Acarbose

Acarbose is an alpha-glucosidase inhibitor that reversibly inhibits intestinal alpha-glucosidases, the enzymes responsible for the metabolism of complex carbohydrates into absorbable monosaccharide units. ^[1] Acarbose can be used as first-line therapy in patients with type 2 diabetes that is poorly controlled by diet alone, and it can also be given in combination with sulphonylureas or insulin. ^[2]

Inhibition of intestinal alpha-glucosidases delays the digestion of starch and sucrose and flattens the postprandial blood glucose excursions, thus mimicking the effects of dieting on hyperglycaemia, hyperinsulinaemia and hypertriglyceridaemia. ^[3] By reversibly inhibiting the enzymatic cleavage of complex carbohydrates to simple absorbable sugars, acarbose reduces postprandial blood glucose and, subsequently, glycosylated hemoglobin (HbA1c) levels. ^[4] Because acarbose has the structural features of a tetrasaccharide and does not cross the enterocytes after ingestion, its pharmacological action is directed exclusively towards the intestinal glucosidases. ^[2]

In placebo-controlled trials, acarbose caused significant improvements in glycemic control indicators, including glycosylated hemoglobin, and demonstrated additional glycemic control when added to other antidiabetic therapies such as sulfonylureas and insulin. ^[1] Among the most promising interventions to slow ageing grouped by the robustness of the preclinical and some clinical results, acarbose is placed in the top tier alongside rapamycin, senolytics, metformin, spermidine, NAD+ enhancers and lithium. ^[5] Acarbose is being investigated as a type 2 diabetes drug that acts as a calorie restriction mimetic, reducing enzymatic degradation and absorption of glucose from complex carbohydrates when taken with a meal. ^[6] In preclinical anti-ageing work on US-FDA-approved medicines, acarbose is likely to demonstrate a lifespan-promoting effect predominantly in male animals.

The most commonly reported adverse drug reactions with acarbose are abdominal pain, diarrhea, and flatulence, which tend to lessen with time. ^[1] Gastrointestinal discomfort is frequently reported as an adverse effect of acarbose administration, but its incidence usually decreases with time. ^[2] Acarbose should not be used in individuals with certain intestinal disorders, including inflammatory bowel disease, and concurrent use with sulfonylureas or insulin may cause an increased frequency of hypoglycemia. ^[1]