apixaban

Contraindicated in:

Previous severe hypersensitivity reactions;
Active pathological bleeding;
Severe hepatic impairment;
Prosthetic heart valves;
PE with hemodynamic instability or requiring thrombolysis or pulmonary embolectomy;
Triple-positive antiphospholipid syndrome (↑ risk of thrombosis);
Lactation: Lactation.

Use Cautiously in:

Neuroaxial spinal anesthesia or spinal puncture, especially if concurrent with an indwelling epidural catheter, drugs affecting hemostasis, history of traumatic/repeated spinal puncture or spinal deformity (↑ risk of spinal hematoma);
Surgery;
Renal impairment (dose ↓ may be required);
Moderate hepatic impairment (↑ risk of bleeding);
Rep: Women of reproductive potential;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

Hemat: bleeding

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

↑risk of bleeding with other anticoagulants, aspirin, clopidogrel, ticagrelor, prasugrel, fibrinolytics, NSAIDs, SNRIs, or SSRIs.
Concurrent use of strong inhibitors of both CYP3A4 and P-glycoprotein (P-gp), including itraconazole, ketoconazole, and ritonavir, ↑ levels and bleeding risk; may need to ↓ apixaban dose or avoid concurrent use.
Inducers of CYP3A4 and P-gp system, including carbamazepine, phenytoin, rifampin, will ↓ levels and may ↑ risk of thromboses; avoid concomitant use.

Drug-Natural Products:

Concurrent use St. John's wort, a strong dual inducer of the CYP3A4 and P-gp enzyme systems can ↓ levels and ↑ risk of thromboses and should be avoided.

Availability ⬆ ⬇

(Generic available)

Tablets: 2.5 mg; 5 mg

Route/Dosage ⬆ ⬇

Reduction in Risk of Stroke/Systemic Embolism in Nonvalvular Atrial Fibrillation

PO (Adults ): 5 mg twice daily; Any 2 of the following: age ≥80 yr, weight ≤60 kg, serum creatinine ≥1.5 mg/dL: 2.5 mg twice daily; Concurrent use of strong inhibitors of both CYP3A4 and P-gp: 2.5 mg twice daily; if patient already taking 2.5 mg twice daily, avoid concomitant use.

Renal Impairment

PO (Adults ): Hemodialysis: 5 mg twice daily; HD and either age ≥80 yr or weight ≤60 kg: 2.5 mg twice daily.

Prevention of Deep Vein Thrombosis Following Knee or Hip Replacement Surgery

PO (Adults ): 2.5 mg twice daily, initiated 12–24 hr postoperatively (when hemostasis is achieved) continued for 35 days after hip replacement or 12 days after knee replacement; Concurrent use of strong inhibitors of both CYP3A4 and P-gp: Avoid concomitant use.

Treatment of Deep Vein Thrombosis or Pulmonary Embolism

PO (Adults ): 10 mg twice daily for 7 days, then 5 mg twice daily; Concurrent use of strong inhibitors of both CYP3A4 and P-gp: 2.5 mg twice daily

Reduction in Risk of Recurrence of Deep Vein Thrombosis or Pulmonary Embolism

PO (Adults ): 2.5 mg twice daily after ≥6 mo of treatment of DVT or PE; Concurrent use of strong inhibitors of both CYP3A4 and P-gp: Avoid concomitant use.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a selective, reversible site inhibitor of factor Xa, inhibiting both free and bound factor. Does not affect platelet aggregation directly, but does inhibit thrombin-induced platelet aggregation. Decreases thrombin generation and thrombus development.

Therapeutic effects:

Treatment and prevention of thromboembolic events.

Classifications ⬆ ⬇

Therapeutic Classification: anticoagulants

Pharmacologic Classification: factor xa inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: 50% absorbed following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Primarily metabolized by the liver by the CYP3A4 isoenzyme; excreted in urine and feces. Biliary and direct intestinal excretion account for fecal elimination.

Half-Life: 6 hr (12 hr after repeated dosing due to prolonged absorption).

Time/Action Profile ⬆ ⬇

(effect on hemostasis)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	3–4 hr‡	24 hr

‡Blood levels.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take apixaban as directed. Take missed doses as soon as remembered on the same day and resume twice daily administration; do not double doses. Do not discontinue without consulting health care professional; may increase risk of having a stroke, DVT, or PE. If temporarily discontinued, restart as soon as possible. Store apixaban at room temperature. Advise patient to read Medication Guide before beginning therapy and with each Rx refill in case of changes.
Inform patient that they may bruise and bleed more easily or longer than usual. Advise patient to notify health care professional immediately if signs of bleeding (unusual bruising, pink or brown urine, red or black, tarry stools, coughing up blood, vomiting blood, pain or swelling in a joint, headache, dizziness, weakness, recurring nose bleeds, unusual bleeding from gums, heavier than normal menstrual bleeding, dyspepsia, abdominal pain, epigastric pain) occurs or if injury occurs, especially head injury.
Caution patient to notify health care professional if skin rash or signs of severe allergic reaction (chest pain or tightness, swelling of face or tongue, trouble breathing or wheezing, feeling dizzy or faint) occur.
Advise patient to notify health care professional of medication regimen prior to treatment or surgery.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's wort. Risk of bleeding is increased with aspirin, NSAIDs, warfarin, heparin, SSRIs or SNRIs.
Inform patient having had neuraxial anesthesia or spinal puncture to watch for signs and symptoms of spinal or epidural hematomas (numbness or weakness of legs, bowel or bladder dysfunction). Notify health care professional immediately if symptoms occur.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. May increase risk of uterine bleeding in pregnant women, fetus, and neonate; advise patient to notify health care professional if significant uterine bleeding occurs.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇