Nateglinide
Generic Name: Nateglinide
Brand Names: Starlix
Nateglinide is a fast-acting meglitinide taken before meals to reduce post-meal blood sugar spikes in type 2 diabetes.
Drug Class
Meglitinide (Phenylalanine Derivative)
Pregnancy
Category C — Animal studies have shown adverse fetal effects. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Available Forms
Tablet
What It's Used For
Dosage Quick Reference
These are general dosage guidelines. Your doctor will determine the appropriate dose for your specific situation.
| Condition | Starting Dose | Maintenance Dose |
|---|---|---|
| Type 2 Diabetes (Monotherapy) | 120 mg three times daily before meals | 120 mg three times daily before meals |
| Type 2 Diabetes (Near goal A1C) | 60 mg three times daily before meals | 60 mg three times daily before meals |
Side Effects
Common Side Effects:
- Upper respiratory tract infection
- Dizziness
- Flu-like symptoms
- Diarrhea
- Back pain
- Arthropathy
Serious Side Effects:
- Hypoglycemia (especially with missed meals, exercise, or alcohol)
- Hypersensitivity reactions (rash, urticaria)
- Elevated liver enzymes (rare)
Drug Interactions
Major Interactions:
- Gemfibrozil — Inhibits CYP2C9 metabolism of nateglinide, significantly increasing nateglinide levels and the risk of prolonged hypoglycemia; avoid concurrent use
- Other antidiabetic agents (e.g., sulfonylureas, insulin) — Additive hypoglycemic effect; increased risk of severe hypoglycemia when combined
- Beta-blockers (e.g., propranolol, metoprolol) — May mask symptoms of hypoglycemia such as tachycardia and tremor, making it harder to recognize low blood sugar episodes
- Corticosteroids (e.g., prednisone) — May antagonize blood glucose–lowering effects, requiring dose adjustment of nateglinide
- CYP2C9 inhibitors (e.g., fluconazole, amiodarone) — May increase nateglinide plasma concentrations and hypoglycemia risk; monitor blood glucose closely
Additional Information
Nateglinide is a rapid-acting insulin secretagogue (meglitinide class) used to improve glycemic control in adults with type 2 diabetes mellitus. By stimulating insulin release in response to meals, it specifically targets postprandial glucose excursions.
Mechanism of Action
Nateglinide stimulates insulin secretion from pancreatic beta cells:
- Binds to and closes ATP-sensitive potassium channels on beta cell membranes
- Causes depolarization of the cell membrane
- Opens voltage-dependent calcium channels
- Increased intracellular calcium triggers insulin exocytosis
The insulin secretion is glucose-dependent and more rapid but shorter-acting than sulfonylureas. This results in meal-time insulin release that mimics physiological patterns.
Available Formulations
Nateglinide is available as oral tablets:
- 60 mg tablets
- 120 mg tablets
Tablets should be taken 1-30 minutes before meals.
Medical Uses
FDA-Approved Indication:
- Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus
May be used as:
- Monotherapy
- In combination with metformin or thiazolidinediones
Not indicated for combination with sulfonylureas due to similar mechanisms.
Dosing Guidelines
Adults:
- Starting dose: 120 mg three times daily before meals
- Patients near HbA1c goal: May start with 60 mg three times daily
- Take 1-30 minutes before meals
- Skip dose if skipping a meal
Timing: The rapid onset and short duration are designed for preprandial (before meal) dosing. Do not take if meal is not consumed.
Important Safety Information
Contraindications:
- Type 1 diabetes mellitus
- Diabetic ketoacidosis
- Known hypersensitivity to nateglinide
Warnings and Precautions:
- Hypoglycemia: Risk increases with irregular meal patterns, strenuous exercise, alcohol, or combination with other antidiabetics
- Hepatic impairment: Use with caution
- Not a substitute for insulin in patients requiring insulin
Hypoglycemia Management: Patients should carry glucose tablets and know symptoms of hypoglycemia.
Drug Interactions
- CYP2C9 inhibitors (fluconazole, amiodarone): May increase nateglinide levels
- CYP2C9 inducers (rifampin): May decrease nateglinide levels
- Other antidiabetics: Additive hypoglycemic effect
- Beta-blockers: May mask hypoglycemia symptoms
- Corticosteroids, thyroid hormones: May reduce glucose-lowering effect
- NSAIDs, salicylates: May enhance glucose-lowering effect
Special Populations
- Hepatic Impairment: Use with caution in moderate to severe impairment
- Renal Impairment: No dose adjustment needed for mild to moderate; use with caution in severe impairment or dialysis
- Elderly: Start conservatively; may be more susceptible to hypoglycemia
- Pregnancy: Category C; not recommended; insulin preferred
- Pediatric: Safety and efficacy not established
Frequently Asked Questions
Questions to Ask Your Doctor
Consider discussing these topics at your next appointment:
- ✓Ask your doctor how to recognize and treat low blood sugar episodes.
- ✓Discuss whether nateglinide can be combined with your other diabetes medications safely.
- ✓Ask how often you should check your blood sugar at home and what your target ranges should be.
- ✓Discuss what your A1C goal should be and how often it should be tested.
Medical Disclaimer: This information is for educational purposes only and should not be considered medical advice. Always consult with your healthcare provider before starting, stopping, or changing any medication. Your doctor can provide personalized recommendations based on your specific health condition and medical history.
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Other medications in the same category
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Understanding Your A1C: What This Number Means for Your Health
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Talk to your doctor or pharmacist about whether Nateglinide is right for you.
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