Pseudoephedrine enhances performance in 1500-m runners / Kate Hodges, Sarah Hancock, Kevin Currell, Bruce Hamilton, Asker E. Jeukendrup. - (Medicine & Science in Sports & Exercise 38 (2006) 2 (February); p. 329-333)

• PMID: 16531903
• DOI: 10.1249/01.mss.0000183201.79330.9c

Abstract

Pseudoephedrine is an over-the-counter drug to relieve nasal and sinus congestion. Although it has been suggested that pseudoephedrine could be a stimulant and ergogenic aid, pseudoephedrine was recently removed from the banned substance list by the International Olympic Committee and placed on the monitoring program (from January 2004). It was felt that evidence was lacking for an ergogenic effect, although few studies have investigated the effects of pseudoephedrine on exercise performance. This study, therefore, aimed to investigate the effects of pseudoephedrine on 1500-m running performance.

Methods: In a double-blind, randomized crossover design, seven male athletes completed two 1500-m running trials on an outdoor track after having completed a familiarization trial. All trials were 7 d apart. After a 12-h overnight fast, subjects reported to the laboratory and received a standardized breakfast (energy asymptotically equal to 500 kcal 50% CHO). Subjects were given either 2.5 mg.kg(-1) bw pseudoephedrine or 2.5 mg.kg(-1) bw maltodextrins (placebo) in gelatin capsules 70 min before the start of the warm-up, which started 20 min before they ran 1500 m all-out. Pre- and postexercise blood samples were collected and analyzed for lactate and glucose concentrations, partial pressure of oxygen (PO2) and carbon dioxide (PCO2), and percent oxygen saturation.

Results: Pseudoephedrine significantly decreased time to completion of 1500-m time trials in the present study by 2.1% (from 279.65 +/- 4.36 s with placebo to 273.86 +/- 4.36 s with pseudoephedrine) with no reported side effects. No changes in the measured blood parameters were found, suggesting a central effect of pseudoephedrine rather than a metabolic effect.

Conclusion: The finding was that 2.5 mg.kg(-1) bw pseudoephedrine ingested 90 min preexercise improves 1500-m running performance.

Interpretation of urinary concentrations of pseudoephedrine and its metabolite cathine in relation to doping control / K. Deventer, P. Van Eenoo, G. Baele, O.J. Pozo, W. Van Thuyne, F.T. Delbeke. - (Drug Testing and Analysis 1 (2009) 5 (May); p. 209-213)

• PMID: 20355197
• DOI: 10.1002/dta.31

Abstract

Until the end of 2003 a urinary concentration of pseudoephedrine exceeding 25 microg/mL was regarded as a doping violation by the World Anti-Doping Agency. Since its removal from the prohibited list in 2004 the number of urine samples in which pseudoephedrine was detected in our laboratory increased substantially. Analysis of 116 in-competition samples containing pseudoephedrine in 2007 and 2008, revealed that 66% of these samples had a concentration of pseudoephedrine above 25 microg/mL. This corresponded to 1.4% of all tested in competition samples in that period. In the period 2001-2003 only 0.18% of all analysed in competition samples contained more than 25 microg/mL. Statistical comparison of the two periods showed that after the removal of pseudoephedrine from the list its use increased significantly. Of the individual sports compared between the two periods, only cycling is shown to yield a significant increase.Analysis of excretion urine samples after administration of a therapeutic daily dose (240 mg pseudoephedrine) in one administration showed that the threshold of 25 microg/mL can be exceeded. The same samples were also analysed for cathine, which has currently a threshold of 5 microg/mL on the prohibited list. The maximum urinary concentration of cathine also exceeded the threshold for some volunteers. Comparison of the measured cathine and pseudoephedrine concentrations only indicated a poor correlation between them. Hence, cathine is not a good indicator to control pseudopehedrine intake. To control the (ab)use of ephedrines in sports it is recommended that WADA reintroduce a threshold for pseudoephedrine.

Elimination of ephedrines in urine following multiple dosing: the consequences for athletes, in relation to doping control / Neil Chester, David R. Mottram, Thomas Reilly, Mark Powell. - (British Journal of Clinical Pharmacology 57 (2004) 1 (January); p. 62-67)

• PMID: 14678341
• PMCID: PMC1884418
• DOI: 10.1046/j.1365-2125.2003.01948.x

Abstract

Aims: To study the elimination of ephedrines with reference to the International Olympic Committee (IOC) doping control cut-off levels, following multiple dosing of over-the-counter decongestant preparations.

Methods: A double-blind study was performed in which 16 healthy male volunteers were administered either pseudoephedrine or phenylpropanolamine in maximal recommended therapeutic doses over a 36-h period. Urine was collected every two hours between 08:00 and 24:00 h and at 04:00 h throughout the testing period of three days. Urine drug levels were quantified using high performance liquid chromatography. Side-effects were assessed, including heart rate and blood pressure, every four hours between 08:00 and 20:00 h.

Results: Mean (95% CI) total phenylpropanolamine and pseudoephedrine eliminated unchanged was 75 (88, 61) and 81 (92, 71)%, respectively. Maximum urine concentrations of phenylpropanolamine and pseudoephedrine were 112.1 (164.2, 59.9) and 148.5 (215.0, 82.1) mg.l(-1), respectively. A peak in drug urine concentration occurred four hours following the final dose. There were no adverse cardiovascular effects and only mild CNS stimulation was evident.

Conclusions: 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. Athletes require informed advice on this from their healthcare professionals.

The effect of ephedra and caffeine on maximal strength and power in resistance-trained athletes / Andrew D. Williams, Paul J. Cribb, Matthew B. Cooke, Alan Hayes. - (Journal of Strength and Conditioning Research 22 (2008) 2 (March); p. 464-470)

• PMID: 18550961
• DOI: 10.1519/JSC.0b013e3181660320

Abstract

Caffeine and ephedrine-related alkaloids recently have been removed from International Olympic Committee banned substances lists, whereas ephedrine itself is now permissible at urinary concentrations less than 10 mug.mL. The changes to the list may contribute to an increased use of caffeine and ephedra as ergogenic aids by athletes. Consequently, we sought to investigate the effects of ingesting caffeine (C) or a combination of ephedra and caffeine (C + E) on muscular strength and anaerobic power using a double-blind, crossover design. Forty-five minutes after ingesting a glucose placebo (P: 300 mg), C (300 mg) or C + E (300 mg + 60 mg), 9 resistance-trained male participants were tested for maximal strength by bench press [BP; 1 repetition maximum (1RM)] and latissimus dorsi pull down (LP; 1RM). Subjects also performed repeated repetitions at 80% of 1RM on both BP and LP until exhaustion. After this test, subjects underwent a 30-second Wingate test to determine peak anaerobic cycling power, mean power, and fatigue index. Although subjects reported increased alertness and enhanced mood after supplementation with caffeine and ephedra, there were no significant differences between any of the treatments in muscle strength, muscle endurance, or peak anaerobic power. Our results do not support the contention that supplementation with ephedra or caffeine will enhance either muscle strength or anaerobic exercise performance.

Regulation of muscle fiber type and running endurance by PPARdelta (Addendum) / Yong-Xu Wang, Chun-Li Zhang, Ruth T. Yu, Helen K. Cho, Michael C. Nelson, Corinne R. Bayuga-Ocampo, Jungyeob Ham, Heonjoong Kang, Ronald M. Evans. - (PLoS Biology 3 (2005) 1 (January); e61)

Regulation of muscle fiber type and running endurance by PPARdelta / Yong-Xu Wang, Chun-Li Zhang, Ruth T. Yu, Helen K. Cho, Michael C. Nelson, Corinne R. Bayuga-Ocampo, Jungyeob Ham, Heonjoong Kang, Ronald M. Evans. - (PLoS Biology 2 (2004) 10 (October); e294, p. 1532-1539)

• PMID: 15328533
• PMCID: PMC509410
• DOI: 10.1371/journal.pbio.0020294

Erratum in:

• PLoS Biol. 2005 Jan;3(1):e61
• DOI: 10.1371/journal.pbio.0030061

Abstract

Endurance exercise training can promote an adaptive muscle fiber transformation and an increase of mitochondrial biogenesis by triggering scripted changes in gene expression. However, no transcription factor has yet been identified that can direct this process. We describe the engineering of a mouse capable of continuous running of up to twice the distance of a wild-type littermate. This was achieved by targeted expression of an activated form of peroxisome proliferator-activated receptor delta (PPARdelta) in skeletal muscle, which induces a switch to form increased numbers of type I muscle fibers. Treatment of wild-type mice with PPARdelta agonist elicits a similar type I fiber gene expression profile in muscle. Moreover, these genetically generated fibers confer resistance to obesity with improved metabolic profiles, even in the absence of exercise. These results demonstrate that complex physiologic properties such as fatigue, endurance, and running capacity can be molecularly analyzed and manipulated.

The physiology of growth hormone and sport / W. Matthew Widdowson, Marie-Louise Healy, Peter H. Sönksen, James Gibney. - (Growth Hormone & IGF Research 19 (2009) 4 (August); p. 308-319)

• PMID: 19505835
• DOI: 10.1016/j.ghir.2009.04.023

Abstract

The growth hormone (GH)/ insulin-like growth factor-I (IGF-I) axis exerts short-and long-term metabolic effects that are potentially important during exercise. Exercise is a potent stimulus to GH release and there is some evidence that the acute increase in GH is important in regulating substrate metabolism post-exercise. Regular exercise also increases 24-hour GH secretion rates, which potentially contributes to the physiologic changes induced by training. The effects of GH replacement in GH-deficient adults provide a useful model with which to study the effects of the more long-term effects of the GH/ IGF-I axis. There is convincing evidence that GH replacement increases exercise capacity. Measures of exercise performance including maximal oxygen uptake (VO2max) and ventilatory threshold (VeT) are impaired in GH deficiency and improved by GH replacement, probably through some combination of increased oxygen delivery to exercising muscle, increased fatty acid availability with glycogen sparing, increased muscle strength, improved body composition and improved thermoregulation. Administration of supraphysiologic doses of GH to athletes increases fatty acid availability and reduces oxidative protein loss particularly during exercise, and increases lean body mass. It is not known whether these effects translate to improved athletic performance, although recombinant human GH is known to be widely abused in sport. The model of acromegaly provides evidence that long-term GH excess does not result in improved performance but it is possible that a "window" exists in which the protein anabolic effects of supraphysiologic GH might be advantageous.

Implementation of the biological passport : the experience of the International Cycling Union / Mario Zorzoli, Francesca Rossi. - (Drug Testing and Analysis 2 (2010) 11-12 (November); p. 542-547). - Special Issue: 28th Cologne Workshop: Advances in Sports Drug Testing

• PMID: 21204287
• DOI: 10.1002/dta.173

Abstract

The concept of the biological passport is to evaluate, on an individual and longitudinal basis, the effects of doping substances and prohibited methods--blood doping and gene doping--on the body. Indirect biological markers can be measured and used to establish an individual's biological profile, when variations in an athlete's profile are found to be incompatible with physiological or medical conditions; a disciplinary procedure may be launched on the presumption that a prohibited substance or method has been used. As such, an athlete with a biological passport is his or her own reference. The International Cycling Union (UCI) launched the biological passport programme in January 2008 in cooperation with the World Anti-Doping Agency (WADA). The UCI programme includes more than 850 athletes. These athletes are subject to urinary and blood anti-doping tests both in- and out-of-competition several times a year. Almost 20 000 samples were collected in 2008 and 2009. In this article, the real-time process from sample collection to the opening of a disciplinary procedure is described. The establishment of this large-scale programme is discussed; the modalities which have to be applied and the difficulties encountered are presented. As for the results, some examples of normal and abnormal profiles are illustrated and indirect deterrent advantages of the programme are shown. Suggestions to improve the efficacy of the fight against doping through the implementation of the biological passport are discussed.

Detection of EPO doping and blood doping: the haematological module of the Athlete Biological Passport / Yorck Olaf Schumacher, Martial Saugy, Torben Pottgiesser, Neil Robinson. - (Drug Testing and Analysis 4 (2012) 11 (November); p. 846-853). - Special Issue: Sports drug testing for erythropoiesis‐stimulating agents and autologous blood transfusion

• PMID: 22374784
• DOI: 10.1002/dta.406

Abstract

The increase of the body's capacity to transport oxygen is a prime target for doping athletes in all endurance sports. For this pupose, blood transfusions or erythropoiesis stimulating agents (ESA), such as erythropoietin, NESP, and CERA are used. As direct detection of such manipulations is difficult, biomarkers that are connected to the haematopoietic system (haemoglobin concentration, reticulocytes) are monitored over time (Athlete Biological Passport (ABP)) and analyzed using mathematical models to identify patterns suspicious of doping. With this information, athletes can either be sanctioned directly based on their profile or targeted with conventional doping tests. Key issues for the appropriate use of the ABP are correct targeting and use of all available information (e.g. whereabouts, cross sectional population data) in a forensic manner. Future developments of the passport include the correction of all concentration-based variables for shifts in plasma volume, which might considerably increase sensitivity. New passport markers from the genomic, proteomic, and metabolomic level might add further information, but need to be validated before integration into the passport procedure. A first assessment of blood data of federations that have implemented the passport show encouraging signs of a decreased blood-doping prevalence in their athletes, which adds scientific credibility to this innovative concept in the fight against ESA- and blood doping.

Detection of homologous blood transfusion / S.C. Voss, M. Thevis, T. Schinkothe, W. Schänzer. - (International Journal of Sports Medicine 28 (2007) 8 (August); p. 633-637)

• PMID: 17614019
• DOI: 10.1055/s-2007-965076

Abstract

The aim of the present study was to improve and validate a flow cytometric method for the detection of homologous blood transfusion in doping control analysis. A panel of eight different primary antibodies and two different phycoerythrin-conjugated secondary antibodies was used for the detection of different blood populations. The flow cytometer used in this study was the BD FACSArray instrument. Mixed red blood cell populations were prepared from phenotype known donors. Linearity, specificity, recovery, precision, robustness and interday-precision were tested for every primary antibody used in the presented assay. The technique of signal amplification was utilized for an improved separation of antigens with weak or heterozygous expression to improve the interpretation of histograms. The resulting method allowed to clearly identify mixed red blood cell populations in homologous blood transfusion samples containing 0.3 - 2.0 % of donor blood.