Nateglinide
Indications
Nateglinide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Pharmacology
Nateglinide, a nonsulfonylurea hypoglycaemic agent which stimulates insulin release from the pancreatic β-cells by blocking ATP-dependent K channels, depolarising the membrane and facilitating Ca entry through Ca channels. This action depends on the amount of existing glucose levels.
Dosage And Administration
Initial dose: 120 mg orally 3 times a day before meals
Maintenance dose: 60 to 120 mg orally 3 times a day before meals
For patients who are near goal HbA1c when therapy is initiated, therapy should be initiated at 60 mg orally 3 times. May be used as monotherapy, or in combination with metformin or a thiazolidinedione. As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Administration
Take orally 1 to 30 minutes before a meal. Patients who skip a meal should be instructed to skip the dose for that meal
Interaction
CYP2C9 and CYP3A4 inhibitors or inducers may alter metabolism of nateglinide. Increased hypoglycaemic effects with MAOIs, nonselective β-adrenergic blockers, NSAIDs, salicylates. Decreased hypoglycaemic effects with corticosteroids, sympathomimetic agents, thiazide diuretics, thyroid hormones.
Contraindications
IDDM, diabetic ketoacidosis.
Side Effects
Hypoglycaemia, upper respiratory tract infection, back pain, flu-like symptoms, dizziness, arthropathy, diarrhoea, accidental trauma, bronchitis, cough.
Pregnancy And Lactation
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Precautions And Warnings
Patient with adrenal and/or pituitary impairment. Severe renal and moderate to severe hepatic impairment. Pregnancy and lactation.
Overdose Effects
Symptoms: Hypoglycaemia.
Management: Use IV glucose in severe reaction.
Therapeutic Class
Meglitinide Analogues
Use in special populations
Renal Dose Adjustments: No adjustment recommended
Mild hepatic impairment: No adjustment recommended
Moderate to severe hepatic impairment: Use caution
Elderly: No adjustment recommended; however, some individuals may have a greater sensitivity to therapy. Insulin therapy may be temporarily needed in times of fever, infection, trauma, or surgery.
Younger than 18 years: Safety and efficacy have not been established in patients younger than 18 years.
Storage Conditions
Store at 25° C.