PPARS - Peroxisome Proliferator Activated Receptor Activators and Fibrates Actions

Sidney Carvalho Fernandes, A. Saldanha, A. Margeotto, A. Gasparoto, T. L. Martinez
{"title":"PPARS - Peroxisome Proliferator Activated Receptor Activators and Fibrates Actions","authors":"Sidney Carvalho Fernandes, A. Saldanha, A. Margeotto, A. Gasparoto, T. L. Martinez","doi":"10.33425/2639-944x.1194","DOIUrl":null,"url":null,"abstract":"Peroxisome Proliferator Activated Receptor sits part of the family of nuclear receptors, which has about 50 known receptors, including thyroid hormone receptors, which have the function of regulating metabolism and metabolizing and eliminating substances. These receptors, to act, must be activated by ligands, form a heterodmer with the retinoic acid receptor, recruit activating cofactors, release inhibitory cofactors to which they are bound, and then act on the responsive element of target gene. Three species of peroxisome proliferator activated receptor are known: PPARa, PPARγ and PPARβ (also known as PPARd or β/d). The prototypes of PPARa activators are the derivatives of fibricacid, of which the first representative was clofibrate, used as a lipid-lowering factor in the 1960s and 1970s. Although there may be a small variation among the various fibrates regarding the mechanism of action, these drugs are basically PPARa activators. In the action of fibrates, there is a reduction of triglycerides, with a decrease in the synthesis of VLDL, increase of HDL particles and transformation of small and dense LDL into larger, less dense LDL and with lower atherogenic potential. Fibrates are second-choice substances, and statins are the first for the treatment of hypertriglyceridemia. Fibrates are efficient for the treatment of patients with low HDL-C, decrease macro and microvascular disease of diabetic patients. The recommendation is do not associate gemfibrozil with statins. Other fibrates may be associated, and preference should be given to the association of statins that are not metabolized by CYP3A4: rosvastatin, pravastatin and fluvastatin.","PeriodicalId":231586,"journal":{"name":"Journal of Medical – Clinical Research & Reviews","volume":"116 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2021-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Medical – Clinical Research & Reviews","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.33425/2639-944x.1194","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

Abstract

Peroxisome Proliferator Activated Receptor sits part of the family of nuclear receptors, which has about 50 known receptors, including thyroid hormone receptors, which have the function of regulating metabolism and metabolizing and eliminating substances. These receptors, to act, must be activated by ligands, form a heterodmer with the retinoic acid receptor, recruit activating cofactors, release inhibitory cofactors to which they are bound, and then act on the responsive element of target gene. Three species of peroxisome proliferator activated receptor are known: PPARa, PPARγ and PPARβ (also known as PPARd or β/d). The prototypes of PPARa activators are the derivatives of fibricacid, of which the first representative was clofibrate, used as a lipid-lowering factor in the 1960s and 1970s. Although there may be a small variation among the various fibrates regarding the mechanism of action, these drugs are basically PPARa activators. In the action of fibrates, there is a reduction of triglycerides, with a decrease in the synthesis of VLDL, increase of HDL particles and transformation of small and dense LDL into larger, less dense LDL and with lower atherogenic potential. Fibrates are second-choice substances, and statins are the first for the treatment of hypertriglyceridemia. Fibrates are efficient for the treatment of patients with low HDL-C, decrease macro and microvascular disease of diabetic patients. The recommendation is do not associate gemfibrozil with statins. Other fibrates may be associated, and preference should be given to the association of statins that are not metabolized by CYP3A4: rosvastatin, pravastatin and fluvastatin.
PPARS -过氧化物酶体增殖物激活受体激活剂和贝特酸盐的作用
过氧化物酶体增殖物激活受体(Peroxisome Proliferator Activated Receptor)是核受体家族的一员,已知约有50种受体,其中包括甲状腺激素受体,具有调节代谢和代谢消除物质的功能。这些受体要发挥作用,必须被配体激活,与视黄酸受体形成异聚体,招募活化辅因子,释放与之结合的抑制性辅因子,然后作用于靶基因的应答元件。已知三种过氧化物酶体增殖物激活受体:PPARa, PPARγ和PPARβ(也称为PPARd或β/d)。PPARa活化剂的原型是纤维酸的衍生物,其中第一个代表是clofibrate,在20世纪60年代和70年代用作降脂因子。尽管不同的贝特类药物在作用机制上可能有微小的差异,但这些药物基本上都是PPARa激活剂。在贝特类药物的作用下,甘油三酯减少,VLDL合成减少,HDL颗粒增加,小而致密的LDL转化为大而不致密的LDL,具有较低的动脉粥样硬化潜力。贝特类药物是治疗高甘油三酯血症的第二选择,他汀类药物是治疗高甘油三酯血症的首选药物。贝特类药物能有效治疗低HDL-C患者,减少糖尿病患者的大血管和微血管病变。建议不要将吉非罗齐与他汀类药物联合使用。其他贝他汀类药物也可能与之相关,应优先考虑不被CYP3A4代谢的他汀类药物:罗伐他汀、普伐他汀和氟伐他汀。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信