由于其独特的替米沙坦是一种很有前途的代谢疾病sartan PPAR-gamma-inducing财产。

文章的细节

引用

复制到剪贴板

山,竹内M

由于其独特的替米沙坦是一种很有前途的代谢疾病sartan PPAR-gamma-inducing财产。

地中海假设。2005;64 (3):476 - 8。

PubMed ID

15617852 (在PubMed

]

文摘

代谢综合征与胰岛素抵抗密切相关,由一系列因素如高血压和高脂血症,提高心血管疾病和糖尿病的风险。事实上,高血压发生大约两倍经常在糖尿病患者与非糖尿病控制。相反,高血压患者更有可能比血压正常的人患糖尿病。此外,多达75%的心血管疾病的糖尿病患者可以归因于高血压。因此,治疗高血压患者胰岛素抵抗的主要目标是2型糖尿病和心血管疾病的预防。然后,什么是最佳的抗高血压靶器官保护方法在这些病人吗?几个临床试验表明,肾素-血管紧张素系统(RAS)的pathogensis扮演关键的角色在糖尿病胰岛素抵抗和心血管疾病。中断的RAS angiotensin-coverting酶抑制剂(acei)或血管紧张素ⅱ1型受体拮抗剂(arb)已被证明,以防止糖尿病高血压患者的发病和减少心血管和肾脏疾病进展与高血压糖尿病患者。然而,我们是否应该推荐ARBs药物对胰岛素resistant-hypertensive病人或2型糖尿病患者肾病由于其insulin-sensitizing财产仍有待澄清。最近,替米沙坦、ARB发现作为patrtial受体激动剂的过氧物酶体proliferator-activated receptor-gamma (- ppar)。 PPAR-gamma influences the gene expression involved in carbohydrate metabolism, and pioglitazone and rosiglitazone, ligands for PPAR-gamma, improve insulin resistance in diabetic patients. Furthermore, there is a growing body of evidence that activators of PPAR-gamma exert anti-inflammatory, anti-oxidative and anti-proliferative effects on vascular wall cells, thus decreasing the risks for atherosclerosis. We hypothesize here that due to its unique PPAR-gamma-modulating activity, telmisartan will become a promising 'cardiometabolic sartan', that targets both diabetes and CVD in hypertensive patients. In this paper, we would like to propose the possible ways of testing our hypothesis. Does telmisartan reduce the development of diabetes and CVD in insulin resistant patients pretreated with maximal doses of other ARBs? Does co-treatment with an activator of PPAR-gamma attenuate the effects of telmisartan in these patients? These clinical studies will provide further information whether the beneficial cardiometabolic actions of telmisartan could be ascribed to its PPAR-gamma-inducing property.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
替米沙坦	过氧物酶体proliferator-activated受体γ	蛋白质	人类	是的	部分激动剂	细节
替米沙坦	1型血管紧张素ⅱ受体	蛋白质	人类	是的	拮抗剂	细节