Table 1 Pharmacologic properties of anticoagulants
From: Management of anticoagulant-related intracranial hemorrhage: an evidence-based review
Drug | Target | Antithrombin dependent | Route | Half-life (hours) | Protein binding | Renal excretion | Monitoring | Antidote | Common indications |
|---|---|---|---|---|---|---|---|---|---|
Warfarin | Factors II, VII, IX, X; proteins C, S | No | p.o. | 30 to 40 | 99% | 92% | INR | Vitamin K | Thromboembolic prophylaxis in AF. Treatment of VTE. Thrombosis prophylaxis in prosthetic valve |
UFH | Factors II, Xa (VIIa, IXa, XIa, XIIa) | Yes | i.v., s.c. | 0.5 to 2.5 (dose dependent) | Variable | Mostly after hepatic metabolism | aPTT | Protamine sulfate | ACS. Thromboprophylaxis. Thromboembolic diseases (including ischemic stroke, CVST) in acute phase |
LMWH | Factors IIa, Xa | Yes | s.c., i.v. | Variable according to the product | Variable | 40% (10% unchanged) | Anti-factor Xa | Protamine sulfate (60%) | ACS. Thromboprophylaxis. Thromboembolic diseases |
Fondaparinux | Factor Xa | Yes | s.c. | 17 to 21 | 94% | ~100% (77% unchanged) | Anti-factor Xa | None (see text) | VTE. Thromboprophylaxis. Selected cases of HIT |
Argatroban | Factor IIa | No | i.v. | 0.75 (prolonged in hepatic dysfunction) | 54% | 22% (16% unchanged) | aPTT, ACT | None | HIT. Thromboprophylaxis in patients suspected of HIT. ACS |
Bivalirudin | Factor IIa | No | i.v. | 0.5 (prolonged in renal impairment) | Only to factor IIa | 20% unchanged | ECT (PT, aPTT, ACT has nonlinear prolongation) | None | HIT. ACS after thrombolysis. Thromboembolic prophylaxis during interventional procedures |
Dabigatran | Factor IIa | No | p.o. | 12 to 14 | 35% | 80% | Modified TT/ECT/anti-factor IIa (also see Table 3) | PCC/FEIBA™/rFVIIa (see text) | Thromboembolic prophylaxis in AF. Treatment and thromboprophylaxis of VTE |
Apixaban | Factor Xa | No | p.o. | 8 to 14 | 87% | ~25% | Anti-factor Xa (also see Table 3) | PCC/FEIBA™/rFVIIa (see text) | Thromboembolic prophylaxis in AF. Treatment and thromboprophylaxis of VTE |
Rivaroxaban | Factor Xa | No | p.o. | 7 to 11 | 93% | 66% (33% unchanged) | Anti-factor Xa (also see Table 3) | PCC/FEIBA™/rFVIIa (see text) | Thromboembolic prophylaxis in AF. Treatment and thromboprophylaxis of VTE |