Drug Groups

approved

Description

Glimepiride is the first III generation sulphonyl urea it is a very potent sulphonyl urea with long duration of action.

Indication

For concomitant use with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus.

Pharmacology

Glimepiride, like glyburide and glipizide, is a "second-generation" sulfonylurea agents. Glimepiride is used with diet to lower blood glucose by increasing the secretion of insulin from pancreas and increasing the sensitivity of peripheral tissues to insulin.

Toxicity

Severe hypoglycemic reactions with coma, seizure, or other neurological impairment.

Affected Organisms

Biotransformation

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.

Absorption

Completely (100%) absorbed following oral administration.

Half Life

Approximately 5 hours following single dose.

Protein Binding

Over 99.5% bound to plasma protein.

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]

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]

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