Pharmacokinetics and acute safety of inhaled testosterone in postmenopausal women

J Clin Pharmacol. 2005 Feb;45(2):177-84. doi: 10.1177/0091270004269840.


This was a preliminary feasibility study to assess the pharmacokinetics and acute safety of a single dose of orally inhaled testosterone via the AERx system, a novel handheld aerosol delivery system in postmenopausal women. Twelve postmenopausal women stabilized on oral estrogen therapy were treated with a single dose of testosterone (0.1, 0.2, or 0.3 mg) by inhalation. Plasma concentrations of sex steroids were measured between 1 and 360 minutes. Pulmonary and cardiovascular adverse events were monitored. Inhaled testosterone produced a dose-dependent increase in plasma total and free testosterone. At the highest dose (0.3 mg), total and free testosterone increased from baseline (mean +/- SD, 0.6 +/- 0.3 nmol/L, 2.5 +/- 1.0 pmol/L) to maximum levels of 62.6 +/- 20.4 nmol/L (total) and 168.2 +/- 50.2 pmol/L(free), occurring 1 to 2 minutes after dosing. A 2-compartment model best described the free and total testosterone pharmacokinetic profile. Dihydrotestosterone levels were higher than baseline at 60 minutes (P < .0002). Estradiol did not vary, but sex hormone binding globulin and albumin fell. There were no adverse events related to the treatment. Administration of inhaled testosterone is safe and achieves a supraphysiologic "pulse" kinetic profile of total and free testosterone with a rapid return to pretreatment levels.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Inhalation*
  • Area Under Curve
  • Blood Pressure / drug effects
  • Blood Pressure / physiology
  • Cough / chemically induced
  • Dihydrotestosterone / metabolism
  • Dose-Response Relationship, Drug
  • Female
  • Half-Life
  • Humans
  • Middle Aged
  • Nebulizers and Vaporizers
  • Patient Selection
  • Postmenopause / drug effects*
  • Postmenopause / physiology
  • Sex Hormone-Binding Globulin / metabolism
  • Testosterone / administration & dosage
  • Testosterone / metabolism
  • Testosterone / pharmacokinetics*
  • Time Factors
  • Treatment Outcome
  • Vital Capacity / drug effects


  • Sex Hormone-Binding Globulin
  • Dihydrotestosterone
  • Testosterone