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Clinical pharmacokinetics of procaterol: Dose proportionality after administration of single oral doses
Author(s) -
Eldon Michael A.,
Blake Debbie S.,
Coon Michael J.,
Nordblom Gerald D.,
Sedman Allen J.,
Colburn Wayne A.
Publication year - 1992
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510130904
Subject(s) - pharmacokinetics , urine , bronchodilator , oral administration , elimination rate constant , pharmacology , radioimmunoassay , oral dose , agonist , chemistry , medicine , volume of distribution , receptor , asthma
Procaterol is a potent, orally active β 2 ‐agonist bronchodilator useful in the treatment of reversible bronchospastic disease. It is effective when administered as single or multiple (Q8H) 50 and 75 μg doses. As part of the clinical development of procaterol, the pharmacokinetics and dose proportionality of single 25, 50, 75, and 100 μg doses were investigated in 14 healthy subjects. Serial blood samples were collected for 16 h and urine was quantitatively collected for 48 h following administration of each dose. Procaterol concentrations in plasma and urine were determined using sensitive and specific radioimmunoassay methods. Mean values for t max , the apparent elimination rate constant, Cl/ F , renal clearance, and per cent of dose excreted unchanged in urine were similar for all doses. Dose‐normalized AUC, C max , and amount excreted unchanged in urine ( A e ) were also similar across dosage levels. Thus, the pharmacokinetics of procaterol appear to be proportional to dose over the range of doses studied.