Glibenclamide + Metformin


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Type 2 diabetes mellitus
Adult: Each tab contains glibenclamide (mg) and metformin (mg): 1.25/250, 2.5/500, 5/500: Patients inadequately controlled on diet and exercise: Initially, 1.25 mg/250 mg 1-2 times daily. Patients w/ HbA1c >9% or fasting plasma glucose (FPG) >200 mg/dL: Initially, 1.25 mg/250 mg bid. May adjust daily dose in increments of 1.25 mg/250 mg at intervals of not less than 2 wk. Max: Glibenclamide 10 mg and metformin 2,000 mg daily. Patients inadequately controlled on sulfonylurea and/or metformin: Initially, 2.5 mg/500 mg or 5 mg/500 mg bid. May adjust daily dose in increments not more than 5 mg/500 mg. Max: Glibenclamide 20 mg and metformin 2,000 mg daily.
Renal Impairment
CrCl (mL/min) Dosage
<60 Contraindicated.
Hepatic Impairment
Contraindicated.
Cách dùng
Should be taken with food.
Chống chỉ định
Diabetic ketoacidosis or diabetic pre-coma; acute conditions which may alter renal function (e.g. dehydration, severe infection, shock); acute or chronic disease which may cause tissue hypoxia (e.g. cardiac or resp failure, recent MI, acute significant blood loss, sepsis, gangrene); major surgery, porphyria. Acute alcohol intoxication/alcoholism. Renal (CrCl <60 mL/min) or hepatic impairment. Lactation. Concomitant use w/ bosentan, miconazole and intravascular admin of iodinated contrast materials.
Thận trọng
Patient w/ impaired adrenal and/or pituitary function, G6PD deficiency, heart failure. Pregnancy.
Phản ứng phụ
Hypoglycaemia, haemolytic anaemia, wt gain, upper resp infection, diarrhoea, headache, nausea and vomiting, abdominal pain, dizziness.
Potentially Fatal: Lactic acidosis.
Thông tin tư vấn bệnh nhân
May impair ability to drive or operate machinery.
MonitoringParameters
Monitor urine for glucose and ketones, FPG, HbA1c, and fructosamine; haematologic parameters, renal and hepatic function; vit B12 and folate levels (if anaemia is suspected); signs and symptoms of hypoglycaemia.
Quá liều
Symptoms: Mild to severe hypoglycaemia which may lead to hypoglycaemic coma (glibenclamide); lactic acidosis (metformin). Management: Mild hypoglycaemia w/o loss of consciousness may be treated w/ oral glucose. Severe hypoglycaemic reactions w/ coma, seizure or other neurological impairment require immediate hospitalisation. Admin rapid IV inj of glucose 50% soln in case of hypoglycaemic coma. Haemodialysis may be useful for removal of accumulated drugs in metformin overdose.
Tương tác
Decreased hypoglycaemic effect w/ thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, oestrogen, OC, phenytoin, nicotinic acid, sympathomimetics, Ca channel blockers, isoniazid. Glibenclamide: Increased hypoglycaemic effect w/ NSAIDs and other highly protein bound drugs, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, MAOIs, β-blockers. Decreased plasma concentration w/ colesevelam. Metformin: Increased plasma concentration w/ furosemide, nifedipine and cimetidine.
Potentially Fatal: Increased risk of hepatotoxicity w/ bosentan. Risk of severe hypoglycaemia w/ miconazole (systemic route, oromucosal gel). Alteration of renal function w/ iodinated contrast materials.
Food Interaction
Alcohol may potentiate the risk of lactic acidosis, avoid use.
Tác dụng
Description: Glibenclamide stimulates insulin secretion from pancreatic β-cells, reduces glucose output from the liver and increases insulin sensitivity at peripheral target sites. Metformin reduces hepatic glucose production by inhibiting gluconeogenesis, delays intestinal glucose absorption and improves insulin sensitivity by increasing peripheral glucose uptake and utilisation.
Pharmacokinetics:
Absorption: Glibenclamide: Readily absorbed from the GI tract. Time to peak plasma concentration: W/in 2-4 hr. Metformin: Slowly and incompletely absorbed from the GI tract. Bioavailability: Approx 50-60%. Time to peak plasma concentration: 2.5 hr.
Distribution: Glibenclamide: Plasma protein binding: Extensively bound (99%). Metformin: Crosses the placenta and enters breast milk (small amounts).
Metabolism: Glibenclamide: Almost completely metabolised in the liver. Metformin: Not metabolised in the liver.
Excretion: Glibenclamide: Via urine (approx 50%) and bile (50%) into the faeces. Metformin: Via urine, as unchanged drug. Elimination half-life: Approx 2-6 hr.
Đặc tính

Chemical Structure Image
Glibenclamide

Source: National Center for Biotechnology Information. PubChem Database. Glyburide, CID=3488, https://pubchem.ncbi.nlm.nih.gov/compound/Glyburide (accessed on Jan. 22, 2020)


Chemical Structure Image
Metformin

Source: National Center for Biotechnology Information. PubChem Database. Metformin, CID=4091, https://pubchem.ncbi.nlm.nih.gov/compound/Metformin (accessed on Jan. 20, 2020)

Bảo quản
Store at or below 25°C. Protect from light.
Phân loại MIMS
References
Anon. Glyburide and Metformin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 21/10/2015.

Buckingham R (ed). Glibenclamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/10/2015.

Buckingham R (ed). Metformin Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/10/2015.

Glyburide and Metformin Hydrochloride Tablet, Film Coated (Teva Pharmaceuticals USA Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 21/10/2015.

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