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Ximelagatran showed good efficacy compared with warfarin in several trials in prevention and treatment of deep vein thrombosis and as thromboprophylaxis in atrial fibrillation. [1] Development was stopped by manufacturer AstraZeneca , however, because of reports of liver enzyme derangements and liver failure .
Side effects may include bleeding, most commonly from the nose, gastrointestinal tract (GI) or genitourinary system. [2] Compared to the risk of bleeding with warfarin use, direct factor Xa inhibitors have a higher risk of GI bleeding, but lower risk of bleeding in the brain . [ 2 ]
Most of those drugs are in the class of direct factor Xa inhibitors, but there is one DTI called AZD0837, [26] which is a follow-up compound of ximelgatran that is being developed by AstraZeneca. It is the prodrug of a potent, competitive, reversible inhibitor of free and fibrin-bound thrombin called ARH0637. [18]
Warfarin is indicated for the prophylaxis and treatment of venous thrombosis and its extension, pulmonary embolism; [9] prophylaxis and treatment of thromboembolic complications associated with atrial fibrillation and/or cardiac valve replacement; [9] and reduction in the risk of death, recurrent myocardial infarction, and thromboembolic events such as stroke or systemic embolization after ...
Type A: augmented pharmacological effects, which are dose-dependent and predictable [5]; Type A reactions, which constitute approximately 80% of adverse drug reactions, are usually a consequence of the drug's primary pharmacological effect (e.g., bleeding when using the anticoagulant warfarin) or a low therapeutic index of the drug (e.g., nausea from digoxin), and they are therefore predictable.
Warfarin necrosis is a rare but severe complication of treatment with warfarin or related anticoagulants. [2] The typical patient appears to be an obese, middle aged woman (median age 54 years, male to female ratio 1:3). [1] [3]: 122–3 This drug eruption usually occurs between the third and tenth days of therapy with warfarin derivatives. [1]
They are categorised as "first-generation" anticoagulants, and have similar effects as warfarin. They have been largely superseded by second-generation anticoagulants because warfarin-resistant rodents have become more common. [6] Anisindione, fluindione, and phenindione are oral anticoagulant medicines with actions similar to warfarin. However ...
In this case, both the therapeutic and toxic targets are the same. To avoid toxicity during treatment, many times the drug needs to be changed to target a different aspect of the illness or symptoms. Statins are an example of a drug class that can have toxic effects at the therapeutic target (HMG CoA reductase). [1]