Chirality of reduced haloperidol in humans.
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.
Eyles
D W
DW
Queensland Centre for Schizophrenia Research, Wolston Park Hospital, Wacol, Brisbane, Australia.
McGrath
J J
JJ
Stedman
T J
TJ
Pond
S M
SM
D000328:Adult; D014150:Antipsychotic Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000652:urine; D002851:Chromatography, High Pressure Liquid; D006220:Haloperidol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000652:urine; D006801:Humans; D008297:Male; D008875:Middle Aged; D010084:Oxidation-Reduction; D013237:Stereoisomerism
D014150:Antipsychotic Agents; C040692:4-(4-(4-chlorophenyl)-4-hydroxy-1-piperidinyl)-1-(4-fluorophenyl)-1-butanol; D006220:Haloperidol