ArticleJournal of psychopharmacology (Oxford, England)2025
Haloperidol dopamine receptor occupancy and antagonism correspond to delirium agitation scores and EPS risk: A PBPK-PD modeling analysis.
Article in Journal of psychopharmacology (Oxford, England), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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Who cites it
2 citing papers in PubMed.
- Xanomeline-Trospium Validates Muscarinic Agonism as an Effective Non-Dopaminergic Treatment for Schizophrenia.International journal of molecular sciences · 2026Review
- Considerations for Augmenting Aripiprazole Long-Acting Injectables with Other Antipsychotics: A Mini-Review.Diseases (Basel, Switzerland) · 2025Review
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Abstract
backgroundDelirium is a severe neuropsychiatric disorder associated with increased morbidity and mortality. Numerous precipitating factors and etiologies merge into the pathophysiology of this condition which can be marked by agitation and psychosis. Judicious use of antipsychotic medications such as intravenous haloperidol reduces these symptoms and distress in critically ill individuals.
aimsThis study aimed to develop a physiologically-based pharmacokinetic (PBPK) model for the antipsychotic medication haloperidol; estimate plasma and unbound interstitial brain concentrations for repetitive haloperidol administrations used in hyperactive delirium treatment; determine dopamine receptor occupancy and antagonism under these conditions; and correlate these results with Richmond Agitation-Sedation Scale (RASS) scores and the risk of developing extrapyramidal symptoms (EPSs).
methodsThe PBPK model for single and repetitive administrations of peroral and intravenous haloperidol was developed with PK-Sim software. The pharmacodynamic (PD) model for RASS scores with haloperidol unbound interstitial brain concentration passed as the regressor was developed with the MonolixSuite 2021R platform.
resultsPeak haloperidol plasma and unbound interstitial brain concentrations following a single 2 mg intravenous dose are 32 ± 5 nM and 2.4 ± 0.4 nM. With repetitive administrations, dopamine receptor occupancy is 70%-83% and D2
conclusionsHaloperidol dopamine receptor occupancy time course and D2
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