Cialis (Tadalafil) steady-state literature

This paper is from 2010, but I'd like to draw attention to it as steady-state has been emphasized in threads about HRT.

Reference

Here are some things covered in this study:



  • Steady state of tadalafil is reached after 5 days. This is probably why the Cialis website notes 4-5 days as being when you should see daily low dosages take effect.

  • Steady-state tadalafil plasma concentration is 1.6 times higher than that of a single dose.

  • Tadalafil 5mg once a day leads to a steady-state trough of 55 ng/mL, which corresponds to 90% PDE5 inhibition [style=font-style: italic;]in vitro[/style], which is the therapy standard likely to produce erections in most men.

  • It is recommended to not consume grapefruit, especially when on a daily dose protocol. It slows the excretion of tadalafil. The study suggests either on-demand exclusively and avoiding grapefruit before taking it, or the lowest possible daily dose(2.5mg once daily).


Based on what I know about grapefruit kinetics in the liver, liver processing of some pharmaceuticals will be slowed for 24 hours. If you use tadalafil on-demand and you have grapefruit or juice, wait at least 24 hours before taking a dose.

Also, others on the forum have also suggested splitting the dosage of tadalafil and taking once every 12 hours. Compared to a single daily dose, this would raise the trough level, but lower the peak for a more regular plasma concentration.
 

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Scientific Reference

Lakshman KM, Kaplan B, Travison TG, Basaria S, Knapp PE, Singh AB, LaValley MP, Mazer NA, Bhasin S. The effects of injected testosterone dose and age on the conversion of testosterone to estradiol and dihydrotestosterone in young and older men. J Clin Endocrinol Metab. 2010 Aug;95(8):3955-64.

DOI: 10.1210/jc.2010-0102 | PMID: 20534765 | PMCID: PMC2913038

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