Repaglinide

Repaglinide lowers blood glucose levels by stimulating the release of insulin from the pancreas. This action is dependent upon functioning beta (ß) cells in the pancreatic islets.

• Repaglinide tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitation of Use: Repaglinide tablets should not be used in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.ICD-10: E10.9, E11.9

• Repaglinide tablets are contraindicated in patients with: Concomitant use of gemfibrozil [see Drug Interactions (7) ] Known hypersensitivity to repaglinide or any inactive ingredients Concomitant use with gemfibrozil (4) Known hypersensitivity to repaglinide or any inactive ingredients (4)contraindicated

The recommended starting dose is 0.5 mg orally before each meal if HbA1c is less than 8%; and 1 or 2 mg orally before each meal if HbA1c is 8% or greater. (2.1) The recommended dose range is 0.5 mg to 4 mg before meals, with a maximum daily dose of 16 mg. (2.1) The patient’s dose should be doubled up to 4 mg with each meal until satisfactory glycemic control is achieved. At least one week should elapse to assess response after each dose adjustment. (2.1) Instruct patients to skip the dose of repaglinide tablets if a meal is skipped. In patients who experience hypoglycemia, the dose of repaglinide tablets should be reduced. (2.1 ; 5.1) Instruct patients to take repaglinide tablets within 30 minutes before meals. (2.1) In patients with severe renal impairment (CrCl = 20 to 40 mL/min), recommended starting dose is 0.5 mg orally before each meal. (2.2) Dose modifications are required when used concominantly with some medications. (2.3 , 7) 2.1 Recommended Dosage and Administration The recommended starting dose for patients whose HbA 1c is less than 8% is 0.5 mg orally before each meal. For patients whose HbA 1c is 8% or greater the starting dose is 1 mg or 2 mg orally before each meal. The recommended dose range is 0.5 mg to 4 mg before meals, with a maximum daily dose of 16 mg. The patient’s dose should be doubled up to 4 mg with each meal until satisfactory glycemic control is achieved. At least one week should elapse to assess response after each dose adjustment. Instruct patients to take repaglinide tablets within 30 minutes before meals.

Hypoglycemia : Repaglinide may cause hypoglycemia. Skip the scheduled dose of repaglinide if a meal is skipped to reduce the risk of hypoglycemia. Reduce the dose of repaglinide if hypoglycemia occurs. (5.1) Serious Cardiovascular Adverse Reactions with Concomitant NPH-insulin : Repaglinide is not indicated for use in combination with NPH-insulin. (5.2) Macrovascular outcomes : There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with repaglinide. (5.3) 5.1 Hypoglycemia All glinides, including repaglinide, can cause hypoglycemia [see Adverse Reactions (6.1) ] . Severe hypoglycemia can cause seizures, may be life-threatening, or cause death. Hypoglycemia can impair concentration ability and reaction time; this may place an individual and others at risk in situations where these abilities are important (e.g., driving or operating other machinery). Hypoglycemia can happen suddenly and symptoms may differ in each individual and change over time in the same individual. Symptomatic awareness of hypoglycemia may be less pronounced in patients with longstanding diabetes, in patients with diabetic nerve disease, in patients using medications that block the sympathetic nervous system (e.g., beta-blockers) [see Drug Interactions (7) ] , or in patients who experience recurrent hypoglycemia.

The following serious adverse reaction is also described elsewhere in the labeling: Hypoglycemia [see Warnings and Precautions (5.1) ] The most common adverse reactions (5% or greater incidence) among patients treated with repaglinide were: hypoglycemia, upper respiratory infection, headache, sinusitis, arthralgia, nausea, diarrhea, and back pain. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Rising Health, LLC at 1-833-395-6928 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying designs, the adverse reaction rates reported in one clinical trial may not be easily compared to those rates reported in another clinical trial, and may not reflect the rates actually observed in clinical practice. Repaglinide has been administered to 2931 individuals during clinical trials. Approximately 1500 of these individuals with type 2 diabetes have been treated for at least 3 months, 1000 for at least 6 months, and 800 for at least 1 year. The majority of these individuals (1228) received repaglinide in one of five 1-year, active-controlled trials. Over one year, 13% of repaglinide patients were discontinued due to adverse reactions. The most common adverse reactions leading to withdrawal were hyperglycemia, hypoglycemia, and related symptoms. Table 1 lists the common adverse reactions for repaglinide patients compared to placebo in trials 12 to 24 weeks duration.

Lactation: Repaglinide is not recommended when breastfeeding (8.2) 8.1 Pregnancy Risk Summary Limited available data from case reports and case series with repaglinide use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with poorly controlled diabetes in pregnancy (see Clinical Considerations) . Teratogenicity was not observed in rats and rabbits administered repaglinide during organogenesis at approximately 60 and 1 times the maximum daily clinical dose, based on body surface area. No adverse developmental effects were observed in offspring of rats administered repaglinide during late gestation and lactation at approximately 4 times the maximum daily clinical dose (see Data). The estimated background risk of major birth defects is 6 to 10% in women with pre-gestational diabetes with a HbA1c>7 and has been reported to be as high as 20 to 25% in women with a HbA1c>10. The estimated background risk of miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Metabolism

The pharmacokinetic parameters of repaglinide obtained from a single-dose, crossover study in healthy subjects and from a multiple-dose, parallel, dose-proportionality (0.5, 1, 2 and 4 mg) study in patients with type 2 diabetes are summarized in Tables 5 and 6. These data indicate that repaglinide did not accumulate in serum.

Severe hypoglycemic reactions with coma, seizure, or other neurological impairment may occur and constitute medical emergencies requiring immediate hospitalization. Hypoglycemic symptoms without loss of consciousness or neurologic findings should be treated aggressively with oral glucose and adjustments in drug dosage and/or meal patterns. Close monitoring may continue until the physician is assured that the patient is out of danger. Patients should be closely monitored for a minimum of 24 to 48 hours, since hypoglycemia may recur after apparent clinical recovery. There is no evidence that repaglinide is dialyzable using hemodialysis.

• Nov 22, 2013ANDAANDA078555Chartwell Rx
• Jan 22, 2014ANDAANDA203820Aurobindo Pharma Ltd
• Mar 22, 2023ANDAANDA207209Macleods Pharms Ltd

1. 1Hypoglycaemia78011%
2. 2Acute Kidney Injury5497.5%
3. 3Drug Interaction4225.8%
4. 4Diarrhoea3725.1%
5. 5Lactic Acidosis3655.0%
6. 6Dyspnoea2823.9%
7. 7Nausea2653.6%
8. 8Asthenia2553.5%
9. 9Anaemia2453.4%
10. 10Vomiting2393.3%
11. 11Off Label Use2333.2%
12. 12Fall2313.2%
13. 13Fatigue2193.0%
14. 14Blood Glucose Increased2092.9%
15. 15Drug Ineffective1952.7%

The 10 most recently updated of 92 ClinicalTrials.gov registrations naming Repaglinide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Study of IDE196 in Patients With Solid Tumors Harboring GNAQ/11 Mutations or PRKC Fusions
  Recruiting · Phase 1 · Phase 2 · Interventional · 336 enrolled · IDEAYA Biosciences
  NCT03947385updated 2026-06-08
• A Study of Neladalkib (NVL-655) in Patients With Advanced NSCLC and Other Solid Tumors Harboring ALK Rearrangement or Activating ALK Mutation (ALKOVE-1)
  Recruiting · Phase 1 · Phase 2 · Interventional · 840 enrolled · Nuvalent Inc.
  NCT05384626updated 2026-05-27
• A Study in Healthy Men and Women to Test Whether BI 1569912 Influences the Amount of Repaglinide, Midazolam and Bupropion in the Blood
  Completed · Phase 1 · Interventional · 18 enrolled · Boehringer Ingelheim
  NCT06367153updated 2026-05-22
• Pharmacokinetic Effect of Y-3 on Repaglinide，Warfarin and Omeprazole in Healthy Participants
  Completed · Phase 1 · Interventional · 24 enrolled · Neurodawn Pharmaceutical Co., Ltd.
  NCT07068841updated 2026-05-22
• To Determine the Effect of CYP Induction Following Administration of Nirogacestat in Healthy Adult Male Participants
  Completed · Phase 1 · Interventional · 20 enrolled · SpringWorks Therapeutics, Inc., a healthcare company of Merck KGaA, Darmstadt, Germany
  NCT07259330updated 2026-05-01
• A Drug-drug Interaction Study to Evaluate the Effects of Pelabresib on the Pharmacokinetics of Repaglinide, Midazolam, and Combined Oral Contraceptive in Patients With Advanced Malignancies
  Not yet recruiting · Phase 1 · Interventional · 24 enrolled · Novartis Pharmaceuticals
  NCT07340190updated 2026-04-02
• A Drug Drug Interaction Study to Evaluate the Effect of VCT220 on the Pharmacokinetics of Repaglinide, Rosuvastatin, and Digoxin in Healthy, Overweight, and Obese Subjects
  Completed · Phase 1 · Interventional · 24 enrolled · Vincentage Pharma Co., Ltd
  NCT07065058updated 2026-03-31
• A Study to Investigate the Effects of Multiple Doses of Rezatapopt on the Pharmacokinetics of Metformin, Rosuvastatin, Repaglinide, and Midazolam in Patients With Advanced Solid Tumors Harboring a TP53 Y220C Mutation.
  Recruiting · Phase 1 · Interventional · 14 enrolled · PMV Pharmaceuticals, Inc
  NCT07372625updated 2026-03-12
• KF2022#4-trial: Effects of a Beta Blocker and NSAID on CYP Mediated Drug Metabolism
  Completed · Interventional · 12 enrolled · Helsinki University Central Hospital
  NCT06566794updated 2026-03-06
• A Pragmatic Randomized Trial to Evaluate the Comparative Effectiveness Between Dapagliflozin and Standard of Care in Type 2 Diabetes Patients
  Completed · Phase 4 · Interventional · 632 enrolled · University of Liverpool
  NCT02616666updated 2026-02-20

Frequently asked questions

How does Repaglinide work?

Repaglinide lowers blood glucose levels by stimulating the release of insulin from the pancreas. This action is dependent upon functioning beta (ß) cells in the pancreatic islets.

What is Repaglinide used for?

According to FDA labeling, Repaglinide carries indications including: Repaglinide tablets are indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitation of Use: Repaglinide tablets should not be used in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Repaglinide?

Repaglinide is classified as Other blood glucose lowering drugs, excl. insulins, Glinide, Insulin Receptor Agonists, Potassium Channel Antagonists, Increased Insulin Secretion.

What are the contraindications for Repaglinide?

Repaglinide labeling lists contraindications including: Repaglinide tablets are contraindicated in patients with: Concomitant use of gemfibrozil [see Drug Interactions (7) ] Known hypersensitivity to repaglinide or any inactive ingredients Concomitant use with gemfibrozil (4) Known hypersensitivity to repaglinide or any inactive ingredients (4). Always consult the full prescribing information and a clinician.