Xarelto (Oral)

Uses

Xarelto (Oral) 2.5 mg:

• For the prevention of atherothrombotic events in adult patients after an Acute Coronary Syndrome (ACS) with elevated cardiac biomarkers (Troponin or CK-MB). It is co-administered with Aspirin alone or with Aspirin plus Clopidogrel orTidopidine.

Xarelto (Oral) 10-20 mg:

• To reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation
• Deep vein thrombosis (DVT) & pulmonary embolism (PE) and reduction in the risk of recurrence of DVT and of PE
• For the prophylaxis of DVT, which may lead to PE in patients undergoing knee or hip replacement surgery

Xarelto (Oral) is also used to associated treatment for these conditions: Cardiovascular Mortality, Deep Vein Thrombosis, Deep vein thrombosis recurrent, Myocardial Infarction, Pulmonary Embolism, Recurrent pulmonary embolism, Stroke, Systemic Embolism

How Xarelto (Oral) works

Xarelto (Oral) competitively inhibits free and clot bound factor Xa. Factor Xa is needed to activate prothrombin (factor II) to thrombin (factor IIa). Thrombin is a serine protease that is required to activate fibrinogen to fibrin, which is the loose meshwork that completes the clotting process. Since one molecule of factor Xa can generate more than 1000 molecules of thrombin, selective inhibitors of factor Xa are profoundly useful in terminating the amplification of thrombin generation. The action of rivaroxaban is irreversible.

Dosage

Xarelto (Oral) dosage

Xarelto (Oral) 2.5 mg:

The recommended dose is 2.5 mg twice daily. Patients should also take a daily dose of 75-100 mg Aspirin or a daily dose of 75-100 mg Aspirin in addition to either a daily dose of 75 mg clopidogrel or a standard daily dose of ticlopidine.

Xarelto (Oral) 10-20 mg:

Nonvalvular Atrial Fibrillation: For patients with Creatinin Clearance >50 mL/min: 20 mg orally, once daily with the evening meal. For patients with Creatinin Clearance 15-50 ml/min: 15 mg orally, once daily with the evening meal

Treatment of DVT & PE: 15 mg orally twice daily with food for the first 21 days for the initial treatment of acute DVT or PE. After the initial treatment period, 20 mg orally once daily with food for the remaining treatment

Prevention in the risk of recurrence of DVT and of PE: 20 mg once daily with food

Prophylaxis of DVT following Hip replacement surgery: 10 mg once daily for 35 days

Prophylaxis of DVT following knee replacement surgery: 10 mg once daily for 12 days

Side Effects

The most common adverse reaction is bleeding. Increased risk of stroke after discontinuation in nonvalvular atrial fibrillation.

Toxicity

Excessive bleeding. Overdosages should be treated using activated charcoal and supportive measures such as mechanical compression and hemodynamic support. If bleeding is not controlled, the following procoagulants can be administered: activated prothrombin complex concentrate, prothrombin complex concentrate and recombinant factor VIIa. There is also a higher chance of post procedural hemorrhage compared to enoxaparin (1.55% vs. 1.39% respectively).

Precaution

Xarelto (Oral) can cause bleeding. Promptly evaluate signs and symptoms of blood loss. Xarelto (Oral) use not recommended in case of Prosthetic heart valves.

Interaction

CYP3A4, P-GP inhibitors and NSAIDs.

Food Interaction

• Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
• Avoid St. John's Wort. Co-administration will decrease levels of this medication.
• Take with food. Xarelto (Oral) 15-20mg dose should be taken with food as food significantly impacts the bioavailability at that dose.
• Take with or without food. Xarelto (Oral) 10mg dose can be taken with or without food as it does not significantly impact the bioavailability at that dose.

Xarelto (Oral) Drug Interaction

Major: aspirin, aspirin, aspirinModerate: omega-3 polyunsaturated fatty acidsUnknown: tadalafil, rosuvastatin, furosemide, atorvastatin, pregabalin, metoprolol, metoprolol, polyethylene glycol 3350, acetaminophen / hydrocodone, acetaminophen, tiotropium, budesonide / formoterol, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol

Xarelto (Oral) Disease Interaction

Major: bleeding, hepatic impairment, renal disease, valvular heart disease, unstable blood pressure

Volume of Distribution

The steady state Vd is 50 L

Elimination Route

Following oral administration, rivaroxaban is rapidly absorbed and reaches peak plasma concentration in 2-4 hours. Bioavailability of the 10 mg dose is >80%. However, the 15-20 mg dose have a lower bioavailability if taken in the fasted state and consequently should be taken with food.

Half Life

The terminal half life is 5-9 hours in adults and 11-13 hours in the elderly.

Clearance

Systemic clearance is approximately 10 L/h, so rivaroxaban is considered a drug with low clearance. Renal clearance is ~3-4 L/h.

Elimination Route

Approximately two-thirds of rivaroxaban is excreted into urine (via active tubular secretion in which approximately 36% as unchanged drug and 30% as inactive metabolism). The remaining third of the administered dose is excreted via feces in which 7% is in the form of unchanged drug and 21% as inactive metabolites.

Pregnancy & Breastfeeding use

There are no adequate or well-controlled studies of Xarelto (Oral) in pregnant women, and dosing for pregnant women has not been established.

Safety and efficacy of Xarelto (Oral) have not been established in breast-feeding women

Contraindication

Active pathological bleeding & severe hypersensitivity reaction to Xarelto (Oral)

Storage Condition

Protect from light, store below 30° C. Keep out of reach of children.

Innovators Monograph

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