What is repaglinide, and how does it work (mechanism of action)?

Repaglinide is an oral medication for lowering blood sugar (glucose) in individuals with type 2 diabetes. It is in a class of drugs for treating diabetes type 2 called meglitinides that are chemically unlike other anti-diabetic medications. Nateglinide (Starlix), is another currently available meglitinide. Approximately 90% of patients with diabetes have type 2 or non-insulin dependent diabetes mellitus. Type 2 diabetes usually occurs in adulthood, and is associated with obesity, and a strong family history of diabetes. Glucose intolerance that causes diabetes type 2 is caused by reduced insulin secretion from the pancreas after meals and resistance of the body’s cells to insulin’s effect which is to stimulate the cells to remove glucose from the blood. This leads to high levels of glucose in the blood.

Like sulfonylureas, for example, glyburide (Diabeta, Glynase), glipizide (Glucotrol, Glucotrol XL), glimepiride (Amaryl), tolbutamide and tolazamide, repaglinide stimulates cells in the pancreas to produce insulin. Glyburide may be more potent than repaglinide at increasing insulin release in persons with low or high blood glucose levels, whereas repaglinide may be more potent in persons with more moderate abnormalities of blood glucose levels. Repaglinide is different because it has a rapid onset of action and a short duration of action. When taken just prior to meals, it promotes the release of insulin that normally occurs with meals and is responsible for preventing blood glucose levels from becoming high. It has been shown to lower hemoglobin A1c (HbA1c) levels by 1.6% to 1.9%. (Hemoglobin A1c is a blood test which measures the effectiveness of a drug in controlling high blood glucose levels over prolonged periods of time; the lower the hemoglobin A1c, the better the control.) Repaglinide was approved by the FDA in 1997.

What brand names are available for repaglinide?


Is repaglinide available as a generic drug?


Do I need a prescription for repaglinide?


What are the side effects of repaglinide?

Hypoglycemia (low blood glucose) is the most frequent side effect and it occurs somewhat less frequently with repaglinide than with sulfonylureas such as glyburide and glipizide. Some symptoms of hypoglycemia include:

Other common side effects include:

Side effects that have been reported post-marketing inlcude:

What is the dosage for repaglinide?

Repaglinide is taken 15 to 30 minutes before a meal. It should be taken with meals and may be administered 2, 3, or 4 times a day.

  • For patients with HbA1c < 8% who are receiving treatment for the first time the starting dose is 0.5 mg with each meal.
  • Patients who have been treated with other diabetes drugs and whose HbA1c is ≥ 8% should start with 1 or 2 mg with each meal.
  • The initial dose may be doubled at weekly intervals until the desired response is achieved or the maximum dose of 4 mg with each meal (16 mg daily) is achieved.

Which drugs or supplements interact with repaglinide?

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Is repaglinide safe to take if I’m pregnant or breastfeeding?

No adequate human studies on the effects of repaglinide on the fetus have been done. Adverse effects have been reported in some animal studies. Animals given repaglinide during both lactation (nursing) and gestation (pregnancy) have developed skeletal defects. Therefore, physicians must weigh the potential benefits and risks of this medication when considering its use in pregnant women.

It is not known whether repaglinide accumulates in breast milk. However, animals given repaglinide during pregnancy and lactation have developed skeletal defects. Because of the possibility of hypoglycemia in nursing infants and the skeletal effects in nursing animals, it is recommended that repaglinide not be used in women who are breastfeeding.

What else should I know about repaglinide?

What preparations of repaglinide are available?

Tablets: 0.5, 1, and 2 mg.

How should I keep repaglinide stored?

Tablets should be stored at room temperature, below 25 C (77 F).

Medically Reviewed on 3/27/2019


Medically reviewed by John P. Cunha, DO, FACOEP; Board Certified Emergency Medicine


FDA Prescribing Information