REPAGLINIDE

Other

Brand names: Repaglinide

Oral

Mechanism of Action

12.1 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.

Indications

See full prescribing information

FDA Warnings

5 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
1) Serious Cardiovascular Adverse Reactions with Concomitant NPH-insulin : Repaglinide is not indicated for use in combination with NPH-insulin
2) Macrovascular outcomes : There have been no clinical studies establishing conclusive evidence of macrovascular risk reduction with repaglinide

Known Side Effects

7 documented side effects by frequency

Diarrhea

1-10%

Shortness of Breath

1-10%

Nausea

1-10%

Weakness

1-10%

Vomiting

0.1-1%

Falls

0.1-1%

Fatigue

0.1-1%

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Formulations

Dosage Forms

Tablet

Route

Oral