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QuickView for Repaglinide (compound)

Name: repaglinide
PubChem Compound ID: 10479034
Molecular formula: C27H36N2O4
Molecular weight: 452.586 g/mol
Name: repaglinide
Name (isomeric): DB00912
Drug Type: small molecule
AG-EE 388 ZW; AG-EE 623 ZW; Repaglinida [INN-Spanish]; Repaglinidum [INN-Latin]
Brand: GlucoNorm, Prandin
Category: Hypoglycemic Agents, Meglitinides, Antidiabetic
CAS number: 135062-02-1
Indication: For the treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
Insulin secretion by pancreatic β cells is partly controlled by cellular membrane potential. Membrane potential is regulated through an inverse relationship between the activity of cell membrane ATP-sensitive potassium channels (ABCC8) and extracellular glucose concentrations. Extracellular glucose enters the cell via GLUT2 (SLC2A2) transporte...
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Mechanism of Action:
Repaglinide activity is dependent on the presence functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, repaglinide has no effect on insulin release in the absence of glucose. Rather, it potentiates the effect of extracellular glucose on ATP-sensitive potassium channel and has little effect on insulin levels bet...
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Absorption: Rapidly and completely absorbed following oral administration. Peak plasma concentrations are observed within 1 hour (range 0.5-1.4 hours). Absolutely bioavailability is approximately 56%. Maximal biological effect is observed within 3-3.5 hours and plasma insulin levels remain elevated for 4-6 hours
Protein binding: >98% (e.g. to to albumin and α1-acid glycoprotein)
Biotransformation: Repaglinide is rapidly metabolized via oxidation and dealkylation by cytochrome P450 3A4 and 2C9 to form the major dicarboxylic acid derivative (M2). Further oxidation produces the aromatic amine derivative (M1). Glucuronidation of the carboxylic acid group of repaglinide yields an acyl glucuronide (M7). Several other unidentified metabolites have been detected. Repaglinide metabolites to not possess appreciable hypoglycemic activity.
Route of elimination: 90% eliminated in feces (<2% as unchanged drug), 8% in urine (0.1% as unchanged drug)
Half Life: 1 hour
Clearance: 33-38 L/hour following IV administration
Toxicity: LD50 >1 g/kg (rat) (W. Grell)
Affected organisms: Humans and other mammals
Food interaction:
Take up to 30 minutes before meals.
Drug interaction:
OxprenololThe beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
ErythromycinThe macrolide, erythromycin, may increase the effect of repaglinide.
BevantololThe beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
EsmololThe beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
MetoprololThe beta-blocker, metoprolol, may decrease symptoms of hypoglycemia.
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