Table 1 Pharmacokinetic properties of direct oral anticoagulants[20–25]

Mechanism of action

Direct Factor Xa inhibitor

Direct Factor Xa inhibitor

Direct Factor Xa inhibitor

Direct thrombin inhibitor

Prodrug

No

No

No

Dabigatran etexilate

Oral bioavailability (%)

80–100

~66

~50

6.5

Fraction unbound in plasma (%)

~5–10

13

~41–60

~65–70

t_max (h)

2.0–4.0

1.0–3.0

1.0–2.0

1.25–3.0

t_½ (h)

5–13

8–15

6–11

12–14

Elimination

36% unchanged via active renal secretion; 30% renal excretion of inactive metabolites; 34% hepatobiliary (7% unchanged)

~25% renal; ~75% hepatobiliary

~35–39% renal; ~61–65% hepatobiliary

80% renal; 20% hepatobiliary

Metabolism

CYP3A4, CYP2J2 and CYP-independent mechanisms; P-gp substrate

CYP3A4; P-gp substrate

CYP3A4; P-gp substrate

P-gp substrate