The Relevance of the Urinary Concentration of Ephedrines in Anti-Doping Analysis: Determination of Pseudoephedrine, Cathine, and Ephedrine After Administration of Over-the-Counter Medicaments

  title={The Relevance of the Urinary Concentration of Ephedrines in Anti-Doping Analysis: Determination of Pseudoephedrine, Cathine, and Ephedrine After Administration of Over-the-Counter Medicaments},
  author={Sabina Strano-Rossi and Daniele Leone and Xavier de la Torre and Francesco Botr{\`e}},
  journal={Therapeutic Drug Monitoring},
This article describes a method for the detection and quantitation of cathine, pseudoephedrine, ephedrine, and methylephedrine in urine, using their deuterated analogues as internal standards and derivatization to form the corresponding trimethylsilyl derivatives after a simple liquid-liquid extraction. The study was designed to evaluate whether the urinary cutoff values set by the World Anti-Doping Agency for the banned ephedrines (cathine >5 μg/mL, ephedrine and methylephedrine >10 μg/mL) can… 
Determination of urinary concentrations of pseudoephedrine and cathine after therapeutic administration of pseudoephedrine-containing medications to healthy subjects: implications for doping control analysis of these stimulants banned in sport.
The results of two WADA-sponsored clinical studies on the urinary excretion of PSE and its metabolite cathine following the oral administration of different PSE formulations to healthy individuals at therapeutic regimes show that the current analytical urinary threshold for the detection of PE as a doping agent in sport has been conservatively established at 150 µg/ml.
Detection and elimination profile of cathinone in equine after norephedrine (Propalin®) administration using a validated liquid chromatography–tandem mass spectrometry method
This is the first such report in any species where administration of norephedrine or ephedrine generates cathinone as the metabolite, and in equine detection of Cathinone in biological fluids could be due to administration of the potent stimulant cathin one or the nonpotent stimulant nore phedrine.
Pseudoephedrine and False‐Positive Immunoassay Urine Drug Tests for Amphetamine
The authors concluded that employers may “confidently make the correct decision to deny employment based only on the CEDIA urine drug test results,” but should exercise caution when interpreting nonnegative immunoassay results, as falsepositive results can and do occur.
Simultaneous identification of the enantiomers and diastereomers of N,O-di-trifluoroacetylated ephedrine and norephedrine in blood plasma using chiral capillary gas chromatography-mass spectrometry with selected ion monitoring.
This chiral capillary SIM GC-MS method was sufficiently effective in the analysis of plasma from users of over-the-counter cold medicines and was also fully applicable to the plasma analysis of guinea pigs following their treatment with racemic EP.
Electro-oxidation and adsorptive stripping voltammetric determination of ephedrine and pseudoephedrine at carboxylated multi-walled carbon nanotube-modified electrode
Carboxylated multi-walled carbon nanotubes (MWCNTs) were directly cast onto a glassy carbon electrode to fabricate a MWCNT-modified electrode. The modified electrode exhibited good promotion towards
Prevalence of legal and illegal stimulating agents in sports
This paper reviews the prevalence of legal and illegal stimulants in relation to doping-control analysis and highlights several early detection techniques including GC–NPD, GC–ECD, and TLC.
Current status and recent advantages in derivatization procedures in human doping control.
Its application is shown to broaden the detectable range of compounds, even in LC-MS analysis, where derivatization is not a prerequisite.
Bioanalytical techniques in discrimination between therapeutic and abusive use of drugs in sport.
The strategies of discrimination and the analytical methods used for the main groups of substances where the distinction is needed (β-2 agonists, ephedrines, glucocorticoids and morphine) will be reviewed.
Pseudoephedrine and circadian rhythm interaction on neuromuscular performance
Ingestion of a single dose of 180 mg of PSE results in enhanced lower body muscle contraction velocity against low and moderate loads only in the mornings, accompanied by undesirable side effects and an 11% risk of surpassing the doping threshold.
Pseudoephedrine and preexercise feeding: influence on performance.
Both plasma epinephrine and blood lactate concentrations were higher in the PSE compared with the PLA trials, and preexercise and postexercise urinary PSE concentrations were significantly higher than the threshold used by WADA to determine illicit PSE use.


Metabolites of ephedrines in human urine after administration of a single therapeutic dose.
Exretion studies of the ephedrine-related drugs have been performed to better understand the metabolic yields of ephedrines in urine and found that a single clinical dose of EPH may exceed threshold level in sport drug testing if the urine samples are tested within approximately 8h post-administration.
Elimination of ephedrines in urine following multiple dosing: the consequences for athletes, in relation to doping control.
Following therapeutic, multiple dosing, drug levels remain above the IOC cut-off levels for a minimum of 6 h and 16 h following final doses of phenylpropanolamine and pseudoephedrine, respectively.
Urinary excretion of chlorpheniramine and pseudoephedrine in humans.
In spite of expected changes in its biological half-life, the overall amount of unchanged pseudoephedrine excreted in urine was not affected by urine pH, presumably because it is primarily excreting in urine as intact drug.
Ephedrines in over-the-counter cold medicines and urine specimens collected during sport competitions.
It is likely that the high incidence of doping violations for ephedrine-related substances was related to misuse of ephedrines present in most OTC common cold medicines and some dietary supplements for relieving cold symptoms, reducing body weight, and preserving muscle.
Clinical Pharmacokinetics of Amfetamine and Related Substances
Because of the physicochemical properties of amfetamine-type stimulants, this group of drugs is one of the most suitable for drug testing in non-conventional matrices and has recently gained much attention because of its possible applications in clinical and forensic toxicology.
Investigation of the silylation of ephedrines using N-methyl-N-trimethylsilyl-trifluoroacetamide.
  • G. Forsdahl, G. Gmeiner
  • Chemistry, Medicine
    Journal of chromatography. B, Analytical technologies in the biomedical and life sciences
  • 2004
The gas chromatography--mass spectrometry method was found to be well suited for quantification of ephedrines in doping control.
Pharmacology of ephedra alkaloids and caffeine after single‐dose dietary supplement use
This work assessed the pharmacokinetics and pharmacodynamics of a dietary supplement that contains ma huang (Ephedra) and guarana (caffeine) and concluded that these herbal stimulants are safe and effective as dietary supplements.
Clinical pharmacokinetics of amphetamine and relates substances
  • Clin Pharmacokinet
  • 2004