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Apixaban is a highly selective, orally bioavailable, and reversible direct inhibitor of free and clot-bound factor Xa. Factor Xa catalyzes the conversion of prothrombin to thrombin, the final enzyme in the coagulation cascade that is responsible for fibrin clot formation. [ 27 ]
The risk of bleeding is increased if used at the same time as other blood thinning drugs such as nonsteroidal anti-inflammatory drugs, antiplatelet drugs and heparin. [2] The blood thinning effects can be reduced if used at the same time as rifampicin and phenytoin , and increased with fluconazole .
Many other anticoagulants exist in research and development, diagnostics, or as drug candidates. Batroxobin, a toxin from snake venom, clots platelet-rich plasma without affecting platelet functions (cleaves fibrinogen). Hementin is an anticoagulant protease from the salivary glands of the giant Amazon leech, Haementeria ghilianii. Vitamin E
Four drugs from the class of direct Xa inhibitors are marketed worldwide. Rivaroxaban (Xarelto) was the first approved FXa inhibitor to become commercially available in Europe and Canada in 2008. [1] The second one was apixaban (Eliquis), approved in Europe in 2011 [2] and in the United States in 2012. [3]
Thrombin demonstrates a high level of allosteric regulation. [2] Allosterism in thrombin is regulated by the exosites 1 and 2 and the sodium binding site. A recent patent review has shown that the general consensus among researchers is that allosteric inhibitors may provide a more regulatable anticoagulant. [3]
When two drugs affect each other, it is a drug–drug interaction (DDI). The risk of a DDI increases with the number of drugs used. [1] A large share of elderly people regularly use five or more medications or supplements, with a significant risk of side-effects from drug–drug interactions. [2] Drug interactions can be of three kinds:
Warfarin – a coumarin – with brand name, Coumadin, is a prescription drug used as an anticoagulant to inhibit formation of blood clots, and so is a therapy for deep vein thrombosis and pulmonary embolism. [9] [10] [11] It may be used to prevent recurrent blood clot formation from atrial fibrillation, thrombotic stroke, and transient ...
The action of drugs on the human body (or any other organism's body) is called pharmacodynamics, and the body's response to drugs is called pharmacokinetics. The drugs that enter an individual tend to stimulate certain receptors, ion channels, act on enzymes or transport proteins. As a result, they cause the human body to react in a specific way.