Document Detail


The direct thrombin inhibitor melagatran/ximelagatran.
MedLine Citation:
PMID:  15487959     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Melagatran is a synthetic, small-peptide direct thrombin inhibitor with anticoagulant activity. Ximelagatran, an oral prodrug, undergoes rapid enzymatic conversion to melagatran. Melagatran has rapid onset of action, fixed twice-daily dosing, stable absorption, apparent low potential for medication interactions, and no requirement for monitoring drug levels or dose adjustment. There is no specific antidote, but the drug has a short plasma elimination half-life (about 4 hours). In clinical studies, melagatran/ximelagatran is not inferior to warfarin for stroke prevention in patients with non-valvular atrial fibrillation, to heparin-warfarin for acute treatment and extended secondary prevention of deep vein thrombosis, and superior to warfarin for prevention of venous thromboembolism after major orthopaedic surgery. Major bleeding with melagatran/ximelagatran occurred at rates similar to those in patients treated with warfarin. 6%-12% of patients taking ximelagatran develop asymptomatic elevated liver enzyme levels (predominantly alanine aminotransferase) after 1-6 months of therapy; this usually resolves with cessation of therapy. Less than 1% of patients develop abnormal liver function while taking ximelagatran; this rarely persists or develops into clinical illness.
Authors:
Timothy A Brighton
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  The Medical journal of Australia     Volume:  181     ISSN:  0025-729X     ISO Abbreviation:  Med. J. Aust.     Publication Date:  2004 Oct 
Date Detail:
Created Date:  2004-10-18     Completed Date:  2005-01-18     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  0400714     Medline TA:  Med J Aust     Country:  Australia    
Other Details:
Languages:  eng     Pagination:  432-7     Citation Subset:  IM    
Affiliation:
Department of Haematology, St George Hospital, Gray Street, Kogarah, NSW 2217, Australia. t.brighton@unsw.edu.au
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MeSH Terms
Descriptor/Qualifier:
Anticoagulants / pharmacology*
Azetidines / pharmacology*
Benzylamines
Blood Coagulation / drug effects
Glycine / analogs & derivatives*,  pharmacology*
Humans
Myocardial Infarction / drug therapy,  prevention & control
Recurrence / prevention & control
Stroke / drug therapy,  prevention & control
Thrombin / antagonists & inhibitors*
Treatment Outcome
Venous Thrombosis / drug therapy,  prevention & control
Chemical
Reg. No./Substance:
0/Anticoagulants; 0/Azetidines; 0/Benzylamines; 0/ximelagatran; 159776-70-2/melagatran; 56-40-6/Glycine; EC 3.4.21.5/Thrombin
Comments/Corrections
Comment In:
Med J Aust. 2005 Mar 7;182(5):254-5   [PMID:  15748144 ]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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