Stereoselective Pharmacokinetics of Esmolol Enantiomers

Okamura, Miyako; Kumagai, Masamichi; Murasaki, Yuko; Ohkura, Takako; Miyamoto, Yukio; Kawai, Yoichiro; Tamura, Takashi; Takariki, Y.; Tomisawa, Hiroki

doi:10.2133/dmpk.16.427

Cited by 2 publications

(2 citation statements)

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“…In the study [61] the stereoselective pharmacokinetics of enantiomers was compared after a single intravenous administration of 14 C-esmolol hydrochloride to dogs. The findings suggest that pharmacokinetics of the particular enantiomers differs slightly in dog, whereas there are no stereoselective differences in human blood kinetics.…”

Section: Propranololmentioning

confidence: 99%

Survey of Pharmacological Activity and Pharmacokinetics of Selected β-Adrenergic Blockers in Regard to Their Stereochemistry

et al. 2019

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The present survey concentrates on pharmacodynamics and pharmacokinetics of selected β-adrenergic blockers from the point of view of their stereochemistry. It could be shown that the activity in the arylaminoethanol and aryloxyaminopropanol group of β-blockers is higher in their (–)-enantiomers as compared with the (+)-enantiomers. The stereoisomers differ also in other types of bioactivity as well as in toxicity. The particular pharmacokinetic stages such as resorption, distribution, and metabolism are discussed in regard to their stereochemistry.

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Section: Propranololmentioning

confidence: 99%

Survey of Pharmacological Activity and Pharmacokinetics of Selected β-Adrenergic Blockers in Regard to Their Stereochemistry

et al. 2019

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“…A limited number of studies have focused on the metabolic disposition of the esmolol enantiomers [5,6], or upon the sterochemical outcomes of the racemic form by using asymmetric derivatization prior to chromatography [5,7,8]. Among these studies, none have deployed direct measurements by chiral column chromatography, and none have thoroughly accounted for the corresponding stereoisomeric metabolites even though the latter's residency times in vivo far out-last that of their enantiomeric parents.…”

Section: Introductionmentioning

confidence: 99%