What it's for (Indications)
- Repaglinide is indicated for the management of Type II diabetes mellitus, particularly in patients unable to achieve adequate glycemic control with diet and exercise alone, or in combination with metformin.
Dosage Information
| Type | Guideline |
|---|---|
| Standard | The recommended starting dose is 0.5 mg orally before each meal if HbA1c is less than 8%, and 1 mg or 2 mg orally before each meal if HbA1c is 8% or greater. The dose can be doubled up to 4 mg with each meal, with at least one week between adjustments, until satisfactory glycemic control is achieved. The recommended dose range is 0.5 mg to 4 mg before meals, with a maximum daily dose of 16 mg. Patients should take repaglinide within 30 minutes before meals and skip the dose if a meal is skipped. For severe renal impairment (CrCl = 20 – 40 mL/min), the recommended starting dose is 0.5 mg orally before each meal. Dose modifications may be required when used concomitantly with some medications. |
Safety & Warnings
Common Side Effects
- Common adverse reactions include hypoglycemia, upper respiratory infection, headache, sinusitis, arthralgia, nausea, diarrhea, back pain, visual disturbances, upset stomach, and rash.
- Patients should consult their doctor if they experience any of these symptoms.
Serious Warnings
- Hypoglycemia is a major risk, and the dose should be reduced if experienced.
- Patients should consult their doctor before taking repaglinide during pregnancy.
- It should be avoided by breastfeeding women.
- Patients should avoid driving due to potential effects on driving ability and avoid consuming alcohol.
- Regular monitoring of blood glucose levels and glycosylated hemoglobin (HbA1c) is crucial to assess treatment efficacy and maintain normal blood glucose ranges.
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.