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Antistasin, the first discovered naturally occurring direct Xa inhibitor Rivaroxaban, the first synthetic direct Xa inhibitor marketed as a drug Prior to the introduction of direct factor Xa inhibitors, vitamin K antagonists such as warfarin were the only oral anticoagulants for over 60 years, and together with heparin have been the main blood ...
Rivaroxaban, sold under the brand name Xarelto among others, is an anticoagulant medication (blood thinner) used to treat and prevent blood clots. [8] Specifically it is used to treat deep vein thrombosis and pulmonary emboli and prevent blood clots in atrial fibrillation and following hip or knee surgery. [ 8 ]
The combination drug acetylsalicylic acid/dipyridamole (trade names Aggrenox, Asasantin) is a drug combination of: [1] Acetylsalicylic acid (Aspirin) - An extremely common NSAID that has anticoagulant effects; Dipyridamole, a drug that inhibits platelet activation [2] when given chronically and causes vasodilation when given at high doses over ...
The morpholinone part of rivaroxaban is “sandwiched” between amino acids Tyr-99 and Phe-174 and the aryl ring of rivaroxaban is oriented perpendicularly across Trp-215. The morpholinone carbonyl group does not have a direct interaction to the FXa backbone, instead, it contributes to a planarization of the morpholinone ring and therefore ...
An anticoagulant, commonly known as a blood thinner, is a chemical substance that prevents or reduces the coagulation of blood, prolonging the clotting time. [1] Some occur naturally in blood-eating animals, such as leeches and mosquitoes, which help keep the bite area unclotted long enough for the animal to obtain blood.
Andexanet alfa is used to stop life-threatening or uncontrollable bleeding in people who are taking rivaroxaban or apixaban. [8] Studies in healthy volunteers show that the molecule binds factor Xa inhibitors and counters their anti-Xa-activity. [11] The first published clinical trial was a prospective, open label, single group study. [12]
There are three types of DTIs, dependent on their interaction with the thrombin molecule. Bivalent DTIs (hirudin and analogs) bind both to the active site and exosite 1, while univalent DTIs bind only to the active site. [1] The third class of inhibitors, which are gaining importance recently, is the allosteric inhibitors.
Often a combination of aspirin plus an ADP/P2Y inhibitor [7] (such as clopidogrel, prasugrel, ticagrelor, or another) is used to obtain greater effectiveness than with either agent alone. This is known as "dual antiplatelet therapy" (or DAPT).