Apixaban


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Prophylaxis of post-op venous thromboembolism 2.5 mg bid, starting 12-24 hours after surgery. Duration of treatment: 10-14 days (knee replacement); 32-38 days (hip replacement). Prophylaxis of stroke and systemic embolism in non-valvular atrial fibrillation 5 mg bid. Deep vein thrombosis; Pulmonary embolism Treatment: Initially, 10 mg bid for 7 days, followed by 5 mg bid. Prophylaxis of recurrent cases: 2.5 mg bid following completion of at least 6 months of anticoagulant treatment.
Dosage Details
Oral
Prophylaxis of postoperative venous thromboembolism
Adult: 2.5 mg bid, starting 12-24 hours after surgery. Duration of treatment: 10-14 days (knee replacement); 32-38 days (hip replacement). Refer to detailed product guideline when transitioning between anticoagulants.

Oral
Deep vein thrombosis, Pulmonary embolism
Adult: Treatment: Initially, 10 mg bid for 7 days, followed by 5 mg bid. Prophylaxis of recurrent cases: 2.5 mg bid following completion of at least 6 months of anticoagulant treatment. Refer to detailed product guideline when transitioning between anticoagulants.

Oral
Prophylaxis of stroke and systemic embolism in non-valvular atrial fibrillation
Adult: 5 mg bid. Refer to detailed product guideline when transitioning between anticoagulants.
Elderly: Refer to Special Patient Group section.
Special Patient Group
Patient taking strong CYP3A4 and P-gp inhibitors (e.g. itraconazole, ketoconazole, or ritonavir): Reduce dose by 50% if taking doses >2.5 mg bid.

Prophylaxis of stroke and systemic embolism in non-valvular atrial fibrillation

Dose reduction: Patients ≥80 years weighing ≤60 kg, serum creatinine ≥1.5 mg/dL (133 micromole/L): Reduce dose to 2.5 mg bid in the presence of at least 2 of the factors.

Patients undergoing cardioversion: 5 mg bid for at least 2.5 days (5 single doses) prior to procedure. For patients meeting the criteria for dose reduction: 2.5 mg bid at least 2.5 days (5 single doses). If cardioversion is required before the completion of 5 single doses: 10 mg loading dose at least 2 hours before cardioversion, followed by 5 mg bid. For patients meeting the criteria for dose reduction: 5 mg loading dose followed by 2.5 mg bid.
Renal Impairment
 Prophylaxis of stroke and systemic embolism in non-valvular atrial fibrillation
 CrCl (mL/min)  Dosage
 15-29  2.5 mg bid. 
Hepatic Impairment
Severe: Not recommended.
Administration
May be taken with or without food.
Contraindications
Active pathological bleeding; hepatic disease associated with coagulopathy and clinically relevant bleeding risk; conditions or lesions with significant risk for major bleeding (e.g. current or recent gastrointestinal ulceration, malignant neoplasms, recent brain, spinal, ophthalmic injury and/or surgery; recent intracranial haemorrhage, known or suspected oesophageal varices, arteriovenous malformations, vascular aneurysms, major intraspinal or intracerebral vascular abnormalities). Concomitant use with parenteral anticoagulants except when given to maintain an open central venous or arterial catheter, or during catheter ablation; oral anticoagulants except when switching to oral anticoagulant therapy.
Special Precautions
Patient with increased risk of bleeding, history of traumatic or repeated epidural/spinal punctures, spinal deformity or surgery; acute illness (e.g. heart or respiratory failure); prosthetic heart valve, significant rheumatic heart disease; history of thrombosis diagnosed with antiphospholipid syndrome. Severe renal and moderate to severe hepatic impairment. Elderly. Pregnancy and lactation. Avoid abrupt discontinuation in the absence of alternative treatment.
Adverse Reactions
Significant: Thromboembolic events (premature discontinuation), bleeding, spinal or epidural haematoma resulting to long term or permanent paralysis.
Blood and lymphatic system disorders: Anaemia, thrombocytopenia.
Gastrointestinal disorders: Nausea, mouth or gingival haemorrhage, gastrointestinal and rectal haemorrhage.
Injury, poisoning and procedural complications: Contusion.
Renal and urinary disorders: Haematuria.
Reproductive system and breast disorders: Vaginal and urogenital haemorrhage.
Vascular disorders: Epistaxis, haematoma.
Potentially Fatal: Serious bleeding.
MonitoringParameters
Monitor CBC, aPTT, prothrombin time, serum creatinine, and LFTs prior to treatment initiation of therapy, or as clinically indicated, and at least annually thereafter. Closely observe for signs of bleeding or anaemia.
Overdosage
Symptoms: Haemorrhagic complications. Management: Initiate appropriate treatment (e.g. surgical haemostasis or transfusion of fresh frozen plasma). May administer activated charcoal within 1-2 hours of ingestion. For uncontrolled life-threatening bleeding, administation of prothrombin complex or recombinant factor VIIa may be considered.
Drug Interactions
Increased exposure with both strong CYP3A4 and P-gp inhibitors (e.g. ketoconazole, itraconazole, voriconazole, posaconazole ritonavir). Decreased plasma level with both strong CYP3A4 and P-gp inducers (e.g. rifampicin, phenytoin, carbamazepine, phenobarbital). Increased plasma concentration with diltiazem, naproxen, clarithromycin, amiodarone, verapamil, quinidine.
Potentially Fatal: Increased risk of bleeding with parenteral anticoagulants (e.g. unfractionated heparin, enoxaparin, dalteparin, fondaparinux), oral anticoagulants (e.g. warfarin, rivaroxaban, dabigatran), antiplatelets (e.g. clopidogrel, dipyridamole, sulfinpyrazone), aspirin, NSAIDs, SSRIs, serotonin norepinephrine reuptake inhibitors (SNRIs).
Food Interaction
Decreased plasma concentration with St. John’s wort. Increased effect and plasma level with grapefruit juice.
Action
Description: Apixaban inhibits thrombin production, conversion of fibrinogen to fibrin and thrombus formation via selective and reversible inhibition of factor Xa (FXa), a part of the prothrombinase complex which catalyses the conversion of prothrombin to thrombin.
Onset: 3-4 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 50%. Time to peak plasma concentration: 3-4 hours.
Distribution: Volume of distribution: Approx 21 L. Plasma protein binding: Approx 87%.
Metabolism: Metabolised in the liver mainly by CYP3A4 and CYP3A5 isoenzymes, and to a lesser extent by CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2J2 isoenzymes via O-demethylation and hydroxylation at the 3-oxopiperidinyl moiety to inactive metabolites.
Excretion: Via urine (approx 27% as unchanged drug); faeces. Elimination half-life: Approx 12 hours.
Chemical Structure

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Storage
Store between 20-25°C.
ATC Classification
B01AF02 - apixaban ; Belongs to the class of direct factor Xa inhibitors. Used in the treatment of thrombosis.
Disclaimer: This information is independently developed by MIMS based on Apixaban from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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