Drug information of Rivaroxaban

Rivaroxaban

Drug group: Anticoagulants

Rivaroxaban is an anticoagulant (blood thinner) that prevents the formation of blood clots. Rivaroxaban is used to prevent or treat a type of blood clot called deep vein thrombosis (DVT), which can lead to blood clots in the lungs (pulmonary embolism).
A DVT can occur after certain types of surgery. Rivaroxaban is also used in people with atrial fibrillation (a heart rhythm disorder) to lower the risk of stroke caused by a blood clot.

Mechanism of effect

Inhibits platelet activation and fibrin clot formation via direct, selective and reversible inhibition of factor Xa (FXa) in both the intrinsic and extrinsic coagulation pathways.
FXa, as part of the prothrombinase complex consisting also of factor Va, calcium ions, factor II and phospholipid, catalyzes the conversion of prothrombin to thrombin.
Thrombin both activates platelets and catalyzes the conversion of fibrinogen to fibrin.

Pharmacodynamic

Rivaroxaban is an anticoagulant which binds directly to factor Xa. Thereafter, it effectively blocks the amplification of the coagulation cascade, preventing the formation of thrombus.

Pharmacokinetics

Following oral administration, rivaroxaban is rapidly absorbed and reaches peak plasma concentration in 2-4 hours. Bioavailability of the 10 mg dose is >80%. Plasma protein binding is about 92% to 95%. Metabolism: Hepatic via CYP3A4/5 and CYP2J2. Excretion: Urine (66% primarily via active tubular secretion [~36% as unchanged drug; 30% as inactive metabolites]); feces (28% [7% as unchanged drug; 21% as inactive metabolites]). Half-Life Elimination: Terminal: 5 to 9 hours; Elderly: 11 to 13 hours.

Dosage

Usual Adult Dose for Atrial Fibrillation
Recommended dose: 20 mg orally once a day
Usual Adult Dose for Deep Vein Thrombosis
Initial dose: 15 mg orally twice a day for first 21 days of therapy
Maintenance dose: 20 mg orally once a day for the remaining duration of treatment.
Usual Adult Dose for Pulmonary Embolism
Initial dose: 15 mg orally twice a day for first 21 days of therapy
Maintenance dose: 20 mg orally once a day for the remaining duration of treatment.
Usual Adult Dose for Deep Vein Thrombosis Prophylaxis after Knee or Hip Replacement Surgery
Initial dose: 10 mg orally once a day starting 6 to 10 hours after surgery
Duration of therapy:
Hip replacement surgery: 35 days
Knee replacement surgery: 12 days

Alerts

1-The most common complication is bleeding; major hemorrhages (eg, intracranial, GI, retinal, epidural hematoma, adrenal bleeding) have been reported.
2- Avoid use in patients with moderate to severe hepatic impairment (Child-Pugh classes B and C) or in patients with any hepatic disease associated with coagulopathy.
3- Use with caution in patients with moderate renal impairment (CrCl 30 to 50 mL/minute) . Discontinue use in patients who develop acute renal failure. Use is not recommended in patients with ESRD requiring hemodialysis
4- Safety and efficacy have not been established in patients with prosthetic heart valves or significant rheumatic heart disease (eg, mitral stenosis).

Points of recommendation

1- Have patient report immediately to prescriber signs of bleeding (vomiting blood or vomit that looks like coffee grounds, coughing up blood, blood in the urine, black, red, or tarry stools, bleeding from the gums, abnormal vaginal bleeding, bruises without a reason or that get bigger, or any bleeding that is very bad or that you cannot stop), severe dizziness, syncope, paresthesia, loss of strength or energy, a fall hitting head, illogical thinking, severe headache, wound site pain, edema, or new drainage
2- Food should be taken with the 15 mg and 20 mg tablet. Food increases the bioavailability of the 20 mg dose.

Pregnancy level

C

Related drugs

Apixaban , Edoxaban


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