Gliclazide


Generic Medicine Info
Indications and Dosage
Oral
Type 2 diabetes mellitus
Adult: As conventional tab: Initially, 40-80 mg daily; may increase as necessary until adequate control is achieved. Max: 320 mg daily. Doses >160 mg daily are given in 2 divided doses. As modified-release tab: Initially, 30 mg daily; may increase in increments of 30 mg at intervals of at least 1 month (or after 2 weeks if no decrease in blood glucose is observed). Max: 120 mg daily. The 80 mg conventional tab is comparable to the 30 mg modified-release tab. Switch may be done with close blood glucose monitoring.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
Should be taken with food.
Contraindications
Hypersensitivity to gliclazide, other sulfonylureas or sulfonamides. Type 1 diabetes mellitus, diabetic coma and pre-coma, diabetic ketoacidosis. Severe hepatic or renal impairment. Pregnancy and lactation. Concomitant use with miconazole.
Special Precautions
Patient with risk factors for hypoglycaemia (e.g. malnourished, severe or poorly compensated endocrine disorders, severe vascular disease), G6PD-deficiency, porphyria, stress-related states (e.g. severe trauma, fever, infection, surgery). Mild to moderate hepatic or renal impairment. Elderly.
Adverse Reactions
Significant: Hypoglycaemia. Rarely, serious skin and hypersensitivity reactions (e.g. rash, pruritus, erythema, urticaria, angioedema, maculopapular rash, bullous reactions [e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis], drug rash with eosinophilia and systemic symptoms [DRESS]).
Blood and lymphatic system disorders: Rarely, reversible anaemia, leucopenia, thrombocytopenia, agranulocytosis.
Eye disorders: Rarely, transient visual disturbances.
Gastrointestinal disorders: Constipation, diarrhoea, nausea, vomiting, epigastric discomfort, abdominal pain, heartburn, dyspepsia.
Hepatobiliary disorders: Rarely, jaundice, cholestasis, hepatitis.
Investigations: Rarely, increased serum creatinine, alkaline phosphatase, ALT, AST, BUN, bilirubin.
Nervous system disorders: Headache.
Patient Counseling Information
This drug may impair concentration or cause transient visual disturbance due to hypoglycaemia, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood glucose, HbA1c (at least twice yearly in patients with stable glycaemic control; quarterly in patients not meeting therapy goals or with changes in treatment), renal and hepatic functions (baseline in all patients then periodically thereafter in patients with mild to moderate impairment). Assess for signs and symptoms of hypoglycaemia.
Overdosage
Symptoms: Hypoglycaemia. Management: For moderate symptoms of hypoglycaemia, without any loss of consciousness or neurological signs: Consider carbohydrate intake, dose adjustment, or change of diet. In case of hypoglycaemic coma, administer a rapid IV inj of 50 mL of concentrated glucose solution (20-30%), followed by continuous infusion of a more dilute glucose solution (10%) at a rate that will maintain blood glucose levels above 1 g/L. Close monitoring is recommended.
Drug Interactions
Increased hypoglycaemic effect with phenylbutazone. Concomitant use with β-blockers, fluconazole, ACE inhibitors (e.g. captopril, enalapril), H2-receptor antagonists, MAOIs, sulfonamides, clarithromycin, NSAIDs and other antidiabetic agents (e.g. insulins, dipeptidyl peptidase-4 inhibitors, glucagon-like peptide-1 receptor agonists, metformin, acarbose, thiazolidinediones) may potentiate the blood glucose lowering effect of gliclazide. Danazol, chlorpromazine (at doses >100 mg daily), glucocorticoids, tetracosactrin, ritodrine, salbutamol, terbutaline, barbiturates, estrogens, and progestogens may reduce blood sugar control with gliclazide by causing increased blood glucose levels. Increased risk of dysglycaemia with fluoroquinolones. May increase the effect of anticoagulants (e.g. warfarin).
Potentially Fatal: Increased hypoglycaemic effect with possible onset of hypoglycaemic symptoms, or even coma with miconazole.
Food Interaction
Increased hypoglycaemic effect with alcohol; avoid concomitant use. Decreased exposure with St. John’s wort.
Action
Description: Gliclazide is an antidiabetic sulfonylurea. It decreases blood glucose levels by increasing insulin sensitivity at peripheral target sites, stimulating insulin release from the β-cells of the islets of Langerhans, and reducing glucose output from the liver. It has haemovascular properties in which it decreases microthrombosis by an action on vascular endothelial fibrinolytic activity with an increase in tissue plasminogen activator (t-PA) activity, and by partial inhibition of platelet aggregation and adhesion.
Duration: 24 hours (modified-release tab).
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract (conventional tab); slow and complete (modified-release tab). Bioavailability: 97% (modified-release tab). Time to peak plasma concentration: 4-6 hours (conventional tab); approx 6 hours (modified-release tab).
Distribution: Distributed to the intracellular fluids. Crosses the placenta. Volume of distribution: 20-40 L. Plasma protein binding: Approx 94-95%.
Metabolism: Extensively metabolised in the liver by CYP2C9 and CYP2C19 isoenzymes to inactive metabolites.
Excretion: Mainly via urine (60-70%, <1% as unchanged drug); faeces (10-20%). Elimination half-life: 10.4 hours (conventional tab); 12-20 hours (modified-release tab).
Chemical Structure

Chemical Structure Image
Gliclazide

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3475, Gliclazide. https://pubchem.ncbi.nlm.nih.gov/compound/Gliclazide. Accessed May 29, 2022.

Storage
Store between 15-30°C.
MIMS Class
Antidiabetic Agents
ATC Classification
A10BB09 - gliclazide ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.
References
Anon. Gliclazide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/04/2022.

Buckingham R (ed). Gliclazide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/04/2022.

Diamicron MR 60 mg (Servier Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 19/05/2022.

Diamicron MR Modified Release Tablet (Les Laboratoires Servier Industrie and Kotra Pharma [M] Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 11/04/2022.

Gliclazide 30 mg Prolonged-release Tablets (Brown & Burk UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 11/04/2022.

Gliclazide 40 mg Tablets (Brown & Burk UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 11/04/2022.

Glyade Tablet (Alphapharm Pty. Ltd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 11/04/2022.

Joint Formulary Committee. Gliclazide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/04/2022.

Mylan New Zealand Ltd. Glizide 80 mg Tablets data sheet 14 October 2019. Medsafe. http://www.medsafe.govt.nz. Accessed 11/04/2022.

Disclaimer: This information is independently developed by MIMS based on Gliclazide 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 © 2022 MIMS. All rights reserved. Powered by MIMS.com
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