Di Luigi Luigi, Baldari Carlo, Sgrò Paolo, Emerenziani Gian Pietro, Gallotta Maria Chiara, Bianchini Serena, Romanelli Francesco, Pigozzi Fabio, Lenzi Andrea, Guidetti Laura
Unit of Endocrinology, Department of Health Sciences, University of Rome Foro Italico, Piazza Lauro de Bosis, 15, 00194 Rome, Italy.
J Clin Endocrinol Metab. 2008 Sep;93(9):3510-4. doi: 10.1210/jc.2008-0847. Epub 2008 Jun 17.
Physical exercise-related stress activates hypothalamus-pituitary-adrenal (HPA) axis; nitric oxide is one of the mediators of the HPA axis response to stress, and phosphodiesterase type 5 inhibitors influences nitric oxide-linked biological activities.
The objective of the study was to investigate whether a single oral long half-life phosphodiesterase type 5 inhibitor (tadalafil) administration influences the HPA axis response to exercise-related stress.
This was a double-blind, cross-over trial.
Participants included nine healthy male athletes.
All subjects performed a maximal exercise test in normoxia, after which they received a single oral administration of tadalafil or placebo. Then after a 2-wk washout period, they were crossed over and repeated the exercise test. Each subject was his own control. Salivary collections, for steroid evaluations [cortisol, dehydroepiandrosterone sulphate (DHEAS), testosterone] and respective ratio calculation (DHEAS to cortisol, testosterone to cortisol, testosterone to DHEAS), were performed before each exercise (Pre-Ex), immediately after (Post-Ex), and at 30 min during recovery.
As expected, mean salivary cortisol concentration increased immediately after exercise after both tadalafil and placebo (P = 0.014 and P =0.036 vs. Pre-Ex, respectively); however, the cortisol increase was significantly higher after tadalafil administration (P = 0.034 vs. placebo). Furthermore, an increased salivary testosterone after exercise was observed only after tadalafil administration (P = 0.029 vs. Pre-Ex). No effects of either exercise and/or tadalafil administration on salivary DHEAS concentrations were observed. DHEAS to cortisol and testosterone to cortisol ratios significantly decreased after exercise after tadalafil administration (P = 0.037, and P = 0.02 vs. placebo, respectively).
Tadalafil administration amplified the salivary cortisol and testosterone responses to a maximal exercise-related stress in healthy trained humans.
与体育锻炼相关的应激会激活下丘脑-垂体-肾上腺（HPA）轴；一氧化氮是HPA轴对应激反应的介质之一，5型磷酸二酯酶抑制剂会影响一氧化氮相关的生物学活性。
本研究旨在调查单次口服长效5型磷酸二酯酶抑制剂（他达拉非）是否会影响HPA轴对运动相关应激的反应。
这是一项双盲交叉试验。
参与者包括9名健康男性运动员。
所有受试者在常氧条件下进行最大运动试验，之后他们单次口服他达拉非或安慰剂。然后经过2周的洗脱期后交叉并重复运动试验。每个受试者自身作为对照。在每次运动前（运动前）、运动后立即（运动后）以及恢复期间30分钟时收集唾液，用于类固醇评估[皮质醇、硫酸脱氢表雄酮（DHEAS）、睾酮]以及各自比值的计算（DHEAS与皮质醇的比值、睾酮与皮质醇的比值、睾酮与DHEAS的比值）。
正如预期的那样，服用他达拉非和安慰剂后运动后唾液皮质醇平均浓度均立即升高（分别与运动前相比，P = 0.014和P =0.036）；然而，服用他达拉非后皮质醇升高显著更高（与安慰剂相比，P = 0.034）。此外，仅在服用他达拉非后观察到运动后唾液睾酮升高（与运动前相比，P = 0.029）。未观察到运动和/或服用他达拉非对唾液DHEAS浓度有影响。服用他达拉非后运动后DHEAS与皮质醇以及睾酮与皮质醇的比值显著降低（分别与安慰剂相比，P = 0.037和P = 0.02）。
在健康训练有素的人群中，服用他达拉非会增强唾液皮质醇和睾酮对最大运动相关应激的反应。
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