Table 2.

Pharmacologic and pharmacokinetic properties of oral anticoagulants [8–11, 18]

Medication (Brand)	Warfarin (Coumadin, Jantoven)	Dabigatran (Pradaxa)	Rivaroxaban (Xarelto)	Apixaban (Eliquis)	Edoxaban (Savaysa)
Mechanism of action	VKOR (factors II, VII, IX, X)	Direct thrombin inhibitor	Factor Xa inhibitor	Factor Xa inhibitor	Factor Xa inhibitor
Bioavailability	~100%	6.5% (prodrug)	80%	~50–66%	62%
Delayed absorption with food	No	Yes	Yes	No	No
Distribution (% protein-bound)	99%	35%	95%	87%	55%
Metabolism	CYP2C9 (primary) T max: 72–96 h T 1/2: 40 h	Hepatic glucuronidation T max: 1–2 h T 1/2: 12–17 h	CYP3A4, CYP2J2 T max: 2.5–4 h T 1/2: 5–9 h	CYP3A4 (primary) T max: 3 h T 1/2: 8–15 h	CYP3A4 (primary) T max: 1–2 h T 1/2: 10–14 h
Renal excretion	92%	80%	67% (33% active)	25%	50%
Drug–drug interactions	Substrate: CYP2C9, 1A2, 3A4, 2C19 Weak inhibitor: CYP2C9, 2C19	Substrate: P-gp Absorption decreased by acid reducers	Substrate: CYP3A4, 2J2, P-gp	Substrate: CYP3A4, 1A2, 2C9, 2C19, P-gp Weak inhibitor: CYP2C19	Substate: CYP3A4, P-gp
Adverse effects (non-bleeding)	Alopecia, tissue necrosis (<0.1%)	Dyspepsia 35%	Peripheral edema ≤6%	Rare	Rare

CYP cytochrome p450, h hours, P-gp P-glycoprotein, T _1/2 half-life, T _max time to maximum concentration, VKOR vitamin K epoxide reductase