Trade Names:Starlix- Tablets 60 mg- Tablets 120 mg
Lowers blood glucose levels by stimulating insulin secretion from the pancreas.
Rapidly absorbed immediately prior to a meal. Oral T max is 1 h (prior to a meal); bioavailability is approximately 73%. Food delays T max and C max .
Nateglinide protein binding is 98% (primarily albumin, and to a lesser extent to alpha-1 acid glycoprotein). Vd is 10 L (IV).
Hydroxylation followed by glucuronide conjugation via CYP2C9 (70%) and CYP3A4 (30%).
Nateglinide is eliminated in urine (83% as metabolites, 16% as parent compound) and feces (10%). The half-life is 1.5 h.
Compared with healthy subjects, patients with type 2 diabetes and moderate to severe renal impairment (CrCl 15 to 50 mL/min) not on dialysis, displayed similar clearance, AUC, and C max . Patients with renal failure on dialysis exhibited reduced overall drug exposure. Hemodialysis patients experienced a reduction in plasma protein binding.Hepatic Function Impairment
The peak and total exposure of nateglinide were increased 30% (mild hepatic insufficiency). Use with caution (chronic hepatic insufficiency).Elderly
Pharmacokinetics not affected by age. No dosage adjustment is needed in elderly patients.Gender
No clinically important differences in pharmacokinetics between men and women. No dosage adjustment is needed based on gender.Race
Race has little influence of the pharmacokinetics.
As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Type 1 diabetes; diabetic ketoacidosis; hypersensitivity to nateglinide or its ingredients.
PO 120 mg 3 times daily, 1 to 30 min before meals, alone or in combination with metformin or a thiazolidinedione. The 60 mg dose of nateglinide may be used, alone or in combination with metformin or a thiazolidinedione, in patients whose glycosylated hemoglobin (HbA 1c ) is near goal levels when treatment is initiated.
Store tablets at controlled room temperature (59° to 86°F). Keep tightly closed.
May reduce the hypoglycemic effects of nateglinide.Fluconazole, MAOIs, nonselective beta-adrenergic blocking agents, NSAIDs, salicylates
May potentiate the hypoglycemic effects of nateglinide.
Uric acid levels may be increased.
Cholestatic hepatitis, elevated LFTs, jaundice (postmarketing).
Rash, itching, urticaria (postmarketing).
Upper respiratory tract infection (11%); bronchitis (3%); coughing (2%).
Back pain, flu-like symptoms (4%); arthropathy, accidental trauma (3%).
Assess response to therapy with periodic glucose values and glycosolated hemoglobin levels.
Category C . Insulin is recommended to maintain blood glucose levels during pregnancy.
Safety and efficacy not established.
Use with caution in patients with moderate to severe impairment or chronic liver disease.
Patients with type 2 diabetes and renal failure on dialysis may exhibit reduced overall drug exposure.
May occur and the risk may be increased by strenuous exercise, alcohol ingestion, insufficient caloric intake on an acute or chronic basis, or use in combination with other oral antidiabetic agents.
Transient loss of glycemic control may occur in patients with fever, infection, trauma, or surgery. At such times, it may be necessary to discontinue nateglinide and administer insulin.
Coma, exaggerated glucose lowering with hypoglycemic symptoms, neurological symptoms, seizure.
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