apixaban


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apixaban

(a-pix-a-ban) ,

Eliquis

(trade name)

Classification

Therapeutic: anticoagulants
Pharmacologic: factor xa inhibitors
Pregnancy Category: B

Indications

Decreases risk of stroke/systemic embolism associated with nonvalvular atrial fibrillation.

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

Decreased thrombotic events associated with atrial fibrillation including stroke and systemic embolization.

Pharmacokinetics

Absorption: 50% absorbed following oral administration.
Distribution: Unknown.
Metabolism and Excretion: 25% metabolized (mostly by CYP3A4) and 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)

ROUTEONSETPEAKDURATION
POunknown3–4 hr†24 hr
†Blood levels.

Contraindications/Precautions

Contraindicated in: Previous severe hypersensitivity reactionsActive pathological bleedingSevere hepatic impairment;Not recommended for use in patients with prosthetic heart valves;Concurrent use of strong dual inducers of CYP3A4 and P-gp; Lactation: Should not be used.
Use Cautiously in: Discontinuation increases the risk of thromboses;Surgery;Renal impairment (dose reduction required for serum creatinine ≥1.5 mg/dL);Moderate hepatic impairment (↑ risk of bleeding);Concurrent use of strong dual inhibitors of CYP3A4 and P-gp systems (dose reduction required); Obstetric: Use during pregnancy only if potential benefit outweighs possible risks to mother and fetus; Pediatric: Safe and effective use in children has not been established.

Adverse Reactions/Side Effects

Hematologic

  • bleeding

Miscellaneous

  • hypersensitivity reactions including anaphylaxis (life-threatening)

Interactions

Drug-Drug interaction

↑ risk of bleeding with other anticoagulants, fibrinolytics, heparins, NSAIDs, SNRIs, SSRIs, or thrombolytics.Concurrent use of strong inhibitors of both the CYP3A4 and P-gP enzyme systems (including clarithromycin, itraconazole, ketoconazole, and ritonavir ) ↑ levels and bleeding risk; dosage of apixaban should be ↓ to 2.5 mg twice daily. If other reasons for ↓ dose exist, apixaban should be avoided.Inducers of the CYP3A4 enzyme system and the P-gp system including carbamzepine, phenytoin, rifampin will ↓ levels and may ↑ risk of thromboses.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.

Route/Dosage

Oral (Adults) 5 mg twice daily; ≥80 yr or body weight ≤60 kg or concurrent use of strong inhibitors of both the CYP3A4 and P-gP enzyme systems—2.5 mg twice daily.

Renal Impairment

Oral (Adults) Serum creatinine ≥1.5mg/dL—2.5 mg twice daily.

Availability

Tablets: 2.5 mg, 5 mg

Nursing implications

Nursing assessment

  • Assess patient for symptoms of stroke or peripheral vascular disease periodically during therapy.

Potential Nursing Diagnoses

Activity intolerance

Implementation

  • When converting from warfarin, discontinue warfarin and start apixaban when INR is <2.0.
  • When converting from apixaban to warfarin, apixaban affects INR, so INR measurements may not be useful for determining appropriate dose of warfarin. If continuous anticoagulation is necessary, discontinue apixaban and begin both a parenteral anticoagulant and warfarin at time of next dose of apixaban, dicontinue parenteral anticoagulant when INR reaches acceptable range.
  • When switching between apixaban and anticoagulants other than warfarin, discontinue one being taken and begin the other at the next scheduled dose.
  • For surgery, discontinue apixaban at least 48 hrs before invasive or surgical procedures with a moderate or high risk of unacceptable or clinically significant bleeding or at least 24 hrs prior to procedures with a low risk of bleeding or where the bleeding would be non-critical in location and easily controlled.
  • Oral: Administer twice daily without regard to food.

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. 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. Risk of bleeding is increased with aspirin, NSAIDs, warfarin, heparin, SSRIs or SNRIs.
  • Advise female patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

Evaluation/Desired Outcomes

  • Reduction in the risk of stroke and systemic embolism.
References in periodicals archive ?
Apixaban is an oral direct factor Xa inhibitor that showed promise last year when trial findings presented at the European Society of Cardiology showed apixaban patients were 54 percent less likely to have a stroke or blood clot than those who took aspirin.
He said that the development of new oral anticoagulant agents, like Apixaban, has raised hope of a standard of care for DVT prevention that is as effective as or more effective than current standard approaches as well as being equally safe and more convenient for patients.
Strong Dual Inhibitors of CYP3A4 and P-gp: Inhibitors of CYP3A4 and P-gp increase exposure to apixaban and increase the risk of bleeding.
On the other hand, apixaban and phenytoin share the hepatic enzyme CYP3 A4, and their concurrent use will lower its effectiveness (Lehne, 2013).
He pointed out that overall, the three novel oral anticoagulants--dabigatran and the factor Xa inhibitors, apixaban and rivaroxaban--approved for the nonvalvular AF indication, appear to reduce the risk of stroke and death, "and across the board, they all show significantly less intracranial hemorrhage.
I hope that I can pronounce them properly - they are dabigatran, rivaroxaban and apixaban.
The Food and Drug Administration has already approved three such medications -- apixaban (Eliquis), dabigatran etexilate mesylate (Pradaxa) and rivaroxaban (Xarelto) -- and others are being studied.
A new anticoagulant, apixaban (Eliquis), is used to reduce the risk of stroke in patients with atrial fibrillation.
Apixaban showed a trend toward a reduction in ischemic events in patients with ACS but also demonstrated an increased bleeding risk particularly in those taking dual antiplatelet therapy (39).
Presently, the US Food and Drug Administration (FDA) and regulatory agencies in other countries have approved one DTI (dabigatran etexilate, Pradaxa[R]) and two DFXaI (rivaroxaban, Xarelto[R]; apixaban, Eliquis[R]) for one or more indications, and clinical trials that were recently completed or are underway will likely bring more drugs in these two classes to market with approval for additional indications (2).
Cardiovascular drugs: Amiodarone, Apixaban, Clopidogrel, Dronedarone, Eplerenone, Felodipine, Nifedipine, Quinidine, Rivaroxaban, Ticagrelor