Editor: Abdelwahab Ward, PharmD.
Pharmacology
- Drug Class: α-Glucosidase inhibitors (AGIs) are a class of oral glucose-lowering drugs used exclusively for treatment or prevention of type 2 diabetes mellitus.
- Mechanism of Action: Acarbose, an inhibitor of intestinal alpha glucosidases, delays the digestion and absorption of starch and sucrose; it has a small but significant effect in lowering blood glucose.
- Available Products: Glucobay 50 mg, Opicroceed 50 mg
Indications and Dose
Acarbose indicated for diabetes mellitus inadequately controlled by diet or by diet with oral antidiabetic drugs. Initially 50 mg daily by mouth, then increased to 50 mg 3 times a day for 6–8 weeks, then increased if necessary to 100 mg 3 times a day (max. per dose 200 mg 3 times a day).
- Dose adjustment
- Hepatic impairment: Manufacturer advises avoid in severe impairment
- Renal impairment: Avoid if eGFR less than 25 mL/ minute
Contraindications
Disorders of digestion or absorption; hernia (condition may deteriorate); inflammatory bowel disease; predisposition to intestinal obstruction.
- Cautions 一 May enhance hypoglycaemic effects of insulin and sulfonylureas (hypoglycaemic episodes may be treated with oral glucose but not with sucrose).
Pharmacokinetics
- Route: Oral
- Peak: 1 hr
- Metabolism: extensively degraded in the intestine by bacterial and digestive enzymes, glucose units are removed from acarbose molecule. Metabolites: 4-methylpyrogallol derivatives (major inactive mets) and other inactive mets. T1/2: 2 hr (adults)
- Excretion: Urine: 34 % as inactive metabolites. Feces: 51% as unabsorbed drug
Adverse Effects
- Common or very common: diarrhea (may need to reduce dose); gastrointestinal discomfort; gastrointestinal disorders
- Nausea and vomiting is uncommon
References
- Medscape.com. Precose, (acarbose) dosing, indications, interactions, adverse effects, and more. [online] Available at: https://reference.medscape.com/drug/precose-acarbose-342701#10 [accessed 29 Nov. 2020]
- McIver, L.A. and Tripp, J. (2020). Acarbose. [online] PubMed. Available at: https://www.ncbi.nlm.nih.gov/books/NBK493214/
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Pharmacology