Repaglinide is indicated as an additional treatment along with diet and exercise to reduce blood glucose levels in patients with type 2 diabetes mellitus (NIDDM) whose blood sugar cannot be adequately controlled by diet and exercise alone. It is also used in combination with Metformin for patients whose hyperglycemia is not properly controlled by diet, exercise, and either Repaglinide or Metformin alone.

Repaglinide is an oral antidiabetic medicine belonging to the meglitinide class, used for the management of type 2 diabetes mellitus (NIDDM). It works by stimulating the pancreas to release more insulin into the bloodstream. It has a rapid onset of action and is eliminated from the body quickly.

Repaglinide binds to specific receptors on the cell membrane of pancreatic beta cells, leading to the closure of ATP-dependent potassium (K⁺) channels and depolarization of the cell membrane. This causes calcium (Ca²⁺) influx into the cells, increases intracellular calcium levels, and stimulates the release of insulin.

• For patients not previously treated or whose HbA1c is <8%, the starting dose should be 0.5 mg before each meal.
• For patients previously treated with blood glucose-lowering drugs and whose HbA1c is >8%, the initial dose is 1 or 2 mg before each meal.
• Repaglinide should be taken immediately or up to 30 minutes before each meal.
• Dosage should be adjusted according to response at intervals of 1-2 weeks; up to 4 mg may be given as a single-dose, maximum 16 mg daily.

Cytochrome P450 inhibitors: Co-administration of Repaglinide with

• inhibitors of the CYP450 enzyme system (e.g. azole antifungals and macrolide antibiotics) may reduce Repaglinide clearance and prolong its half-life, thereby increasing its glucose-lowering effect and risk of hypoglycaemia.
• Cytochrome P450 inducers: Drugs such as Rifampin, Phenobarbital, Carbamazepine, Troglitazone, etc. may induce CYP enzymes, leading to increased metabolism of Repaglinide, reduced plasma concentration, and decreased therapeutic effect.
• Cimetidine: Does not significantly affect the absorption or clearance of Repaglinide.
• Other drugs: Repaglinide does not significantly affect Digoxin, Theophylline, or Warfarin. Highly protein-bound drugs (e.g. NSAIDs) may increase free Repaglinide levels and enhance its hypoglycaemic effect.
• Additional interactions: Risk of hypoglycaemia may increase when Repaglinide is used with salicylates, sulphonamides, Chloramphenicol, coumarins, Probenecid, monoamine oxidase (MAO) inhibitors, and adrenergic blockers.

Repaglinide is contraindicated in patients with:

• Diabetic ketoacidosis, with or without coma
• Type 1 diabetes mellitus
• Known hypersensitivity to Repaglinide or any of its inactive ingredients

The most common adverse effect is hypoglycaemia and related symptoms. Other reported effects include upper respiratory tract infection, diarrhoea, constipation, nausea, and vomiting. Hypersensitivity reactions such as skin rash and urticaria may also occur.

Safety in pregnancy has not been established. Repaglinide should be used during pregnancy only if clearly needed. It is not known whether it is excreted in human milk. Because many drugs are excreted in breast milk and due to potential adverse effects in nursing infants, a decision should be made whether to discontinue breastfeeding or the drug, considering the importance of treatment for the mother.

Insulin therapy should be used in situations such as severe illness (myocardial infarction, coma, infection, trauma) and during surgery. All oral glucose-lowering agents may cause hypoglycaemia. Repaglinide should be taken with meals to reduce the risk of hypoglycaemia.

Doses up to 80 mg have been associated mainly with excessive blood glucose lowering. Hypoglycaemia was generally prevented when meals were taken. Severe hypoglycaemia with coma, seizures, or neurological impairment is rare.

Meglitinide Analogues

Do not store above 30°C. Keep away from light and out of reach of children.