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Saturday, May 29, 2021

RIVAROXABAN TAB

 


 

 

 Rivaroxaban is an anticoagulant medication (blood thinner) used to treat and prevent blood clots. 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. It is taken by mouth.



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 C19H18ClN3O5S

Common side effects include bleeding. Other serious side effects may include spinal hematoma and anaphylaxis. It is unclear if use in pregnancy and breastfeeding is safe. Compared to warfarin it has fewer interactions with other medications. It works by blocking the activity of the clotting protein factor Xa.

 

Rivaroxaban was patented in 2007 and approved for medical use in the United States in 2011. In the United States, it will not be available as a generic medication until 2024. In 2018, it was the 100th most commonly prescribed medication in the United States, with more than 7 million prescriptions.

USES     -    In those with non-valvular atrial fibrillation, it appears to be as effective as warfarin in preventing ischemic strokes and embolic events. Rivaroxaban is associated with lower rates of serious and fatal bleeding events than warfarin, though rivaroxaban is associated with higher rates of bleeding in the gastrointestinal tract. 

In July 2012, the UK's National Institute for Health and Clinical Excellence recommended rivaroxaban to prevent and treat venous thromboembolism.


MECHANISM OF ACTION

Rivaroxaban inhibits both free Factor Xa and Factor Xa bound in the prothrombinase complex. It is a highly selective direct Factor Xa inhibitor with a rapid onset of action. Inhibition of Factor Xa interrupts the intrinsic and extrinsic pathway of the blood coagulation cascade, inhibiting both thrombin formation and development of thrombi. Rivaroxaban does not inhibit thrombin (activated Factor II), and no effects on platelets have been demonstrated. It allows predictable anticoagulation and dose adjustments and routine coagulation monitoring; dietary restrictions are not needed. 

Unfractionated heparin (UFH), low molecular weight heparin (LMWH), and fondaparinux also inhibit the activity of factor Xa, indirectly, by binding to circulating antithrombin (AT III) and must be injected, whereas the orally active warfarin, phenprocoumon, and acenocoumarol are vitamin K antagonists (VKA), decreasing a number of coagulation factors, including Factor X. 

Rivaroxaban has predictable pharmacokinetics across a wide spectrum of patients (age, gender, weight, race) and has a flat dose response across an eightfold dose range (5–40 mg). The oral bioavailability decreases with higher doses and increases when taken with food.

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