| Class | Antiplatelet agent |
|---|---|
| Chemistry |
Tyrosine derivative |
| Routes of administration |
IV only |
| Absorption |
2.2% oral bioavailability (in rats...) |
| Solubility |
pKa 3.7; slightly soluble in water |
| Distribution |
VOD = 0.4-1.0L/kg; 64% protein bound |
| Metabolism |
Minimal metabolism |
| Elimination |
Cleared renally as unchanged drug |
| Time course of action |
Half-life about 2 hours. |
| Target receptor |
GP IIb/IIIa receptor |
| Mechanism of action |
Tirofiban binds to the GPIIb/IIIa receptor which inhibits platelet aggregation by preventing the binding of fibrinogen fibrin and von Willebrand factor, thus preventing platelet crosslinking. This binding is reversible. |
| Clinical effects |
Apart from the risk of bleeding (which is serious!), no other major side effects |
| Literature reference |
TGA PI document |
| CICM details of understanding | Level 3 |
| Mentioned around Deranged Physiology | |
| Related SAQs |
Question 3 from thw second paper of 2013 (mechanism) Question 5 from the second paper of 2010 (mechanism) |