Adult: As an adjunct to diet and exercise: As monotherapy or in combination with metformin: Initially, 0.5 mg; may adjust dose at intervals of 1-2 weeks up to a Max of 4 mg/dose before each meal. Usual maintenance dose: 0.5-1 mg before each meal. Max: 16 mg daily. Doses are given within 15 minutes of the meal, but time may vary from immediately preceding the meal to as long as 30 minutes before the meal; may be given preprandially 2, 3 or 4 times/day based on the changes in meal pattern. If a meal is skipped, the dose for that meal should be skipped. Dosage is individualised and adjusted to optimise glycaemic control.
What are the brands available for Repaglinide in Hong Kong?
Repaglinide 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.
Contraindications
Diabetic ketoacidosis (with or without coma); type 1 diabetes mellitus (C-peptide negative). Severe hepatic impairment. Concurrent use with gemfibrozil.
Special Precautions
Patient exposed to stress (e.g. fever, trauma, infection, surgery). Debilitated or malnourished patients. Renal and mild to moderate hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Cardiac disorders: Acute coronary syndrome (e.g. MI), chest pain. Gastrointestinal disorders: Diarrhoea, abdominal pain, nausea. Immune system disorders: Rarely, allergic reactions. Musculoskeletal and connective tissue disorders: Back pain, arthralgia. Nervous system disorders: Headache, dizziness. Renal and urinary disorders: UTI. Respiratory, thoracic and mediastinal disorders: URTI, sinusitis, bronchitis. Potentially Fatal: Severe hypoglycaemia.
This drug may cause hypoglycaemia which may impair ability to concentrate or react; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor fasting plasma glucose and HbA1c.
Overdosage
Symptoms: Severe hypoglycaemia. Management: Give oral glucose and adjust drug dosage and/or meal patterns for hypoglycaemic symptoms without loss of consciousness or neurologic findings. Administer IV glucose in severe cases.
Drug Interactions
May enhance and/or prolong the hypoglycaemic effect with ciclosporin, CYP2C8 inhibitors (e.g. clopidogrel, trimethoprim, deferasirox), CYP3A4 inhibitors (e.g. clarithromycin, erythromycin, itraconazole, ketoconazole), other antidiabetic agents, MAOIs, non-selective β-blockers, ACE inhibitors, salicylates, NSAIDs and octreotide. Concomitant use with oral contraceptives, rifampicin, barbiturates, carbamazepine, thiazides, corticosteroids, danazol, thyroid hormones and sympathomimetics (e.g. salbutamol, terbutaline) may reduce the hypoglycaemic effect of repaglinide. Potentially Fatal: Significantly increased exposure with gemfibrozil.
Food Interaction
May enhance and/or prolong the hypoglycaemic effect with alcohol.
Action
Description: Mechanism of Action: Repaglinide is a short-acting meglitinide antidiabetic agent which blocks ATP-dependent K channels, leading to membrane depolarisation and Ca entry through Ca channels. The resulting increase in intracellular Ca stimulates the release of insulin from the pancreatic β-cells. Pharmacokinetics: Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: 56% ± 9%. Time to peak plasma concentration: Within 1 hour. Distribution: Volume of distribution: 31 L. Plasma protein binding: >98% to albumin. Metabolism: Extensively metabolised in the liver mainly via oxidation by CYP3A4 and CYP2C8 isoenzymes and glucuronidation into inactive metabolites. Excretion: Mainly via faeces (approx 90%, <2% as unchanged drug); urine (approx 8%, 0.1% as unchanged drug). Elimination half-life: Approx 1 hour.
Chemical Structure
Repaglinide Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 65981, Repaglinide. https://pubchem.ncbi.nlm.nih.gov/compound/Repaglinide. Accessed Jan. 28, 2025.
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