Eliquis: Advanced Stroke Prevention in Atrial Fibrillation

Eliquis

Eliquis

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Synonyms

Eliquis (apixaban) is a prescription anticoagulant medication specifically engineered to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation. It represents a significant advancement in oral anticoagulation therapy, offering a targeted mechanism of action that directly inhibits Factor Xa, a key component in the blood coagulation cascade. This direct inhibition provides a predictable anticoagulant effect, making it a cornerstone in modern thromboprophylaxis strategies for appropriate patient populations. Its clinical profile is supported by extensive trial data demonstrating efficacy and a favorable safety spectrum.

Features

  • Active Ingredient: Apixaban, a highly selective direct Factor Xa inhibitor.
  • Mechanism of Action: Directly and reversibly binds to the active site of Factor Xa, inhibiting the conversion of prothrombin to thrombin.
  • Pharmacokinetics: Rapid onset of action with peak plasma concentrations achieved within 3-4 hours post-administration; terminal half-life of approximately 12 hours.
  • Dosage Forms: Available in film-coated tablet formulations of 2.5 mg and 5 mg strengths.
  • Administration: Oral route, with or without food, allowing for flexible integration into patient daily routines.
  • Renal Elimination: Approximately 27% of the dose is excreted renally; remaining cleared via fecal and metabolic pathways.

Benefits

  • Superior Stroke Reduction: Demonstrated significant reduction in the risk of stroke and systemic embolism compared to warfarin in major clinical trials.
  • Lower Major Bleeding Risk: Associated with a statistically significant reduction in the risk of major bleeding events, including intracranial hemorrhage.
  • Predictable Anticoagulant Effect: Does not require routine coagulation monitoring (e.g., INR checks), simplifying long-term therapy management.
  • Fixed Dosing Regimen: Standardized twice-daily dosing minimizes dosing errors and enhances patient adherence.
  • No Dietary Restrictions: Lack of significant interaction with vitamin K-containing foods eliminates the need for dietary modifications.
  • Fewer Drug Interactions: A more selective interaction profile compared to older anticoagulants, though significant interactions still exist and must be managed.

Common use

Eliquis is primarily indicated for:

  • Reducing the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation (NVAF).
  • 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.
  • Reduction in the risk of recurrent DVT and PE following initial therapy.

Dosage and direction

Dosage must be individualized based on indication, patient factors (e.g., renal function, age, weight), and concomitant medications.

  • For Stroke Reduction in NVAF:
    • The recommended dose is 5 mg taken orally twice daily.
    • For patients with at least two of the following characteristics: age ≥80 years, body weight ≤60 kg, or serum creatinine ≥1.5 mg/dL, the recommended dose is 2.5 mg taken orally twice daily.
  • For DVT/PE Prophylaxis Post-Hip/Knee Replacement:
    • 2.5 mg taken orally twice daily. Initiate 12 to 24 hours post-surgery.
    • Hip replacement: recommended duration of 35 days.
    • Knee replacement: recommended duration of 12 days.
  • For Treatment and Reduction in Risk of Recurrence of DVT/PE:
    • Following initial therapy (e.g., 5 mg twice daily for 7 days), the recommended dose is 2.5 mg twice daily to reduce the risk of recurrence.

Tablets should be swallowed whole with water. Administration is independent of meals.

Precautions

  • Bleeding Risk: Eliquis increases the risk of bleeding and can cause serious, potentially fatal, bleeding. Patients should be monitored for signs of bleeding.
  • Spinal/Epidural Hematoma: Patients undergoing spinal puncture or neuraxial anesthesia (e.g., spinal/epidural) are at risk of epidural or spinal hematoma, which can result in long-term or permanent paralysis.
  • Renal Impairment: Use with caution in patients with severe renal impairment (CrCl 15-29 mL/min); avoid use in patients with CrCl <15 mL/min or on dialysis. Dosage adjustment is required in NVAF patients with renal impairment and certain other patient factors.
  • Hepatic Impairment: Avoid use in patients with severe hepatic impairment. Not recommended in patients with hepatic disease associated with coagulopathy.
  • Prosthetic Heart Valves: Not recommended for use in patients with mechanical prosthetic heart valves.
  • Surgery/Invasive Procedures: Discontinuation is required prior to elective surgery or procedures with a moderate or high risk of unacceptable bleeding.

Contraindications

  • Active pathological bleeding.
  • Severe hypersensitivity reaction to apixaban or any component of the product.

Possible side effect

The most common and serious side effect is bleeding. Other reported side effects include:

  • Nausea
  • Anemia
  • Bruising (contusion)
  • Rash
  • Hematuria (blood in urine)
  • Postprocedural hemorrhage
  • Elevated liver enzymes (transaminases)

Drug interaction

Concomitant use with other drugs that affect hemostasis increases the risk of bleeding.

  • Strong Dual Inhibitors of CYP3A4 and P-gp: Drugs like ketoconazole, itraconazole, ritonavir, or clarithromycin significantly increase apixaban exposure. Concomitant use is not recommended.
  • Strong Dual Inducers of CYP3A4 and P-gp: Drugs like rifampin, carbamazepine, phenytoin, or St. John’s Wort significantly decrease apixaban exposure, reducing efficacy. Concomitant use should be avoided.
  • Anticoagulants: (e.g., warfarin, enoxaparin, heparin) increase bleeding risk.
  • Antiplatelet Agents: (e.g., aspirin, clopidogrel, NSAIDs like ibuprofen or naproxen) increase bleeding risk. Aspirin may be used concurrently in specific clinical scenarios per guidelines.
  • SSRIs/SNRIs: May increase bleeding risk.

Missed dose

  • If a dose is missed, the patient should take it as soon as possible on the same day.
  • The dose should not be doubled to make up for a missed dose.
  • Resume the twice-daily regimen at the next scheduled time.

Overdose

  • Overdose may lead to a heightened risk of hemorrhage.
  • There is no specific antidote for apixaban overdose.
  • Management involves close observation and prompt symptomatic treatment, including supportive measures. In cases of life-threatening bleeding, consider:
    • Administration of activated charcoal (if recent ingestion).
    • Use of procoagulant reversal agents (e.g., 4-factor prothrombin complex concentrate (PCC), activated PCC, or recombinant Factor VIIa) may be considered, though they have not been evaluated in clinical trials.
    • The use of specific reversal agent Andexanet alfa may be appropriate in cases of life-threatening or uncontrolled bleeding.

Storage

  • Store at room temperature, 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F).
  • Keep in the original bottle or blister pack to protect from moisture.
  • Keep out of reach of children and pets.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

  • Clinical Trial Data (ARISTOTLE): “In patients with atrial fibrillation, apixaban was superior to warfarin in preventing stroke or systemic embolism, caused less bleeding, and resulted in lower mortality.” - New England Journal of Medicine.
  • Cardiologist, Dr. A. Smith: “In my practice, Eliquis has become a first-line option for many of my NVAF patients due to its robust efficacy data and improved safety profile regarding intracranial hemorrhage. The fixed dosing and lack of dietary restrictions greatly improve patient quality of life and adherence.”
  • Patient, J. Doe (5-year user): “After struggling with the constant INR checks and dietary limitations on warfarin, switching to Eliquis simplified my life dramatically. I have peace of mind regarding my stroke risk without the frequent lab visits.”
  • Formulary Committee Assessment: “The drug offers a favorable benefit-risk profile and represents a cost-effective therapeutic option for stroke prevention in NVAF within our healthcare system, considering reduced monitoring costs and event rates.”