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Haloperidol reduction can be assayed in human red blood cells.
1Department of Pharmacology, Faculty of Medicine, University of Toronto, Ont., Canada.
Canadian Journal of Physiology and Pharmacology
|November 1, 1989
Summary
Human red blood cells can convert haloperidol to reduced haloperidol, a key plasma metabolite. This biotransformation process utilizes a reductase enzyme that requires nicotinamide adenine dinucleotide phosphate (NADPH).
Area of Science:
- Pharmacology
- Biochemistry
- Drug Metabolism
Background:
- Haloperidol is an antipsychotic medication.
- Reduced haloperidol is a known plasma metabolite of haloperidol.
- The metabolic pathways of haloperidol are not fully elucidated.
Purpose of the Study:
- To investigate the potential of human red blood cells to metabolize haloperidol.
- To identify the enzymatic machinery involved in haloperidol biotransformation in erythrocytes.
Main Methods:
- Incubation of haloperidol with human red blood cells in vitro.
- Analysis of reaction products using appropriate biochemical assays.
- Enzyme cofactor requirement determination (NADPH).
Main Results:
- Human red blood cells successfully converted haloperidol to reduced haloperidol.
- The conversion process was dependent on the presence of NADPH.
- The identified reductase shares cofactor dependency with hepatic haloperidol (ketone) reductase.
Conclusions:
- Erythrocytes possess the enzymatic capacity to reduce haloperidol.
- NADPH-dependent reductase activity in red blood cells contributes to haloperidol metabolism.
- This finding suggests a potential role for red blood cells in the overall pharmacokinetics of haloperidol.