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Chirality of reduced haloperidol in humans.

European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology (1998-06-10)
D W Eyles, J J McGrath, T J Stedman, S M Pond
ABSTRACT

In vitro, cytosolic human ketone reductases catalyse the stereospecific (i.e. >99%) formation of S(-) reduced haloperidol (RHP) from haloperidol (HP). Whether this situation is reflected in patients taking the drug is unknown. In this study in nine patients taking HP, only 73.2+/-18.2% of the RHP excreted in urine was the S(-) enantiomer. Thus, enzymes other than cytosolic ketone reductases must be responsible for the formation of the minor enantiomer.