Mooradian A D, Thurman J E
Department of Internal Medicine, St Louis University Medical School, Missouri 63104, USA.
Drugs. 1999 Jan;57(1):19-29. doi: 10.2165/00003495-199957010-00003.
It is widely accepted that the most challenging goal in the management of patients with diabetes mellitus is to achieve blood glucose levels as close to normal as possible. In general, normalising postprandial blood glucose levels is more difficult than normalising fasting hyperglycaemia. In addition, some epidemiological studies suggest that postprandial hyperglycaemia (PPHG) or hyperinsulinaemia are independent risk factors for the development of macrovascular complications of diabetes mellitus. Recently, several drugs with differing pharmacodynamic profiles have been developed which target PPHG. These include insulin lispro, amylin analogues, alpha-glucosidase inhibitors and meglitinide analogues. Insulin lispro has a more rapid onset of action and shorter duration of efficacy compared with regular human insulin. In clinical trials, the use of insulin lispro was associated with improved control of PPHG and a reduced incidence of hypoglycaemic episodes. Repaglinide, a meglitinide analogue, is a short-acting insulinotropic agent which. when given before meals, stimulates endogenous insulin secretions and lowers postprandial hyperglycaemic excursions. Both insulin lispro and repaglinide are associated with postprandial hyperinsulinaemia. In contrast, amylin analogues reduce PPHG by slowing gastric emptying and delivery of nutrients to the absorbing surface of the gut. Alpha-Glucosidase inhibitors such as acarbose, miglitol and voglibose also reduce PPHG primarily by interfering with the carbohydrate-digesting enzymes and delaying glucose absorption. With the availability of agents which preferentially reduce postprandial blood glucose excursions, it is now possible to achieve glycaemic goals in a larger proportion of individuals with diabetes mellitus.
人们普遍认为,糖尿病患者管理中最具挑战性的目标是使血糖水平尽可能接近正常。一般来说,使餐后血糖水平正常化比使空腹高血糖正常化更困难。此外,一些流行病学研究表明,餐后高血糖(PPHG)或高胰岛素血症是糖尿病大血管并发症发生的独立危险因素。最近,已经开发出几种具有不同药效学特征的药物来针对PPHG。这些药物包括赖脯胰岛素、胰淀素类似物、α-葡萄糖苷酶抑制剂和格列奈类药物。与常规人胰岛素相比,赖脯胰岛素起效更快,疗效持续时间更短。在临床试验中,使用赖脯胰岛素与改善PPHG控制和降低低血糖发作发生率相关。格列奈类药物瑞格列奈是一种短效促胰岛素分泌剂,在餐前服用时,可刺激内源性胰岛素分泌并降低餐后高血糖波动。赖脯胰岛素和瑞格列奈都与餐后高胰岛素血症有关。相比之下,胰淀素类似物通过减慢胃排空和营养物质向肠道吸收表面的输送来降低PPHG。阿卡波糖、米格列醇和伏格列波糖等α-葡萄糖苷酶抑制剂也主要通过干扰碳水化合物消化酶和延迟葡萄糖吸收来降低PPHG。随着优先降低餐后血糖波动的药物的出现,现在有可能在更大比例的糖尿病患者中实现血糖目标。