[格列齐特:代谢和血管作用的综述]。

Diabete & metabolisme Pub Date : 1994-11-01
K G Alberti
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摘要

格列齐特是第二代磺酰类药物,广泛用于治疗非胰岛素依赖型糖尿病(2型糖尿病)。根据其代谢和非代谢作用,它被推荐使用。它对2型糖尿病的代谢控制有明显的有益作用。血糖和血脂水平降低。降糖作用是继发于胰岛素分泌增强和胰岛素抵抗降低。前者是由于β细胞中K+三磷酸腺苷(ATP)通道的关闭。胰岛素对肝脏和肌肉的作用增强的机制尚不清楚。它似乎不涉及胰岛素受体,尽管糖原合成酶激活增强,但这可能不明确。事实证明很难将格列齐特的代谢作用与改善控制的作用分开。代谢作用可能也与过磺脲类相同。格列齐特除了改善自由基状态外,对血小板行为和功能以及内皮也有有益的影响。这些作用应该有利于糖尿病微血管病变的预防。预防糖尿病视网膜病变恶化的一些证据已经出现,但结果是可变的,需要更令人信服的研究。格列齐特的许多非代谢作用似乎是这种药物所独有的。因此,从代谢和非代谢的角度来看,格列齐特似乎是治疗饮食失败的2型糖尿病的合理选择。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Gliclazide: review of metabolic and vascular action].

Gliclazide is a second-generation sulfonylures that is widely used in the treatment of non-insulin-dependent diabetes mellitus (Type 2 diabetes). It has been recommended for use on the basis of both its metabolic and nonmetabolic effects. It has a clear beneficial effect on metabolic control in Type 2 diabetes. Blood glucose and lipid levels are lowered. The glucose-lowering effects are secondary to both enhanced insulin secretion and a decrease in insulin resistance. The former is due to closure of a K+ adenosine triphosphate (ATP) channel in the beta cell. The mechanism whereby insulin action on the liver and muscle are potentiated remains unknown. It does not appear to involve the insulin receptor, and although glycogen synthase activation is enhanced, this is probably not specified. It has proven difficult to separate the metabolic effects of gliclazide form the effects of improved control. The metabolic actions are probably also shared with over sulfonylureas. Gliclazide also has beneficial effects on platelet behavior and function and on the endothelium, in addition to improving free radical status. These effects should be beneficial for the prevention of diabetic microangiopathy. Some evidence has appeared for the prevention of deterioration of diabetic retinopathy, but results are variable and more convincing studies are required. Many of the nonmetabolic effects of gliclazide appear to be unique to this agent. Gliclazide thus appears to be a reasonable choice in the treatment of Type 2 diabetes with diet failure, both from the metabolic and non-metabolic standpoint.

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