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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] It is taken by mouth. [8]
The monitoring of warfarin and keeping the international normalized ratio (INR) between 2.0 and 3.0, along with avoiding over and under treatment, has driven a search for an alternative. [3] [14] A naturally occurring inhibitor of factor Xa was reported in 1971 by Spellman et al. from the dog hookworm. [15]
The abbreviation DVT/PE refers to a VTE where a deep vein thrombosis (DVT) has moved to the lungs (PE or pulmonary embolism). [4] Since the veins return blood to the heart, if a piece of a blood clot formed in a vein breaks off it can be transported to the right side of the heart, and from there into the lungs.
Deep vein thrombosis (DVT) is a type of venous thrombosis involving the formation of a blood clot in a deep vein, most commonly in the legs or pelvis. [9] [a] A minority of DVTs occur in the arms. [11] Symptoms can include pain, swelling, redness, and enlarged veins in the affected area, but some DVTs have no symptoms. [1]
Rivaroxaban. During the SAR development of rivaroxaban, researchers realized that adding a 5-chlorothiophene-2-carboxamide group to the oxazolidonine core could increase the potency by 200 fold, which had previously been too weak for medical use. In addition to this discovery, a clear preference for the (S)-configuration was confirmed.
Hospital admissions in the US for pulmonary embolism are 200,000 to 300,000 yearly. [10] Thrombosis that develops into DVT will affect 900,000 people and kill up to 100,000 in the US. On average 28,726 hospitalized adults aged 18 and older with a VTE blood clot diagnosis die each year. [11] Risk of thrombosis is related to hospitalization. [4]
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