Clinical Pharmacokinetics and Relative Bioavailability of Oral Procaterol

Publisher Website
Google Scholar
Abstract
The pharmacokinetics and relative oral bioavailability of procaterol, an orally active β2-adrenergic agonist bronchodilator were evaluated in healthy volunteers. Procaterol was rapidly absorbed after oral administration. Mean plasma procaterol concentration–time profiles and pharmacokinetic parameters for both formulations were essentially superimposable. Following tablet administration, the mean Cmax was 358 pg/mL and the corresponding mean tmax was 1.6 hr. Mean renal clearance was 163 mL/min and accounted for approximately one-sixth of the mean apparent oral plasma clearance (988 mL/min). The mean apparent elimination half-life of procaterol was 4.2 hr. Hepatic metabolism appears to be the primary mechanism for elimination of procaterol from the body, and first-pass metabolism may limit systemic bioavailability.