Elimination of ephedrines in urine following multiple dosing: the consequences for athletes, in relation to doping control

Br J Clin Pharmacol. 2004 Jan;57(1):62-7. 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.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Blood Pressure / drug effects
  • Doping in Sports / prevention & control*
  • Double-Blind Method
  • Enzyme-Linked Immunosorbent Assay
  • Ephedrine / urine*
  • Heart Rate / drug effects
  • Humans
  • Male
  • Nasal Decongestants / urine*
  • Nonprescription Drugs
  • Phenylpropanolamine / urine*
  • Substance Abuse Detection / methods*
  • Sympathomimetics / urine*

Substances

  • Nasal Decongestants
  • Nonprescription Drugs
  • Sympathomimetics
  • Phenylpropanolamine
  • Ephedrine