Dosing & Uses
Dosage Forms & Strengths
capsule
- 40mg
- 80mg
Venous Thromboembolism Prevention
Indicated for prophylaxis of venous thromboembolism (VTE) in adults hospitalized for acute medical illness who are at risk for thromboembolic complications owing to moderate or severe restricted mobility and other risk factors for VTE
Initial single dose: 160 mg PO, THEN 80 mg PO qDay
Recommended duration of treatment: 35-42 days
Dosage Modifications
Coadministration with P-gp inhibitors
- Initial single dose of 80 mg, then 40 mg PO qDay x35-42 days
- Patients taking P-gp inhibitor who also have severe renal impairment: Not recommended
Renal impairment
- Mild-to-moderate (CrCl >30 mL/min): No dose adjustment needed
- Severe (CrCl ≥15 to <30 mL/min): Initial single dose of 80 mg, then 40 mg PO qDay x35-42 days
Hepatic impairment
- Not recommended; drug was not evaluated in hepatic impairment, because these patients may have intrinsic coagulation abnormalities
Dosing Considerations
Limitations of use
- Safety and efficacy not established for patients with prosthetic heart valves (not studied)
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
1-10%
Clinically relevant nonmajor bleeding (2.45%)
Epistaxis (2%)
Hematuria (2%)
<1%
Bleeding
- Major bleeding (0.67%)
- GI bleeding (0.51%)
- Intracranial hemorrhage (0.05%)
- Fatal bleeding (0.03%)
Warnings
Black Box Warnings
Spinal/epidural hematoma
- Epidural or spinal hematomas may occur in patients who are receiving neuraxial anesthesia or undergoing spinal puncture
- These hematomas may result in long-term or permanent paralysis
- Monitor patients frequently for signs and symptoms of neurological impairment (eg, numbness or weakness of legs, bowel, or bladder); if neurological compromise is noted, urgent treatment is necessary
- Consider the benefits and risks before neuraxial intervention in patients who are anticoagulated or to be anticoagulated
- Management
- Do not remove an epidural catheter earlier than 72 hr after the last administration of betrixaban
- Do not administer the next betrixaban dose earlier than 5 hr after catheter removal
- If traumatic puncture occurs, delay administering betrixaban for 72 hr
- Factors that can increase the risk include
- Use of indwelling epidural catheters
- Concomitant use of other drugs that affect hemostasis (eg, NSAIDs, platelet inhibitors, other anticoagulants)
- History of traumatic or repeated epidural or spinal punctures
- History of spinal deformity or spinal surgery
- Optimal timing between the administration of drug and neuraxial procedures is not known
Contraindications
Active pathological bleeding
Severe hypersensitivity
Cautions
Increases bleeding risk and can cause serious and potentially fatal bleeding; promptly evaluate any signs or symptoms of blood loss; there is no established way to reverse betrixaban’s anticoagulant effect, which can persist for at least 72 hr after the last dose; protamine, vitamin K, and tranexamic acid are not expected to reverse betrixaban anticoagulant activity
Risk of paralysis with neuraxial anesthesia (see Black Box Warnings)
Increased bleeding risk with severe renal impairment (see Dosage Modifications)
Drug interaction overview
- P-gp substrate
- Reduce betrixaban dose if coadministration with P-gp inhibitors, owing to increased bleeding risk; avoid coadministration in patients with severe renal impairment receiving concomitant P-gp inhibitors
- Coadministration with drugs affecting hemostasis increases bleeding risk; examples include aspirin and other antiplatelet agents, other anticoagulants, heparin, thrombolytic agents, SSRIs, SNRIs, and NSAIDs
Pregnancy
Pregnancy
No data exist with use in pregnant women, but treatment is likely to increase risk of hemorrhage during pregnancy and delivery
Use during pregnancy only if the potential benefit outweighs the potential risk to the mother and fetus
Animal studies
- Although betrixaban has not been associated with adverse developmental fetal outcomes in animals, maternal toxicity (ie, hemorrhage) was identified in these studies
Lactation
Unknown if distributed in human breast milk
Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition
Pregnancy Categories
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Pharmacology
Mechanism of Action
Oral factor Xa (FXa) inhibitor that selectively blocks the active site of FXa and does not require a cofactor (eg, antithrombin III) for activity; inhibits free FXa and prothrombinase activity
By directly inhibiting FXa, betrixaban decreases thrombin generation
Has no direct effect on platelet aggregation
Blood coagulation cascade is dependent upon the activation of factor X to FXa via the intrinsic and extrinsic pathways, which play a central role in the blood coagulation cascade
Absorption
Bioavailability: 34%
Peak plasma time: 3-4 hr
Distribution
Protein bound: 60%
Vd: 32 L/kg
Metabolism
Unchanged betrixaban is the predominant component found in human plasma
Two inactive major metabolites formed by CYP-independent hydrolysis comprise the other components in plasma, accounting for 15-18% of the circulating drug-related material
Elimination
Half-life: 19-27 hr
Excretion: 85% feces; 11% urine
Administration
Oral Administration
Take with food at approximately the same time each day
Missed dose: Take as soon as possible on the same day; do not double dosage to make up for a missed dose
Storage
Store at room temperature 20-25°C (68-77°F)
Images
Patient Handout
Formulary
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