A GC-MS method for the determination of sildenafil, vardenafil and tadalafil and their metabolites in human urine

Sabina Strano Rossi, Luca Anzillotti, Xavier De La Torre, Francesco Botrè

Risultato della ricerca: Contributo in rivistaArticolo in rivistapeer review

45 Citazioni (Scopus)


Sildenafil (SDF), vardenafil (VDF) and tadalafil (TDF) are phosphodiesterase type 5 enzyme inhibitors (PDE5Is), used in the treatment of erectile disorders and to improve breathing efficiency in pulmonary hypertension. The increasing incidence of their use among young athletes has drawn the attention of the anti-doping authorities to the possible abuse of PDE5Is by athletes due to their pharmacological activities. This paper describes a method for the determination in urine of PDE5Is and their metabolites by gas chromatography/mass spectrometry (GC/MS) after liquid/liquid extraction of the analytes from urine and derivatisation to obtain trimethylsilyl derivatives. The metabolic profile was studied on real samples collected from subjects taking PDE5Is (Viagra, Levitra or Cialis); the main urinary metabolites were identified and their MS fragmentation characterized. The sample pre-treatment and GC/MS conditions for the detection of the metabolites have been optimised. A method for their preliminary screening and subsequent confirmation is described that takes into account the general requirements of a routine doping analysis to be used for the screening of large numbers of samples. The main metabolites identified can be included in a general purpose screening method and all the metabolites in a more specific confirmation method. The method developed has been applied for the screening of PDE5Is in 5000 urine samples. Based on the obtained results, the proposed method appears to be of practical use in analytical and forensic toxicology, including doping analysis.
Lingua originaleEnglish
pagine (da-a)1697-1706
Numero di pagine10
RivistaRapid Communications in Mass Spectrometry
Stato di pubblicazionePubblicato - 2010


  • PDE5Is analysis, sildenafil metabolites, vardenafil metabolites, tadalafil metabolites, GC/MS


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