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Inhaled Corticosteroids in Asthma: A Dose‐Proportionality Study with Triamcinolone Acetonide Aerosol
Author(s) -
Zaborny B. A.,
Lukacsko P.,
BarinovColligon I.,
Ziemniak J. A.
Publication year - 1992
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1992.tb03863.x
Subject(s) - pharmacokinetics , triamcinolone acetonide , cmax , medicine , inhalation , crossover study , dosing , corticosteroid , anesthesia , pharmacology , radioimmunoassay , adverse effect , placebo , surgery , alternative medicine , pathology
The systemic exposure to triamcinolone acetonide (TAA) after inhalation of aerosolized drug has not been examined previously. This study evaluates the plasma concentrations, pharmacokinetics and dose proportionality of TAA after single oral inhalations at doses of 400, 800, and 1600 mcg. Nine moderately asthmatic male patients received each of the doses in a randomized crossover manner using a 1‐week washout period between dosing. Serial blood samples were collected for 10 hours postdosing for the determination of plasma TAA concentrations by using a specific radioimmunoassay. The pharmacokinetic profiles that were obtained showed slow and limited absorption over the first 4 hours after dosing followed by rapid elimination with a half‐life of approximately 2 hours (range: 1.8–2.3 hr). Comparison of pharmacokinetic parameters from each dose group showed excellent proportionality and consistent absorption for all patients. Mean C max values ranged from 0.51 ng/mL after the 400 mcg dose to 1.01 ng/mL and 1.97 ng/mL after the 800 and 1600 mcg doses, respectively. Mean AUC 0–10 values for these same doses were 2.6 ng × hr/mL, 5.3 ng × hr/mL and 10.5 ng × hr/mL, respectively. The results suggest that systemic exposure to TAA is minimal after oral inhalation, occurs in a dose proportional fashion, and produces circulating plasma concentrations which are unlikely to have significant adverse systemic effects.