XCARD 2.5/MG TAB 60/TAB

Indications

Approved Uses

To reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation, Prophylaxis of deep vein thrombosis (DVT) which may lead to pulmonary embolism (PE) in patients who have undergone hip or knee replacement surgery, Treatment of DVT and PE, To reduce the risk of recurrent DVT and PE following initial therapy.

Off-Label Uses

Cancer-associated thrombosis (treatment/secondary prevention) and left ventricular thrombus are commonly encountered off-label uses (practice varies by guideline and patient factors).

Dosage & Administration

Dosing by Condition

Nonvalvular AF stroke prevention: 5 mg twice daily (2.5 mg twice daily if ≥2 of age ≥80, weight ≤60 kg, SCr ≥1.5 mg/dL). DVT/PE treatment: 10 mg twice daily for 7 days, then 5 mg twice daily. Prevention of recurrent DVT/PE: 2.5 mg twice daily after at least 6 months of treatment. Post-hip or knee replacement VTE prophylaxis: 2.5 mg twice daily starting 12-24 hours after surgery (knee 10-14 days; hip 32-38 days).

Initial Dose

2.5mg twice daily (for DVT/PE secondary prevention and VTE prophylaxis post-surgery); 10mg twice daily for 7 days for acute DVT/PE treatment

Maintenance Dose

2.5mg twice daily (secondary prevention and post-surgical prophylaxis); 5mg twice daily (AF and DVT/PE treatment after initial phase)

Maximum Dose

10mg twice daily (during initial 7-day DVT/PE treatment phase)

Children's Dosage

Safety and efficacy not established in children under 18 years; approved for VTE in pediatric patients from birth after initial treatment (specific weight-based dosing).

Dose Adjustment Notes

Nonvalvular AF: reduce to 2.5 mg twice daily if the patient has at least 2 of the following-age ≥80 years, body weight ≤60 kg, serum creatinine ≥1.5 mg/dL. Renal impairment: no adjustment for mild-moderate impairment; use with caution in severe impairment; for NVAF, not recommended in CrCl <15 mL/min and/or dialysis in many guidelines/labels (local labeling may vary).

How to Take

Swallow tablet whole with water, with or without food. If unable to swallow, the tablet may be crushed and mixed in water, 5% dextrose in water, apple juice, or applesauce and administered promptly; crushed tablet may also be delivered via nasogastric tube in water or D5W.

Side Effects

Common Side Effects

Bleeding (bruising, epistaxis, gingival bleeding, hematuria, gastrointestinal bleeding), nausea, anemia

Side Effect Frequency

Common (1-10%): Bleeding events (e.g., epistaxis, contusion, hematuria, gingival bleeding), Nausea, Anemia. Uncommon (0.1-1%): Thrombocytopenia, Hypotension, Gastrointestinal hemorrhage. Rare (0.01-0.1%): Allergic reaction, Intracranial hemorrhage.

Safety & Warnings

Contraindications

Contraindicated in: active pathological/clinically significant bleeding; hypersensitivity to apixaban/excipients; hepatic disease associated with coagulopathy and clinically relevant bleeding risk (severe hepatic impairment generally not recommended/avoid).

Warnings & Precautions

Key warnings/precautions: increased risk of serious/fatal bleeding; boxed warnings for premature discontinuation (thrombosis) and neuraxial hematoma; caution with concomitant antiplatelets/NSAIDs and strong CYP3A4/P-gp inhibitors/inducers; avoid/not recommended in severe hepatic impairment or hepatic coagulopathy; limited data/avoid in mechanical prosthetic valves and not indicated for moderate-to-severe mitral stenosis; assess renal function and bleeding risk.

Age Restriction

Not approved/recommended for patients <18 years (pediatric use not established).

Driving Warning

Safe

Drug Interactions

Drug Interactions

Strong dual inhibitors of CYP3A4 and P-gp (ketoconazole, itraconazole, ritonavir, clarithromycin - increase apixaban exposure), strong dual inducers of CYP3A4 and P-gp (rifampicin, phenytoin, carbamazepine, St. John's Wort - decrease apixaban exposure), other anticoagulants and antiplatelets (increased bleeding risk), NSAIDs (increased bleeding risk), SSRIs/SNRIs (increased bleeding risk)

Interaction Severity

MAJOR: Strong dual CYP3A4 and P-gp inhibitors (e.g., ketoconazole, itraconazole, ritonavir/cobicistat) increase apixaban exposure/bleeding risk; strong dual CYP3A4 and P-gp inducers (e.g., rifampin, carbamazepine, phenytoin, St. John’s wort) reduce exposure/efficacy; concomitant anticoagulants (additive bleeding). MODERATE: Antiplatelets (aspirin, clopidogrel), NSAIDs, SSRIs/SNRIs (increased bleeding risk); moderate CYP3A4/P-gp inhibitors (e.g., diltiazem, verapamil, erythromycin) increase exposure modestly.

Food Interaction

No restriction.

Special Populations

Pregnancy

Consult Doctor

Children

Safety and efficacy not established in children under 18 years; approved for VTE in pediatric patients from birth after initial treatment (specific weight-based dosing).

Elderly

In patients with nonvalvular atrial fibrillation, dose reduction to 2.5mg twice daily is recommended if age is ≥80 years and accompanied by either a body weight ≤60 kg or a serum creatinine ≥1.5 mg/dL.

Kidney Impairment

NVAF: standard 5 mg BID, reduce to 2.5 mg BID if patient has ≥2 of: age ≥80 years, weight ≤60 kg, serum creatinine ≥1.5 mg/dL; ESRD on hemodialysis (per some labeling): 5 mg BID, reduce to 2.5 mg BID if age ≥80 or weight ≤60; VTE treatment/prophylaxis: no routine renal dose adjustment but use caution in severe impairment and avoid/insufficient data when CrCl <15 mL/min.

Liver Impairment

Child-Pugh A (mild): no dose adjustment; Child-Pugh B (moderate): use with caution (limited data); Child-Pugh C (severe) or hepatic disease with coagulopathy: avoid/not recommended.

Storage & Patient Advice

Storage Conditions

Store below 30°C

Missed Dose

Take the missed dose as soon as remembered on the same day, then continue with the next dose at the usual time; do not take a double dose to make up for a missed dose.

Stopping the Medicine

Do not discontinue abruptly without medical supervision; if stopping is necessary, ensure timely transition to alternative anticoagulation to reduce thrombotic risk.

Overdose

Overdose: expect excessive bleeding/hemorrhage; management is supportive (hold drug, local hemostasis, transfusion as needed), consider activated charcoal if recent ingestion, and for life-threatening bleeding use andexanet alfa where available or 4-factor PCC as alternative; urgent medical care required.

Patient Counseling

Take exactly as prescribed twice daily and do not stop without medical advice. Watch for and report bleeding/bruising (e.g., black/tarry stools, blood in urine, coughing/vomiting blood, severe headache). Tell all healthcare providers/dentists before procedures. Avoid unnecessary NSAIDs and discuss OTC/herbals (e.g., St. John’s wort). If a dose is missed, take it the same day when remembered and do not double. Carry anticoagulant/alert information (e.g., patient alert card) if provided.

Monitoring Requirements

No routine coagulation test monitoring is required. Periodically assess renal function (and more often if renal status may change), consider baseline/periodic hepatic function, and monitor clinically for bleeding, anemia, adherence, and interacting medications.

Pharmacology

Mechanism of Action

Direct, selective, reversible inhibitor of factor Xa, reducing thrombin generation and thrombus formation (does not require antithrombin).

Onset of Action

Peak effect occurs about 3-4 hours after a dose.

Duration of Effect

Approximately 12 hours per dose (hence twice-daily dosing), with residual anticoagulant activity persisting for about 24 hours after the last dose in many patients.

Half-Life

Approximately 12 hours.

Bioavailability

Approximately 50%.

Metabolism

Metabolized primarily by CYP3A4/5, with minor contributions from other CYP enzymes (e.g., CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2J2); it is also a substrate of P-gp and BCRP.

Excretion

Elimination occurs via multiple pathways: renal excretion about 27%, with the remainder via biliary/fecal and direct intestinal excretion and metabolism.

Protein Binding

Approximately 87%.

Product Information

Available Dosage Forms

Tablet (oral, blister pack).

Composition per Dose

Each tablet: 2.5mg apixaban

Generic Availability

Yes

OTC Alternatives

No OTC alternative

Cv Drug Class

Anticoagulant

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