Xenobiotica the fate of foreign compounds in biological systems
ISSN: 0049-8254 (Print) 1366-5928 (Online) Journal homepage: http://www.tandfonline.com/loi/ixen20
Pharmacokinetics and metabolism of oral doses of a 4′-methylthio derivative of propranolol in man T. Walle, U. K. Walle, T. D. Cowart, E. C. Conradi & T. E. Gaffney To cite this article: T. Walle, U. K. Walle, T. D. Cowart, E. C. Conradi & T. E. Gaffney (1990) Pharmacokinetics and metabolism of oral doses of a 4′-methylthio derivative of propranolol in man, Xenobiotica, 20:3, 321-331 To link to this article: http://dx.doi.org/10.3109/00498259009046850
Published online: 27 Aug 2009.
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Full Terms & Conditions of access and use can be found at http://www.tandfonline.com/action/journalInformation?journalCode=ixen20 Download by: [University of California, San Diego]
Date: 12 November 2015, At: 18:00
XENOBIOTICA,
1990, VOL. 20, NO. 3, 321-331
Pharmacokinetics and metabolism of oral doses of a 4'-methylthio derivative of propranolol in man T, WALLE, U. K. WALLE, T. D. COWARTV, E. C. CONRAD1 and T. E. GAFFNEY
Downloaded by [University of California, San Diego] at 18:00 12 November 2015
Departments of Cell and Molecular Pharmacology and Experimental Therapeutics and Medicine, Medical University of South Carolina, 171 Ashley Avenue, Charleston, SC 29425, U.S.A. Received 1 7 February 1989; revised 17 October 1989 1. The objective of this study was to determine the oral dose pharmacokinetics and metabolism of 4'-methylthiopropranolol (MTP) in man and compare the results with observations for propranolol in previous studies. 2. Three women and five men received single oral doses of MTP, dose range 5-320 mg. Plasma concentration of MTP over time were measured by gas chromatography-mass spectrometry. M T P metabolites in urine were identified by comparativehigh-performance liquid chromatographic (HPLC) retention times and mass spectrometry with previously characterized reference compounds and quantified by HPLC. 3. The oral clearance of MTP of 1*2-1-4l/minfor the 80, 160 and 320mg doses was about one third of the value previously reported for propranolol. The half-life for MTP (3.3-4.1 h) was, however, similar to that of propranolol. In contrast to propranolol, the peak (2.5 h) plasma concentrations of MTP increased linearly with dose (5-32Omg). 4. The oral clearance for MTP was about 2-fold higher in the men than in the women (P
ISSN: 0049-8254 (Print) 1366-5928 (Online) Journal homepage: http://www.tandfonline.com/loi/ixen20
Pharmacokinetics and metabolism of oral doses of a 4′-methylthio derivative of propranolol in man T. Walle, U. K. Walle, T. D. Cowart, E. C. Conradi & T. E. Gaffney To cite this article: T. Walle, U. K. Walle, T. D. Cowart, E. C. Conradi & T. E. Gaffney (1990) Pharmacokinetics and metabolism of oral doses of a 4′-methylthio derivative of propranolol in man, Xenobiotica, 20:3, 321-331 To link to this article: http://dx.doi.org/10.3109/00498259009046850
Published online: 27 Aug 2009.
Submit your article to this journal
Article views: 2
View related articles
Full Terms & Conditions of access and use can be found at http://www.tandfonline.com/action/journalInformation?journalCode=ixen20 Download by: [University of California, San Diego]
Date: 12 November 2015, At: 18:00
XENOBIOTICA,
1990, VOL. 20, NO. 3, 321-331
Pharmacokinetics and metabolism of oral doses of a 4'-methylthio derivative of propranolol in man T, WALLE, U. K. WALLE, T. D. COWARTV, E. C. CONRAD1 and T. E. GAFFNEY
Downloaded by [University of California, San Diego] at 18:00 12 November 2015
Departments of Cell and Molecular Pharmacology and Experimental Therapeutics and Medicine, Medical University of South Carolina, 171 Ashley Avenue, Charleston, SC 29425, U.S.A. Received 1 7 February 1989; revised 17 October 1989 1. The objective of this study was to determine the oral dose pharmacokinetics and metabolism of 4'-methylthiopropranolol (MTP) in man and compare the results with observations for propranolol in previous studies. 2. Three women and five men received single oral doses of MTP, dose range 5-320 mg. Plasma concentration of MTP over time were measured by gas chromatography-mass spectrometry. M T P metabolites in urine were identified by comparativehigh-performance liquid chromatographic (HPLC) retention times and mass spectrometry with previously characterized reference compounds and quantified by HPLC. 3. The oral clearance of MTP of 1*2-1-4l/minfor the 80, 160 and 320mg doses was about one third of the value previously reported for propranolol. The half-life for MTP (3.3-4.1 h) was, however, similar to that of propranolol. In contrast to propranolol, the peak (2.5 h) plasma concentrations of MTP increased linearly with dose (5-32Omg). 4. The oral clearance for MTP was about 2-fold higher in the men than in the women (P
