Excretion study of clomiphene in human urine: evaluation of endogenous steroids profile after multiple oral doses

Journal of the Brazilian Chemical Society

Dayamín Martínez Brito¹  Rodny Montes De Oca Porto¹  Margarita Teresa Correa Vidal¹  Roberto Socarrás Ojeda¹  Arístides Rosado Pérez¹ 

[1] ,Instituto de Medicina del Deporte Laboratorio Antidopin Ciudad de la Habana,Cuba

关键词: clomiphene;    gas chromatography-mass spectrometry;    oestrogens;    steroids profile;    doping control;   

DOI  :  10.1590/S0103-50532010001200008

来源: SciELO

【 摘 要 】

Selective estrogen receptor modulators are classified as prohibited substances according to the list of forbidden substances in sports by the International Olympic Committee and the World Anti-doping Agency. Clomiphene (2-(4-(2-chloro-1,2-diphenylethenyl)phenoxy)-N,N-diethyl-ethanamine) is mainly used for the treatment of infertility because it acts inducing the ovulation by direct stimulations of gonadotropic activity. Clomiphene citrate (50 mg per day for 5 days) was orally administered to one healthy female with infertility treatment. Urine samples were collected up to 1 week post-dose. A new metabolite using gas chromatography-mass spectrometry has been identified in addition to the hydroxyclomiphene previously reported. It has been proposed as hydroxymethoxyclomiphene. Monitorization of this metabolite have been proposed for doping control keeping in mind that the main metabolite hydroxyclomiphene is excreted relatively faster than hydroxymethoxyclomiphene from urine. On the other hand, significant changes on steroids profile after multiple doses were observed. The main variation was observed on absolute concentration of oestrogens and their ratios.

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