Ximelagatran Guide, Meaning , Facts, Information and Description

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Ximelagatran
ethyl N-[(R)-cyclohexyl [[(2S)-2-[[4-(hydroxycarbamimidoyl)benzyl]carbamoyl]-1-azetidinyl]carbonyl]methyl] glycinate.
CAS number 192939-46-1	ATC code B01AE05
Chemical formula	CHNO
Molecular weight	474 (429 after conversion)
Bioavailability	20%
Metabolism	None
Elimination half life	3-5h
Excretion	Renal (80%)
Delivery	Oral

Ximelagatran (Exanta®, H 376/95) is an anticoagulant that has been investigated extensively but is awaiting approval by the Food and Drug Administration (FDA). Its manufacturer, AstraZeneca, is marketing it as a replacement for warfarin that does not need close monitoring.

Table of contents

1 Method of action 2 Uses 3 Side-effects 4 Marketing 5 References 6 External link

Method of action

It is the first member of the novel drug class of direct thrombin inhibitors, as it acts solely by inhibiting the actions of thrombin. It is taken orally twice daily, and rapidly absorbed by the small intestine. The liver converts it to the active component melagatran by replacing the ethyl and hydroxyl groups with hydrogen.

Uses

Ximelagatran is expected to replace warfarin and sometimes aspirin and heparin in many therapeutic settings, including deep venous thrombosis and atrial fibrillation.

An advantage, according to its manufacturer, is that it can be taken orally without any monitoring of its anticoagulant properties. This sets it apart from warfarin and heparin, which require monitoring of the international normalized ratio (INR) and the partial thromboplastin time (PTT), respectively. A disadvantage is the absence of an antidote in case acute bleeding develops, while warfarin can be antagonised by Vitamin K and heparin by protamine sulfate.

Side-effects

Ximelagatran was generally well tolerated in the trial populations, but a small proportion (5-6%) developed elevated liver enzyme levels.

Marketing

Several large studies have been conducted to test the efficacy and safety of ximelagatran in patients with deep venous thrombosis and atrial fibrillation. Despite the evidence, the FDA rejected the initial application in March 2004 for potential liver toxicity considerations.

References

• Weitz J. I. New anticoagulants for treatment of venous thromboembolism. Circulation 2004;110(Suppl 1):19-26.

External link

• Present FDA application for ximelagatran

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