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Stereoselective binding of zopiclone to human plasma proteins

✍ Scribed by Christine Fernandez; François Gimenez; Alain Thuillier; Robert Farinotti

Publisher
John Wiley and Sons
Year
1999
Tongue
English
Weight
63 KB
Volume
11
Category
Article
ISSN
0899-0042

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✦ Synopsis

The binding of racemic zopiclone (ZOP) and of its two enantiomers to plasma proteins, albumin and ␣1-acid glycoprotein were compared. Our work shows that the binding of ZOP to human plasma proteins is stereoselective. The total plasma protein binding percentages were 79.3 ± 5.5%, 83.8 ± 5.2%, and 75.1 ± 2.1%, for racemic zopiclone, (-)zopiclone and (+)zopiclone, respectively. These results were confirmed by the analysis of samples obtained from healthy volunteers after the oral administration of ZOP. The anticoagulant used for sampling was also shown to have an influence on the percentage binding and on its stereoselectivity. Considering albumin and ␣1-acid glycoprotein separately, stereoselectivity was also observed. Chirality 11:129-132, 1999.

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