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Nateglinide
- indication:For use as monotherapy to lower blood glucose in patients with Type 2 diabetes (non-insulin dependent diabetes mellitus, NIDDM) whose hyperglycemia cannot be adequately controlled by diet and physical exercise and who have not been chronically treated with other anti-diabetic agents. Also indicated for use in combination with metformin.
- pharmacologypharmacology:
- mechanism: Nateglinide interacts with the ATP-sensitive potassium (K+<sub>ATP</sub>) channel on pancreatic beta-cells. The subsequent depolarization of the beta cell opens the calcium channel, producing calcium influx and insulin secretion. The extent of insulin release is glucose dependent and diminishes at low glucose levels. Nateglinide is highly tissue selective with low affinity for heart and skeletal muscle.
- toxicity: An overdose may result in an exaggerated glucose-lowering effect with the development of hypoglycemic symptoms.
- absorprion: Rapidly absorbed following oral administration prior to a meal, absolute bioavailability is estimated to be approximately 73%.
- halflife: 1.5 hours
- roouteelimination:
- volumedistribution: 10 liters in healthy subjects
- clearance: