Pharmacology: Glimepiride is a sulfonylurea. Glimepiride decreases blood glucose concentrations 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-dependent over the dose range of 1 to 6 mg. The physiological response to acute physical exercise, i,e, reduction of insulin secretion, is still present with Glimepiride.
There was no significant difference in effect regardless of whether the drug was given to 30 minutes or immediately before 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 concentrations 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 concentrations under multiple-dose conditions, is about 5 to 8 hours. After single dose radio labeled Glimepiride, 58% of the radioactivity was recovered in the urine and 35% in the faeces. No unchanged substance was detected in the urine. Pharmacokinetics was similar in males and females, as well as in young and elderly patients.