Type 2 diabetes mellitus
Adult: Usual initial dose: 0.5 mg, taken within 30 minutes of main meals. Initial doses of 1 or 2 mg may be used in patients who have had previous hypoglycaemic treatment. May adjust dose at intervals of 1-2 wk, up to 4 mg before meals. Max dose: 16 mg daily.
Hepatic impairment: May require longer intervals between dosage adjustments.
Diabetic ketoacidosis; severe hepatic impairment, type 1 diabetes; hypersensitivity. Lactation.
Warnings / Precautions
Myocardial infarction, coma, trauma during surgery, elderly, malnourished and debilitated patients. Hepatic or severe renal impairment. Pregnancy.
Adverse Reactions
Hypoglycaemia, nausea, diarrhoea, constipation, vomiting, dyspepsia, arthralgia, sinusitis, rhinitis, back pain; rash, pruritus, urticaria; visual disturbances.
Overdose Reactions
Severe hypoglycaemic reactions with coma, seizure and other neurological impairment may occur.
Drug Interactions
Cytochrome P450 3A4 inducers eg. rifampicin, barbiturates and carbamazepine may increase repaglinide metabolism. NSAIDs and other highly protein bound drugs eg, salicylates, sulphonamides, phenylbutazone, oral anticoagulants and hydantoins may potentiate action of repaglinide. Ketoconazole, fluconazole, itraconazole and erythromycin may increase plasma conc of repaglinide. Antagonistic effect with drugs causing hyperglycaemia. Concurrent use with gemfibrozil may lead to enhanced and prolonged blood glucose lowering effect.
Potentially Fatal: Increased risk of myocardial infarction when used with isophane insulin.
See Below for More repaglinide Drug Interactions
Food Interactions
Absorption may be affected when given with food.
Mechanism of Actions
Repaglinide stimulates release of insulin from pancreatic β-cells by inhibiting K efflux via closure of ATP regulated K channels. This results in depolarization of the cell and opening of voltage-dependent Ca channels, which increases influx of Ca into the beta cells and causes release of insulin.
Absorption: Rapid and complete; peak plasma concentrations after 1 hr (oral).
Distribution: Protein-binding: >98%.
Metabolism: Completely metabolised by oxidative biotransformation and direct conjugation with glucuronic acid.
Excretion: Urine (about 8%); faeces (90%).
Should be taken with food. (Usually taken w/in 15 min of the meal but time may vary from immediately before to 30 min before the meal.)
Storage Conditions
Oral: Store below 25°C. Protect from moisture.
ATC Classification
A10BX02 - repaglinide ; Belongs to the class of other blood glucose lowering drugs excluding insulins. Used in the management of diabetes.
Oral: Store below 25°C. Protect from moisture.
Available As
  • Repaglinide 0.5 mg
  • Repaglinide 1 mg
  • Repaglinide 2 mg
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