Nateglinide


Generic Medicine Info
Indications and Dosage
Oral
Type 2 diabetes mellitus
Adult: 60 or 120 mg tid. Max: 180 mg tid.
Administration
Should be taken with food. Take immediately before or up to 30 min before meals.
Contraindications
IDDM, diabetic ketoacidosis.
Special Precautions
Patient w/ adrenal and/or pituitary impairment. Severe renal and moderate to severe hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Hypoglycaemia, upper resp tract infection, back pain, flu-like symptoms, dizziness, arthropathy, diarrhoea, accidental trauma, bronchitis, cough.
Monitoring Parameters
Monitor wt, lipid profile; fasting blood glucose and glycosylated Hb (HbA1c) levels.
Overdosage
Symptoms: Hypoglycaemia. Management: Use IV glucose in severe reaction.
Drug Interactions
CYP2C9 and CYP3A4 inhibitors or inducers may alter metabolism of nateglinide. Increased hypoglycaemic effects w/ MAOIs, nonselective β-adrenergic blockers, NSAIDs, salicylates. Decreased hypoglycaemic effects w/ corticosteroids, sympathomimetic agents, thiazide diuretics, thyroid hormones.
Food Interaction
Delayed absorption w/ food. Decreased serum concentration w/ St John's wort. Increased hypoglycaemic effects w/ alcohol.
Action
Description:
Mechanism of Action: 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.
Onset: Approx 20 min.
Duration: 4 hr.
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI tract. Food delays absorption. Bioavailability: 73%. Time to peak plasma concentration: W/in 1 hr.
Distribution: Volume of distribution: 10 L. Plasma protein-binding: 98%, primarily to albumin.
Metabolism: Hepatic metabolism via hydroxylation followed by glucuronide conjugation by CYP2C9 and CYP3A4 (lesser extent) isoenzymes.
Excretion: Mainly via urine (as unchanged drug and metabolites) and faeces (approx 10%). Elimination half-life: Approx 1.5 hr.
Chemical Structure

Chemical Structure Image
Nateglinide

Source: National Center for Biotechnology Information. PubChem Database. Nateglinide, CID=5311309, https://pubchem.ncbi.nlm.nih.gov/compound/Nateglinide (accessed on Jan. 22, 2020)

Storage
Store at 25°C.
MIMS Class
Antidiabetic Agents
ATC Classification
A10BX03 - nateglinide ; Belongs to the class of other blood glucose lowering drugs excluding insulins. Used in the treatment of diabetes.
References
Anon. Nateglinide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/10/2015.

Buckingham R (ed). Nateglinide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/10/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Nateglinide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 14/10/2015.

Nateglinide Tablet (Dr. Reddy’s Laboratories Limited) . DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 14/10/2015.

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