Santeusanio F, Compagnucci P
Istituto di Medicina Interna e Scienze Endocrine e Metaboliche, University of Perugia, Italy.
Drug Saf. 1994 Dec;11(6):432-44. doi: 10.2165/00002018-199411060-00005.
Acarbose is an alpha-glucosidase inhibitor proposed for the treatment of diabetic patients. It acts by competitively inhibiting the alpha-glucosidases in the intestinal brush border. The principal action of these enzymes is to convert nonabsorbable dietary starch and sucrose into absorbable monosaccharides (e.g. glucose). Enzyme inhibitors delay this conversion, slowing the formation and consequently the absorption of monosaccharides, and thus reducing the concentration of postprandial blood glucose. Both starch and sucrose are influenced, whereas lactose and glucose are not. Many studies in experimental animals, healthy volunteers and patients with non-insulin-dependent diabetes mellitus (NIDDM) have shown that acarbose decreases postprandial blood glucose, with a lesser reduction of fasting blood glucose, plasma triglycerides and postprandial insulin levels. In long term studies in NIDDM patients, acarbose significantly reduced glycosylated haemoglobin levels. Acarbose is only minimally absorbed from the gut and no systemic adverse effects have been demonstrated after long term administration. The drug allows undigested carbohydrates to pass into the large bowel where they are fermented causing flatulence, bloating and diarrhoea. These symptoms, which occur in approximately 30 to 60% of patients, tend to decrease with time and seem to be dose-dependent. They are minimised by starting therapy with low doses (such as 50mg 3 times daily) which may be effective in many patients. An increase in serum hepatic transaminases observed in earlier studies in the US, where doses of acarbose up to 900mg daily were used, has been not reported with the lower doses of the drug actually recommended [150 to 300mg (up to 600mg) daily]. In conclusion, acarbose may be useful in patients with NIDDM when diet alone is no longer able to maintain satisfactory blood glucose control. Furthermore, it may be a valid alternative to sulphonylurea or biguanide therapy when these drugs are contraindicated and insulin administration may be delayed. Acarbose seems also to be a useful adjunct to hypoglycaemic oral agents but its precise role in this field has not been fully clarified.
阿卡波糖是一种被提议用于治疗糖尿病患者的α-葡萄糖苷酶抑制剂。它通过竞争性抑制肠道刷状缘的α-葡萄糖苷酶起作用。这些酶的主要作用是将不可吸收的膳食淀粉和蔗糖转化为可吸收的单糖（如葡萄糖）。酶抑制剂会延迟这种转化，减慢单糖的形成并因此减少其吸收，从而降低餐后血糖浓度。淀粉和蔗糖都会受到影响，而乳糖和葡萄糖则不受影响。在实验动物、健康志愿者和非胰岛素依赖型糖尿病（NIDDM）患者中进行的许多研究表明，阿卡波糖可降低餐后血糖，对空腹血糖、血浆甘油三酯和餐后胰岛素水平的降低作用较小。在对NIDDM患者的长期研究中，阿卡波糖显著降低了糖化血红蛋白水平。阿卡波糖从肠道的吸收极少，长期给药后未显示出全身性不良反应。该药物会使未消化的碳水化合物进入大肠，在那里它们被发酵，导致肠胃胀气、腹胀和腹泻。这些症状在大约30%至60%的患者中出现，往往会随着时间推移而减轻，并且似乎与剂量有关。通过低剂量（如每日3次，每次50mg）开始治疗可将这些症状降至最低，低剂量对许多患者可能有效。在美国早期研究中，使用每日高达900mg的阿卡波糖剂量时观察到血清肝转氨酶升高，但实际推荐的较低剂量[每日150至300mg（最高600mg）]并未报告这种情况。总之，当仅靠饮食已无法维持令人满意的血糖控制时，阿卡波糖可能对NIDDM患者有用。此外，当这些药物禁忌且可能延迟胰岛素给药时，它可能是磺脲类或双胍类治疗的有效替代药物。阿卡波糖似乎也是降血糖口服药物的有用辅助药物，但其在该领域的确切作用尚未完全阐明。
