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Pharmacokinetics of haloperidol.
J S Froemming1, Y W Lam, M W Jann
1Department of Pharmacy Practice, Mercer University, Southern School of Pharmacy, Atlanta, Georgia.
Clinical Pharmacokinetics
|December 1, 1989
Summary
Monitoring plasma haloperidol levels is clinically useful for psychotic disorders. Interindividual variability in haloperidol concentration may be linked to metabolism and enterohepatic recycling, impacting therapeutic response.
Area of Science:
- Pharmacology
- Psychiatry
- Clinical Chemistry
Background:
- Haloperidol is a key antipsychotic for psychotic disorders.
- Plasma haloperidol concentration monitoring is considered clinically valuable.
- Various assay methods exist, each with unique precision, sensitivity, and specificity.
Purpose of the Study:
- To review the clinical utility of monitoring plasma haloperidol concentrations.
- To explore factors contributing to interindividual variability in haloperidol pharmacokinetics.
- To define the therapeutic plasma concentration range for haloperidol.
Main Methods:
- Review of existing literature on haloperidol assays and pharmacokinetics.
- Comparison of different analytical techniques: HPLC, GLC, RIA, and radioreceptor assay.
- Analysis of pharmacokinetic data, including bioavailability, metabolism, and elimination.
Main Results:
- Oral bioavailability of haloperidol ranges from 60-65%.
- Significant interindividual variability in plasma concentrations and pharmacokinetic parameters exists.
- A therapeutic plasma haloperidol range of 4-25 µg/L is suggested, though not conclusive.
- Haloperidol decanoate exhibits flip-flop pharmacokinetics with a 3-week elimination half-life.
Conclusions:
- Plasma haloperidol monitoring can be useful, but variability poses challenges.
- Metabolic pathways, enterohepatic recycling, and ethnic differences may explain variability.
- Further research into physiological parameters like homovanillic acid is warranted.