Acarbose


Concise Prescribing Info
Indications/Uses
Type 2 DM.
Dosage/Direction for Use
Adult : PO Initial: 50 mg/day. May increase to 50 mg tid, then if necessary after 6-8 wk to 100 mg tid. Max: 200 mg tid.
Dosage Details
Oral
Type 2 diabetes mellitus
Adult: Initially, 50 mg daily increased to 50 mg tid, then increased if necessary after 6-8 wk to 100 mg tid. Max: 200 mg tid.
Renal Impairment
CrCl Dosage
<25 Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
Should be taken with food. Take w/ 1st bite of each main meal.
Contraindications
Patient w/ inflammatory bowel disease, diabetic ketoacidosis or cirrhosis, colonic ulceration, partial intestinal obstruction or predisposition to this condition, chronic intestinal diseases associated w/ marked disorders of digestion or absorption and state/s which may deteriorate as a result of increased gas formation in the intestine (e.g. larger hernias). Severe hepatic and renal impairment (CrCl <25 mL/min).
Special Precautions
Patient exposed to stress (e.g. fever, trauma, infection, surgery). Mild to moderate hepatic and renal impairment. Pregnancy and lactation.
Adverse Reactions
Flatulence, abdominal pain and distension, diarrhoea, nausea, vomiting, abnormal LFTs, thrombocytopenia, pneumatosis cystoidis intestinalis. Rarely, ileus, jaundice, hepatitis, skin reactions and oedema.
Potentially Fatal: Fulminant hepatitis.
Patient Counseling Information
Adhere strictly to the prescribed diabetic diet.
MonitoringParameters
Monitor postprandial glucose, glycosylated Hb levels, renal function (serum creatinine) and BP. Monitor serum transaminase levels 3 mthly during the 1st yr of treatment and periodically thereafter.
Drug Interactions
May enhance effects of other antidiabetics including insulin. Diminished effects w/ GI adsorbents (e.g. charcoal) and digestive enzyme preparations containing carbohydrate splitting enzymes (e.g. amylase, pancreatin). Neomycin and colestyramine may enhance effects of acarbose. May inhibit absorption of digoxin.
Action
Description: Acarbose competitively and reversibly inhibits pancreatic α-amylase and intestinal brush border α-glucosidases, resulting in delayed hydrolysis of ingested complex carbohydrates and disaccharides, and glucose absorption; dose-dependent reduction in postprandial serum insulin and glucose peaks; inhibits metabolism of sucrose to glucose and fructose.
Pharmacokinetics:
Absorption: <2% (as active drug) and approx 35% (as metabolites) are absorbed from the GI tract. Time to peak plasma concentration: Approx 1 hr.
Metabolism: Metabolised exclusively via GI tract, principally by microbial flora and intestinal enzymes.
Excretion: Via urine (approx 34% as inactive metabolites; <2% parent drug and active metabolite) and faeces (approx 51% as unabsorbed drug).
Chemical Structure

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)

Storage
Store below 25°C. Protect from moisture.
MIMS Class
ATC Classification
A10BF01 - acarbose ; Belongs to the class of alpha glucosidase inhibitors. Used in the treatment of diabetes.
References
Anon. Acarbose. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/08/2014.

Buckingham R (ed). Acarbose. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/08/2014.

Joint Formulary Committee. Acarbose. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/08/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Acarbose. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 14/08/2014.

Precose Tablets. U.S. FDA. https://www.fda.gov/. Accessed 14/08/2014.

Disclaimer: This information is independently developed by MIMS based on Acarbose 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 © 2020 MIMS. All rights reserved. Powered by MIMS.com
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