Table 1 Characteristics of new oral anticoagulants

Clinical indications and dosing^a

Atrial fibrillation

Normal renal function: 150 mg bid

CrCl >50 mL/min: 20 mg od

CrCl ≥25 mL/min: 5 mg bid

>75 years: 110 mg bid

CrCl 30-49 mL/min: 15 mg od

If 2 or more of the following: age ≥80, weight ≤60 kg or creatinine ≥1.5 mg/dL: 2.5 mg bid

Deep vein thrombosis without symptomatic pulmonary embolism (Canada)

Not approved

CrCl > 50 mL/min: 15 mg bid × 21 days then 20 mg od for at least 3-6 months

Not approved

Deep vein thrombosis and pulmonary embolism (US)

CrCl 30-49 mL/min: 15 mg bid × 21 days then 15 mg od for at least 3-6 months

Venous thromboembolism prophylaxis after total hip replacement surgery (14-35 days)

Normal renal function: 220 mg od × 10 days

10 mg od × 35 days

2.5 mg bid × 32-38 days

>75 years or CrCl 30-50 mL/min: 150 mg od × 10 days

Venous thromboembolism prophylaxis after total knee replacement surgery (14-35 days)

Normal renal function: 220 mg od × 28-35 days

10 mg od × 14 days

2.5 mg bid × 10-14 days

>75 years or CrCl 30-50 mL/min: 150 mg od × 28-35 days

Pharmacologic characteristics

Mechanism of action

Direct thrombin (FIIa) inhibitor

Direct factor Xa inhibitor

Direct factor Xa inhibitor

Clearance

Renal ~85%

Renal ~66% (active and unchanged drug and inactive metabolites)

Renal ~27%

Biliary/Fecal ~20%

Biliary/Fecal ~33% (active drug)

Biliary/Fecal ~75% (active drug)

Half-life

Normal renal function (CrCl >80 mL/min)

~13 hours

5-9 hours

~12 hours

Mild renal impairment (CrCl 50-80 mL/min)

~15 hours

5-9 hours

~12 hours

Moderate renal impairment (CrCl 30-49 mL/min)

~18 hours

11-13 hours

10-14 hours

Severe renal impairment (CrCl <30 mL/min)

Contraindicated

Contraindicated

Contraindicated^b

Onset of action (after oral intake)

1-3 hours

1-4 hours

3-4 hours

Food or alcohol interactions

None

None

None

Drug interactions

P-glycoprotein inhibitors^c (increase systemic exposure)

P-glycoprotein inhibitors^c (increase systemic exposure)

P-glycoprotein inhibitors^c (increase systemic exposure)

P-glycoprotein inducers^d (decrease systemic exposure)

P-glycoprotein inducers^d (decrease systemic exposure)

P-glycoprotein inducers^d (decrease systemic exposure)

Strong CYP 3A4 inhibitors and inducers^e

Strong CYP 3A4 inhibitors and inducers^e