Ephedrines in Over-the-Counter Cold Medicines and Urine Specimens Collected during Sport Competitions

Abstract

Ephedrine (EPH), pseudoephedrine (PEPH), phenylpropanolamine (PPA), and methylephedrine (MEPH) are ephedrine alkaloids commonly found in cold medications and are banned by the International Olympic Committee (IOC). These compounds were detected in the urinary doping tests during the national sport competitions in Taiwan. To study the sources of these compounds, 91 over-the-counter (OTC) nonprescription cold remedies, along with 1803 athletes' urine samples collected (from 1999 to 2001) in competitions were analyzed using gas chromatography-nitrogen-phosphorus detection (GC-NPD) for initial screening and GC-mass spectrometry (MS) for confirmation. We found that 80% of OTC cold medicines showed banned ephedrines in their ingredients lists, in which MEPH (52%) was the most common drug labeled. However, when these OTC cold medicines were analyzed by GC-NPD and GC-MS, EPH (35.4%) was found substantially higher than that labeled in the OTC products (1.3%). In the total urine specimens tested, approximately 2.8% contained banned ephedrines and 1.3% exceeded the IOC cutoff levels. Within the urine specimens that exceeded the IOC cutoff values, PEPH accounted for a 44% occurrence rate, followed by EPH (28%), PPA (17%), and MEPH (11%). In agreement with the other report, bodybuilders showed a high incidence rate for ephedrines misuse. Nevertheless, 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.

Investigação da presença de efedrinas em Ephedra tweediana Fisch & C.A. Meyer e em E. triandra Tul. (Ephedraceae) coletadas em Porto Alegre/RS

“…Muitos métodos têm sido relatados na literatura científi ca para detecção de efedrina em extratos vegetais, suplementos alimentares e amostras biológicas, utilizando as técnicas de cromatografi a à líquido de alta efi ciência (JP XIII, 1996;Gurley et al, 1998;Gmeiner et al, 2002), cromatografi a à gas (Garcia et al, 2005;Marchei et al, 2006), eletroforese capilar (MateusAvois et al, 2003) e espectrometria de massas (Gay et al, 2001;Spyridaki et al, 2001;Tseng et al, 2003). Entretanto, a maioria destes métodos está relacionada à análise de efedrinas em urina ou suplementos alimentares, reportando extensas fases de preparação da amostra e não permitindo efi ciente separação de EF e PEF (Spyridaki et al, 2001;Tseng et al, 2003), o que é de extrema importância em se tratando de análises toxicológicas, dopagem e monitoramento terapêutico, uma vez que ambos isômeros apresentam diferentes atividades farmacológicas e ações sobre o SNC, considerando que metodologias envolvendo detector de massas são preferidas em alto grau para identifi cação de substâncias contidas em produtos de origem desconhecida, esta foi à metodologia escolhida para a realização deste trabalho.…”

“…Entretanto, a maioria destes métodos está relacionada à análise de efedrinas em urina ou suplementos alimentares, reportando extensas fases de preparação da amostra e não permitindo efi ciente separação de EF e PEF (Spyridaki et al, 2001;Tseng et al, 2003), o que é de extrema importância em se tratando de análises toxicológicas, dopagem e monitoramento terapêutico, uma vez que ambos isômeros apresentam diferentes atividades farmacológicas e ações sobre o SNC, considerando que metodologias envolvendo detector de massas são preferidas em alto grau para identifi cação de substâncias contidas em produtos de origem desconhecida, esta foi à metodologia escolhida para a realização deste trabalho.…”

Comparison of urine analysis and dried blood spot analysis for the detection of ephedrine and methylephedrine in doping control

“…[3] They include ephedrine, pseudoephedrine, norephedrine, methylephedrine, cathine (norpseudoephedrine), and methylpseudoephedrine. [5] The misuse of ephedrine, methylephedrine, pseudoephedrine, and cathine by athletes is currently forbidden by the World Anti-Doping Agency (WADA). [5] The misuse of ephedrine, methylephedrine, pseudoephedrine, and cathine by athletes is currently forbidden by the World Anti-Doping Agency (WADA).…”

“…[5] The misuse of ephedrine, methylephedrine, pseudoephedrine, and cathine by athletes is currently forbidden by the World Anti-Doping Agency (WADA). [5,[7][8][9][10][11] Since the threshold levels for ephedrines were defined by the Medical Commission of the International Olympic Committee in 2001, [12] the current thresholds of ephedrine, methylephedrine, cathine, and pseudoephedrine have been set at 10 μg/mL, 10 μg/mL, 5 μg/mL, and 150 μg/mL, respectively. anabolic steroids, diuretics) or those that are only prohibited during in-competition (e.g.…”

Simultaneous Ion-Pair LC Analysis of Ephedrine and Pseudoephedrine in Rat Liver Microsomal Incubations: Application to In-Vitro Metabolism

“…1a, b), have been identified as the main pharmacologically active ingredients. EPH and PEPH are a pair of optical isomers also commonly found in 80% of overthe-counter cold medicines [2] and some weight-loss dietary supplements [3,4]. Reports of severe adverse events of EPH and PEPH associated with stimulation of the central nervous and cardiovascular systems have been common in recent years [5,6].…”