Glimin Mechanism of Action

Pharmacology: Mode of action: Glimepiride is a sulfonylurea. Glimepiride decreases blood glucose concentration mainly by stimulating insulin release from pancreatic beta cells. This effect is based predominantly on an improved responsiveness of the pancreatic beta cells to the physiological glucose stimulus.
Glimepiride also has extra pancreatic (insulin-sensitizing and insulin-mimetic) effects.
The effect of Glimepiride is dose-depended over the dose range of 1 to 6mg. The physiological response to acute physical exercise, i.e. reduction of insulin secretion, is still present with Glimepiride.
Summary of pharmacodynamics and pharmacokinetics: There was no significant difference in effect regardless of whether the drug was given 30 minutes or immediately before a meal. In diabetic patients, metabolic control over 24 hours can be achieved with a single dose.
The absolute bioavailability of Glimepiride is complete. Food intake has no relevant influence on absorption. Maximum serum concentrations are reached approximately 2.5 hours after oral intake and there is a linear relationship between dose and both maximum concentration and area under the time/concentration curve.
Glimepiride has a high protein binding (>99%). Mean dominant serum half-life, which is of relevance for the serum concentration under multiple-dose conditions, is about 5 to 8 hours. After single dose radio labelled Glimepiride, 58% of the radioactivity was recovered in the urine, and 35% in the faeces. No unchanged substance was detected in the urine.
Pharmacokinetic was similar in males and females, as well as in young and elderly patients.