Systemic exposure and urinary cortisol effects of fluticasone propionate formulated with hydrofluoroalkane in 4- to 11-year-olds with asthma

J Clin Pharmacol. 2008 Jan;48(1):108-16. doi: 10.1177/0091270007309704.

Abstract

The systemic exposure of fluticasone propionate with hydrofluoroalkane propellant compared with chlorofluoro-carbon propellant and the effect of fluticasone propionate hydrofluoroalkane on 24-hour urinary cortisol in children aged 4 to 11 years with asthma were evaluated. Study 1 was an open-label, 2-way crossover study in which 16 subjects were randomized to 7.5 days each of fluticasone propionate hydrofluoroalkane 88 mug twice a day or fluticasone propionate chlorofluorocarbon 88 mug twice a day. In study 2, 63 subjects received 13.5 days of placebo followed by 27.5 days of fluticasone propionate hydrofluoroalkane 88 mug twice a day. The main outcome measure for study 1 was the difference between fluticasone propionate hydrofluoroalkane and fluticasone propionate chlorofluorocarbon in fluticasone propionate AUC(last) (area under the plasma fluticasone propionate concentration-time curve from zero up to the last quantifiable plasma concentration), and for study 2, 24-hour overnight urinary cortisol excretion. In study 1, fluticasone propionate systemic exposure was significantly lower (55%) with hydrofluoroalkane metered dose inhaler compared with chlorofluorocarbon metered dose inhaler. Study 2 showed no statistically significant changes in 24-hour overnight urinary cortisol excretion and no relationship to fluticasone propionate systemic exposure at this dose. The results of these 2 studies showed that in children aged 4 to 11 years with asthma, fluticasone propionate hydrofluoroalkane has lower systemic exposure compared with chlorofluorocarbon and no hypothalamic-pituitary-adrenal axis effects as measured by 24-hour urinary cortisol excretion.

Publication types

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

MeSH terms

  • Administration, Inhalation
  • Aerosol Propellants / chemistry
  • Androstadienes / blood
  • Androstadienes / pharmacokinetics
  • Androstadienes / therapeutic use*
  • Anti-Asthmatic Agents / administration & dosage
  • Anti-Asthmatic Agents / adverse effects
  • Anti-Asthmatic Agents / chemistry
  • Area Under Curve
  • Asthma / drug therapy*
  • Asthma / metabolism
  • Child
  • Child, Preschool
  • Chlorofluorocarbons / chemistry
  • Cough / chemically induced
  • Cross-Over Studies
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Female
  • Fever / chemically induced
  • Fluticasone
  • Half-Life
  • Headache / chemically induced
  • Humans
  • Hydrocarbons, Fluorinated / chemistry*
  • Hydrocortisone / analogs & derivatives
  • Hydrocortisone / urine*
  • Male
  • Metered Dose Inhalers
  • Nausea / chemically induced
  • Respiratory Tract Infections / chemically induced

Substances

  • Aerosol Propellants
  • Androstadienes
  • Anti-Asthmatic Agents
  • Chlorofluorocarbons
  • Hydrocarbons, Fluorinated
  • 6 beta-hydroxycortisol
  • Fluticasone
  • apaflurane
  • Hydrocortisone