Apixaban

Apixaban is a novel oral anticoagulant (NOAC) that helps prevent and treat blood clots. It works by directly, selectively and reversibly inhibiting factor Xa, preventing platelet activation and fibrin clot formation. This prevents the conversion of thrombin and subsequent thrombus formation.

Apixaban is used to reduce the risk of stroke and systemic embolism in non-valvular atrial fibrillation, to prevent DVT and PE after hip or knee replacement surgery, and to treat DVT and PE and reduce the risk of recurrence.

Common side effects include bleeding more easily than normal (nosebleeds, bruising), nausea, skin rash, and low blood pressure.

• Reduce risk of stroke and systemic embolism in non-valvular atrial fibrillation
• Prophylaxis of DVT and PE after hip or knee replacement surgery
• Treatment of DVT and PE
• Reduction in risk of recurrent DVT and PE following initial therapy

Apixaban is a selective factor Xa inhibitor that directly, selectively and reversibly inhibits free and clot-bound factor Xa in both intrinsic and extrinsic coagulation pathways. Inhibition of factor Xa prevents the conversion of thrombin and subsequent thrombus formation.

As a result of FXa inhibition, apixaban prolongs clotting tests such as prothrombin time (PT), INR, and activated partial thromboplastin time (aPTT). However, changes observed at therapeutic doses are small and not useful in monitoring the anticoagulation effect.

Apixaban inhibits factor Xa, an enzyme essential for the conversion of prothrombin to thrombin. Thrombin converts fibrinogen to fibrin, leading to clot formation. By blocking factor Xa, apixaban prevents this cascade and reduces blood clot formation.

Standard Dose: 5 mg twice daily

Dose Adjustment (2.5 mg twice daily) - if any 2 of the following:

• Age ≥80 years
• Body weight ≤60 kg
• Serum creatinine ≥1.5 mg/dL

With strong CYP3A4 & P-gp inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin): 2.5 mg twice daily

VTE Prophylaxis (Hip/Knee Replacement): 2.5 mg twice daily, first dose 12-24 hr post-op. Hip: 32-38 days, Knee: 10-14 days.

DVT/PE Treatment: 10 mg twice daily for 7 days, then 5 mg twice daily. Recurrence prevention: 2.5 mg twice daily after 6 months.

Hepatic Impairment: Mild: No adjustment; Moderate: Limited data; Severe: Not recommended.

Renal Impairment (Non-valvular AF): Mild-moderate: No adjustment; ESRD on hemodialysis: 5 mg BID (2.5 mg BID if age ≥80 or weight ≤60).

Take this medicine in the dose and duration as advised by your doctor. Swallow the tablet whole, do not chew, crush or break. May be taken with or without food, but take at a fixed time.

If you miss a dose, take it as soon as possible on the same day and resume your normal schedule. Do not double the dose to make up for a missed dose.

• Epistaxis (nosebleeds)
• Haematoma
• Anaemia
• Haematuria (blood in urine)
• Contusion (bruising)
• Nausea
• GI, rectal or gingival haemorrhage
• Skin rash

Potentially Fatal: Epidural or spinal haematoma, fatal bleeding.

Serious Precautions:

• Discontinuing apixaban increases risk of thrombotic events - cover with another anticoagulant
• Increased risk of bleeding - be careful while shaving, cutting nails, using sharp objects or contact sports
• Discontinue at least 48 hours before surgery (high risk) or 24 hours (low risk)
• Do not use in severe kidney or liver problems, active bleeding, or with other anticoagulants
• No routine PT-INR monitoring required (advantage over other anticoagulants)
• Caution during pregnancy and lactation
• Do not stop or change dose without consulting your doctor

• Hypersensitivity to Apixaban
• Clinically significant active bleeding
• Hepatic disease associated with coagulopathy and clinically relevant bleeding risk
• Lesion or condition at significant risk of major bleeding
• Concomitant treatment with other anticoagulant agents

• Strong CYP3A4 & P-gp inhibitors (e.g., clarithromycin, itraconazole, ketoconazole, ritonavir): Increase apixaban exposure and bleeding risk → reduce dose to 2.5 mg BID
• Strong CYP3A4 & P-gp inducers (e.g., rifampicin, phenytoin, carbamazepine): Decrease apixaban exposure and increase stroke risk
• Drugs affecting haemostasis (e.g., aspirin, heparin, fibrinolytics, SSRIs, NSAIDs): Increase bleeding risk
• Switching from warfarin: Discontinue warfarin and start apixaban when INR is below 2.0

[CAUTION] Caution is advised when consuming alcohol with Apixaban. Please consult your doctor.

[SAFE IF PRESCRIBED] Apixaban is generally considered safe to use during pregnancy. Animal studies have shown low or no adverse effects. However, treatment may increase risk of hemorrhage during pregnancy and delivery. Use only if potential benefit outweighs the risk.

[CONSULT YOUR DOCTOR] It is unknown whether apixaban or its metabolites are excreted in human milk. A decision should be made to either discontinue breastfeeding or discontinue apixaban therapy, considering the importance of the drug to the mother.

Safety and effectiveness in pediatric patients have not been established.

In clinical studies, >69% of subjects were 65 and older, and >31% were 75 and older. The effects of apixaban on stroke and major bleeding risk were maintained in geriatric subjects.

[CAUTION] Use with caution in kidney disease. No dose adjustment needed in mild-moderate renal impairment. Limited data in severe renal impairment (CrCl <15 mL/min or on dialysis).

[CAUTION] Use with caution in liver disease. No dose adjustment needed in mild hepatic impairment. Limited data in moderate impairment. Not recommended in severe hepatic impairment.

There is no antidote to apixaban. Overdose increases the risk of bleeding. Activated charcoal may be useful in the management of apixaban overdose.

Store below 30°C in a dry place. Protect from light. Keep out of reach of children.