Glimepiride

Glimepiride is an orally available medium-to-long-acting sulfonylurea antidiabetic drug. It is sometimes classified as either the first third-generation sulfonylurea, or as second-generation.

Glimepiride

Glimepiride; Amaryl; Amarel; Glimepirida

Abepride, Adglim, Adride, Amaryl, Asoride, Astapride, Azulix, Beglim, Bepride, Betaglim, Blisto, Capril, Cgryl, Chempride, Conpride, Cupride, Daoride, Daoryl, Diaglim, Diagraph, Diapride, Diaset, Diaswich, Diazero, Dibiglim, Dipride, Elim, Emperide, Euglim, Euroglip, Flexiglim, G-Tab, G-Tab Forte, G-Tab M, Gadz, Geminor, Gepride, Gimip, Gitae, Givov, Glador, Glamor, Gleam, Gli, Glicmiz, Glicon-M, Glimcare, Glimchek, Glimcip, Glimcom

3-ethyl-4-methyl-2-oxo-N-(2-{4-[({[(1r,4r)-4-methylcyclohexyl]-C-hydroxycarbonimidoyl}amino)sulfonyl]phenyl}ethyl)-2,5-dihydro-1H-pyrrole-1-carboximidic acid

Oral absorption 100%. Hepatic metabolism.

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

The recommended dose is 1-2 mg once daily with food PO.

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

Vomiting, GI pain, diarrhoea; pruritus, erythema, urticaria, morbilliform, maculopapular eruptions; leukopenia, agranulocytosis, thrombocytopenia, haemolytic anaemia, aplastic anaemia and pancytopenia; hyponatraemia; changes in accommodation, blurred vision, jaundice.

• Corticosteroids, thiazides and other diuretics, phenothiazines, oestrogens, thyroid products, oral contraceptives, nicotinic acid, phenytoin, sympathomimetics, rifampicin, CYP2C9 inducers and isoniazid may reduce hypoglycaemic effect of glimepiride.
• NSAIDs, sulphonamides, salicylates, coumarin, chloramphenicol, CYP2C9 inhibitors, probenecid, fibric acid derivatives, TCAs, pegvisomant, MAOIs and β-adrenergic blockers may potentiate the hypoglycaemic action of glimepiride.
• May increase the serum levels of ciclosporin. Serum levels may be increased by fluconazole.
• May increase the serum levels of ciclosporin.
• Serum levels may be increased by fluconazole.

Diabetic ketoacidosis with or without coma

Store at 15-30°C

Molecular weight

490.62

Molecular formula

C24H34N4O5S

CAS number

93479-97-1

Precautions

• Increased risk of CV mortality.
• Elderly; hepatic and renal impairment.
• Syndrome of inappropriate secretion of antidiuretic hormone (SIADH) in patients with CHF or hepatic cirrhosis.
• Monitor blood-glucose concentration.
• Pregnancy, lactation.