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acarbose
Acarbose is an anti-diabetic drug used to treat type 2 diabetes mellitus and, in some countries, prediabetes. It is a generic sold in Europe and China as Glucobay (Bayer AG), in North America as Precose (Bayer Pharmaceuticals), and in Canada as Prandase (Bayer AG). It is cheap and popular in China, but not in the U.S. One physician explains the use in the U.S. is limited because it is not potent enough to justify the side effects of diarrhea and flatulence.〔(China’s Thirst for New Diabetes Drugs Threatens Bayer’s Lead ), By Naomi Kresge, Bloomberg, November 21, 2011.〕 However, a recent large study concludes "acarbose is effective, safe and well tolerated in a large cohort of Asian patients with type 2 diabetes."〔(A Multinational, Observational Study to Investigate the Efficacy, Safety and Tolerability of Acarbose as Add-On or Monotherapy in a Range of Patients: The GlucoVIP Study. )〕A possible explanation for the differing opinions is an observation that acarbose is significantly more effective in patients eating a relatively high carbohydrate Eastern diet 〔(Comparison of the Hypoglycemic Effect of Acarbose Monotherapy in Patients With Type 2 Diabetes Mellitus Consuming an Eastern or Western Diet: A Systematic Meta-analysis. )〕
It is a starch blocker, and inhibits alpha glucosidase, an intestinal enzyme that releases glucose from larger carbohydrates. It is composed of an acarviosin moiety with a maltose at the reducing terminus.
==Mechanism of action==
Acarbose inhibits enzymes (glycoside hydrolases) needed to digest carbohydrates, specifically, alpha-glucosidase enzymes in the brush border of the small intestines and pancreatic alpha-amylase. Pancreatic alpha-amylase hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, whereas the membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. Inhibition of these enzyme systems reduces the rate of digestion of complex carbohydrates. Less glucose is absorbed because the carbohydrates are not broken down into glucose molecules. In diabetic patients, the short-term effect of these drugs therapies is to decrease current blood glucose levels; the long-term effect is a reduction in HbA1c level.〔''Drug Therapy in Nursing'', 2nd Edition.〕 This reduction averages an absolute decrease of 0.7%, which is a decrease of about 10% in typical HbA1c values in diabetes studies.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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