Description

Simple

Clinical

Overview

Ximelagatran is an anticoagulant intended to become a replacement for warfarin by overcoming the dietary restrictions, drug interaction, and monitoring issues associated with the former. In 2006, its manufacturer AstraZeneca announced that it would not attempt to market ximelagatran after reports of hepatotoxicity (liver damage) during trials, and to discontinue its distribution in countries where the drug had been approved.

Pharmacology

Indication

For the treatment of acute deep vein thrombosis.

Pharmacodynamic

Information currently not available.

Mechanism of action

Ximelagatran was the first member of the drug class of direct thrombin inhibitors that can be taken orally. Its effect is solely related to the inhibition of thrombin.

Absorption

Rapidly absorbed by the small intestine with an oral bioavailability of 20%.

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

3-5 hours

Route of elimination

Information currently not available.

Toxicity

Hepatotoxicity (liver damage) was reported during trials.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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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 Ximelagatran.
(R)-warfarin
The risk or severity of bleeding can be increased when Ximelagatran is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of bleeding can be increased when Ximelagatran is combined with (S)-Warfarin.
1-Testosterone
1-Testosterone may increase the anticoagulant activities of Ximelagatran.
18-methyl-19-nortestosterone
18-methyl-19-nortestosterone may increase the anticoagulant activities of Ximelagatran.
3,5-Diiodotyrosine
3,5-Diiodotyrosine may increase the anticoagulant activities of Ximelagatran.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when Ximelagatran is combined with 4-hydroxycoumarin.
4-Hydroxytestosterone
4-Hydroxytestosterone may increase the anticoagulant activities of Ximelagatran.
5beta-dihydrotestosterone
5beta-dihydrotestosterone may increase the anticoagulant activities of Ximelagatran.
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 Ximelagatran.
Abatacept
The metabolism of Ximelagatran can be increased when combined with Abatacept.
Abciximab
The risk or severity of bleeding can be increased when Abciximab is combined with Ximelagatran.
Abiraterone
The metabolism of Ximelagatran can be decreased when combined with Abiraterone.
Aceclofenac
The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Ximelagatran.
Acemetacin
The risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Ximelagatran.
Acenocoumarol
The metabolism of Acenocoumarol can be decreased when combined with Ximelagatran.
Acetohexamide
The metabolism of Ximelagatran can be decreased when combined with Acetohexamide.
Acetyl sulfisoxazole
The metabolism of Ximelagatran can be decreased when combined with Acetyl sulfisoxazole.
Acetylsalicylic acid
Acetylsalicylic acid may increase the anticoagulant activities of Ximelagatran.
Adalimumab
The metabolism of Ximelagatran can be increased when combined with Adalimumab.
5 References
  1. 1 . Eriksson H, Wahlander K, Gustafsson D, Welin LT, Frison L, Schulman S: A randomized, controlled, dose-guiding study of the oral direct thrombin inhibitor ximelagatran compared with standard therapy for the treatment of acute deep vein thrombosis: THRIVE I. J Thromb Haemost. 2003 Jan;1(1):41-7.PubMed: 12871538
  2. 2 . Weitz JI: New anticoagulants for treatment of venous thromboembolism. Circulation. 2004 Aug 31;110(9 Suppl 1):I19-26.PubMed: 15339877
  3. 3 . Francis CW, Berkowitz SD, Comp PC, Lieberman JR, Ginsberg JS, Paiement G, Peters GR, Roth AW, McElhattan J, Colwell CW Jr: Comparison of ximelagatran with warfarin for the prevention of venous thromboembolism after total knee replacement. N Engl J Med. 2003 Oct 30;349(18):1703-12.PubMed: 14585938
  4. 4 . Bergqvist D, Solhaug JH, Holmdahl L, Eriksson UG, Andersson M, Boberg B, Ogren M: Pharmacokinetics, preliminary efficacy and safety of subcutaneous melagatran and oral ximelagatran : a multicentre study of thromboprophylaxis in elective abdominal surgery. Clin Drug Investig. 2004;24(3):127-36.PubMed: 17516699
  5. 5 . Koscielny J, Kiesewetter H, Jorg I, Harenberg J: Ximelagatran for treatment and prophylaxis of recurrent events in deep vein thrombosis. Clin Appl Thromb Hemost. 2007 Jul;13(3):299-307.PubMed: 17636192