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QuickView for Glimepiride (compound)

Name: glimepiride
PubChem Compound ID: 11787804
Molecular formula: C43H55ClN6O8S2
Molecular weight: 883.517 g/mol
Name: glimepiride
Name (isomeric): DB00222
Drug Type: small molecule
Glimepride; Glimepirida; Glimepiridum; Glimepirid
Brand: Novo-glimepiride, Amaryl, Amarel, Sandoz glimepiride, Ratio-glimepiride, PMS-glimepiride, Endial
Brand name mixture: Avandaryl(glimepiride + rosiglitazone maleate)
Category: Hypoglycemic Agents, Antiarrhythmic Agents, Sulfonylureas, Anti-Arrhythmia Agents, Immunosuppressive Agents
CAS number: 93479-97-1
Indication: For concomitant use with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus.
Pharmacology: Glimepiride, like glyburide and glipizide, is a "second-generation" sulfonylurea agents. Glimepiride is used with diet to lower blood glucose by increasing the secretion of insulin from pancreas and increasing the sensitivity of peripheral tissues to insulin.
Mechanism of Action:
The mechanism of action of glimepiride in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin. Glimepiride likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium c...
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Absorption: Completely (100%) absorbed following oral administration.
Protein binding: Over 99.5% bound to plasma protein.
Biotransformation: Hepatic. Following either an intravenous or oral dose, glimepiride is completely metabolized by oxidative biotransformation to a major metabolite, cyclohexyl hydroxymethyl derivative (M1), via the hepatic cytochrome P450 II C9 subsystem. M1 is further metabolized to the carboxyl derivative (M2) by one or several cytosolic enzymes. M1, but not M2, possessed approximately one third of the pharmacologic activity of its parent in an animal model. However, whether the glucose-lowering effect of M1 is clinically significant is not clear.
Half Life: Approximately 5 hours following single dose.
Clearance: 52.1 +/- 16.0 mL/min [Normal subjects with single oral dose] 48.5 +/- 29.3 mL/min [Patients with Type 2 diabetes, with single oral dose] 52.7 +/- 40.3 mL/min [Patients with Type 2 diabetes, with multiple oral dose] 47.8 mL/min [healthy after intravenous (IV) dosing]
Toxicity: Severe hypoglycemic reactions with coma, seizure, or other neurological impairment.
Affected organisms: Humans and other mammals
Food interaction:
Even though food reduces product absorption, the manufacturer recommends taking the product with the first meal of the day.
Avoid alcohol.
Drug interaction:
GlucosaminePossible hyperglycemia
KetoconazoleKetoconazole increases the effect of rosiglitazone
TolbutamideTolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Glimepiride. Consider alternate therapy or monitor for changes in Glimepiride therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed.
GemfibrozilGemfibrozil increases the effect and toxicity of rosiglitazone/pioglitazone
CyclosporineThe sulfonylurea, glimepiride, may increase the effect of cyclosporine.
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