title: Determination of esmolol and metabolite enantiomers within human plasma using chiral column chromatography.
abstract: A high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed for the simultaneous determination of each of esmolol's enantiomers at the 25-1000 ng/ml concentrations observed in human plasma upon intravenous administration of this rapidly metabolized beta-adrenergic receptor blocking agent. Alternatively, a high performance liquid chromatography (HPLC) UV detection method has been developed for the simultaneous determination of each of the enantiomers for esmolol's metabolite which, in turn, achieve 2.5-50 microg/ml concentrations in human plasma. Utilizing chiral columns, these methods do not require a precolumn asymmetric derivatization step. Linearity in all cases was >0.99. Precision and accuracy at all but the lowest concentrations were within +/-6% for the esmolol enantiomers and within +/-2.5% for the esmolol metabolite enantiomers. These values should be suitable for performing thorough pharmacokinetic studies for all of the stereoisomers of this prototypical soft drug and its corresponding metabolite.
authors: Department of Medicinal and Biological Chemistry, Center for Drug Design and Development, University of Toledo, College of Pharmacy, Toledo, OH 43606, USA.
authors: Lei
authors: L
authors: Fang
authors: Crystal
authors: C
authors: Bykowski-Jurkiewicz
authors: Jeffrey G
authors: JG
authors: Sarver
authors: Paul W
authors: PW
authors: Erhardt
mesh_terms: D058671:Adrenergic beta-1 Receptor Antagonists / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D006801:Humans; D016014:Linear Models; D011412:Propanolamines / Q000097:blood* / Q000737:chemistry / Q000493:pharmacokinetics; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D013237:Stereoisomerism
chemical_list: D058671:Adrenergic beta-1 Receptor Antagonists; D011412:Propanolamines; C036604:esmolol