Rivaroxaban is the first orally active, direct inhibitor of factor Xa that is an anticoagulant. In contrast to warfarin, routine laboratory monitoring of the international normalized ratio (INR) is not required. However, there is no effective antidote in the event of a significant hemorrhage. Only the 10 mg tablet may be taken regardless of food intake. The tablets of 15 mg and 20 mg should be taken with food. Rivaroxaban was first licensed for medicinal use in the United States in 2011. The FDA granted approval on July 1, 2011.
Rivaroxaban
Uses of Rivaroxaban
Rivaroxaban, often known as Xarelto, is an anticoagulant (blood thinner) drug used to treat and prevent blood clots. It is specifically used to treat deep vein thrombosis (DVT; a blood clot, typically in the leg) and pulmonary embolism (PE) in people. Rivaroxaban is also used to prevent recurrences of DVT and PE in adults after initial therapy has been completed. It is also used to help prevent strokes or major blood clots in individuals with atrial fibrillation that is not caused by heart valve disease (a condition in which the heart beats irregularly, raising the risk of clots accumulating in the body and possibly causing strokes). Rivaroxaban is also used to prevent DVT and PE in adults undergoing hip or knee replacement surgery or in hospitalized patients with significant illnesses who are at risk of developing a clot due to limited mobility or other risk factors.
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Along with aspirin, it is used to reduce the risk of heart attack, stroke, or death in individuals with coronary artery disease (narrowing of the blood arteries that supply the heart) or peripheral arterial disease (poor circulation in the blood vessels that supply blood to the arms and legs). Rivaroxaban is also used to treat and prevent recurrences of DVT and PE in babies and children who have undergone at least 5 days of initial anticoagulation (blood thinner) therapy. It is also used to prevent DVT and PE following heart surgery in children with congenital heart disease who are at least 2 years old (an abnormality in the heart that develops before birth). Rivaroxaban belongs to the class of drugs known as factor Xa inhibitors. It functions by inhibiting the action of a natural chemical that aids in the formation of blood clots.
Doses of Rivaroxaban
Oral Rivaroxaban is available as a tablet and a suspension (liquid). This can be purchased at a reduced cost using Xarelto coupons. When used to treat DVT or PE in adults, rivaroxaban is often administered with food twice daily for 21 days, followed by once daily with food. When used to prevent DVT or PE in adults, rivaroxaban is typically administered once daily, with or without food, following at least six months of anticoagulant (blood thinner) therapy. When used to prevent a stroke in patients with atrial fibrillation, rivaroxaban is typically administered once a day with dinner. When rivaroxaban is administered to prevent DVT and PE after hip or knee replacement surgery, it is typically administered once daily, with or without food. The initial dose should be administered between 6 and 10 hours after surgery. Rivaroxaban is typically administered for 35 days after a hip replacement and 12 days after a knee replacement. When rivaroxaban is given to prevent DVT and PE in hospitalized individuals with serious illnesses who are at risk of developing a clot due to limited mobility, it is often taken with or without meals once a day, beginning while in the hospital, and lasts for 31 to 39 days. Adults with coronary artery disease or peripheral arterial disease typically take rivaroxaban and aspirin twice daily, with or without food. When rivaroxaban is used to treat or prevent DVT or PE in children and infants, it is typically administered 1 to 3 times daily with food following at least 5 days of anticoagulant (blood thinner) medication. After heart surgery, rivaroxaban is often administered 1 to 3 times daily, with or without meals, to children 2 years of age or older who have congenital heart disease.
Interactions
Rivaroxaban is contraindicated in the following drugs
- Betrixaban: Increases levels by anticoagulation. Contraindicated. Therapeutic duplication; may be used temporarily when switching anticoagulants.
- Defibrotide: defibrotide increases the effects of rivaroxaban by pharmacodynamic synergism. Contraindicated. Coadministration of defibrotide is contraindicated with antithrombotic/fibrinolytic drugs. This does not include use for routine maintenance or reopening of central venous lines.
- Mifepristone: mifepristone increases the toxicity of rivaroxaban by anticoagulation. Contraindicated.
- Omacetaxine: omacetaxine increases the toxicity of rivaroxaban by anticoagulation. Contraindicated.
- Prothrombin complex concentrate: pharmacodynamic antagonism. Contraindicated.
- Vorapaxar: vorapaxar increases the toxicity of rivaroxaban by anticoagulation. Contraindicated.
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Mechanism of Action of Rivaroxaban
Rivaroxaban inhibits both free and clot-bound factor Xa in a competitive manner. The activation of prothrombin (factor II) to thrombin requires factor Xa (factor IIa). Thrombin is a serine protease essential to convert fibrinogen to fibrin, the loose meshwork that completes the blood clotting process. Due to the fact that one molecule of factor Xa can generate over a thousand molecules of thrombin, specific inhibitors of factor Xa are extraordinarily effective at stopping the amplification of thrombin production. Rivaroxaban has an irreversible effect.
Absorption
Bioavailability: 80-100%
Peak plasma time: 2-4 hr
AUC: 29-56% decrease when released in the proximal small intestine compared with gastric absorption
Distribution
Protein-bound: 92-95% (mainly albumin)
Vd: 50 L
Metabolism
Metabolized by oxidative degradation catalyzed by CYP3A4/5 and CYP2J2; also metabolized by hydrolysis
Unchanged rivaroxaban is the predominant moiety in plasma with no major or active circulating metabolites (50% higher in patients of Japanese descent)
Substrate of P-gp and ABCG2 (Bcrp) efflux transporter proteins
Elimination
Half-life: 5-9 hr; 11-13 hr (elderly)
Total body clearance: 10 L/hr (following IV administration)
Excretion: feces (21% as metabolites; 28% unchanged), urine (30% as metabolites; 36% unchanged)
Side Effects of Rivaroxaban
Hematoma (<3%)
Back pain (2.9%)
Wound secretion (2.8%)
Abdominal pain (2.7%)
Dizziness (2.2%)
Pruritus (2.1-2.2%)
Pain in extremities (1.7%)
Insomnia (1.6%)
Anxiety (1.4%)
Blister (1.4%)
Fatigue (1.4%)
Muscle spasm (1.3%)
Syncope (1.2%)
Muscle spasm (1.2%)
Depression (1.2%)
Atrial fibrillation (6%)
DVT prophylaxis (<1%)
DVT treatment (1%)
VTE prophylaxis (0.7%)
References
Medscape. (n.d.). Rivaroxaban (Rx). Retrieved January 4, 2024, from https://reference.medscape.com/drug/xarelto-rivaroxaban-999670#0
National Library of Medicine. (n.d.). Rivaroxaban: MedlinePlus Drug Information. Retrieved January 4, 2024, from https://medlineplus.gov/druginfo/meds/a611049.html
DrugBank. (n.d.). Rivaroxaban. Retrieved January 4, 2024, from https://go.drugbank.com/drugs/DB06228
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