eliquis
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| Product dosage: 5mg | |||
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Synonyms | |||
Apixaban, marketed under the brand name Eliquis, represents a significant advancement in anticoagulation therapy. As a direct Factor Xa inhibitor, it offers predictable pharmacokinetics without requiring routine coagulation monitoring, which fundamentally changed how we manage thromboembolic disorders. I remember when we first started using it in our cardiology department back in 2013 - there was both excitement and skepticism among the team.
Key Components and Bioavailability of Eliquis
The active pharmaceutical ingredient in Eliquis is apixaban, a small molecule with molecular weight of 459.5 Daltons. What’s particularly interesting about its formulation is the bioavailability - approximately 50% for oral administration, which is quite good for this class of medications. The elimination half-life ranges from 8-15 hours, allowing for twice-daily dosing that maintains therapeutic levels without significant peaks and troughs.
We’ve found the 2.5 mg and 5 mg tablet strengths cover most clinical scenarios, though there’s also a 10 mg tablet for initial postoperative dosing in some orthopedic protocols. The tablets use a standard immediate-release formulation without special coating requirements, which improves patient adherence compared to some other anticoagulants that have more complex administration instructions.
Mechanism of Action of Eliquis: Scientific Substantiation
Eliquis works by directly inhibiting Factor Xa in the coagulation cascade. Unlike warfarin that affects multiple vitamin K-dependent factors, apixaban specifically targets the point where intrinsic and extrinsic pathways converge. This selective action means it doesn’t interfere with other clotting factors, which explains the different bleeding profile we observe clinically.
The biochemistry is elegant - apixaban binds reversibly to the active site of Factor Xa, preventing conversion of prothrombin to thrombin. Without thrombin generation, fibrinogen isn’t converted to fibrin, so clot formation is inhibited at a crucial amplification step. I’ve found this mechanism particularly useful when explaining to patients why they don’t need frequent blood tests like with warfarin.
Indications for Use: What is Eliquis Effective For?
Eliquis for Stroke Prevention in Atrial Fibrillation
This is where we see the strongest evidence. The ARISTOTLE trial demonstrated superiority over warfarin with 21% relative risk reduction in stroke/systemic embolism and 31% reduction in major bleeding. In practice, I’ve seen this translate to fewer intracranial hemorrhages - perhaps the most feared complication of anticoagulation.
Eliquis for Treatment of Venous Thromboembolism
The AMPLIFY trial showed non-inferiority to conventional therapy (enoxaparin followed by warfarin) for acute DVT and PE treatment, with 69% reduction in major bleeding. What’s impressed me clinically is how smoothly we can transition patients from hospital to home management without bridge therapy.
Eliquis for Post-Orthopedic Surgery Thromboprophylaxis
The ADVANCE program established efficacy following hip and knee replacement surgeries. We’ve adopted it as first-line at our institution because the bleeding risk profile allows earlier mobilization - crucial for joint recovery outcomes.
Instructions for Use: Dosage and Course of Administration
Dosing requires careful consideration of patient factors. For atrial fibrillation, the standard is 5 mg twice daily, but we reduce to 2.5 mg twice daily if patients meet at least two of these criteria: age ≥80 years, body weight ≤60 kg, or serum creatinine ≥1.5 mg/dL.
For VTE treatment, we start with 10 mg twice daily for 7 days, then continue with 5 mg twice daily. The simplicity of this regimen compared to traditional approaches cannot be overstated - no INR monitoring, no dietary restrictions, minimal drug interactions.
| Indication | Initial Dose | Maintenance | Duration |
|---|---|---|---|
| Atrial Fibrillation | 5 mg twice daily | 5 mg twice daily | Long-term |
| DVT/PE Treatment | 10 mg twice daily × 7 days | 5 mg twice daily | 3-6 months minimum |
| Hip Replacement | 2.5 mg twice daily | 2.5 mg twice daily | 35 days |
| Knee Replacement | 2.5 mg twice daily | 2.5 mg twice daily | 12 days |
Contraindications and Drug Interactions with Eliquis
Absolute contraindications include active pathological bleeding and severe hypersensitivity reactions. We’re particularly cautious with triple therapy (adding antiplatelets to Eliquis) - the bleeding risk escalates dramatically. I learned this the hard way with a 68-year-old gentleman who developed GI bleeding despite appropriate dosing.
The pharmacokinetics are favorable regarding interactions - primarily metabolized via CYP3A4 with some P-gp transport. We watch for strong dual inhibitors of both pathways like ketoconazole and ritonavir. The renal clearance (~27%) means we monitor renal function periodically, especially in elderly patients.
Clinical Studies and Evidence Base for Eliquis
The evidence portfolio for Eliquis is robust. Beyond the landmark trials I mentioned earlier, real-world data continues to accumulate. Our institution participated in a registry that showed consistent results with clinical trials - something we don’t always see with novel agents.
The AVERROES trial was particularly telling - comparing apixaban to aspirin in patients unsuitable for warfarin. The stroke reduction was substantial without significant increase in major bleeding. This trial convinced several of our reluctant clinicians that newer anticoagulants offered meaningful advantages.
Comparing Eliquis with Similar Products and Choosing Quality
When patients ask about Eliquis versus other DOACs, I explain that each has slight advantages in different scenarios. Eliquis consistently shows favorable bleeding profiles, particularly for gastrointestinal bleeding compared to some alternatives. The twice-daily dosing theoretically provides more consistent anticoagulation, though in practice adherence becomes more crucial.
The manufacturing quality has been consistent in my experience. We’ve had fewer supply issues compared to some other specialty medications, which matters for chronic conditions where treatment interruptions can be dangerous.
Frequently Asked Questions (FAQ) about Eliquis
What should I do if I miss a dose of Eliquis?
If remembered within 6 hours of the missed dose, take it immediately. If beyond 6 hours, skip the dose and continue regular schedule. Don’t double dose - this isn’t like warfarin where we can adjust later.
Can Eliquis be taken with food?
Yes, absorption isn’t significantly affected by food. Many of my patients take it with meals as part of their routine.
What monitoring is required with Eliquis?
No routine coagulation monitoring, but we check renal function annually and complete blood count periodically. More frequent monitoring if clinical condition changes.
Is there an antidote for Eliquis?
Andexanet alfa is approved for reversal of life-threatening bleeding. Prothrombin complex concentrates may also be used off-label. Having reversal options available has made our emergency department more comfortable managing these patients.
Conclusion: Validity of Eliquis Use in Clinical Practice
The risk-benefit profile of Eliquis supports its position as first-line anticoagulant for most indications. The predictable pharmacology, reduced monitoring requirements, and favorable bleeding profile have transformed how we approach thromboprophylaxis and treatment.
I recall one patient, Margaret, 72 with atrial fibrillation and frequent falls. We’d hesitated with warfarin, but Eliquis allowed us to provide stroke protection without the constant worry about traumatic intracranial hemorrhage. Three years later, she remains event-free and actively gardening - the quality of life impact is real.
Another case that stays with me - David, 45 with unprovoked PE. Traditional therapy would have meant months of INR checks disrupting his work schedule. With Eliquis, he completed 6 months of treatment with minimal lifestyle impact. When his cancer diagnosis came 18 months later (the likely provoking factor), we were able to seamlessly continue anticoagulation during chemotherapy.
The development wasn’t without challenges though. Early on, our pharmacy committee debated cost concerns, and some senior physicians were reluctant to abandon warfarin despite the evidence. It took seeing consistent results in our own patient population to build universal comfort. We even had one patient who developed recurrent DVT on Eliquis - turned out he was crushing his tablets despite our instructions, significantly reducing bioavailability. These practical lessons aren’t in the clinical trials.
Long-term follow up of our cohort shows maintained efficacy with persistence rates higher than we ever saw with warfarin. The convenience factor genuinely matters for chronic conditions. I’ve had patients tell me they’d probably have discontinued warfarin due to monitoring burden, but they’ve stayed compliant with Eliquis for years now.
The data continues to evolve - we’re now seeing studies exploring extended duration therapy for VTE and potential applications in other thrombotic disorders. As with any medication, staying current with emerging evidence remains crucial, but Eliquis has firmly established its role in modern antithrombotic management.