Nateglinide; Uses, Dosage, Side Effects, Interactions

Nateglinide; Uses, Dosage, Side Effects, Interactions

Nateglinide is a phenylalanine derivative of the meglitinide class of agents with hypoglycemic activity. Nateglinide, compared to repaglinide, binds with a higher affinity to the SUR1 subunit and with a faster onset of action and a shorter duration of action. This agent is metabolized by the cytochrome P450 isoenzyme CYP2C9, and, to a lesser extent, by CYP3A4. The parent drug and metabolites are mainly excreted in the urine and its half-life is about 1.5 hours. Nateglinide is an oral hypoglycemic agent and amino acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Nateglinide has been linked to rare instances of clinically apparent acute liver injury.

Nateglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to β cells of the pancreas to stimulate insulin release. Nateglinide is an amino acid derivative that induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal.

Mechanism of Action of Nateglinide

Nateglinide activity is dependent on the presence of functioning β cells and glucose. In contrast to sulfonylurea insulin secretatogogues, nateglinide has no effect on insulin release in the absence of glucose. Rather, it potentiates the effect of extracellular glucose on ATP-sensitive potassium channel and has little effect on insulin levels between meals and overnight. As such, nateglinide is more effective at reducing postprandial blood glucose levels than fasting blood glucose levels and requires a longer duration of therapy (approximately one month) before decreases in fasting blood glucose are observed. The insulinotropic effects of nateglinide are highest at intermediate glucose levels (3 to 10 mmol/L) and it does not increase insulin release already stimulated by high glucose concentrations (greater than 15 mmol/L). Nateglinide appears to be selective for pancreatic β cells and does not appear to affect skeletal or cardiac muscle or thyroid tissue.

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Indications of Nateglinide

  • Type 2 Diabetes Mellitus
  • Treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
  • For the treatment of non-insulin dependent-diabetes mellitus in conjunction with diet and exercise.
  • Combination therapy with metformin in type 2 diabetic patients inadequately controlled despite a maximally tolerated dose of metformin alone.
  • Combination therapy with metformin in type 2 diabetic patients inadequately controlled despite a maximally tolerated dose of metformin alone

Contra-Indications of Nateglinide

  • Low blood sugar
  • Pituitary hormone deficiency
  • Decreased function of the adrenal gland
  • Inadequate vitamin B12
  • Excess body acid
  • Extreme loss of body water
  • The habit of drinking too much alcohol
  • Alcohol intoxication
  • Heart attack
  • Suddenly serious symptoms of heart failure
  • Liver problems
  • Recent operation
  • Fever
  • Shock
  • Severe vomiting
  • Severe diarrhea
  • Serious lack of oxygen in the blood
  • Weakened patient
  • Injury
  • Sepsis syndrome
  • X-Ray Study with intravenous iodine contrast agent
  • Kidney disease with a likely reduction in kidney function
  • Acute inflammation of the pancreas
  • Chronic inflammation of the pancreas
  • Moderate to Severe kidney impairment.

Dosage of Nateglinide

Strengths: 60 mg; 120 mg

Diabetes Type 2

  • Initial dose: 120 mg orally 3 times a day before meals
  • Maintenance dose: 60 to 120 mg orally 3 times a day before meals

Side Effects of Nateglinide

Most common

More common

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Less common

  • Abnormal stools
  • bad, unusual, or unpleasant (after) taste
  • change in taste
  • difficulty with moving
  • discoloration of the fingernails or toenails
  • flu-like symptoms
  • joint pain
  • rash
  • a runny nose
  • sneezing
  • stuffy nose
  • swollen joints

Drug Interactions of Nateglinide

Canagliflozin  may interact with following drugs, supplements & may decrease the efficacy of the drug

Pregnancy & Lactation of Nateglinide

FDA Pregnancy Category C


This medication should not be used during pregnancy. If you think you may be pregnant or if you become pregnant while taking this medication, contact your doctor immediately.


It is not known if nateglinide passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.


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