Acarbose


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Type 2 diabetes mellitus
Adult: In patients inadequately controlled on diet alone, or on diet and oral hypoglycaemic agents: As adjunct to diet and exercise to improve glycaemic control: Usual dose: Initially, 25 mg or 50 mg tid. May also initiate with 25 mg or 50 mg daily to minimise gastrointestinal effects, then gradually increase to 25 mg or 50 mg tid. After 4-8 weeks, may further increase dose if necessary, up to 100-200 mg tid. Doses must be individualised according to patient response and tolerance. Dosage regimen recommendations may vary among individual products or between countries (refer to specific product guideline).
Suy thận
CrCl (mL/min) Dosage
<25 Not recommended.
Suy gan
Contraindicated.
Cách dùng
Should be taken with food. Take w/ 1st bite of each main meal.
Chống chỉ định
Inflammatory bowel disease, colonic ulceration, partial intestinal obstruction or predisposition to intestinal obstruction; chronic intestinal disease associated with marked disorders of digestion or absorption; conditions that may deteriorate due to elevated gas formation in the intestine (e.g. hernia), diabetic ketoacidosis, cirrhosis. Hepatic impairment.
Thận trọng
Patient exposed to stress-related states (e.g. trauma, fever, surgery, infection); may consider temporary insulin administration and treatment discontinuation in these patients if necessary. Not recommended in patients with severe renal impairment (CrCl <25 mL/min). Pregnancy and lactation. Concomitant use with intestinal adsorbents (e.g. charcoal) and digestive enzyme preparations containing carbohydrate-splitting enzymes (e.g. pancreatin, amylase).
Tác dụng không mong muốn
Significant: Increased serum transaminase levels. Rarely, hyperbilirubinaemia.
Blood and lymphatic system disorders: Thrombocytopenia.
General disorders and administration site conditions: Rarely, oedema.
Gastrointestinal disorders: Flatulence, diarrhoea, abdominal pain, nausea, vomiting, dyspepsia. Rarely, pneumatosis cystoides intestinalis, ileus or subileus.
Hepatobiliary disorders: Rarely, jaundice, hepatitis.
Immune system disorders: Hypersensitivity skin reactions (e.g. rash, erythema, exanthema, urticaria).
Potentially Fatal: Fulminant hepatitis.
Chỉ số theo dõi
Monitor serum transaminase levels every 3 months during the 1st year and periodically thereafter; postprandial glucose, HbA1c (at least twice yearly in patients with stable glycaemic control or those meeting treatment goals; quarterly in patients with therapy change or those not meeting treatment goals); serum creatinine.
Tương tác
May reduce the effect when used with intestinal adsorbents (e.g. charcoal) and digestive enzyme preparations containing carbohydrate splitting enzymes (e.g. pancreatin, amylase). May potentiate the hypoglycaemic effects of insulin and sulfonylureas. May cause enhanced reductions of postprandial blood glucose and increased frequency and severity of gastrointestinal side effects with oral neomycin. Colestyramine may enhance the effects of acarbose. May affect the bioavailability of digoxin. May result in loss of blood glucose control when used with certain agents that produce hyperglycaemia (e.g. thiazides and other diuretics, phenothiazines, corticosteroids, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, Ca channel blockers, isoniazid).
Tương tác với thức ăn
Increased intake of foods containing sucrose (cane sugar) during therapy may result in gastrointestinal symptoms (e.g. flatulence, bloating, occasional diarrhoea, loose stools).
Tác dụng
Description: Acarbose competitively and reversibly inhibits membrane-bound intestinal α-glucosidases and pancreatic α-amylase resulting in the delayed absorption of glucose and degradation of ingested complex carbohydrates and disaccharides in the small intestine. This action leads to a reduced post-prandial rise in blood glucose, therefore decreasing blood glucose fluctuations.
Pharmacokinetics:
Absorption: <2% (as active drug) and approx 35% (as metabolites) are absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 1 hour (active drug).
Metabolism: Exclusively metabolised in the gastrointestinal tract mainly by intestinal bacteria and digestive enzymes into at least 13 metabolites, including sulfate, methyl, and glucuronide conjugates as the major metabolites.
Excretion: Via urine (approx 34% as inactive metabolites; <2% as unchanged drug and active metabolites); faeces (approx 51% as unabsorbed drug). Elimination half-life: Approx 2 hours.
Đặc tính

Chemical Structure Image
Acarbose

Source: National Center for Biotechnology Information. PubChem Database. Acarbose, CID=41774, https://pubchem.ncbi.nlm.nih.gov/compound/Acarbose (accessed on Jan. 20, 2020)

Bảo quản
Store below 25°C. Protect from moisture.
Phân loại MIMS
Thuốc trị đái tháo đường
Phân loại ATC
A10BF01 - acarbose ; Belongs to the class of alpha glucosidase inhibitors. Used in the treatment of diabetes.
Tài liệu tham khảo
Acarbose 50 mg Tablets (Glenmark Pharmaceuticals Europe Limited). MHRA. https://products.mhra.gov.uk. Accessed 02/03/2021.

Acarbose Tablet (Alvogen, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/03/2021.

Anon. Acarbose. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 02/03/2021.

Buckingham R (ed). Acarbose. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/03/2021.

Glucobay 50 mg, 100 mg Tablets (Bayer Co. [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/03/2021.

Joint Formulary Committee. Acarbose. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/03/2021.

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