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SULT 1A3 single-nucleotide polymorphism and the single dose pharmacokinetics of inhaled salbutamol enantiomers: Are some athletes at risk of higher urine levels?

Citation

Jacobson, GA and Yee, KC and Wood-Baker, R and Walters, EH, SULT 1A3 single-nucleotide polymorphism and the single dose pharmacokinetics of inhaled salbutamol enantiomers: Are some athletes at risk of higher urine levels?, Drug testing and analysis, 7 Article 1645. ISSN 1942-7611 (2015) [Refereed Article]

Copyright Statement

Copyright 2014 John Wiley & Sons

DOI: doi:10.1002/dta.1645

Abstract

The study was designed to investigate the effect of a common genetic variation of the main salbutamol metabolizing enzyme SULT1A3 (single nucleotide polymorphism 105A>G, rs1975350) on the stereoselective pharmacokinetics of salbutamol. Subjects were administered a 400 g dose of inhaled salbutamol via a large volume spacer and blood samples were collected over 4 h. Plasma levels of (R)- and (S)-salbutamol were determined by an enantioselective liquid chromatography-tandem mass spectrometry (LC-MS/MS) assay. Twenty-five subjects with asthma were recruited and underwent SULT1A3 genotyping, from which four SNP homozygote (GG) subjects and nine wild-type (AA) subjects were selected to participated in the pharmacokinetic investigation. There were no differences in pharmacokinetic parameters (t1/2, Cmax, AUC0-4h) between SNP and wild-type genotypes for either the R- or S-enantiomer. Observed Cmax of R- and S-salbutamol [mean (SD)] was 0.64 (0.30) ng/mL and 1.32 (0.98) ng/mL, respectively. The mean t1/2 of R- and S-salbutamol was estimated at 2.94 (1.17) h and 7.86 (6.14) h respectively. The AUC0-4h of R- and S-salbutamol was 14.0 (6.8) and 38.3 (19.5) ng/mL.h respectively. In conclusion, the common SULT1A3 SNP 105A>G is not an important determinant of salbutamol enantiomer pharmacokinetics under normal clinical use and does not place some individuals at greater risk of accumulation in the body.

Item Details

Item Type:Refereed Article
Keywords: enantiomer, salbutamo, albuterol, metabolism, pharmacogenetics, sports doping
Research Division:Medical and Health Sciences
Research Group:Pharmacology and Pharmaceutical Sciences
Research Field:Pharmaceutical Sciences
Objective Division:Health
Objective Group:Other Health
Objective Field:Health not elsewhere classified
Author:Jacobson, GA (Dr Glenn Jacobson)
Author:Yee, KC (Dr Kwang Yee)
Author:Wood-Baker, R (Professor Richard Wood-Baker)
Author:Walters, EH (Professor Haydn Walters)
ID Code:90374
Year Published:2015 (online first 2014)
Web of Science® Times Cited:7
Deposited By:Pharmacy
Deposited On:2014-04-02
Last Modified:2017-11-02
Downloads:0

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