| Class | Direct thrombin inhibitor |
|---|---|
| Chemistry |
L- arginine derivative |
| Routes of administration |
IV ands subcut |
| Absorption |
Oral bioavailability is minimal, less than 1%. |
| Solubility |
pKa 13.4 (thus, minimal oral absorption); |
| Distribution |
VOD=0.2L/kg; 54% plasma protein bound |
| Metabolism |
Metabolised in the liver by hydroxylation and aromatisation of the 3- methyltetrahydroquinoline ring |
| Elimination |
Inactive metabolites are renally cleared. |
| Time course of action |
Half life is about 45 minutes |
| Target receptor |
Thrombin |
| Mechanism of action |
Binds to the catalytic site of 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 |
FDA PI document |
| CICM details of understanding | Not specifically listed in the CICM syllabus |
| Mentioned around Deranged Physiology | |
| Related SAQs |