The phosphodiesterases type 5 inhibitor tadalafil reduces the activation of the hypothalamus-pituitary-adrenal axis in men during cycle ergometric exercise
Academic Article
Publication Date:
2012
abstract:
Objective: Phosphodiesterase type 5 (PDE5) inhibitors may influence human physiology,
health and performance by also modulating endocrine pathways. We evaluated the effects
of a two-days tadalafil administration on adenohypophyseal and adrenal hormones
adaptation to exercise in humans. Methods: fourteen healthy males were included in a
double blind crossover trial. Each volunteer randomly received two tablets of placebo or
tadalafil (20 mg/die with 36 h of interval) before a maximal exercise was performed.
After a two-week washout, the volunteers were crossed over. Blood samples were
collected -30, -15 min and immediately before exercise, immediately after, and during
recovery (+15, +30, +60 and +90 min) for adrenocorticotropin (ACTH), β-endorphin,
growth hormone (GH), prolactin (PRL), cortisol (C), corticosterone,
dehydroepiandrosterone-sulfate (DHEAS) and cortisol binding globulin (CBG) assays.
C/CBG (free cortisol index, FCI) and DHEAS/C ratios were calculated. Exercise
intensity, perceived exertion rate, O2 consumption, CO2 and blood lactate concentration
were evaluated. Results: ACTH, GH, C, corticosterone and CBG absolute concentrations
and/or areas under curve (AUC) increased after exercise after both placebo and tadalafil.
Exercise increased DHEAS only after placebo. Compared to placebo, tadalafil
administration reduced the ACTH, C, corticosterone and FCI responses to exercise and
was associated to higher β-endorphin AUC and DHEAS/C ratio during recovery, without
influencing cardio-respiratory and performance parameters. Conclusion: Tadalafil
reduced the activation of the hypothalamus-pituitary-adrenal axis during exercise by
probably influencing brain’s nitric oxide-cyclic guanosine monophosphate mediated
pathways. Further studies are necessary to confirm our results and to identify the involved
mechanisms, possible health risks and potential clinical uses.
health and performance by also modulating endocrine pathways. We evaluated the effects
of a two-days tadalafil administration on adenohypophyseal and adrenal hormones
adaptation to exercise in humans. Methods: fourteen healthy males were included in a
double blind crossover trial. Each volunteer randomly received two tablets of placebo or
tadalafil (20 mg/die with 36 h of interval) before a maximal exercise was performed.
After a two-week washout, the volunteers were crossed over. Blood samples were
collected -30, -15 min and immediately before exercise, immediately after, and during
recovery (+15, +30, +60 and +90 min) for adrenocorticotropin (ACTH), β-endorphin,
growth hormone (GH), prolactin (PRL), cortisol (C), corticosterone,
dehydroepiandrosterone-sulfate (DHEAS) and cortisol binding globulin (CBG) assays.
C/CBG (free cortisol index, FCI) and DHEAS/C ratios were calculated. Exercise
intensity, perceived exertion rate, O2 consumption, CO2 and blood lactate concentration
were evaluated. Results: ACTH, GH, C, corticosterone and CBG absolute concentrations
and/or areas under curve (AUC) increased after exercise after both placebo and tadalafil.
Exercise increased DHEAS only after placebo. Compared to placebo, tadalafil
administration reduced the ACTH, C, corticosterone and FCI responses to exercise and
was associated to higher β-endorphin AUC and DHEAS/C ratio during recovery, without
influencing cardio-respiratory and performance parameters. Conclusion: Tadalafil
reduced the activation of the hypothalamus-pituitary-adrenal axis during exercise by
probably influencing brain’s nitric oxide-cyclic guanosine monophosphate mediated
pathways. Further studies are necessary to confirm our results and to identify the involved
mechanisms, possible health risks and potential clinical uses.
Iris type:
1.1 Articolo in rivista
Keywords:
nitric oxide; exercise; tadalafil; ACTH; cortisol
List of contributors:
Di Luigi, L; Sgrò, P; Baldari, C; Gallotta, Mc; Emerenziani, Gp; Crescioli, C; Bianchini, S; Romanelli, F; Lenzi, A; and Guidetti, L.
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