Repaglinide

What it is and how it works

Mechanism of Action 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. Insulin release is glucose-dependent and diminishes at low glucose concentrations. Repaglinide closes ATP-dependent potassium channels in the ß-cell membrane by binding at characterizable sites. This potassium channel blockade depolarizes the ß-cell, which leads to an opening of calcium channels. The resulting increased calcium influx induces insulin secretion. The ion channel mechanism is highly tissue selective with low affinity for heart and skeletal muscle.

Mechanism class: Potassium Channel Antagonists

Indications

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. Repaglinide tablets are a glinide indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Limitation of Use : Not for treatment of type 1 diabetes mellitus or diabetic ketoacidosis

Dosage and administration (summary)

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. 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 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 .

Contraindications

Repaglinide tablets are contraindicated in patients with: Concomitant use of gemfibrozil Known hypersensitivity to repaglinide or any inactive ingredients Concomitant use with gemfibrozil Known hypersensitivity to repaglinide or any inactive ingredients

Warnings and precautions

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. Serious Cardiovascular Adverse Reactions with Concomitant NPH-insulin : Repaglinide is not indicated for use in combination with NPH-insulin. Macrovascular outcomes : There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with repaglinide. Hypoglycemia All glinides, including repaglinide, can cause hypoglycemia .

Pregnancy

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.

Storage and supply

Repaglinide Tablets USP, 0.5 mg are white to off white, round, biconvex uncoated tablets, debossed with ‘H’ on one side and ‘10’ on other side. NDC: 63629-4866-1: 30 Tablets in a BOTTLE NDC: 63629-4866-2: 90 Tablets in a BOTTLE Store at 20° to 25°C (68° to 77°F) . Protect from moisture. Keep bottles tightly closed.

Source: Repaglinide (Repaglinide) — US FDA prescribing information, 2025-01-16, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.