Usefulness of antidiabetic alpha-glucosidase inhibitors: a review on the timing of administration and effects on gut hormones

Abstract

Elevation of postprandial plasma glucose is correlated with an increase in cardiovascular events, and alphaglucosidase inhibitors (αGIs) are effective at reducing postprandial glucose levels. In Japan, the αGIs acarbose, voglibose, and miglitol have been available since 1993, 1994, and 2006 inhibitors are also effective at reducing postprandial glucose levels, and they have been available in Japan since 2009. A combination therapy of αGI, miglitol, and the DPP-4 inhibitor, sitagliptin, is more effective at decreasing postprandial glucose levels than monotherapy with either miglitol or sitagliptin. Moreover, the combination therapy of miglitol and sitagliptin is more effective at increasing postprandial active glucagon-like peptide-1 (GLP-1) levels than monotherapy. Peptide YY (PYY) has appetitesuppressing and gastric-emptying effects similar to GLP-1. In healthy individuals, miglitol increases the postprandial total PYY; however, combination therapy of miglitol and vildagliptin does not change postprandial total PYY levels. αGIs are typically prescribed to be taken just before a meal, which can result in decreased drug adherence. Different patterns of αGI intake were examined, and the results showed that miglitol or acarbose administration after a meal is effective. The effects of taking miglitol dissolved in water during a meal appeared to be similar to that of taking miglitol as a tablet just before a meal. The long-term effects of taking miglitol dissolved in water should be evaluated in future studies. αGIs may be effective even when they are not taken before a meal, and a more flexible administration may improve drug adherence.

Sitagliptin protects liver against aflatoxin B1‐induced hepatotoxicity through upregulating Nrf2/ARE/HO‐1 pathway

“…45,46 AFB1-prompted rodents treated with sitagliptin presented a noteworthy Nrf2 signaling upregulation confirmed by the increased expression of Nrf2, NQO-1, HO-1, SOD, CAT, and GPx levels. 47,48 The present examination added backing to our past discoveries where the sitagliptin administration updirected Nrf2 signaling in the cerebrum and liver in hyperammonemia and hepatocarcinogenesis animal models, individually. 49,50 Although enacted by ROS, Nrf2 signaling downregulated in the rodents of AFB1-actuated rodents could be an immediate outcome of extreme ROS formation.…”

The potential of chalcone-capped gold nanoparticles for the management of diabetes mellitus

“…Inhibition of activities of α-glucosidase and α-amylase enzymes have been reported to reduce the risk of obesity, kidney failure and cardiovascular diseases during Type-2 diabetic (T2D) management [11]. Acarbose, voglibose, miglitol and metfomin are conventional antidiabetic drugs commonly prescribed to inhibit hepatic glucose production due to the breakdown of carbohydrate by α-glucosidase and α -amylase enzymes [2]. However, due to the potential side effect of increasing gas build up in the intestine and liver toxicity on prolong usage [9], there is a need for the evaluation of alternative drugs in the nano range.…”

Combination therapy of bioactive compounds with acarbose: A proposal to control hyperglycemia in type 2 diabetes

“…The dose can increase to 100 mg per day (maximum) depending on the drug's tolerance and PHG and glycosylated hemoglobin. The most important limiting factor for increased use of ACB is low tolerability and the various frequent gastrointestinal side effects (Aoki et al, 2019; Derosa & Maffioli, 2012; DiNicolantonio et al, 2015).…”