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Allopathic Medicines
Published in Varma H. Rambaran, Nalini K. Singh, Alternative Medicines for Diabetes Management, 2023
Varma H. Rambaran, Nalini K. Singh
Alpha-glucosidase inhibitors (AGIs), such as acarbose (Glucobay) (Figure 2.9a), miglitol (Figure 2.9b), and voglibose (Figure 2.9c), form a new class of “suppressing-based” therapy that target the enzyme, α-glucosidase (AG). AG is an exo-type carbohydrase that is responsible for breaking down complex carbohydrates to glucose in the upper gastrointestinal tract (Kumar, Narwal et al. 2011, Lebovitz 1998). As such, the inhibition of the AG enzyme results in a decrease in complex carbohydrate catabolism, which as a consequence, retards the rise in postprandial BG levels (Lebovitz 1998).Structural formulae of α-glucosidase inhibitors: (a) acarbose, (b) miglitol, and (c) voglibose.
Selected topics
Published in Henry J. Woodford, Essential Geriatrics, 2022
If it is preferable to avoid insulin (including patient choice), then adding an unused drug from the choice of a short-acting sulfonylurea, DPP-4 inhibitor or pioglitazone is possible. Finally, either a GLP-1 agonist, SGLT2 inhibitor or alpha-glucosidase inhibitor could be added. Drugs that promote weight loss (i.e. metformin, GLP-1 agonists or SGLT2 inhibitors) are likely to be inappropriate for frail older people with reduced oral intake or low body mass (e.g. BMI < 18 kg/m2).
Anti-Diabetic Drugs
Published in Awanish Kumar, Ashwini Kumar, Diabetes, 2020
Alpha-glucosidase inhibitors (AGIs) are another class of anti-diabetic drugs that are considered comparatively safe. This class include drugs such as Acarbose, Miglitol and Voglibose. AGIs, as the name suggests, inhibit the alpha-glucosidase enzyme at the brush border of the small intestines, thus reducing the absorption of carbohydrates from the gut. This results in a decrease in blood glucose level. The major positive aspect is that these drugs do not cause hypoglycaemia, but major adverse effects include abdominal pain, flatulence and bloating. AGIs are very effective in decreasing the post-prandial glucose level and also the glycated haemoglobin (HbA1c) level. Other positive effects of AGIs include decreased lipid levels, improved GLUT-4-based glucose uptake and GLP-1 stimulation that in turn improves insulin sensitivity and action [1,4].
Careful use to minimize adverse events of oral antidiabetic medications in the elderly
Published in Expert Opinion on Pharmacotherapy, 2021
Alpha-glucosidase inhibitors reduce postprandial hyperglycemia and have a moderate effect on fasting plasma glucose levels, resulting in a significant but only moderate reduction in HbA1c levels. Both acarbose [58] and miglitol [59] are generally well tolerated and safe in the elderly. One major advantage of alpha-glucosidase inhibitors in comparison with insulin-secretagogues is the absence of hypoglycemia. As alpha-glucosidase inhibitors reduce postprandial hyperglycemia and may reduce the risk of delayed hypoglycemia, these agents may contribute to dampen the overall glycemic variability. They are considered as a useful and relatively safe therapeutic option in elderly patients with T2D [60]. As in younger individuals, most discontinuations after initiation of alpha-glucosidase inhibitors were due to gastrointestinal side effects such as flatulence and diarrhea. Of note, however, a few case reports of paralytic ileus were reported between 1996 and 2006, all in Japan, in elderly (but also in middle-aged) diabetic patients treated with acarbose and voglibose [61]. Despite the potential advantages of alpha-glucosidase inhibitors in elderly patients with T2D, there is a lack of studies focusing specifically on that population and no studies with hard clinical outcomes that demonstrated a protection against diabetic complications.
Beneficial effects of rutin in diabetes-induced deficits in acquisition learning, retention memory and pain perception in rats
Published in Nutritional Neuroscience, 2020
Parisa Hasanein, Abbasali Emamjomeh, Nasibeh Chenarani, Mussa Bohlooli
Hyperglycemia as the hallmark of diabetes is the main possible candidate in pathophysiology of diabetes and its complications.3,8 For example, hyperglycemia is a causative factor in protein glycation, the post-translational changes in protein structures and functions, which underlie pathological sequelae of diabetes.7,46 Search for efficient inhibitors of glycation is therefore of considerable importance.47 It has been reported that RUT inhibits glycation of bovine serum albumin (90 μM) incubated in an in vitro system.46 Furthermore, RUT administration (50 and 100 mg/kg) orally for 3 weeks could significantly reduce glycosylated hemoglobin in a type 2 diabetic model.7 Another possible mechanism in the hypoglycemic effect of RUT may be related to its role as a α-glucosidase inhibitor which targets α-glucosidase in the small intestine, an intestinal enzyme that catabolizes non-absorbable complex carbohydrates into absorbable monosaccharides. Alpha-glucosidase inhibitors, such as acarbose, are commonly used oral hypoglycemic agents which block the degradation of carbohydrates and delay the absorption of glucose and fructose in the upper small intestine.47,48 The results of a recent computational study using docking technique showed that RUT interacted with four amino acids residues (His 239, His 279, Glu 304, and Pro 309) in the enzyme α-glucosidase, changing its potential binding mode at molecular level in the catalytic site and therefore inhibiting its activity.15
Considerations when using alpha-glucosidase inhibitors in the treatment of type 2 diabetes
Published in Expert Opinion on Pharmacotherapy, 2019
Maka S. Hedrington, Stephen N. Davis
Alpha-glucosidase inhibitors (AGIs) are oral antihyperglycemic drugs that act by competitive and reversible inhibition of intestinal alpha-glucosidase [2]. The latter are upper gastrointestinal enzymes that break down poly- and disaccharide carbohydrates into glucose. By inhibiting these enzymes, the absorption of glucose is delayed, which in turn slows surges in postprandial blood glucose (PPG) and contributes to improved glycemic control. Three AGIs – acarbose, miglitol and voglibose have been approved by various national agencies for drug regulation. Two of them (acarbose – the most commonly used AGI and miglitol) are available in the US. The AGIs can be used as monotherapy or part of combination therapy. When used as monotherapy, average reduction in hemoglobin A1c (HbA1c) is 0.8% [3]. The volume of decrease in HbA1c is proportional to the baseline HbA1c. The effect is greater (−0.93%) in higher (>9%) but reduced (−0.56%) in lower baseline HbA1c (<7%) levels. Average reduction in fasting blood glucose (FBG) is 1.09 mmol/L and 1 h PPG – 2.32 mmol/L. The risk of hypoglycemia is not increased and there is none to minimal effect on body weight. Most common side effects are gastrointestinal (diarrhea, abdominal pain, flatulence) and the occurrence and severity of these symptoms are dose-dependent.