Pixorel(Apixaban)

Therapeutic Group: Others

Presentation

Pixorel 2.5: Each Tablet contains Apixaban INN 2.5 mg.

Pixorel 5: Each Tablet contains Apixaban INN 5 mg.

Description

Apixaban is a selective inhibitor of clotting factor Xa (FXa). It does not require a cofactor (such as Anti-thrombin III) for activity. Apixaban inhibits free FXa, clot bound FXa and prothrombinase activity. Apixaban indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, Apixaban decreases thrombin generation.

Indications

• Prevention of stroke and systemic embolism in adult patients with Non-valvular atrial fibrillation (AF)

• Treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE), and prevention of recurrent DVT and PE in adults.

• For the prophylaxis of DVT, in patients undergoing knee or hip replacement surgery

Dosage & Administration

Prevention of stroke and systemic embolism in non-valvular AF: the recommended dose is 5 mg orally twice daily. But patient with age≥ 80 years, body weight> 60 kg, serum creatinine> 1.5 mg/dl: Usual dose is 2.5 mg twice daily
Treatment of DVT and PE: 10 mg taken orally twice daily for first 7 days followed by 5 mg taken twice daily.
Reduction in the risk of recurrence of DVT and PE: 2.5 mg taken orally twice daily.
Prophylaxis of DVT Following Hip or Knee Replacement Surgery: 2.5 mg taken orally twice daily

Side Effects

Haemorrhage, nausea, vomiting, diarrhoea, constipation, dyspepsia, abdominal pain, hypotension, dizziness, headache, renal impairment, pain in extremity, fever, peripheral oedema, fatigue. Other less common side effects include-thrombocythemia, allergic reaction, syncope, tachycardia, abnormal hepatic function.

Precautions

Premature discontinuation of apixaban, in the absence of adequate alternative anticoagulation increases the risk of thrombotic events. Apixaban increases the risk of bleeding that can be fatal in presence of following risk factors- bleeding disorders, uncontrolled severe arterial hypertension, gastrointestinal disease (e.g., inflammatory bowel disease, oesophagitis, gastritis and gastroesophageal reflux disease), vascular retinopathy, bronchiectasis, history of pulmonary bleeding, Signs or symptoms of neurological impairment should be monitored in case of neuraxial anesthesia (spinal/epidural anesthesia) or spinal puncture as epidural or spinal hematoma can occur. Apixaban is not recommended in patients with pulmonary embolism who present with hemodynamic instability or who may receive thrombolysis or pulmonary embolectomy.

Use in Pregnancy & Lactation

Pregnancy: Pregnancy category B. There are no adequate and well-controlled studies in pregnant women.
Lactation: Safety and efficacy of Apixaban have not been established in breast feeding women. A decision must be made whether to discontinue breast feeding or to discontinue/abstain from therapy.

Drug Interaction

Concomitant use with drugs that are combined P-gp and CYP3A4 inhibitors (ketoconazole, ritonavir, clarithromycin, erythromycin, fluconazole, diltiazem, verapamil, dronedarone), increases in apixaban exposure and pharmacodynamic effects (i.e., factor Xa inhibition and PT prolongation) thus should be avoided. Co-administration of apixaban with a combined P-gp and strong CYP3A4 inducer (e.g., rifampicin, phenytoin, carbamazepine) decreases efficacy of apixaban and also should be avoided. The concomitant use of other drugs like- anti-platelet agents, heparin, fibrinolytic therapy may cause increased risk of
bleeding.

Over Dose

Overdose of apixaban may lead to hemorrhage. Discontinue apixaban and initiate appropriate therapy if bleeding complications associated with overdosage occur. A specific antidote for apixaban is not available. The use of activated charcoal to reduce absorption in case of apixaban overdose may be considered. Partial reversal of laboratory anticoagulation parameters may be achieved with use of plasma products.

Storage

Store at 20°C to 25°C; excursions permitted to 15°-30°C.

Commercial Pack

Pixorel 2.5: Each box contains 2 blister strips of 10 tablets
Pixorel 5: Each box contains 1 blister strip of 10 tablets