Correlation Engine 2.0
Clear Search sequence regions
Bookmark Forward

QuickView for Nateglinide (compound)

Name: nateglinide
PubChem Compound ID: 443871
Molecular formula: C19H27NO3
Molecular weight: 317.423 g/mol
C12508; D01111; Starsis; Nateglinide (JAN/USAN); Starsis (TN); 105816-04-4; Nateglinide
Name: nateglinide
Name (isomeric): DB00731
Drug Type: small molecule
SDZ-DJN 608; Nateglinide [INN]
Brand: Starlix, Starsis, Fastic
Category: Hypoglycemic Agents, Meglitinides
CAS number: 105816-04-4
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) transporters. O...
show more »
Mechanism of Action:
Nateglinide activity is dependent on the presence functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, nateglinide 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 between ...
show more »
Absorption: Rapidly absorbed following oral administration prior to a meal, absolute bioavailability is estimated to be approximately 73%. Peak plasma concentrations generally occur within 1 hour of oral administration. Onset of action is <20 minutes and the duration of action is approximately 4 hours.
Protein binding: 98% bound to serum proteins, primarily serum albumin and to a lesser extent α1 acid glycoprotein
Biotransformation: Hepatic, via cytochrome P450 isoenzymes CYP2C9 (70%) and CYP3A4 (30%). Metabolism is via hydroxylation followed by glucuronidation. The major metabolites have less antidiabetic activity than nateglinide, but the isoprene minor metabolite has antidiabetic activity comparable to that of nateglinide.
Route of elimination: Urine (83%) and feces (10%)
Half Life: 1.5 hours
Toxicity: An overdose may result in an exaggerated glucose-lowering effect with the development of hypoglycemic symptoms.
Affected organisms: Humans and other mammals
Food interaction:
Take upto 30 minutes before meals.
Drug interaction:
GlucosaminePossible hyperglycemia
Somatropin recombinantSomatropin may antagonize the hypoglycemic effect of nateglinide. Monitor for changes in fasting and postprandial blood sugars.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of nateglinide by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of nateglinide if voriconazole is initiated, discontinued or dose changed.
TelithromycinTelithromycin may reduce clearance of Nateglenide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nateglenide if Telithromycin is initiated, discontinued or dose changed.
TolbutamideTolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Nateglinide. Consider alternate therapy or monitor for changes in Nateglinide therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed.