THERAPEUTICS

Brands

• Eliquis

Generic?

• No

Class

• Anticoagulant

Commonly Prescribed for

(FDA approved in bold)

• Prevention of stroke and systemic embolism in adult patients with nonvalvular atrial fibrillation (NVAF)

• Primary prevention of venous thromboembolic (VTE) events in adult patients who have undergone elective total hip arthroplasty (THA) or total knee arthroplasty (TKA)

• Treatment of cerebral venous thromboembolism

How the Drug Works

• Apixaban is a selective reversible inhibitor of both free and clot-bound factor Xa, and prothrombinase activity, thereby reducing the conversion of prothrombin to thrombin and thrombus formation. Thrombin-induced platelet aggregation is also inhibited

How Long Until It Works

• Peak concentration in 3–4 hours

If It Works

• Monitor for signs of bleeding. Assess liver function periodically as clinically indicated

If It Doesn't Work

• Correct the underlying disorder. Use a higher dose or switch to different anticoagulant

Best Augmenting Combos for Partial Response or Treatment-Resistance

• None

Tests

• The degree of anticoagulation does not need to be assessed

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Reduced coagulation due to inhibited thrombin formation

Notable AEs

• Bleeding, nausea/vomiting, constipation

Life-Threatening or Dangerous AEs

• The yearly incidence of life-threatening bleed is 0.11 %, intracranial hemorrhage 0.3 %, and major GI bleed 0.83%

Weight Gain

• Unusual

Sedation

• Unusual

What to Do About AEs

• Discontinue treatment, supportive care. Active charcoal reduces absorption. Not effective: vitamin K, protamine sulfate, hemodialysis

Best Augmenting Agents to Reduce AEs

• In most cases discontinuation and changing to another medication is more practical than trying to reduce AEs with another medication

DOSING AND USE

Usual Dosage Range

• 2.5–5mg twice daily

Dosage Forms

• Tablet. 2.5 and 5mg

How to Dose For NVAF

• 2.5 mg twice daily for patients with any 2 of the following 3 factors: > 80 years old, body weight< 60 kg, serum Cr > 1.5 mg/dL