Single- and multiple-dose pharmacokinetics of R-(−)- and S-(+)-prenylamine in man

✍ Scribed by Y. Gietl; H. Spahn; H. Knauf; E. Mutschler

• Publisher: Springer
• Year: 1990
• Tongue: English
• Weight: 616 KB
• Volume: 38
• Category: Article
• ISSN: 0031-6970
• DOI: 10.1007/bf00278587

✦ Synopsis

The pharmacokinetics of S-(+)- and R-(-)-prenylamine was studied in eight healthy volunteers given single and repeated oral doses of the racemic drug. Distinct differences in various pharmacokinetic parameters were found between the S- and R-enantiomer. The maximum plasma concentrations and AUCs of the R-enantiomer exceeded those of the S-enantiomer five-fold; the apparent oral clearance of the S-form was five-times and the renal clearance three-times higher than of the R-form. Acid catalyzed hydrolysis of urine samples released more S-prenylamine, indicating stereoselective glucuronidation of unchanged prenylamine. Plasma protein binding also differed between the two enantiomers, generally with a higher unbound fraction of the S-form, whereas analysis of the bound fractions showed that prenylamine was bound to different plasma proteins with inverse stereoselectivity.