Ruilian Repaglinide Tablets

1. Indications and Usage
Glycemic Control: Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Combination Therapy: Can be used in combination with metformin.
Restrictions: Contraindicated in patients with type 1 diabetes mellitus or diabetic ketoacidosis.
2. Dosage and Administration
Starting Dose: The recommended starting dose is 0.5 mg taken orally 15 minutes before each main meal (three times daily).
Titration: The dose can be increased by 0.5 mg to 1 mg increments every 1-2 weeks based on glycemic response. The maximum recommended single dose is 4 mg, and the maximum daily dose is 16 mg.
Missed Dose: If a meal is skipped or a dose is taken after eating, it should be omitted to reduce the risk of hypoglycemia.
3. Mechanism of Action
Insulin Secretion: Repaglinide stimulates insulin secretion from pancreatic beta cells.
Target Protein: It acts by binding to the sulfonylurea receptor 1 (SUR1) subunit of the ATP-dependent potassium channel.
Glucose-Dependent Effects: It accelerates the closure of potassium channels, leading to depolarization and calcium influx, thereby promoting rapid insulin release in response to food intake.
4. Safety and Warnings
Hypoglycemia: There is a risk of hypoglycemia, particularly if meals are delayed or skipped.
Hepatic Impairment: Use is not recommended in patients with hepatic dysfunction or a history of liver disease.
Renal Impairment: Use with caution in patients with renal dysfunction, although it is primarily metabolized by the liver.
Hypersensitivity: Do not use in patients with known hypersensitivity to repaglinide or related compounds.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: Hypoglycemia, hypoglycemic symptoms (sweating, palpitations), and gastrointestinal disturbances (nausea, abdominal pain).
Liver Function: Elevations in liver enzymes (AST, ALT) have been reported.
Other Adverse Effects: Visual disturbances, rash, pruritus, and abnormal hematological findings may occur rarely.
Clinical Findings: Clinical trials have demonstrated significant reductions in postprandial glucose levels and HbA1c.
6. Drug Interactions
CYP3A4 and CYP2C8 Inhibitors: Strong inhibitors (e.g., gemfibrozil, ketoconazole, clarithromycin) may significantly increase repaglinide exposure and the risk of hypoglycemia.
CYP3A4 and CYP2C8 Inducers: Strong inducers (e.g., rifampin, St. John’s wort) may decrease repaglinide exposure, reducing its efficacy.
Hypoglycemic Agents: Concomitant use with other antidiabetic agents may increase the risk of hypoglycemia.
7. Pharmaceutical Information
Active Ingredient: Repaglinide.
Strengths: Typically available as 0.5 mg, 1 mg, and 2 mg tablets.
Appearance: White to off-white tablets.
Storage: Store at controlled room temperature (20°C to 25°C) in a dry place, protected from light and moisture.