb;52(2):69-82. doi: 10.1007/s40262-012-0030-9.
  • PMID: 20551237
    Ebner T, Wagner K, Wienen W: Dabigatran acylglucuronide, the major human metabolite of dabigatran: in vitro formation, stability, and pharmacological activity. Drug Metab Dispos. 2010 Sep;38(9):1567-75. doi: 10.1124/dmd.110.033696. Epub 2010 Jun 15.
  • PMID: 23408233
    van Ryn J, Goss A, Hauel N, Wienen W, Priepke H, Nar H, Clemens A: The discovery of dabigatran etexilate. Front Pharmacol. 2013 Feb 12;4:12. doi: 10.3389/fphar.2013.00012. eCollection 2013.
  • PMID: 31164248
    Negrier C, Shima M, Hoffman M: The central role of thrombin in bleeding disorders. Blood Rev. 2019 Nov;38:100582. doi: 10.1016/j.blre.2019.05.006. Epub 2019 May 22.
  • PMID: 17598008
    Wienen W, Stassen JM, Priepke H, Ries UJ, Hauel N: In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.
  • PMID: 20671233
    Eisert WG, Hauel N, Stangier J, Wienen W, Clemens A, van Ryn J: Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin. Arterioscler Thromb Vasc Biol. 2010 Oct;30(10):1885-9. doi: 10.1161/ATVBAHA.110.203604. Epub 2010 Jul 29.
Menampilkan 8 dari 16 artikel.

Contoh Produk & Brand

Produk: 125 • International brands: 2
Produk
  • Apo-dabigatran
    Capsule • 75 mg • Oral • Canada • Generic • Approved
  • Apo-dabigatran
    Capsule • 110 mg • Oral • Canada • Generic • Approved
  • Apo-dabigatran
    Capsule • 150 mg • Oral • Canada • Generic • Approved
  • Dabigatran
    Capsule • 75 mg/1 • Oral • US • Generic • Approved
  • Dabigatran
    Capsule • 150 mg/1 • Oral • US • Generic • Approved
  • Dabigatran
    Capsule • 110 mg/1 • Oral • US • Generic • Approved
  • Dabigatran
    Capsule • 150 mg/1 • Oral • US • Generic • Approved
  • Dabigatran
    Capsule • 75 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 125 produk.
International Brands
  • Pradax — Boehringer Ingelheim
  • Rendix

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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