Rivaroxaban


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Prophylaxis of postoperative venous thromboembolism 10 mg once daily starting 6-10 hours after surgery. Duration of treatment: 5 weeks (major hip surgery); 2 weeks (major knee surgery). Deep vein thrombosis; Pulmonary embolism Initial: 15 mg bid for 3 weeks. Maintenance: 20 mg once daily. Prophylaxis of recurrent cases: 10 mg once daily following completion of at least 6 months of anticoagulant treatment or 20 mg once daily in patients with high risk of recurrence. Prophylaxis of stroke and systemic embolism in non-valvular atrial fibrillation 20 mg once daily, with the evening meal. Prophylaxis of cardiovascular events in high-risk patients In patients with coronary or peripheral artery disease in combination with aspirin: 2.5 mg bid.
Dosage Details
Oral
Deep vein thrombosis, Pulmonary embolism
Adult: Treatment: Initially, 15 mg bid for 3 weeks. Maintenance: 20 mg once daily. Prophylaxis of recurrent cases: 10 mg once daily following completion of at least 6 months of anticoagulant treatment or 20 mg once daily in patients with high risk of recurrence.

Oral
Prophylaxis of stroke and systemic embolism in non-valvular atrial fibrillation
Adult: 20 mg once daily, with the evening meal.

Oral
Prophylaxis of postoperative venous thromboembolism
Adult: 10 mg once daily starting 6-10 hours after surgery. Duration of treatment: 5 weeks (major hip surgery); 2 weeks (major knee surgery).

Oral
Prophylaxis of cardiovascular events in high-risk patients
Adult: In patients with coronary or peripheral artery disease in combination with aspirin: 2.5 mg bid.
Renal Impairment
Prophylaxis of postoperative venous thromboembolism; Prophylaxis of cardiovascular events in high-risk patients:
CrCl (mL/min)
Dosage 
<15
Contraindicated.

Deep vein thrombosis; Pulmonary embolism:

CrCl (mL/min)
Dosage
<15 Contraindicated. 
15-50 Initially, 15 mg bid for 3 weeks, followed by 20 mg once daily. May reduce maintenance dose to 15 mg once daily if risk of bleeding outweighs risk of recurrence.

Prophylaxis of stroke and systemic embolism in non-valvular atrial fibrillation:
CrCl (mL/min) Dosage
<15 Contraindicated. 
15-50 15 mg once daily.
Hepatic Impairment
Moderate to severe (Child-Pugh class B and C): Contraindicated.
Administration
10-Mg Tab: May be taken with or without food.
15- &Amp; 20-Mg Tab: Should be taken with food.
Contraindications
Active pathological bleeding, lesions or conditions at increased risk of major haemorrhage (e.g. recent gastrointestinal ulceration, recent brain or spinal injury or surgery, recent intracranial haemorrhage). Renal impairment (CrCl <15 mL/min) or undergoing dialysis. Moderate to severe hepatic impairment (Child-Pugh Class B and C) or hepatic disease associated with coagulopathy. Pregnancy and lactation. Concomitant use with azole-antimycotics (e.g. ketoconazole) or HIV protease inhibitors (e.g. ritonavir); other anticoagulants such as heparin (e.g. enoxaparin, dalteparin), heparin derivatives (e.g. fondaparinux) or oral anticoagulants (e.g. warfarin, dabigatran, apixaban).
Special Precautions
Patient with risks of bleeding (e.g. bacterial endocarditis, congenital or acquired bleeding disorders, vascular retinopathy, uncontrolled severe hypertension, bronchiectasis or history of pulmonary bleeding); significant rheumatic heart disease, prosthetic heart valves. Renal impairment (CrCl 15-50 mg/mL). Avoid abrupt discontinuation in the absence of alternative treatment.
Adverse Reactions
Significant: Bleeding (e.g. as epistaxis, gingival, genitourinary bleeding), anaemia (prolonged use).
Gastrointestinal disorders: Abdominal pain.
Injury, poisoning and procedural complications: Wound secretion.
Investigations: Increased serum transaminases.
Musculoskeletal and connective tissue disorders: Back pain, limb pain.
Nervous system disorders: Dizziness.
Skin and subcutaneous tissue disorders: Pruritus.
Potentially Fatal: Major bleeding, post haemorrhagic anaemia.
Patient Counseling Information
This drug may cause syncope and dizziness, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor renal function and CBC prior to initiation of therapy and at least annually; LFT; signs of bleeding.
Overdosage
Symptoms: Haemorrhagic complications. Management: Symptomatic and supportive treatment. Activated charcoal may be given to reduce absorption within 8 hours of ingestion.
Drug Interactions
Increased risk of bleeding with NSAIDs (e.g. aspirin), antiplatelet agents (e.g. clopidogrel), SSRI, and serotonin-norepinephrine reuptake inhibitors (SNRI). Decreased serum concentration with strong CYP3A4 inducers (e.g. rifampicin, phenytoin, carbamazepine, phenobarbital).
Potentially Fatal: Increased plasma concentration and increased risk of bleeding with CYP3A4 and P-gp inhibitors (e.g. ketoconazole, itraconazole, voriconazole, posaconazole); HIV protease inhibitors (e.g. ritonavir); other anticoagulants such as unfractionated heparin, low molecular weight heparin (e.g. enoxaparin, dalteparin), heparin derivatives (e.g. fondaparinux), oral anticoagulants (e.g. warfarin, dabigatran, apixaban).
Food Interaction
Decreased serum concentration with St. John’s wort.
Lab Interference
Prolonged clotting in PT, aPTT, HepTest and anti-factor Xa activity.
Action
Description: Rivaroxaban is an anticoagulant which selectively and directly inhibits factor Xa (activated factor X) in both the intrinsic and extrinsic pathways of the blood coagulation cascade thereby, inhibiting thrombin formation and development of thrombi. Factor Xa converts prothrombin to thrombin leading to fibrin clot formation and platelet activation.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 80-100%. Time to peak plasma concentration: 2-4 hours.
Distribution: Crosses placenta and enters breastmilk. Volume of distribution: Approx 50 L. Plasma protein binding: Approx 92-95%, mainly to albumin.
Metabolism: Metabolised in the liver by CYP3A4/5 and CYP2J2 via oxidative degradation and hydrolysis.
Excretion: Via urine (66%; approx 36% as unchanged drug, 30% as inactive metabolites); faeces (28%; 7% as unchanged drug, 21% as inactive metabolites). Elimination half-life: 5-9 hours.
Chemical Structure

Chemical Structure Image
Rivaroxaban

Source: National Center for Biotechnology Information. PubChem Database. Rivaroxaban, CID=9875401, https://pubchem.ncbi.nlm.nih.gov/compound/Rivaroxaban (accessed on Jan. 23, 2020)

Storage
Store below 30°C.
ATC Classification
B01AF01 - rivaroxaban ; Belongs to the class of direct factor Xa inhibitors. Used in the treatment of thrombosis.
References
Anon. Rivaroxaban. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/09/2014.

Buckingham R (ed). Rivaroxaban. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/08/2019.

Joint Formulary Committee. Rivaroxaban. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/08/2019.

McEvoy GK, Snow EK, Miller J et al (eds). Rivaroxaban. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/09/2014.

Xarelto Tablet (Janssen Ortho LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/08/2019.

Xarelto Tablets. U.S. FDA. https://www.fda.gov/. Accessed 01/09/2014.

Disclaimer: This information is independently developed by MIMS based on Rivaroxaban from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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