Table 3.
Drug | Mechanism | Half-life | Metabolism | Elimination | Onset | Notes | |
---|---|---|---|---|---|---|---|
UFH | AT-III mediated factor Xa and thrombin inhibitor |
IV or SC | 1–2 h | Hepatic | Extra-renal at therapeutic doses | Immediate (IV), 30 min (SC) |
Inactive on clot-associated thrombin Unpredictable bioavailability |
Enoxaparin | AT-III mediated factor Xa and thrombin inhibitor |
SC | 5–7 h | Hepatic | Renal | 3–5 h | Inactive on clot-associated thrombin More factor Xa selectivity |
Fondaparinux | Indirect factor Xa inhibitor | SC | 17–21 h | Excreted largely as unchanged drug | Renal | 2–3 h | Inactive on clot-associated thrombin |
Not for use in advanced CKD | |||||||
Rivaroxaban | Direct factor Xa inhibitor | Oral | 9–13 h | Hepatic | Renal and gastrointestinal | 2–4 h | Phase III trials underway |
Apixaban | (−) Factor Xa (direct) | Oral | 12 h | Renal and biliary | 3 h | Phase III trials underway | |
Otamixaban | (−) Factor Xa (direct) | IV | 2–3 h | Biliary | Immediate | Phase III trials underway | |
Bivalirudin | Direct thrombin inhibitor, reversible | IV | 25 min | Plasma proteases | Renal | Immediate | Inhibits clot-associated thrombin |
Dabigatran | Direct thrombin inhibitor, reversible | Oral | 12–17 h | Hepatic and plasma | Renal and gastrointestinal | 1 h | Pro-drug, low bioavailability |