The relationship between dose, pharmacokinetics, plasma-concentrations and antithrombotic effects of nafazatrom.

Nafazatrom is rapidly and almost completely absorbed after oral administration. However, the plasma levels of unchanged nafazatrom are very low, suggesting an extensive biotransformation during a first passage through the liver. The concentrations of nafazatrom in the plasma therefore, may only reflect indirectly the effective concentration at the receptor site. Concentrations, half-life and distribution of nafazatrom between aqueous and liquid compartments suggest that the cellular membrane may be the site of action.