Repaglinide


Concise Prescribing Info
Indications/Uses
Type 2 diabetes mellitus
Dosage/Direction for Use
Adult : PO As monotherapy or combined with metformin: Initial: 0.5 mg. Patient transferring from another hypoglycaemic agent: Initial: 1mg. All doses taken 30 minutes before each main meal. May adjust dose at intervals of 1-2 weeks, up to max 4 mg/dose. Max: 16 mg/day.
Dosage Details
Oral
Type 2 diabetes mellitus
Adult: As monotherapy or in combination with metformin: Initially, 0.5 mg. Patient transferring from another hypoglycaemic agent: Initially, 1mg. All doses taken 30 minutes before each main meal. May adjust dose at intervals of 1-2 weeks, up to max 4 mg per dose. Max: 16 mg daily.
Renal Impairment
Severe CrCl 20-40 mL/min: Initially, 0.5 mg before meals, adjust according to patient’s requirement.
Administration
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. Concomitant use with gemfibrozil.
Special Precautions
Hepatic and severe renal impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Severe hypoglycaemia, acute coronary syndrome (e.g. MI).
Gastrointestinal disorders: Abdominal pain, diarrhoea.
Musculoskeletal and connective tissue disorders: Arthralgia, back pain.
Nervous system disorders: Headache.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, sinusitis, bronchitis.
Patient Counseling Information
This drug may cause dizziness due to hypoglycaemia, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor FBS periodically and during dose adjustment; HbA1C at least twice yearly.
Overdosage
Symptoms: Hypoglycaemic reactions (e.g. dizziness, sweating, tremor, headache, seizure, loss of consciousness or coma). Management: Mild hypoglycaemic symptoms without loss of consciousness or neurologic findings may be treated with oral glucose and adjustments in drug dosage and/or meal patterns. Severe hypoglycaemia should be treated with IV glucose. Closely monitor patient for a minimum of 24-48 hours.
Drug Interactions
Increased metabolism with CYP3A4 inducers (e.g. rifampicin, barbiturates, carbamazepine). Enhanced effect with NSAIDs and other highly protein bound drugs (e.g. salicylates, sulphonamides, phenylbutazone, oral anticoagulants and hydantoins). Increased plasma concentration with ketoconazole, fluconazole, itraconazole and erythromycin.
Potentially Fatal: Enhanced and prolonged effect with gemfibrozil.
Action
Description: Repaglinide is a short-acting meglitinide analogue which lowers blood glucose by blocking ATP-dependent K channels in the β-cell membrane resulting to depolarisation. This leads to the opening of Ca channels. The resulting Ca influx stimulates the release of insulin from the pancreatic β-cells.
Pharmacokinetics:
Absorption: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: Approx 56%. Time plasma peak concentration: Within 1 hour.
Distribution: Volume of distribution: 31 L. Plasma protein binding: >98% to albumin.
Metabolism: Extensively metabolised in the liver by the CYP3A4 and CYP2C8 via oxidation; further metabolised by uridine diphosphate glucuronosyltransferase 1A1 (UGT1AI) enzyme via glucuronidation.
Excretion: Via faeces (approx 90%, <2% as unchanged drug); urine (approx 8%, 0.1% as unchanged drug). Elimination half-life: Approx 1 hour.
Chemical Structure

Chemical Structure Image
Repaglinide

Source: National Center for Biotechnology Information. PubChem Database. Repaglinide, CID=65981, https://pubchem.ncbi.nlm.nih.gov/compound/Repaglinide (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C. Protect from moisture.
MIMS Class
ATC Classification
A10BX02 - repaglinide ; Belongs to the class of other blood glucose lowering drugs excluding insulins. Used in the treatment of diabetes.
References
Anon. Repaglinide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 16/11/2018.

Anon. Repaglinide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 16/11/2018.

Buckingham R (ed). Repaglinide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/11/2018.

Joint Formulary Committee. Repaglinide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/03/2019.

Repaglinide (Sandoz Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 16/11/2018.

Disclaimer: This information is independently developed by MIMS based on Repaglinide from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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