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.
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.
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.
OTHER BRANDS
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