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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 amino acids residues Phe-174, Tyr-99, and Trp-215 form a narrow hydrophobic channel that is the S4 binding pocket. 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 ...
Andexanet alfa, sold under the brand name Andexxa among others, is an antidote for the medications rivaroxaban and apixaban, when reversal of anticoagulation is needed due to uncontrolled bleeding. [8] It has not been found to be useful for other factor Xa inhibitors. [9] It is given by injection into a vein. [9]
The enhancement to the molecule takes the form of a larger lipophilic group to enhance the fat solubility of the poison and greatly increase the time it acts within the animal's body. [5] However, as described above, the superwarfarins do not inhibit vitamin K and their effect is easily inhibited by vitamin K.
Edoxaban, sold under the brand name Lixiana among others, is an anticoagulant medication and a direct factor Xa inhibitor. [3] It is taken by mouth. [3]Compared with warfarin it has fewer drug interactions.
Stevens–Johnson syndrome (SJS) is a milder form of toxic epidermal necrolysis (TEN). [50] These conditions were first recognized in 1922. [ 27 ] A classification first published in 1993, that has been adopted as a consensus definition, identifies Stevens–Johnson syndrome, toxic epidermal necrolysis, and SJS/TEN overlap.
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