Microdialysis study of the blood-brain equilibration of thiopental enantiomers.

Abstract:

:Thiopental is a racemate of equimolar R- and S-thiopental enantiomers that have different potencies in laboratory experiments. We measured concentrations of R- and S-thiopental in plasma, tissues and brain microdialysate of rats after computer-controlled infusion of thiopental i.v. to a plasma concentration of 40 micrograms ml-1 for 20 min in two pharmacokinetic studies. In study 1, animals were found to maintain their target plasma concentrations, which then decayed biphasically after infusion. Brain microdialysate concentrations of both enantiomers increased from about 3% of corresponding plasma concentrations at 1 min to 9% at 20 min. In study 2, thiopental concentrations were found to be highest at 20 min in CNS tissue, at 30 min in muscle and at 60 min in fat. Tissue:plasma distribution coefficients of R-thiopental were greater than those of S-thiopental when calculated from total or unbound plasma concentrations. We found no pharmacokinetic evidence to support differences between the thiopental enantiomers in rates of equilibration across the blood-brain barrier after infusion of rac-thiopental.

journal_name

Br J Anaesth

authors

Mather LE,Edwards SR,Duke CC,Cousins MJ

doi

10.1093/oxfordjournals.bja.a013385

subject

Has Abstract

pub_date

2000-01-01 00:00:00

pages

67-73

issue

1

eissn

0007-0912

issn

1471-6771

pii

S0007-0912(17)38234-X

journal_volume

84

pub_type

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