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Apixaban Dose

Apixaban Dose

DESCRIPTION

ELIQUIS (apixaban), a factor Xa (FXa) inhibitor, is chemically described as 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4c]pyridine-3-carboxamide. Its molecular formula is C25H25N5O4, which corresponds to a molecular weight of 459.5. Apixaban has the following structural formula:

ELIQUIS® (apixaban) - Structural Formula  - Illustration

Apixaban is a white to pale-yellow powder. At physiological pH (1.2-6.8), apixaban does not ionize; its aqueous solubility across the physiological pH range is ~0.04 mg/mL.

DRUG INTERACTIONS

• Combined P-gp and Strong CYP3A4 Inhibitors: Inhibitors of P-glycoprotein (P-gp) and cytochrome P450 3A4 (CYP3A4) increase exposure to apixaban and increase the risk of bleeding. For patients receiving ELIQUIS doses of 5 mg or 10 mg twice daily, reduce the dose of ELIQUIS by 50% when ELIQUIS is coadministered with drugs that are combined P-gp and strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, or ritonavir). In patients already taking 2.5 mg twice daily, avoid coadministration of ELIQUIS with combined P-gp and strong CYP3A4 inhibitors.

 Clarithromycin Although clarithromycin is a combined P-gp and strong CYP3A4 inhibitor, pharmacokinetic data suggest that no dose adjustment is necessary with concomitant administration with ELIQUIS.

Usual Adult Dose for Prevention of Thromboembolism in Atrial Fibrillation

5 mg orally 2 times a day

Use:

Reduction of risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation.

Usual Adult Dose for Thromboembolic Stroke Prophylaxis

5 mg orally 2 times a day

WARNINGS

Included as part of the PRECAUTIONS section.

DOSAGE AND ADMINISTRATION

Recommended Dose

Reduction Of Risk Of Stroke And Systemic Embolism In Patients With Nonvalvular Atrial Fibrillation

The recommended dose of ELIQUIS for most patients is 5 mg taken orally twice daily.

The recommended dose of ELIQUIS is 2.5 mg twice daily in patients with at least two of the following characteristics:

  • age greater than or equal to 80 years
  • body weight less than or equal to 60 kg
  • serum creatinine greater than or equal to 1.5 mg/dL

PRECAUTIONS

Increased Risk Of Thrombotic Events After Premature Discontinuation

Premature discontinuation of any oral anticoagulant, including ELIQUIS, in the absence of adequate alternative anticoagulation increases the risk of thrombotic events. An increased rate of stroke was observed during the transition from ELIQUIS to warfarin in clinical trials in atrial fibrillation patients. If ELIQUIS is discontinued for a reason other than pathological bleeding or completion of a course of therapy, consider coverage with another anticoagulant [see DOSAGE AND ADMINISTRATION and Clinical Studies.

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