Efecto de una Dosis de 50 mg de Enantato de Noretisterona y 5 mg de Valerato de Estradiol en los Niveles de Testosterona Total en Hombres Mexicanos Sanos

Abstract

This clinical research was a clinical trial; analytic, open-label, prospective and logitudinal, which primary objective was to determine the effect of a single dose of 50 mg of noretisterone enanthate (E-NET) and 5 mg of estradiol valerate (VAL-E), in total testosterone (T) plasma concentrations from 32 healthy male Mexican subjects. All volunteers received a singledose of the combination on study day 0; blood samples were drawn on days -2, -1, 0, 1, 2, 3, 4, 5, 6, 7, 10, 14, 18, 22, 26 and 30 days with the purpose of measuring total testosterone plasma concentrations on days 0, 14, and 30; estradiol plasma concentrations on days -2, -1, and 0; and the bioavailability of NET y E2 on every sample from days 0 to 30. The incidence of adverse events was also registered. Total testosterone concentrations before investigational product administration were (mean ± SD) 5.03 ± 1.30 ng/mL, these values were reduced to 0.61 ± 0.55 ng/mL 14 days after the dose, and recovered to 3.75 ± 1.16 ng/mL for the day 30 of the study (p<0.05). These values demonstrated that E-NET y VAL-E dose suppress T plasma concentrations in this subjects. Noretisterone pharmacokinetics parameters were Cmáx=523.08±487.31pg/mL, AUC0-30d= 6459.95±2982.69 day*pg/mL, tmáx=7.06±4.85 days and Ke=0.0461±0.0162. Estradiol pharmacokinetics 19 parameters were: Cmáx= 368.31±146.74 pg/mL, AUC0-30d= 2,392.75±655.12 day*pg/mL, tmáx=2.5±1.16 days, Ke=0.1707±0.0774. Study subjects presented 9 non-serious adverse events during the study, from which only one had a relation (uncertain) to the investigational product.