Edoxaban
Indications
Edoxaban is used for:
Indicated to reduce risk of stroke and systemic embolism associated with nonvalvular atrial fibrillation (NVAF), deep vein thrombosis (DVT), pulmonary embolism (PE), in patients who have been initially treated with a parenteral anticoagulant
Adult Dose
Stroke Prophylaxis with Atrial Fibrillation
Indicated to reduce risk of stroke and systemic embolism associated with nonvalvular atrial fibrillation (NVAF)
60 mg PO qDay
DVT or PE Treatment
Indicated for treatment of deep vein thrombosis (DVT) and pulmonary embolus (PE) in patients who have been initially treated with a parenteral anticoagulant for 5-10 days
>60 kg: 60 mg PO qDay
<60 kg: 30 mg PO qDay
Hepatic impairment
Mild (Child-Pugh A): No dose adjustment required
Moderate-to-severe (Child-Pugh B/C): Not recommended; these patients have intrinsic coagulation abnormalities
Child Dose
Renal Dose
Renal impairment (NVAF)
CrCl >95 mL/min: Do not use; increased ischemic stroke compared with warfarin (see Black Box Warnings)
CrCl >50 to 95 mL/min: No dosage adjustment required
CrCl 15-50 mL/min: 30 mg PO qDay
Renal impairment (DVT/PE)
>50 mL/min: No dosage adjustment required
15-50 mL/min: 30 mg PO qDay
Administration
May take with or without food
Contra Indications
Active pathological bleeding
Precautions
Efficacy reduced in patients with nonvalvular atrial fibrillation (NVAF) with CrCl >95 mL/min
Increased risk of stroke with discontinuation in patients with NVAF
Do not use neuraxial anesthesia (spinal/epidural anesthesia) or spinal/epidural puncture; patients treated with antithrombotic agents for prevention of thromboembolic complications are at risk of developing an epidural or spinal hematoma, which can result in long-term or permanent paralysis
Increases the risk of bleeding and can cause serious and potentially fatal bleeding; promptly evaluate any signs or symptoms of blood loss; discontinue if patient experiences active pathological bleeding; concomitant drugs that affect coagulation can increase this risk
Not recommended for patients with mechanical heart valves or moderate-to-severe mitral stenosis; safety and efficacy have not been established
Pregnancy-Lactation
Pregnancy
Available data about use in pregnant women are insufficient to determine whether there are drug-associated risks for adverse developmental outcomes; in animal developmental studies, no adverse developmental effects were seen when administered orally to pregnant rats and rabbits during organogenesis at up to 16-times and 8-times, respectively, the human exposure, when based on body surface area and AUC, respectively
Pregnancy confers an increased risk of thromboembolism that is higher for women with underlying thromboembolic disease and certain high-risk pregnancy conditions; published data describe that women with a previous history of venous thrombosis are at high risk for recurrence during pregnancy
Use may increase risk of bleeding in fetus and neonate; monitor neonates for bleeding
Labor or delivery
All patients receiving anticoagulants, including pregnant women, are at risk for bleeding; use during labor or delivery in women who are receiving neuraxial anesthesia may result in epidural or spinal hematomas; consider use of a shorter acting anticoagulant as delivery approaches
Lactation
There are no data on presence in human milk, or effects on breastfeeding infant or on milk production; drug was present in rat milk; because of potential for serious adverse reactions in nursing infants, including hemorrhage, advise patients that breastfeeding is not recommended during treatment
Interactions
Side Effects
Side effects of Edoxaban :
1-10% (ENGAGE AF-TIMI-48 study)
Abnormal LFTs (4.8%)
Rash (4.2%)
1-10% (Hokusai VTE study)
Abnormal LFTs (7.8%)
Rash (3.6%)
Anemia (1.7%)
<1% (ENGAGE AF-TIMI-48 study)
Interstitial lung disease (0.2%)
Bleeding (ENGAGE AF-TIMI-48 study)
Clinically relevant nonmajor bleeding (9.4%); warfarin (10.9%)
Anemia-related adverse events (9.6%); warfarin (6.8%)
Gastrointestinal bleeding
Major GI bleed (1.8%); warfarin (1.3%)
Upper GI (1.06%); warfarin (0.74%)
Lower GI (0.73%); warfarin (0.54%)
Severe, caused hemodynamic compromise requiring intervention (0.14%); warfarin (0.14%)
Fatal (<0.1%); warfarin (<0.1%)
Major bleeding
Major (3.1%); warfarin (3.7%)
Intracranial (0.5%); warfarin (1%)
Type of intracranial bleeding
Hemorrhagic stroke (0.3%); warfarin (0.6%)
Other ICH (0.2%); warfarin (0.5%)
Fatal bleeding
Fatal (1.8%); warfarin (0.4%)
ICH (0.2%); warfarin (0.4%)
Non-intracranial (<0.1%); warfarin (<0.1%)
Mode of Action
Factor Xa (FXa) inhibitor; inhibits platelet activation by selectively and reversibly blocking the active site of FXa without requiring a cofactor (eg, antithrombin III) for activity
Inhibits free FXa, prothrombinase activity, and thrombin-induced platelet aggregation
Inhibition of FXa in the coagulation cascade reduces thrombin generation and reduces thrombus formation