Pharmacokinetics of Terazosin Enantiomers in Healthy Chinese Male Subjects

• Published in: Chirality (New York, N.Y.) Vol. 24; no. 12; pp. 1047 - 1050
• Main Authors: Liu, Man, Zhang, Dan, Yang, Man, Zhao, Ting, Wang, Xiaolin, Zhang, Yanan, Han, Jing, Liu, Huichen
• Format: Journal Article
• Language: English
• Published: United States Blackwell Publishing Ltd 01.12.2012; Wiley Subscription Services, Inc
• Subjects: Adult; Asian Continental Ancestry Group; Blood Chemical Analysis - methods; Chirality; Chromatography, High Pressure Liquid; determination; enantiomer; Enantiomers; Health; HPLC-FD; Humans; Male; Males; Pharmacokinetics; plasma; Prazosin - analogs & derivatives; Prazosin - blood; Prazosin - chemistry; Prazosin - pharmacokinetics; Spectrometry, Fluorescence; Stereoisomerism; terazosin; Young Adult
• ISSN: 0899-0042; 1520-636X; 1520-636X
• DOI: 10.1002/chir.22095

ABSTRACT The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2‐mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma concentrations of (+)‐(R)‐terazosin at all time points were higher than those of (−)‐(S)‐terazosin. The area under the plasma concentration–time curve (AUC0–∞) and maximum plasma concentration of (+)‐(R)‐terazosin were significantly greater than those of the (−)‐(S)‐terazosin (P < 0.01, respectively). The R/S ratio of AUC0–∞ of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. Chirality 24:1047–1050, 2012. © 2012 Wiley Periodicals, Inc.