Pharmacology of direct thrombin inhibitors (DTI).
| DTI . | Valence . | Mr(Da)† . | Ki(mol/L)‡ . | t½§ . | Excretion . |
|---|---|---|---|---|---|
| † Molecular weight (daltons) | |||||
| ‡ Inhibition constant. | |||||
| § Plasma half-life | |||||
| Lepirudin (Refludan®) Desirudin (Revasc®) | Bivalent: active site and exosite 1 | 698 | 0.2 × 10−12 | 60–80 mins (IV) 120 mins (SC) | renal |
| Bivalirudin (Hirulog®, Angiomax®) | 218 | 2.3 × 10−9 | 25 mins | non renal, non hepatic | |
| Argatroban (Novastan®) | Univalent: active site, noncovalent | 527 | 3.9 × 10−8 | 45 mins | biliary secretion |
| Melagatran | 430 | 0.2 × 10−8 | 2–3 hrs | renal | |
| Ximelagatran (Exanta®) | 474 | 37 × 10−8 | 3–5 hrs | ||
| Dabigatran/BIBR-1048 | – | 4.5 × 10−8 | 12 hrs | – | |
| DTI . | Valence . | Mr(Da)† . | Ki(mol/L)‡ . | t½§ . | Excretion . |
|---|---|---|---|---|---|
| † Molecular weight (daltons) | |||||
| ‡ Inhibition constant. | |||||
| § Plasma half-life | |||||
| Lepirudin (Refludan®) Desirudin (Revasc®) | Bivalent: active site and exosite 1 | 698 | 0.2 × 10−12 | 60–80 mins (IV) 120 mins (SC) | renal |
| Bivalirudin (Hirulog®, Angiomax®) | 218 | 2.3 × 10−9 | 25 mins | non renal, non hepatic | |
| Argatroban (Novastan®) | Univalent: active site, noncovalent | 527 | 3.9 × 10−8 | 45 mins | biliary secretion |
| Melagatran | 430 | 0.2 × 10−8 | 2–3 hrs | renal | |
| Ximelagatran (Exanta®) | 474 | 37 × 10−8 | 3–5 hrs | ||
| Dabigatran/BIBR-1048 | – | 4.5 × 10−8 | 12 hrs | – | |