Tirofiban

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.
Clinical effect duration:platelet activity returns to normal 4-8 hours after the infusion is ceased

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)