Additional studies on triamcinolone acetonide use and misuse in sports: Elimination profile after intranasal and high-dose intramuscular administrations

Abstract

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.

Periarticular Analgesic Injection Containing A Corticosteroid Reduces D-Dimer Levels After Total Hip Arthroplasty: Retrospective Comparative Cohort Study

“…It is an intermediate-acting glucocorticoid with a halflife between 18 and 36 hours [25,28]. Intramuscular administration of triamcinolone acetonide provides a slow absorption and prolonged duration [28,29]. In this study, CRP levels and CK levels on POD 7 were lower in the PAI group than in the control group.…”

“…Additionally, postoperative in ammation affects the immediate functional recovery after THA [31], and pain management following THA is important for early postoperative rehabilitation [32]. This study demonstrated the analgesic effect of PAI containing a corticosteroid on POD 7 owing to the anti-in ammatory effect of a corticosteroid that has a long duration of activity [28,29]. Therefore, the analgesic effect of PAI containing a corticosteroid may accelerate early postoperative rehabilitation.…”

Annual banned‐substance review: Analytical approaches in human sports drug testing 2019/2020

“…Investigations into the elimination of the legitimate use of intraarticular THA applications however demonstrated that urinary TA was determined at levels exceeding 30 ng/ml for up to 4 days. In addition, a profound impact of the intraarticular THA injection on plasma cortisol concentrations was observed, corroborating a systemic effect of the glucocorticoid application, leading to the conclusion that a revision of the currently permitted route of intraarticular drug administration is warranted 165 …”

“…Similarly, the metabolic transformation and elimination of triamcinolone acetonide (TA) as well as triamcinolone hexacetonide (THA) was studied, with TA being administered either intranasally (220 μg/day for 3 days) or intramuscularly (single dose, 40 mg), 165 and THA intraarticularly (single dose, 40 mg) 166 . Urinary TA concentrations remained below 3.5 ng/ml upon intranasal administrations, while the main metabolite 6β‐hydroxytriamcinolone increased to 93 ng/ml.…”

“…Aiming at supporting the differentiation of legitimate from illegitimate use of corticoids in sport, a series of elimination studies was conducted with various glucocorticoids including budesonide, triamcinolone (hex)acetonide, prednisone, and prednisolone, and time-aligned urinary concentrations of respective markers were determined. Budesonide was administered intranasally (256 μg/ Similarly, the metabolic transformation and elimination of triamcinolone acetonide (TA) as well as triamcinolone hexacetonide (THA) was studied, with TA being administered either intranasally (220 μg/ day for 3 days) or intramuscularly (single dose, 40 mg),165 and THA intraarticularly (single dose, 40 mg) 166. Urinary TA concentrations remained below 3.5 ng/ml upon intranasal administrations, while the main metabolite 6β-hydroxytriamcinolone increased to 93 ng/ml.…”