Name: | nateglinide |
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PubChem Compound ID: | 443871 |
Molecular formula: | C19H27NO3 |
Molecular weight: | 317.423 g/mol |
Synonyms: |
C12508; D01111; Starsis; Nateglinide (JAN/USAN); Starsis (TN); 105816-04-4; Nateglinide
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Name: | nateglinide |
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Name (isomeric): | DB00731 |
Drug Type: | small molecule |
Synonyms: |
SDZ-DJN 608; Nateglinide [INN]
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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. |
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Pharmacology: |
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...
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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 ...
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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: |
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Drug interaction: |
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