Glimepiride


Generic Medicine Info
Indications and Dosage
Oral
Type 2 diabetes mellitus
Adult: As an adjunct to diet and exercise: Dosage is individualised based on patient's blood glucose level. Initially, 1-2 mg daily, may increase in increments of 1-2 mg at intervals of 1-2 weeks according to response. Maintenance: 4 mg daily. Max: 6 mg or 8 mg daily.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
Should be taken with food. Take immediately before or during breakfast, or the 1st main meal of the day. Do not skip meals.
Contraindications
Hypersensitivity to glimepiride, other sulfonylureas, or sulfonamides. Type 1 diabetes mellitus, diabetic coma, ketoacidosis. Severe renal or hepatic impairment.
Special Precautions
Patient with G6PD deficiency, stress-related states (e.g. fever, trauma, infection, surgery). Patient with a predisposition to hypoglycaemia (e.g. debilitated or malnourished patient or those with deficient caloric intake; patient with certain uncompensated endocrine disorders affecting carbohydrate metabolism or counter-regulation of hypoglycaemia such as adrenal or pituitary impairment, those who have undergone severe or prolonged exercise). Mild to moderate renal and hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Hypoglycaemia (may be severe), haemolytic anaemia (particularly in patients with G6PD deficiency), hypersensitivity reaction (e.g. anaphylaxis, angioedema, Stevens-Johnson syndrome), weight gain.
Blood and lymphatic system disorders: Leucopenia, agranulocytosis, aplastic anaemia, pancytopenia, thrombocytopenia.
Endocrine disorders: Syndrome of inappropriate antidiuretic hormone secretion (SIADH).
Eye disorders: Visual disturbances.
Gastrointestinal disorders: Abdominal pain, diarrhoea, nausea, vomiting, dysgeusia.
Hepatobiliary disorders: Cholestasis, jaundice, hepatitis, liver failure, hepatic porphyria.
Metabolism and nutrition disorders: Disulfiram-like reactions, hyponatraemia.
Nervous system disorders: Headache, dizziness.
Skin and subcutaneous tissue disorders: Photosensitivity, alopecia.
Patient Counseling Information
This drug may cause visual disturbances and an impaired ability to react due to hypoglycaemia; if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor blood and urine glucose, glycosylated Hb level, renal function, signs and symptoms of hypoglycaemia. Regular hepatic and haematological monitoring (particularly leucocytes and thrombocytes).
Overdosage
Symptoms: Nausea, vomiting, epigastric pain, hypoglycaemia, restlessness, tremor, visual disturbances, coordination problems, sleepiness, coma, convulsions. Management: Induce vomiting followed by administration of lemonade with activated charcoal and Na sulfate to prevent absorption. May employ gastric lavage if large quantities have been ingested. Administer glucose via IV bolus inj of 50 mL of a 50% solution followed by infusion of a 10% solution.
Drug Interactions
Increased hypoglycaemic effect with NSAIDs (e.g. phenylbutazone), insulin, oral antidiabetics (e.g. metformin), salicylates, fluoxetine, anabolic steroids and androgens, antibiotics (e.g. chloramphenicol, sulfonamides, tetracyclines, quinolones, clarithromycin), coumarin anticoagulants, disopyramide, fibrates, ACE inhibitors, MAOIs, allopurinol, probenecid, sulfinpyrazone, cyclophosphamide, fluconazole, miconazole and pentoxifylline. Decreased hypoglycaemic effect with estrogens, oral contraceptives, thiazide diuretics, glucocorticoids, phenothiazine derivatives (e.g. chlorpromazine), sympathomimetics (e.g. epinephrine, salbutamol, terbutaline), nicotinic acid (high doses) and nicotinic acid derivatives, laxative (prolonged use), phenytoin, diazoxide, glucagon, barbiturates, rifampicin and isoniazid. Signs of hypoglycaemia may be reduced or absent in patients taking sympatholytic drugs (e.g. β-blockers, clonidine, guanethidine, reserpine). May potentiate or weaken the blood glucose lowering effect with histamine (H2) antagonists, β-blockers, clonidine, and reserpine. Concurrent use with colesevelam may decrease the serum concentration of glimepiride; administer glimepiride at least 4 hours before colesevelam.
Food Interaction
May potentiate the hypoglycaemic effect with alcohol.
Action
Description: Glimepiride, an antidiabetic sulfonylurea, reduces blood glucose by stimulating the insulin release from pancreatic β-cells and decreases glucose output from the liver. Additionally, it increases insulin sensitivity at peripheral target sites.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Completely absorbed from the gastrointestinal tract. Time to peak plasma concentration: 2-3 hours.
Distribution: Crosses the placenta. Volume of distribution: 8.8 L. Plasma protein binding: >99.5%.
Metabolism: Extensively metabolised in the liver via oxidative biotransformation by CYP2C9 into M1 metabolite which is then further metabolised into M2 metabolite (inactive) by 1 or several cytosolic enzymes.
Excretion: Via urine (60%; 80-90% as M1 and M2 metabolites); faeces (40%; 70% as M1 and M2 metabolites). Elimination half-life: 5-9 hours.
Chemical Structure

Chemical Structure Image
Glimepiride

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 3476, Glimepiride. https://pubchem.ncbi.nlm.nih.gov/compound/3476. Accessed July 26, 2022.

Storage
Store below 25°C.
MIMS Class
Antidiabetic Agents
ATC Classification
A10BB12 - glimepiride ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.
References
Amaryl (Sanofi-Aventis [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 06/07/2022.

Anon. Glimepiride. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/07/2022.

Buckingham R (ed). Glimepiride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/07/2022.

Glimepiride 4 mg Tablets (Brown and Burk UK Ltd). MHRA. https://products.mhra.gov.uk. Accessed 06/07/2022.

Glimepiride Tablet (Micro Labs Limited). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/07/2022.

Joint Formulary Committee. Glimepiride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/07/2022.

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