Generic
Betrixaban
2 brands available in the market
At a glance
Betrixaban is a factor Xa inhibitor used to prevent venous thromboembolism (VTE) in hospitalized adults with acute medical illness who have restricted mobility and other risk factors. It reduces thrombin generation by blocking factor Xa and increases bleeding risk.
Description
Betrixaban is an oral factor Xa inhibitor that selectively blocks the active site of factor Xa and does not require antithrombin III for activity. It inhibits free FXa and prothrombinase activity, decreasing thrombin generation. It is indicated for VTE prophylaxis in patients with restricted mobility and other risk factors. Dosage: initial 160 mg single dose, then 80 mg once daily with food for 35–42 days. In severe renal impairment (CrCl 15–<30 mL/min): initial 80 mg, then 40 mg daily. Bleeding is the main side effect; neuraxial anesthesia poses a paralysis risk.
Indications
Prophylaxis of venous thromboembolism (VTE) in adult patients hospitalized for acute medical illness with moderate or severe restricted mobility and other risk factors for VTE.
Therapeutic class
Anticoagulant
Pharmacological class
Factor Xa Inhibitor
Pharmacology
Betrixaban is a factor Xa inhibitor that selectively blocks the active site of FXa and does not require a cofactor (e.g., antithrombin III) for activity. It inhibits free FXa and prothrombinase activity, thereby decreasing thrombin generation. It has no direct effect on platelet aggregation.
Mechanism of action
Betrixaban directly inhibits factor Xa, reducing prothrombinase activity and thrombin production, thus preventing the final steps of the coagulation cascade.
Dosage
Severe renal impairment (CrCl 15–<30 mL/min): Initial 80 mg, then 40 mg once daily.
Mild hepatic impairment: no adjustment; moderate to severe: avoid use.
Administration
Take with food at approximately the same time each day. Follow the prescribed dose and schedule.
Missed dose
If you miss a dose, take it as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not double the dose.
Side effects
Most common: Bleeding (clinically relevant non-major 2.45%, epistaxis 2%, hematuria 2%). Others: Major bleeding (0.67%), GI bleeding (0.51%), intracranial hemorrhage (0.05%), fatal bleeding (0.03%).
Precautions & warnings
Increases bleeding risk and can cause serious and fatal bleeding. Promptly evaluate signs of blood loss. Risk of epidural/spinal hematoma with neuraxial anesthesia, which may cause permanent paralysis. Severe renal impairment and P-gp inhibitors increase bleeding risk.
Contraindications
Active pathological bleeding, severe hypersensitivity to betrixaban.
Drug interactions
P-gp inhibitors (e.g., ketoconazole, amiodarone) increase betrixaban levels. P-gp inducers (e.g., rifampin) decrease levels. Anticoagulants, antiplatelets, thrombolytics, SSRIs, SNRIs, NSAIDs increase bleeding risk.
Food interactions
Take with food; no specific food interaction established.
Use in pregnancy
No data in pregnant women; treatment may increase hemorrhage risk. Use only if potential benefit outweighs risk.
Use in lactation
Unknown if excreted in human milk. Consider benefits of breastfeeding against the mother's need and potential risks.
Pediatric use
Safety and efficacy in pediatric patients have not been established.
Geriatric use
No specific dose adjustment for elderly, but caution (consider renal function).
Renal / hepatic impairment
Renal impairment: Mild-moderate (CrCl >30 mL/min): no adjustment; severe (CrCl 15–<30): initial 80 mg, then 40 mg daily. Hepatic impairment: mild no adjustment; moderate-severe avoid.
Overdose effects
Overdose may increase bleeding risk. Seek medical attention immediately if symptoms occur.
Storage conditions
Store below 30°C, away from light and moisture. Keep out of reach of children.
Chemical structure
Betrixaban