Table 2 TSOAC Pharmacokinetics

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