Glimepiride

Glimepiride is a medium-to-long acting sulfonylurea anti-diabetic drug. It is marketed as Amaryl by Sanofi-Aventis and GLIMY by Dr.Reddy's Labs. Glimepiride is the first third-generation sulfonylurea, and is very potent.

It is sometimes classified as third-generation, and sometimes classified as second-generation.

Indications
Type 2 Diabetes Mellitus

Contraindications

 * Hypersensitivity to glimepiride or other sulfonylureas
 * Pregnancy

Adverse effects
GI disturbance, rarely thrombocytopenia, leukopenia, hemolytic anemia, occasionally allergic reactions occur. In the initial weeks of treatment, the risk of hypoglycemia may be increased.

Pharmacokinetics
With glimepiride GI absorption is complete, with no interference of meals. Significant absorption of glimepiride was seen within 1 hour, and distributed throughout the body, bound to the plasma protein to an extent of 99.5% and it is metabolized by oxidative biotransformation and 60% is excreted in the urine, the remaining being excreted in the feces.

Mechanism of action
Like all sulfonylureas, glimepiride acts as a secretagogue. It lowers blood sugar by stimulating the release of insulin by pancreatic beta cells and by inducing increased activity of intracellular insulin receptors.

Not all secondary sufonylureas have the same risks of hypoglycemia. Glibenclamide (glyburide) is associated with an incidence of hypoglycemia of up to 20–30%, compared to 2% to 4% with glimepiride. Glibenclamide also interferes with the normal homeostatic suppression of insulin secretion in reaction to hypoglycemia, whereas glimepiride does not have this property. Furthermore, glibenclamide diminishes the glucagon secretion in reaction to hypoglycemia, whereas glimepiride does not suppress this counter-regulatory reaction.

Interactions
With NSAIDs like Salicylates, Sulphonamides, Chloramphenicol, coumadin and probencid may potentiate the hypoglycemic action of glimepiride. Thiazides, other diuretic, phothiazides, thyroid products, oral contraceptives, phenytoin tend to produce hyperglycemia.