Drug Study: Glimepiride (Getryl)

Generic Name: Glimepiride

Brand Name: Getryl

Dosage: 1 mg, 2mg, 3 mg, 4mg TABLET (Oral Hypoglycaemic)

Description: Glimepiride (Getryl) is an oral blood glucose lowering drug of the sulfonylurea class. Chemically glimepiride is 1-[[p-[2-(3-Ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)ethyl]phenyl]-sulphonyl]-3-(trans-4-methylcyclohexyl)urea. The molecular formula is C24H34N4O5S.

Clinical Pharmacology:

Mechanism of Action
The primary mechanism of action of glimepiride appears to be dependent on stimulating the release of insulin from functioning pancreas beta cells. In addition, extra-pancreatic effects (e.g. reduction of basal hepatic glucose production and increased peripheral tissue sensitivity to insulin and glucose uptake) may also play a role in the activity of glimepiride. However, as with other sulfonylureas, the mechanism by which glimepiride lowers blood glucose during long-term administration has not been clearly established.

After oral administration glimepiride is completely absorbed from the GI tract. The oral bioavailability is approximately 100%. Peak plasma concentrations occur in 2-3 hours. More than 99% of the drug is bound to plasma proteins. Glimepiride is completely metabolized by oxidative biotransformation into two main metabolites, a hydroxyl derivative and a carboxy derivative. The elimination half-life (t1/2) after multiple doses is about 5-8 hours. Approximately 60% of dose is eliminated in the urine and 40% in the feces.

Special Populations

Renal Insufficiency
A single-dose clinical study glimepiride showed that glimepiride serum levels decreased as renal function decreased. However, metabolite serum levels (mean AUC values) increased. The apparent terminal half-life (t1/2) for glimepiride did not change, while the half-lives for metabolites increased as renal function decreased. Mean urinary excretion of metabolites as percent of dose, however, decreased.

Glimepiride (Getryl) is indicated as an adjunct to diet and exercise to lower the blood glucose in patients with non-insulin-dependent (Type 2) diabetes mellitus (NIDDM) whose hyperglycemia cannot be controlled by diet and exercise alone. Glimepiride (Getryl) may be used concomitantly with metformin when diet, exercise, and Glimepiride (Getryl) or metformin alone o not result in adequate glycemic control. Glimepiride (Getryl) is also indicated for use in combination with insulin to lower blood glucose in patients whose hyperglycemia cannot be controlled by diet and exercise in conjunction with an oral hypoglycemic agent.

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