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  • Indomethacin  (1)
  • Key words Corticosteroids; systemic effects  (1)
  • 1
    ISSN: 1432-1041
    Schlagwort(e): Key words Corticosteroids; systemic effects ; plasma cortisol suppression ; white blood cell count ; healthy volunteers
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Abstract The systemic effects of single and multiple doses of inhaled fluticasone propionate (FP) and budesonide were examined in 24 healthy male volunteers (age range 18–29 years). The study was of an open, placebo-controlled, randomized, three-way crossover design. On each study day, multiple blood samples were taken over a 20 h period after drug administration (after a single dose and after the last of seven doses) and area under the curve (AUC0–20) for plasma cortisol and white blood cell (WBC) counts was calculated. Results: The present study shows that multiple dosing with FP 1.0 mg b.i.d. for 3.5 days (seven doses) resulted in a marked cortisol suppression from placebo which, at 55%, was more than double that seen with a single dose (25% suppression). Multiple dosing with budesonide 0.8 mg b.i.d. resulted in a 34% suppression in plasma cortisol compared with a suppression of 26% with a single dose. The increase in systemic activity of FP after multiple dosing is confirmed by both the number of subjects with 0800 hours plasma cortisol values below normal limits and by the changes in WBC and differential counts. Conclusion: The results of the present study confirm previous findings with regard to the more marked systemic effect of FP following multiple dosing as compared with a single dose. This increase in systemic effect from single dosing to multiple dosing is significantly greater for FP than for budesonide.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 42 (1992), S. 301-305 
    ISSN: 1432-1041
    Schlagwort(e): Indomethacin ; Osteoarthritis ; pharmakokinetics ; intraarticular administration
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of intraarticular indomethacin was evaluated in 10 patients with osteoarthritis in an open labelled, randomized, cross-over study. Each patient received a single dose of 10 mg indomethacin by the intraarticular and the intravenous routes with a seven-day interval between the injections. Blood was repeatedly collected and urine was collected for 24 h after dosing. Indomethacin was rapidly absorbed from the joint, giving a maximum serum concentration (Cmax) of 0.60 μg · ml−1 approximately 1 h after dosing. The systemic bioavailability (f) was 80% and the mean absorption time (MAT) was about 2 h. The apparent terminal half-life and mean residence time (MRT) were 2.8 h and 4 h, respectively. The urinary recovery of total indomethacin (unchanged + glucuronides) was 24% of the dose and renal clearance (CLR) was estimated to be about 21 ml · min−1. The disposition of indomethacin after intravenous and intraarticular administration appeared to be similar. The results suggest that the intraarticular administration of indomethacin would not exclude the risk of developing untoward, systemic, concentration-dependent effects.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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