NSTK · 01.2026Independent supplement reference
NutriStack
Edition 1.0Reviewed May 26, 2026

Repaglinide

Prescription ·Strong evidence ·Reviewed May 2026

Repaglinide is a short-acting oral insulin secretagogue used before meals to improve postprandial glucose control in adults with type 2 diabetes. It can cause hypoglycemia, especially if meals are skipped or when combined with glucose-lowering supplements or interacting drugs. Concomitant gemfibrozil is contraindicated because it markedly increases repaglinide exposure.

What it's good for
  • Lowers postprandial glucose in type 2 diabetes1,2
  • Flexible pre-meal dosing1,2
  • Shorter action than many sulfonylureas
  • Can reduce A1c when used with diet and exercise
What to watch for
  • Hypoglycemia
  • Weight gain
  • Headache
  • Concomitant gemfibrozil use2,3
  • Hypersensitivity to repaglinide1,2

The bottom line

Evidence rating strong. Most-documented uses: lowers postprandial glucose in type 2 diabetes, flexible pre-meal dosing, shorter action than many sulfonylureas. 3 sources indexed (2000–2026), with 3 interaction records on file.

The science

How it works, mechanistically.

Core mechanism

Repaglinide binds ATP-dependent potassium channels on pancreatic beta cells, causing membrane depolarization, calcium influx, and meal-timed insulin release. It is metabolized mainly by CYP2C8 and CYP3A4 and transported partly by hepatic uptake pathways, so inhibitors can increase hypoglycemia risk and inducers can reduce efficacy. Its short duration is why it is dosed before meals and skipped when a meal is skipped.1,2

Class
Meglitinide insulin secretagogue
Absorption
Water-soluble; take with food
Dosing

Dosing & protocol.

Common range
0.5-4 mg orally before meals, usually 2-4 times daily; maximum 16 mg/day; skip dose if meal is skipped
Recommended form
Oral tablet taken within 30 minutes before meals

Take before meals; skip the dose if a meal is skipped to reduce hypoglycemia risk.

Safety

Full safety detail.

Side effects

  • Hypoglycemia
  • Weight gain
  • Headache
  • Upper respiratory infection
  • Nausea
  • Diarrhea
  • Arthralgia
  • Rare severe hepatic dysfunction

Contraindications

  • Concomitant gemfibrozil use2,3
  • Hypersensitivity to repaglinide1,2
  • Type 1 diabetes or diabetic ketoacidosis1
  • Use with caution in hepatic impairment, older adults, inconsistent meal intake, or hypoglycemia unawareness
Interactions

Interaction records.

ModerateCaution

Berberine

Berberine may lower glucose and add to the glucose-lowering effects of Repaglinide, increasing hypoglycemia risk.

Recommendation: Increase glucose monitoring when starting, stopping, or changing the supplement; coordinate diabetes medication adjustments with the prescriber.

ModerateCaution

Alpha-Lipoic Acid

Alpha-Lipoic Acid may lower glucose and add to the glucose-lowering effects of Repaglinide, increasing hypoglycemia risk.

Recommendation: Increase glucose monitoring when starting, stopping, or changing the supplement; coordinate diabetes medication adjustments with the prescriber.

SeriousCaution

St. John's Wort

St. John's Wort can induce drug-metabolizing enzymes and transporters and may lower Repaglinide exposure or undermine therapy.

Recommendation: Avoid starting or stopping St. John's Wort without prescriber review while taking Repaglinide.

Sources

Sources, by evidence tier.

Numbered references. Citations throughout the page link here.

Reviews & position papers

1
  • 1Repaglinide: a review of its therapeutic use in type 2 diabetes mellitusNeeds reviewNo linkScott LJ et al. · Drugs · 2000

    Review summarized meal-time insulin secretagogue efficacy and safety.

Reference material

2
  • 2Repaglinide tablets US prescribing informationNeeds reviewNo linkUS Food and Drug Administration · DailyMed FDA Label · 2026

    Label lists gemfibrozil contraindication and glucose monitoring needs.

  • 3Gemfibrozil greatly increases plasma concentrations of repaglinideNeeds reviewNo linkNiemi M et al. · Clinical Pharmacology and Therapeutics · 2003

    Gemfibrozil increased repaglinide exposure and hypoglycemia risk.

Keep exploring

Deep dives & adjacent profiles.

This page is educational. Do not start, stop, or change a supplement or medication based on it without checking with a qualified healthcare professional.

Use this with your stack

Repaglinide in NutriStack.

Add it to your stack, see how it interacts with everything else you take, and get a Stack Score that updates the moment it does.

NutriStack is an informational and organizational tool, not a medical service, and not a substitute for professional advice. Always consult a qualified healthcare professional before starting, stopping, or changing any supplement or medication.