IMIM (Hospital del Mar Medical Research Institute), Doping Control Research Group, Catalonian Antidoping Laboratory, Barcelona, Spain; Department of Experimental and Health Sciences, Universitat Pompeu Fabra, Barcelona, Spain.
IMIM (Hospital del Mar Medical Research Institute), Doping Control Research Group, Catalonian Antidoping Laboratory, Barcelona, Spain.
Steroids. 2019 Nov;151:108464. doi: 10.1016/j.steroids.2019.108464. Epub 2019 Jul 22.
Triamcinolone acetonide (TA) is a glucocorticoid (GC) widely used in sports medicine. GCs are prohibited in sports competitions by oral, intramuscular (IM), intravenous and rectal administrations, and they are allowed by other routes considered of local action such as intranasal administration (INT). We examined the urinary profiles of TA and its metabolites after INT and high-dose IM administrations. We also measured concentrations of TA and cortisol (CORT) in plasma following IM administration. TA was administered to healthy volunteers using INT route (220 μg/day for 3 days, n = 4 males and 4 females) or IM route (single dose of 40 mg, n = 4 males and 4 females and single dose 80 mg, n = 4 males). Urine and plasma samples were collected before and after administration at different time periods, and were analysed by liquid chromatography-tandem mass spectrometry. TA concentrations in urine were constant during 23 days after IM injection (range 1.4-129.0 ng/mL), and were very low after INT administration (range 0.0-3.5 ng/mL). For 6β-hydroxy-triamcinolone, the main TA metabolite, higher concentrations were detected (0.0-93.7 ng/mL and 15.7-973.9 ng/mL after INT and IM administrations, respectively). On the other hand, TA was detected in all plasma samples collected during 23 days after IM administration (range 0.2-5.7 ng/mL). CORT levels were largely suppressed after IM injection, and were recovered in a dose-dependent manner. In view of the results obtained, we propose a reporting level of 5 ng/mL for TA to distinguish forbidden from allowed TA administrations in sports. We also suggest that other GCs with faster urinary elimination from the body should be considered for IM therapies in out-of-competition rather than TA, in order to reduce the possibility of reporting false adverse analytical findings.
曲安奈德（TA）是一种在运动医学中广泛使用的糖皮质激素（GC）。GC 通过口服、肌肉内（IM）、静脉和直肠给药在运动竞赛中被禁止，而通过其他被认为具有局部作用的途径，如鼻腔内给药（INT），则被允许。我们检查了 INT 和高剂量 IM 给药后 TA 及其代谢物在尿液中的特征。我们还测量了 IM 给药后血浆中 TA 和皮质醇（CORT）的浓度。TA 通过 INT 途径（4 名男性和 4 名女性，每天 220μg，连续 3 天）或 IM 途径（40mg 单剂量，4 名男性和 4 名女性和 80mg 单剂量，4 名男性）给予健康志愿者。在不同的时间段内，在给药前和给药后采集尿液和血浆样本，并通过液相色谱-串联质谱法进行分析。在 IM 注射后 23 天内，尿液中的 TA 浓度保持不变（范围 1.4-129.0ng/mL），而在 INT 给药后非常低（范围 0.0-3.5ng/mL）。对于主要的 TA 代谢物 6β-羟基曲安奈德，检测到更高的浓度（INT 和 IM 给药后分别为 0.0-93.7ng/mL 和 15.7-973.9ng/mL）。另一方面，在 IM 给药后 23 天内采集的所有血浆样本中均检测到 TA（范围 0.2-5.7ng/mL）。IM 注射后 CORT 水平受到极大抑制，并呈剂量依赖性恢复。鉴于所获得的结果，我们提出了 5ng/mL 的 TA 报告水平，以区分运动中禁止和允许的 TA 给药。我们还建议，在非比赛期间，应考虑使用其他在体内更快消除的 GC 进行 IM 治疗，而不是 TA，以降低报告假阳性分析结果的可能性。
