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.