背景:在竞技运动中,运动员使用β2-激动剂的高患病率使得人们倾向于推测非法使用β2-激动剂会提高成绩。然而,关于吸入β2-激动剂的潜在性能增强作用及其潜在分子基础的数据很少.
方法:总共,24名竞技耐力运动员(12f/12m)参加了一项临床双盲平衡四向阻滞交叉试验,以研究β2-激动剂沙丁胺醇(SAL)和福莫特罗(FOR)的单一与联合作用,评估SAL(1200µg,Cyclocaps,PbPharmaGmbH),对于(36微克,山德士,HEXALAG)和SAL+FOR(1200微克+36微克)与安慰剂(PLA,明胶胶囊含有乳糖一水合物,大学医院的药房乌尔姆)。测量包括骨骼肌基因和蛋白质表达,内分泌调节,尿/血清β2-激动剂浓度,心脏标志物,心肺功能和肺功能测试以及自行车测力计上的10分钟时间试验(TT)性能作为结果变量。血液和尿液样本收集前,post-,3小时后和24小时后TT。
结果:TT期间的平均功率输出在研究组之间没有差异。关于肺功能的治疗效果(p<0.001),观察到超声心动图(左心室收缩末期容积p=0.037;心内膜整体纵向应变p<0.001)和代谢变量(例如NR4A2和ATF3通路)对性能无任何影响。在女运动员中,SAL和FOR的血清β2激动剂总浓度较高.微阵列肌肉基因分析显示,SALFOR(NR4A2;p=0.001)对能量代谢中目标基因的治疗作用最强。在内分泌变量中,卵泡刺激素(TT后3小时),促黄体生成素(3小时Pre-TT)和胰岛素(Post-Pre-TT)浓度显示出治疗效果(所有p<0.05)。
结论:对SAL没有耐力表现增强作用,尽管对健康参与者的肺和心脏功能以及内分泌和代谢变量有急性影响,但与PLA相比,在允许的剂量内发现了FOR或SAL+FOR。联合β2-激动剂对分子和心脏水平的性能和性别特异性阈值的影响及其潜在的长期性能增强或健康影响仍有待确定。
背景:在EudraCT注册,编号:2015-005598-19(09.12.2015)和DRKS,编号为DRKS00010574(16.11.2021,回顾性注册)。
BACKGROUND: High prevalence rates of β2-agonist use among athletes in competitive sports makes it tempting to speculate that illegitimate use of β2-agonists boosts performance. However, data regarding the potential performance-enhancing effects of inhaled β2-agonists and its underlying molecular basis are scarce.
METHODS: In total, 24 competitive endurance athletes (12f/12m) participated in a clinical double-blinded balanced four-way block cross-over
trial to investigate single versus combined effects of β2-agonists salbutamol (SAL) and formoterol (FOR), to evaluate the potential performance enhancement of SAL (1200 µg, Cyclocaps, Pb Pharma GmbH), FOR (36 µg, Sandoz, HEXAL AG) and SAL + FOR (1200 µg + 36 µg) compared to placebo (PLA, Gelatine capsules containing lactose monohydrate, Pharmacy of the University Hospital Ulm). Measurements included skeletal muscle gene and protein expression, endocrine regulation, urinary/serum β2-agonist concentrations, cardiac markers, cardiopulmonary and lung function testing and the 10-min time
trial (TT) performance on a bicycle ergometer as outcome variables. Blood and urine samples were collected pre-, post-, 3 h post- and 24 h post-TT.
RESULTS: Mean power output during TT was not different between
study arms. Treatment effects regarding lung function (p < 0.001), echocardiographic (left ventricular end-systolic volume p = 0.037; endocardial global longitudinal strain p < 0.001) and metabolic variables (e.g. NR4A2 and ATF3 pathway) were observed without any influence on performance. In female athletes, total serum β2-agonist concentrations for SAL and FOR were higher. Microarray muscle gene analysis showed a treatment effect for target genes in energy metabolism with strongest effect by SAL + FOR (NR4A2; p = 0.001). Of endocrine variables, follicle-stimulating hormone (3 h Post-Post-TT), luteinizing hormone (3 h Post-Pre-TT) and insulin (Post-Pre-TT) concentrations showed a treatment effect (all p < 0.05).
CONCLUSIONS: No endurance performance-enhancing effect for SAL, FOR or SAL + FOR within the permitted dosages compared to PLA was found despite an acute effect on lung and cardiac function as well as endocrine and metabolic variables in healthy participants. The impact of combined β2-agonists on performance and sex-specific thresholds on the molecular and cardiac level and their potential long-term performance enhancing or health effects have still to be determined.
BACKGROUND: Registered at Eudra CT with the number: 2015-005598-19 (09.12.2015) and DRKS with number DRKS00010574 (16.11.2021, retrospectively registered).