Doping Control Research Group, Catalonian Antidoping Laboratory, IMIM (Hospital del Mar Medical Research Institute), Barcelona, Spain.
Integrative Pharmacology and Systems Neuroscience Group, IMIM (Hospital del Mar Medical Research Institute), Barcelona, Spain.
Drug Test Anal. 2021 Mar;13(3):571-582. doi: 10.1002/dta.2966. Epub 2020 Nov 20.
Prednisolone (PRED) and prednisone (PSONE) are prohibited in sports competitions when administered by systemic routes, and they are allowed by other routes for therapeutic purposes. There is no restriction of use in out-of-competition periods. The present study aimed to evaluate the urinary excretion of PRED, PSONE, and their most important metabolites after systemic and nonsystemic treatments in order to verify the suitability of the current reporting level of 30 ng/ml used to distinguish allowed and prohibited administrations and to establish washout periods for oral treatments performed in out-of-competition periods. PRED was studied after dermatological administration (5 mg/day for 5 days, n = 6 males) and oral administration (5 mg, n = 6 males; 10 mg, n = 2 males). PSONE was studied after oral administration (10 mg, n = 2 males; 30 mg, n = 1 male and 1 female). Concentrations in urine were measured using an LC-MS/MS method. Concentrations after dermatological treatment were low for all metabolites. After oral administration, concentrations were very high during the first 24 h after administration ranging from 1.6 to 2261 ng/ml and from 4.6 to 908 ng/ml for PRED and PSONE, respectively. Concentrations of most of the metabolites measured were lower than 30 ng/ml from 24 h after all oral administrations. New reporting levels are proposed for PRED and PSONE considering data of our study and other information published after nonsystemic administrations of the compounds. Washout periods of at least 24 h are recommended to ensure no false positives when oral treatments need to be performed in out-of-competition periods.
泼尼松龙(PRED)和泼尼松(PSONE)经全身途径给药时在体育竞赛中被禁用,而经其他途径给药时用于治疗目的则被允许。在非比赛期间没有使用限制。本研究旨在评估全身和非全身治疗后 PRED、PSONE 及其最重要的代谢物在尿中的排泄情况,以验证目前用于区分允许和禁止给药的 30ng/ml 报告水平的适用性,并为非比赛期间进行的口服治疗建立冲洗期。PRED 经皮给药(5mg/天,共 5 天,n=6 名男性)和口服给药(5mg,n=6 名男性;10mg,n=2 名男性)后进行了研究。PSONE 经口服给药(10mg,n=2 名男性;30mg,n=1 名男性和 1 名女性)后进行了研究。使用 LC-MS/MS 方法测量尿液中的浓度。所有代谢物经皮治疗后的浓度均较低。口服给药后,在给药后 24 小时内浓度非常高,范围为 1.6 至 2261ng/ml 和 4.6 至 908ng/ml,分别为 PRED 和 PSONE。从所有口服给药后 24 小时开始,大多数测量的代谢物的浓度均低于 30ng/ml。考虑到我们的研究数据和其他非系统性给药后公布的信息,提出了 PRED 和 PSONE 的新报告水平。建议至少 24 小时的冲洗期,以确保在非比赛期间进行口服治疗时不会出现假阳性。