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Table 1 Pharmacokinetic properties of direct oral anticoagulants

From: Perioperative management of patients on direct oral anticoagulants

  Dabigatran Rivaroxaban Apixaban Edoxaban
Target Factor lla Factor Xa Factor Xa Factor Xa
Prodrug Yes No No No
Tmax (h) 1.0–3.0 2.0–4.0 3.0–4.0 1.0–2.0
Half-life (h) 12-17 h 5–9: healthy individuals
11–13: elderly
8–15: healthy individuals 10–14
Bioavailability 3–7%
pH sensitive
For 2.5 mg and 10 mg: 80–100% (fasting or fed)
For 15-20 mg:
66%: (fasting)
almost 100% (fed)
± 50% 62%
Metabolism Conjugation CYP-dependent and independent mechanism CYP-dependent mechanism (25%) CYP-dependent (<5%) and independent mechanism (<10%)
Active metabolites Yes - acylglucuronides No No Yes (<15%)
Elimination of absorbed dose 80% renal 33% unchanged via the kidney 27% renal 50% renal
  20% bile (glucuronide conjugation) 66% metabolized in the liver into inactive metabolites then eliminated via the kidney or the colon in an approximate 50% ratio 73% through the liver, the residue is excreted by the hepatobiliary route 50% metabolism and biliary/intestinal excretion
CYP substrate No CYP3A4, CYP2J2 CYP3A4 CYP3A4 (<5%)
P-gp substrate DE: Yes Yes Yes Yes
BRCP substrate No Yes Yes No
  1. Tmax: time to reach peak concentration; CYP3A4: cytochrome P450 isozyme 3A4;
  2. P-gp: P-glycoprotein; BRCP: Breast cancer resistance protein