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羟苯磺酸钙:与用于糖尿病视网膜病变相关的药理学概况。

Calcium dobesilate: pharmacological profile related to its use in diabetic retinopathy.

作者信息

Berthet P, Farine J C, Barras J P

机构信息

Biometrix SA, Gland, Switzerland.

出版信息

Int J Clin Pract. 1999 Dec;53(8):631-6.

PMID:10692760
Abstract

Calcium dobesilate (Doxium) is used in the treatment of diabetic retinopathy. Clinical studies show a slowdown of the progression of the disease after long-term oral treatment. The main action of the drug is related to a reduction of microvascular permeability as measured by different parameters and methods (vitreous fluorophotometry, retinal haemorrhages, skin capillary resistance, blood albumin leakage, blood viscosity) leading to improved visual acuity. The pharmacological activity may be explained in part by the antioxidant properties of calcium dobesilate and its action on endothelium through the synthesis of nitric oxide, increasing the endothelium-dependent relaxation. The antioxidant effect was demonstrated in different in vitro and in vivo models by decreasing the peritoneal permeability in rats induced by pro-oxidant substances. Moreover, vascular leakage was also decreased by calcium dobesilate in a reperfusion model in streptozotocin induced diabetic rats after ischaemia of the central artery of the retina. Doxium may also preserve vascular endothelial function by acting directly as antioxidant to protect lipids from peroxidation.

摘要

羟苯磺酸钙(多贝斯)用于治疗糖尿病视网膜病变。临床研究表明,长期口服治疗后该病的进展会减缓。该药物的主要作用与通过不同参数和方法(玻璃体荧光光度法、视网膜出血、皮肤毛细血管阻力、血液白蛋白渗漏、血液粘度)测量的微血管通透性降低有关,从而提高视力。其药理活性部分可通过羟苯磺酸钙的抗氧化特性及其通过一氧化氮合成对内皮细胞的作用来解释,增加内皮依赖性舒张。通过降低促氧化物质诱导的大鼠腹膜通透性,在不同的体外和体内模型中证明了抗氧化作用。此外,在链脲佐菌素诱导的糖尿病大鼠视网膜中央动脉缺血后的再灌注模型中,羟苯磺酸钙也降低了血管渗漏。多贝斯还可通过直接作为抗氧化剂保护脂质免受过氧化作用来维持血管内皮功能。

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