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词汇介绍
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解析
terbutaline /tə'bju:təli:n/
释 义 n. 特布他林;间羟舒喘宁;间羟叔丁肾上腺素
例 句 A recent study conducted at Duke University illustrated the risk of terbutaline to infants. 最近杜克大学一项研究说明了特布他林对婴儿的危害。
概述
基本信息
药品“喘康速”药物成分为硫酸特布他林。硫酸特布他林化学式:(士)α-[(叔丁氨基)甲基]-3,5-二羟基苯甲醇硫酸盐(2:1)。硫酸特布他林分子式:(C12H19NO3)·H2SO4。硫酸特布他林分子量:548.66。
作用机制
特布他林(间羟叔丁肾上腺素)为高选择性β2受体激动药,对支气管β2受体的选择性与沙丁胺醇相似,对心脏的兴奋作用仅为沙丁胺醇的1/10。可舒张支气管平滑肌,并能抑制肥大细胞释放组胺等过敏物质,尚有增加纤毛-黏液毯廓清能力,促进痰液排出,减轻咳嗽症状。
药动学
口服生物利用度为15%±6%,30min后起效。不易被体内儿茶酚-O-甲基转移酶和单胺氧化酶这两种酶所代谢灭活,故作用可维持5~8h。血浆蛋白结合率为25%。2~4h作用达峰值。气雾剂吸入后5~15min显效,作用持续4h左右。皮下注射后5~15min起效,0.5~1h作用达峰值,持续1.5~4h。
适应症及用量
用于支气管哮喘、喘息性支气管炎、肺气肿等。
片剂:成人开始1~2周,1.25mg bid~tid,以后可增至2.5mg tid。
气雾吸入,0.25mg/喷,200喷/瓶,1喷/次,每日3~4次。
皮下注射,0.25mg/次,如15~30分钟无明显改善,可重复注射1次,但4小时内总量不能超过0.5mg。
禁忌症
对特布他林或其他肾上腺素受体激动剂过敏者禁用。高血压、冠心病、心功能不全、甲状腺功能亢进、闭角型青光眼患者和妊娠初期妇女禁用。
不良反应
主要为震颤、头痛、恶心、强直性痉挛、心动过速和心悸,大多在开始用药1-2周内自然消失。可能会发生皮疹和荨麻疹,睡眠失调和行为失调,如易激动、多动、坐立不安。
注意事项
1.大剂量应用可使有癫痫病史的患者发生酮症酸中毒。
2.长期应用可产生耐受性。
3.可能会引起低钾血症,当与黄嘌呤衍生物、类固醇、利尿药合用及缺氧的情况下需检测血清钾的浓度。
4.如果雾化液被意外弄进眼睛,应用水冲洗眼睛。
5.运动员慎用。
6.老年人或对本品敏感的患者,应从小剂量开始,以免引起心慌、手抖等症状。
Terbutaline Accumulates in Blood and Urine after Daily Therapeutic Inhalation复制标题
每日治疗性吸入后,特布他林在血液和尿液中积聚。
发表时间:2017-06-18
影响指数:4.5
作者: Nanna Krogh
期刊:Med Sci Sports Exerc
Elite athletes have a higher prevalence of asthma and exercise induced bronchoconstriction than the general population. Beta 2-adrenoceptor agonists (β 2-agonists) are considered first-line treatment of asthma to relieve bronchoconstriction. Therefore, β 2-agonists are commonly used by elite athletes, making them among the most used drugs in competitive sports. Given potential health risks and performance-enhancing effects of β 2-agonists, their use is restricted by the World Anti-Doping Agency (WADA). As of 2016, all β 2-agonists are prohibited, except therapeutic inhalation of salbutamol, salmeterol and formoterol. Terbutaline, which is commonly prescribed in Northern Europe, on the other hand, is prohibited, unless the athletes acquire a therapeutic use exemption (TUE) for inhalation in therapeutic doses pro re nata. Nevertheless, 4% of all adverse analytical findings in doping cases in 2014 where attributed to β 2 -agonists, with terbutaline accounting for 76%.
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