Hormone Use and Abuse

Lanfranco, Fabio; Motta, Gabriela Almeida

doi:10.1016/b978-0-12-801238-3.00103-3

Cited by 1 publication

(2 citation statements)

References 119 publications

(158 reference statements)

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“…For indeed, glucocorticoids exert a beneficial impact on muscle responsiveness and recovery during sport performances, by increasing the availability of metabolic substrates and reducing the feeling of fatigue and the pain of efforts, especially if systemically and short‐term administered 13–15 . The WADA have therefore restricted their use in sport, also considering the several adverse reactions they can induce 16,17 . According to the current limitations, glucocorticoids are banned if administered by any injectable, oral and rectal routes during competition.…”

Section: Introductionmentioning

confidence: 99%

“… 13 , 14 , 15 The WADA have therefore restricted their use in sport, also considering the several adverse reactions they can induce. 16 , 17 According to the current limitations, glucocorticoids are banned if administered by any injectable, oral and rectal routes during competition. A reporting level of 30 ng/ml was initially established by the WADA to discriminate the allowed (topical) and the prohibited (systemic) administration.…”

Section: Introductionmentioning

confidence: 99%

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Urinary excretion profile of prednisolone and prednisone after rectal administration: Significance in antidoping analysis

Iannella

Comunità

Botrè

et al. 2022

Drug Testing and Analysis

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The rectal administration of glucocorticoids, as well as any injectable, and oral ones, is currently prohibited by the World Anti-Doping Agency when occurs "in competition." A reporting level of 100 ng/ml for prednisolone and 300 ng/ml for prednisone was established to discriminate the allowed and the prohibited administration. Here, the urinary excretion profiles of prednisone and prednisolone were evaluated in five volunteers in therapy with glucocorticoid-based rectal formulations containing prednisone or prednisolone caproate. The urinary levels of the excreted target compounds were determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) following the procedure validated and currently in use in our laboratory to detect and quantitate glucocorticoids in urine. Predictably, the excretion trend of the analytes of interest were generally comparable with those obtained after oral administration, even if the excretion profile showed a broad interindividual variability, with the absorption rate and the systemic bioavailability after rectal administration being strongly influenced by the type of formulations (suppository or rectal cream, in our case) as well as the physiological conditions of the absorption area. Results showed that the target compounds were detectable for at least 30 h after drug administration. After suppository administration, prednisolone levels reached the maximum after 3 h from drug administration and then dropped below the reporting level after 15-21 h; prednisone reached the maximum after 3 h from drug administration, and then dropped below the reporting level after 12-15 h. After cream administration, both prednisone and prednisolone levels remained in a concentration below the reporting level throughout the entire monitored period.

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Section: Introductionmentioning

confidence: 99%