Internal Medicine, Kanagawa Dental University, Yokosuka, Japan.
Department of Endocrinology and Metabolism, Yokohama City University Graduate School of Medicine, Yokohama, Japan.
Endocr J. 2019 May 28;66(5):395-401. doi: 10.1507/endocrj.EJ19-0041. Epub 2019 Apr 23.
Elevation of postprandial plasma glucose is correlated with an increase in cardiovascular events, and alpha-glucosidase 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, respectively. Dipeptidyl peptidase-4 (DPP-4) 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 appetite-suppressing 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.
餐后血糖升高与心血管事件增加相关，α-葡萄糖苷酶抑制剂（αGIs）可有效降低餐后血糖水平。在日本，αGIs 阿卡波糖、伏格列波糖和米格列醇分别于 1993 年、1994 年和 2006 年上市。二肽基肽酶-4（DPP-4）抑制剂也可有效降低餐后血糖水平，于 2009 年在日本上市。αGI、米格列醇和 DPP-4 抑制剂西格列汀联合治疗可更有效地降低餐后血糖水平，优于米格列醇或西格列汀单药治疗。此外，米格列醇和西格列汀联合治疗可更有效地增加餐后活性胰高血糖素样肽-1（GLP-1）水平，优于单药治疗。肽 YY（PYY）具有与 GLP-1 相似的抑制食欲和促进胃排空作用。在健康个体中，米格列醇可增加餐后总 PYY；然而，米格列醇和维格列汀联合治疗并不改变餐后总 PYY 水平。αGIs 通常在餐前服用，这可能导致药物依从性降低。研究了不同的 αGI 摄入模式，结果表明餐后服用米格列醇或阿卡波糖是有效的。用餐时服用水溶性米格列醇的效果似乎与餐前服用米格列醇片相似。在未来的研究中应评估用餐时服用水溶性米格列醇的长期效果。即使不餐前服用，αGIs 也可能有效，更灵活的给药方式可能会提高药物依从性。
