Table 2.
TSOAC Pharmacokinetics
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 |
CrCl = Creatinine Clearance, CYP = Cytochrome P450.