手性沙丁胺醇(R/S)人体药动学过程及其有效与安全性的相关研究进展  

Progress of Pharmacokinetics of Chiral Salbutamol(R/S)and Its Efficacy and Safety in Humans

作　　者：陈阳[1] 卢金淼[1] 蔡杰 王广飞[1] 张晓波 李智平[1] CHEN Yang;LU Jinmiao;CAI Jie;WANG Guangfei;ZHANG Xiaobo;LI Zhiping(Dept.of Clinical Pharmacy,National Children’s Medical Center/Children’s Hospital of Fudan University,Shanghai 201102,China;Dept.of Respiratory Medicine,National Children’s Medical Center/Children’s Hospital of Fudan University,Shanghai 201102,China)

机构地区：[1]国家儿童医学中心/复旦大学附属儿科医院临床药学部,上海201102 [2]国家儿童医学中心/复旦大学附属儿科医院呼吸科,上海201102

出　　处：《中国医院用药评价与分析》2023年第3期381-384,共4页Evaluation and Analysis of Drug-use in Hospitals of China

基　　金：上海市科学技术委员会科研项目(No.18DZ1910604)。

摘　　要：沙丁胺醇(SAL)是一种经典短效β2受体激动剂,能够舒张气道平滑肌,缓解支气管痉挛,抑制炎症因子释放,常用作平喘药。目前市售SAL以外消旋(R/S)混合物为主,其中R-SAL为优势异构体。R/S-手性SAL在药动学及药理作用方面存在差异,但由于药理学优势争议及经济因素,R-SAL尚未完全代替SAL。除应用于传统哮喘治疗外,SAL在罕见神经系统疾病领域有一定治疗潜力,在炎症与疼痛辅助治疗方面也有应用。在安全性方面,SAL有罕见不良反应报道,总体安全性高。本文对SAL对映异构体的区别及在其他领域的临床应用进展进行综述,为临床更好地应用该药提供参考。Salbutamol(SAL)is a classic short-actingβ2 adrenergic receptor agonist,which can alleviate airway smooth muscle,relieve bronchospasm,inhibit the release of inflammatory factors,and is commonly used as an antiasthmatic drug.Currently,commercially available SAL is dominated by racemic(R/S)mixtures,of which R-SAL is the dominant isomer.R/S-chiral SAL has different pharmacokinetics and pharmacological effects,yet R-Sal has not completely replaced SAL due to the controversy of pharmacological advantages and economic factors.In addition to the treatment of asthma,SAL has potential in the field of rare neurological diseases and in anti-inflammatory and pain adjuvant therapy.SAL has high safety while rare adverse drug reactions have been reported.This paper reviews the distinction between enantiomers of SAL and its application in other fields,and provide comprehensive reference for further clinical application.

关 键 词：沙丁胺醇 药动学 药效学 安全性 

分 类 号：R974.3[医药卫生—药品]