Description

Simple

A medication or "blood thinner" used to to prevent blood clots and stroke associated with surgical procedures or conditions in the heart, such as abnormal heart rhythms.

Clinical

An anticoagulant used for the prevention of venous thromboembolic events or stroke in patients with recent elective hip or knee replacement surgery and atrial fibrillation.

Overview

Dabigatran etexilate is an oral prodrug that is hydrolyzed to the competitive and reversible direct thrombin inhibitor [dabigatran][Label,5,A6970]. Dabigatran etexilate may be used to decrease the risk of venous thromboembolic events in patients in whom anticoagulation therapy is indicated[5]. In contrast to warfarin, because its anticoagulant effects are predictable, lab monitoring is not necessary[5]. Dabigatran etexilate was approved by the FDA in 2010[6].

Pharmacology

Indication

Dabigatran is indicated for the prevention of venous thromboembolic events in patients who have undergone elective hip or knee replacement surgery (based on RE-NOVATE, RE-MODEL, and RE-MOBILIZE trials)[ Read more

Pharmacodynamic

Dabigatran directly inhibits thrombin in a concentration-dependent, reversible, specific, and competitive manner which results in a prolongation of aPTT (partial thromboplastin time), ECT (Ecarin clotting time), and TT (thrombin time)[Label, Read more

Mechanism of action

Dabigatran is hydrolysed to the active dabigatran by an esterase which induces hydrolysis[Label, Read more

Absorption

Oral dabigatran is 3-7% bioavailable, reaching a maximum concentration 1 hour after administration in fasted subjects[Label]. When taken with a meal that is high in fat, the time to maximum concentration increases to 2 hours, though this does not affect dosing[Label, Read more

Protein binding

Dabigatran is approximately 35% protein plasma bound[Label, Read more

Volume of distribution

50-70L[Label].

Clearance

Information currently not available.

Half life

12 to 17 hours[Label,5].

Route of elimination

7% of the dose is recovered in urine and 86% is recovered in the feces[Label].

Toxicity

No human studies involving pregnancy, labor and delivery, nursing, or pediatrics[Label]. Geriatric patients are at higher risk of adverse effects than younger patients but the risk to benefit ratio is generally still favourable for older patients[Label]. Patients with a creatinine clearance of 15-30... Read more

Adverse Effects

Contraindications

  • Route:
    • Oral
  • Dose Form:
    • Capsule
  • Recommended Actions:
    • Avoid
  • Regions: US
  • Patient Conditions:
      • Name: Active pathological bleeding
      • Drugbank Id: DBCOND0107496
  • Route:
    • Oral
  • Dose Form:
    • Capsule
  • Recommended Actions:
    • Avoid
  • Regions: US
  • Patient Conditions:
      • Name: Mechanical prosthetic heart valve
      • Drugbank Id: DBCOND0108448
  • Route:
    • Oral
  • Dose Form:
    • Capsule
  • Hypersensitivity:
    • true
  • Recommended Actions:
    • Avoid
  • Sex Group: all
  • Regions: US

Food Interactions

  • Avoid St. John's Wort.
  • Take with a full glass of water.
  • Take with or without food.

Interactions

Type in a drug name to check for interaction with Dabigatran etexilate
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(1,2,6,7-3H)Testosterone
(1,2,6,7-3H)Testosterone may increase the anticoagulant activities of Dabigatran etexilate.
(R)-warfarin
Dabigatran etexilate may increase the anticoagulant activities of (R)-warfarin.
(S)-Warfarin
Dabigatran etexilate may increase the anticoagulant activities of (S)-Warfarin.
1-Testosterone
1-Testosterone may increase the anticoagulant activities of Dabigatran etexilate.
18-methyl-19-nortestosterone
18-methyl-19-nortestosterone may increase the anticoagulant activities of Dabigatran etexilate.
3,5-Diiodotyrosine
3,5-Diiodotyrosine may increase the anticoagulant activities of Dabigatran etexilate.
4-hydroxycoumarin
Dabigatran etexilate may increase the anticoagulant activities of 4-hydroxycoumarin.
4-Hydroxytestosterone
4-Hydroxytestosterone may increase the anticoagulant activities of Dabigatran etexilate.
5beta-dihydrotestosterone
5beta-dihydrotestosterone may increase the anticoagulant activities of Dabigatran etexilate.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Dabigatran etexilate.
Abacavir
Abacavir may decrease the excretion rate of Dabigatran etexilate which could result in a higher serum level.
Abciximab
Dabigatran etexilate may increase the anticoagulant activities of Abciximab.
Acarbose
Acarbose may decrease the excretion rate of Dabigatran etexilate which could result in a higher serum level.
Aceclofenac
The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Dabigatran etexilate.
Acemetacin
The risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Dabigatran etexilate.
Acenocoumarol
Dabigatran etexilate may increase the anticoagulant activities of Acenocoumarol.
Acetaminophen
Acetaminophen may decrease the excretion rate of Dabigatran etexilate which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Dabigatran etexilate which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
Dabigatran etexilate may increase the anticoagulant activities of Acetylsalicylic acid.
Aclidinium
Dabigatran etexilate may decrease the excretion rate of Aclidinium which could result in a higher serum level.
7 References
  1. 1 . 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.PubMed: 17764540
  2. 2 . 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.PubMed: 17869635
  3. 3 . 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.PubMed: 23292752
  4. 4 . 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.PubMed: 20551237
  5. 5 . 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.PubMed: 23408233
  6. 6 . FDA Drug Approval Package for Dabigatran Etexilate Link
  7. 7 . Apotex Inc. Product Monograph: Dabigatran Etexilate File