Glimepiride


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Type 2 diabetes mellitus
Adult: Dosage is individualised based on patient’s blood glucose level. Initially, 1 mg daily, may increase in increments of 1 mg at intervals of 1-2 weeks according to response. Maintenance: 4 mg daily. Max: 6 mg daily.
Elderly: Initially, 1 mg once daily.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Cách dùng
Should be taken with food. Take immediately before or during breakfast, or the 1st main meal of the day. Do not skip meals.
Chống chỉ định
Hypersensitivity to glimepiride, other sulfonylureas or sulfonamides. Type 1 diabetes or insulin-dependent diabetes, and diabetic ketoacidosis (with or without coma). Severe renal or hepatic impairment.
Thận trọng
Patient with G6PD deficiency, stress-related states (e.g. fever, trauma, infection, surgery). Mild to moderate renal and hepatic impairment. Elderly. Pregnancy and lactation.
Phản ứng phụ
Significant: Hypoglycaemia, haemolytic anaemia (in G6PD deficiency), hypersensitivity reaction (e.g. anaphylaxis, angioedema, Stevens-Johnson syndrome), weight gain.
Blood and lymphatic system disorders: Leukopenia, agranulocytosis, aplastic anaemia, pancytopenia, thrombocytopenia.
Endocrine disorders: Inappropriate antidiuretic hormone secretion (SIADH).
Eye disorders: Visual disturbances.
Gastrointestinal disorders: Abdominal pain, diarrhoea, nausea, vomiting, dysgeusia.
General disorders and administration site conditions: Asthenia.
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.
Thông tin tư vấn bệnh nhân
This drug may cause hypoglycaemia and visual disturbances, 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 (leukocytes and thrombocytes).
Quá liều
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. In case of severe overdose, administer glucose by bolus IV inj of 50 mL of a 50% solution followed by infusion of a 10% solution.
Tương tác
Increased hypoglycaemic effect with NSAIDs (e.g. phenylbutazone), insulin, oral antidiabetics (e.g. metformin), salicylates, fluoxetine, anabolic steroids and androgens, antibiotics (e.g. chloramphenicol, sulphonamides, tetracyclines, quinolones, clarithromycin), coumarin anticoagulants, disopyramide, fibrates, ACE inhibitors, MAOIs, allopurinol, probenecid, sulfinpyrazone, cyclophosphamide, fluconazole and pentoxifylline. Decreased hypoglycaemic effect with oestrogens, oral contraceptives, thiazide diuretics, glucocorticoids, phenothiazine derivatives (e.g. chlorpromazine), sympathomimetics (e.g. epinephrine, albuterol, terbutaline), nicotinic acid (high doses) and nicotinic acid derivatives, laxative (long term use), phenytoin, diazoxide, glucagon, barbiturates, rifampicin and isoniazid. Signs of hypoglycaemia may be reduced or absent in patients taking sympatholytic drugs (e.g. ß-blockers, clonidine, guanethidine, reserpine). May cause severe hypoglycaemia with miconazole.
Food Interaction
May cause rare disulfiram reaction with alcohol.
Tác dụng
Description: Glimepiride, an antidiabetic sulphonylurea, reduces blood glucose by stimulating the insulin release from pancreatic ß-cells and decreases glucose output from the liver. It also increases insulin sensitivity at peripheral target sites.
Onset: Blood glucose reductions: 2-3 hours.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Completely absorbed from gastrointestinal tract. Time to peak plasma concentration: 2-3 hours.
Distribution: Volume of distribution: 8.8 L. Plasma protein binding: >99.5%
Metabolism: Extensively metabolised in the liver via oxidative biotransformation by CYP2C9 to cyclohexyl hydroxy methyl derivative (M1) and further metabolised to inactive carboxyl derivative (M2).
Excretion: Mainly via urine (approx 60%, 80-90% as M1 and M2 metabolites), as faeces (approx 40%, 70% as M1 and M2 metabolites). Elimination half-life: Approx 9 hours.
Đặc tính

Chemical Structure Image
Glimepiride

Source: National Center for Biotechnology Information. PubChem Database. Glimepiride, CID=3476, https://pubchem.ncbi.nlm.nih.gov/compound/Glimepiride (accessed on Jan. 22, 2020)

Bảo quản
Store below 30°C. Protect from moisture.
Phân loại MIMS
Phân loại ATC
A10BB12 - glimepiride ; Belongs to the class of sulfonylureas. Used in the treatment of diabetes.
References
Anon. Glimepiride. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 27/05/2019.

Buckingham R (ed). Glimepiride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/05/2019.

Glimepiride Tablet (Accord Healthcare Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 27/05/2019.

Joint Formulary Committee. Glimepiride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 27/05/2019.

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