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 ?
Results showed that, while effective in reversing inhibition of thrombin generation in plasma from patients treated with warfarin, 4F-PCCs did not appear to have an effect on the inhibition of thrombin generation by apixaban or rivaroxaban unless the Factor Xa inhibitor concentration was less than 75 ng/mL.
"Minor bleeds could potentially be managed by temporarily discontinuing the drug in question--but the lack of antidotes likely deterred some people from taking DOACs despite their advantages." There are now effective DOAC reversal agents: idarucizumab (Praxbind[R]) reverses the action of dabigatran, while andexanet alfa (Andexxa[R]) reverses rivaroxaban, apixaban, and edoxaban.
The apixaban plus P2Y12 inhibitor (typically, clopidogrel) combination "resulted in less bleeding and fewer hospitalizations without significant differences in ischemic events than regimens that included a vitamin K antagonist, aspirin, or both," Renato D.
The researchers found the risk of gastrointestinal bleeding was highest in patients taking rivaroxaban (1,278 patients; 144 per 10,000 person-years; 95% CI, 136-152) and lowest when taking apixaban (279 patients; 120 per 10,000 person-years; incidence rate ratio, 1.97; 95% CI, 1.73-2.25), compared with dabigatran (629 patients; 120 per 10,000 person-years; IRR, 1.19; 95% CI, 1.08-1.32) and warfarin (4,933 patients; 113 per 10,000 person-years; IRR, 1.27; 95% CI, 1.19-1.35).
Portola president and CEO, Scott Garland, said, 'It is clear from the response to the Andexxa Early Supply Program that there is significant need for a specific reversal agent that can address life-threatening bleeding associated with the use of the Factor Xa inhibitors apixaban and rivaroxaban.
Apixaban is another oral direct factor (DOACs) Xa inhibitor and has been studied in several clinical trials.
Drugs targeting venous or stasis-induced thrombi include the traditional anticoagulants (heparin, low-molecular-weight (LMW) heparins and fondaparinux), the VKAs (warfarin), and more recently the novel or direct-acting oral anticoagulants (DOACs) (dabigatran, rivaroxaban and apixaban).
Rivaroxaban and apixaban closely followed dabigatran to the market; they were first indicated for NVAF patients, and then were approved to use in patients at risk of thrombosis following orthopedic surgery, and for thrombosis prevention and treatment in other patient types.
WEDNESDAY, July 11, 2018 (HealthDay News) -- Apixaban seems to be the safest direct oral anticoagulant (DOAC) compared with warfarin, according to a study published July 4 in The BMJ.
Newer drugs, such as apixaban (Eliquis) and dabigatran (Pradaxa), are taken twice daily and require no monitoring or blood testing; a reversal agent is pending for apixaban; dabigatran already has a reversal agent available.
We present a case of spontaneous massive hemothorax in patient taking apixaban for venous thromboembolism disease.
Rivaroxaban has been consistently used in the most studies examining the role of NOACs in the treatment of PVT either as a single agent or in combination with a second agent such as apixaban or dabigatran [8-12, 19, 21-23].