| Class | Direct thrombin inhibitor |
|---|---|
| Chemistry |
Polypeptide |
| Routes of administration |
IV ands subcut |
| Absorption |
Oral bioavailability 10% |
| Solubility |
pKa 4.4; good water solubility |
| Distribution |
VOD=0.3L/kg; minimally protein bound (only to thrombin) |
| Metabolism |
Minimally metabolised; some hydrolysis in the liver occurs, whcih liberates [eptide fragments and amino acids |
| Elimination |
48% of the drug is cleared renally. 35% as unchanged drug and the rest as fragments |
| Time course of action |
Half-life is about 1.3 hours |
| Target receptor |
Thrombin |
| Mechanism of action |
Binds to thrombin, deactivating it and preventing the formation of fibrin (as well as inhibiting other thrombin-driven parts of haemostasis, such as the activation of platelets) |
| Clinical effects |
Anticoagulation is the only clinically apparent effect; no significant side effects apart from bleeding complications |
| Literature reference |
Greinacher et a, 1991 |
| CICM details of understanding | Not specifically listed in the CICM syllabus |
| Mentioned around Deranged Physiology | |
| Related SAQs |