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Table 2 TSOAC Pharmacokinetics

From: The role of prothrombin complex concentrates in reversal of target specific anticoagulants

  Dabigatran Rivaroxaban Apixaban
Target Factor IIa Factor Xa Factor Xa
Dosage Form capsule tablet tablet
Bioavailability 6% 60-80% 50-85%
Time to Peak 1-2 hours 2-4 hours 1-3 hours
Metabolism Conjugation; No CYP involvement Oxidation via CYP3A4 Oxidation via CYP3A4
Renal Excretion 80% 33% 25%
Substrate of p- glycoprotein? Yes Yes Yes
FDA approved dosing for stroke prevention in a- fib 150 mg twice daily for 20 mg by mouth once daily for patients CrCL > 50 ml/min 5 mg by mouth twice daily
patients CrCL > 30 ml/min 15 mg by mouth once daily 2.5 mg by mouth twice daily for patients with 2 or more of the following: Age > 80, weight < 60 kg or Serum Cr > 1.5
75 mg by mouth twice daily for CrCL 15–30 ml/min for patients with CrCL 15-50 ml/min
FDA approved dosing for VTE prevention in hip N/A 10 mg once daily for patients with CrCL > 30 ml/min N/A
and knee
replacement
FDA approved N/A 15 mg by mouth twice daily N/A
dosing for {1) treatment of acute DVT or PE, or {2) long term prevention of   for 21 days, then 20 mg once daily for patients with CrCL > 30 ml/min
recurrent DVTfPE   20 mg once daily for patients with CrCL > 30 ml/min
  1. CrCl = Creatinine Clearance, CYP = Cytochrome P450.