EDOBAN 60

Indications

• Prophylaxis of stroke and systemic embolism in non-valvular atrial fibrillation
• Treatment of deep vein thrombosis
• Prophylaxis of recurrent deep vein thrombosis
• Treatment of pulmonary embolism
• Prophylaxis of recurrent pulmonary embolism

Dosage

Adults: For adults with body weight up to 61 kg: 30 mg once daily. For adults with body weight 61 kg and above: 60 mg once daily. Treatment duration should be adjusted according to risk factors.

Mechanism of action

Edoxaban selectively inhibits factor Xa, an essential serine endopeptidase in the coagulation cascade necessary for the conversion of prothrombin into thrombin. By binding directly to factor Xa, it prevents thrombus formation by inhibiting both free and prothrombinase-bound factor Xa, as well as thrombin-induced platelet aggregation.

Pharmacodynamics

The administration of edoxaban leads to a prolongation of clotting time as measured by tests such as activated partial thromboplastin time (aPTT), prothrombin time (PT), and international normalized ratio (INR). This pharmacodynamic effect directly correlates with its anticoagulant activity.

Pharmacokinetics

Edoxaban is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1 to 2 hours. It has a bioavailability of approximately 62% and is primarily eliminated via the kidneys, with renal impairment affecting its clearance. The half-life of edoxaban is approximately 10 to 14 hours, allowing for once-daily dosing. It is also subject to moderate hepatic metabolism.

Contra-indications

• Active bleeding
• Severe renal impairment (creatinine clearance <15 mL/min)
• Concomitant treatment with other anticoagulants
• Hypersensitivity to edoxaban or any excipients

Adverse effects

• Bleeding complications
• Anemia
• Thrombocytopenia
• Liver enzyme abnormalities
• Gastrointestinal disturbances

Interactions

• Increased exposure with eliglustat
• Increased exposure with tucatinib
• Unknown interaction with antiepileptics (fosphenytoin, phenobarbital, phenytoin, primidone)
• Unknown interaction with aspirin
• Unknown interaction with ceritinib
• Unknown interaction with ciclosporin
• Unknown interaction with lapatinib
• Unknown interaction with mirabegron
• Unknown interaction with pitolisant
• Unknown interaction with ranolazine

Precautions

• Monitor renal function regularly
• Use with caution in patients with increased bleeding risk
• Counsel patients on signs and symptoms of bleeding
• Regularly review the need for continued treatment

Pregnancy

Edoxaban is not recommended during pregnancy due to potential risks to the fetus.

Breast-feeding

It is not known if edoxaban is excreted in human milk. Caution is advised when administering to nursing mothers.

Storage

Store at room temperature (15-30°C) in a tightly closed container, protected from moisture.

Formulations

• Edoxaban 30 mg tablets
• Edoxaban 60 mg tablets

Mechanism of action

Edoxaban is a selective inhibitor of factor Xa, a serine endopeptidase of the clotting cascade required for cleavage of prothrombin into thrombin. Edoxaban tosylate monohydrate, an oral, direct activated factor X (Xa) inhibitor, is an anticoagulant. Factor Xa plays a central role in the blood coagulation cascade by serving as the convergence point for the intrinsic and extrinsic pathways; inhibition of coagulation factor Xa by edoxaban prevents conversion of prothrombin to thrombin and subsequent thrombus formation. The drug binds directly and selectively to factor Xa without the need for a cofactor (e.g., antithrombin III), and inhibits both free and prothrombinase-bound factor Xa as well as thrombin-induced platelet aggregation.

Pharmacodynamics

Administration of edoxaban results in prolongation of clotting time tests such as aPTT (activated partial thromboplastin time), PT (prothrombin time), and INR (international normalized ratio).