Dược Động Học :
▧ Absorption :
Completely (100%) absorbed following oral administration.
▧ Volume of Distribution :
* 21.8 ± 13.9 L [Volunteers]
* 19.8 ± 12.7 L [Patients with Type 2 diabetes, Single Dose]
* 37.1 ± 18.2 L [Patients with Type 2 diabetes, Multiple Dose]
▧ Protein binding :
Over 99.5% bound to plasma protein.
▧ Metabolism :
Hepatic. Following either an intravenous or oral dose, glimepiride is completely metabolized by oxidative biotransformation to a major metabolite, cyclohexyl hydroxymethyl derivative (M1), via the hepatic cytochrome P450 II C9 subsystem. M1 is further metabolized to the carboxyl derivative (M2) by one or several cytosolic enzymes. M1, but not M2, possessed approximately one third of the pharmacologic activity of its parent in an animal model. However, whether the glucose-lowering effect of M1 is clinically significant is not clear.
▧ Half Life :
Approximately 5 hours following single dose.
▧ Clearance :
* 52.1 +/- 16.0 mL/min [Normal subjects with single oral dose]
* 48.5 +/- 29.3 mL/min [Patients with Type 2 diabetes, with single oral dose]
* 52.7 +/- 40.3 mL/min [Patients with Type 2 diabetes, with multiple oral dose]
* 47.8 mL/min [healthy after intravenous (IV) dosing]