【藥品性質提示】 根據 2019 AGS Beers Criteria，本藥品為【潛在不適當用藥 (PIM)】，腎功能不佳之老年人 (CrCl<25mL/min) 須避免使用。 #高警訊藥品

抗凝血口服 Prevention of stroke and systemic embolism in adult patients with non-valvular atrial fibrillation, with one or more risk factors, such as (1) prior stroke or transient ischemic attack (TIA); (2) age ≥ 75 years; (3) hypertension; (4) diabetes mellitus; (5) symptomatic heart failure (NYHA Class ≥ II)
#仿單變更2021 #仿單變更2022

Anticoagulant, Factor Xa Inhibitor; Direct Oral Anticoagulant (DOAC)
Apixaban is an oral, reversible, and selective active site inhibitor of free and clot-bound Factor Xa. It has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FactorXa, apixaban decreases thrombin generation and thrombus development.

Absorption:
1. Onset: 3 to 4 hours
2. Bioavailability: ~50%
3. Time to peak: 3 to 4 hours
Metabolism:
1. Hepatic predominantly via CYP3A4/5 and to a lesser extent via CYP1A2, 2C8, 2C9, 2C19, and 2J2 to inactive metabolites
2. Substrate of P-gp and breast cancer resistant protein (BCRP)
3. Elimination half-life: ~12 hours. Apixaban should be discontinued at least 24-48 hours prior to surgery or invasive procedures.
Excretion:
Urine (~27% as parent drug); feces

1. Active pathological bleeding
2. Severe hypersensitivity (eg, anaphylactic reactions) to apixaban
3. Patients with antiphospholipid syndrome: For patients with a history of thrombosis who are diagnosed with antiphospholipid syndrome, safety and efficacy have not been established. Patients positive for all 3 antiphospholipid antibodies (lupus anticoagulant, anticardiolipin, and anti-beta 2-glycoprotein I) may have increased rates of recurrent thrombotic events compared with vitamin K antagonist therapy <20210316>

Data are insufficient to evaluate the safety of direct acting oral anticoagulants during pregnancy and use in pregnant patients is not recommended.
Women who need anticoagulant therapy should discuss with their physician if they plan to become pregnant.<20230215>

Until safety data are available, direct acting oral anticoagulants are not recommended for use in patients who are breastfeeding; use of an alternative anticoagulant is preferred

Common:
Hemorrhage (heavy menstrual bleeding, gingival, hematuria, anemia, rectal, hemoptysis)
Post-marketing:
Hepatic: Increased serum alkaline phosphatase, increased serum bilirubin, increased serum transaminases <20220119> Warnings:
1. Antiphospholipid syndrome: Patients with APS (especially if triple positive for all 3 antiphospholipid antibodies [lupus anticoagulant, anticardiolipin, and anti-beta 2-glycoprotein I])<20220119> may have increased rates of recurrent thrombotic events compared with vitamin K antagonist therapy.
2. Valvular disease: Avoid use in patients with surgically implanted mechanical heart valve, transcatheter aortic valve replacement with no other indication for anticoagulation, moderate to severe mitral stenosis, or significant rheumatic heart disease.

Nonvalvular atrial fibrillation (to prevent stroke and systemic embolism):
5 mg twice daily unless patient has any 2 of the following: Age 80 years, body weight ≤60 kg, or serum creatinine ≥1.5 mg/dL, then reduce dose to 2.5 mg twice daily
Venous thromboembolism (DVT and/or PE):
10 mg twice daily for 7 days followed by 5 mg twice daily

1. Venous thromboembolism (DVT and/or PE) treatment and prophlyaxis: No dosage adjustment is recommended; Not dialyzable
2. Nonvalvular atrial fibrillation (to prevent stroke and systemic embolism):
(1) SCr <1.5 mg/dL: No dosage adjustment necessary unless ≥80 years of age and body weight ≤60 kg, then reduce dose to 2.5 mg twice daily.
(2) SCr ≤1.5 mg/dL and either ≥80 years of age or body weight ≤60 kg: 2.5 mg twice daily
(3) ESKD not requiring dialysis: Apixaban is considered appropriate
(4) Hemodialysis: Not dialyzable