Table 1.
Comparative pharmacokinetics
| UFH | LMWH | Fondaparinux | FII inhibitor | FXa inhibitors | |||
|---|---|---|---|---|---|---|---|
| Dabigatran | Rivaroxaban | Apixaban | Edoxaban | ||||
| Route of administration | iv | sc | sc | Oral | Oral | Oral | Oral |
| Molecular weight | 3–30 kDa | 5000 Da | 1726 Da | 627 Da | 435 Da | 459 Da | 548 Da |
| Predictable pharmacokinetics | No | Yes | Yes | Yes | Yes | Yes | Yes |
| t max (h) | Minutes | 4–6 | 2–4 | 1–3 | 2–4 | 3–4 | 1–2 |
| t 1/2 (h) | 0.5–1.5 | 3–6 | 17–21 | 12–17 | 5–13 | 9–14 | 10–14 |
| Bioavailability (%) | 100 | >90 | 100 | 3–10 | >80 | 50 | 62 |
| Volume of distribution (l kg −1 ) | 0.07 | 0.04–0.06 | 0.1–0.2 | 0.8–1 | 0.71 | 0.3 | 0.77 |
| Plasma protein binding (%) | >90 | >90 | >97 | 35 | 92–95 | 87 | 55 |
| Renal elimination (%) | Only in high dose | >80 | >80 | 80 | 33 | 27 | 50 |
| CYP metabolism (%) | None | None | None | None | 66 | 25 | <4 |
| P‐gp | None | None | None | Yes | Yes | Yes | Yes |
| Risk of HIT | Yes | Low | None | None | None | None | None |
| Pregnancy | Not‐contraindicated | Not‐contraindicated | Unknown/contraindicated | Unknown/contraindicated | Unknown/contraindicated | Unknown/contraindicated | Unknown/contraindicated |
| Reversal agent | Protamin | Protamin (partly) | Not available | Idarucizumab | Not available | Not available | Not available |
FXa, factor Xa; HIT, heparin‐induced thrombocytopenia; iv, intravenously; LMWH, low molecular weight heparin; NA, not applicable; p‐gp, p‐glycoprotein (for relevant drug interactions, see the interaction table in the online supplement); sc, subcutaneously; t 1/2, half‐life; t max, time to maximum concentration; UFH, unfractionated heparin