Apigy 5mg Tablet (Each tablet contains Apoxaban 5mg)

Indications

• Prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation
• Treatment of deep vein thrombosis (DVT)
• Treatment of pulmonary embolism (PE)
• Prevention of recurrence of DVT and PE

Dosage

Children: Refer to the BNF for Children text for specific dosing recommendations.

Adults: Refer to the BNF for specific dosing recommendations based on indication and patient factors.

Mechanism of action

Apixaban selectively inhibits Factor Xa, an essential enzyme in the coagulation cascade that converts prothrombin to thrombin. This inhibition decreases the production of thrombin, leading to reduced formation of fibrin clots.

Pharmacodynamics

Apixaban exhibits dose-dependent anticoagulant activity. The drug increases the activated partial thromboplastin time (aPTT) and prothrombin time (PT), reflecting its anticoagulant effects. The onset of action is rapid, with peak plasma concentrations occurring approximately 3 to 4 hours after administration. The anticoagulant effect is monitored indirectly through changes in coagulation parameters, though specific monitoring of apixaban levels is not routinely required.

Pharmacokinetics

Apixaban is rapidly absorbed, with peak plasma concentrations achieved within 3 to 4 hours after oral administration. It has a bioavailability of approximately 50%, with extensive hepatic metabolism via the cytochrome P450 system, particularly CYP3A4. The drug is eliminated primarily through hepatic metabolism and renal excretion, with a half-life of about 12 hours in healthy individuals. Factors such as age, renal function, and concomitant medications can influence its pharmacokinetics.

Contra-indications

• Active bleeding
• Severe renal impairment (CrCl < 15 mL/min)
• Severe hepatic impairment
• Hypersensitivity to apixaban or any excipients

Adverse effects

• Bleeding complications (e.g. gastrointestinal bleeding, intracranial hemorrhage)
• Anemia
• Nausea
• Elevated liver enzymes
• Rash
• Allergic reactions

Interactions

• Strong dual inhibitors of CYP3A4 and P-glycoprotein (e.g. ketoconazole, itraconazole) can increase apixaban levels
• Strong inducers of CYP3A4 (e.g. rifampicin, carbamazepine) can decrease apixaban levels
• Anticoagulants and antiplatelet agents may increase bleeding risk
• NSAIDs may increase the risk of gastrointestinal bleeding

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of bleeding in patients with risk factors
• Discontinue use prior to surgical procedures
• Use with caution in elderly patients due to increased risk of bleeding

Pregnancy

Apixaban is not recommended during pregnancy due to potential risks to the fetus. Limited data is available on its safety.

Breast-feeding

It is not known whether apixaban is excreted in human milk. Caution should be exercised when administered to breastfeeding women.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets: 2.5 mg, 5 mg