Haloperidol glucuronide

Figure 3.21. Constant-neutral-loss scan (top panels) triggered product ion spectrum (bottom panel) of haloperidol glucuronide.

H.D. Eddington and D. Young Biliary excretion of reduced haloperidol glucuronide, Psychopharmacology (BerL) 1990, 100, 46-48. 

Haloperidol is a butyrophenone neuroleptic drug. The enzymes involved in its biotransformation include oxidative cytochrome P450 isozymes, carbonyl reductase, and uridine diphosphoglucose glucuronosyltransferase (1). It is mainly cleared by glucuronidation. 

Haloperidol undergoes extensive metabolism to form a myriad of primary and secondary metabolites (479-486). The principal phase I reactions involve the following oxidative N-dealkylation to initially form 4-fluoro-phenylbenzoylpropionaldehyde (which is rapidly oxidized to the acid) and 4-(4-chlorophenyl)-4-hydroxypiperidine (479,480, 483-485) N-oxidation to form haloperidol-iV-oxide (485) and reversible reduction of the carbonyl group to the alcohol, or reduced haloperidol (481,487). A phase II metabolite, hal-operidol-O-glucuronide, accounts for as much... 

Amperozide, amphetamine, methamphetamine, bambuterol, antidepressants (paroxetine, fluvoxamine, mianserin, and citalopram), anabolic steroids (glucuronides) promethazine, methadone, haloperidol, ibuprofen, naproxen, ketoprofen, propofol, ropivacaine Pb(ll), Mn(ll)... 

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