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Nateglinide
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DOI：10.2165/00003495-200060030-00007.png)
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Abstract
En 中文
Nateglinide is a novel D-phenylalanine derivative that inhibits ATP-sensitive K+ channels in pancreatic beta-cells in the presence of glucose and thereby stimulates the prandial release of insulin. Nateglinide reduces fasting and mealtime blood glucose levels in animals, healthy volunteers, and patients with type 2 (non-insulin-dependent) diabetes mellitus, and produces prompt prandial insulin responses with return to baseline insulin levels between meals. In randomised, double-blind 24-week studies in patients with type 2 diabetes, oral nateglinide 120mg 3 times daily before meals improved glycaemic control significantly relative to placebo. Nateglinide 120mg plus metformin 500mg, both 3 times daily conferred greater glycaemic improvement than either drug given alone, and nateglinide 60 or 120mg 3 times daily plus metformin 1g twice daily was superior to metformin plus placebo. Nateglinide 120mg 3 times daily significantly reduced hyperglycaemia relative to placebo in a 16-week double-blind study in patients with type 2 diabetes mellitus. Combination therapy with troglitazone 600mg daily produced significantly better glycaemic control than either drug given as monotherapy. Mild hypoglycaemia was the most frequently reported adverse event (1.3% of patients) after treatment with nateglinide 120mg 3 times daily in a 16-week clinical study, No clinically significant abnormalities in laboratory results, ECGs, vital signs or physical examination findings have been noted in patients taking the drug.
Keywords:
PERFUSED RAT PANCREAS
DERIVATIVE HYPOGLYCEMIC AGENT
N-<(TRANS-4-ISOPROPYLCYCLOHEXYL)-CARBONYL>-D-PHENYLALANINE A-4166
MEGLITINIDE ANALOGS
INSULIN-SECRETION
GLIBENCLAMIDE
SOMATOSTATIN
INCREASES
GLUCOSE
CELLS