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Haloperidol dopamine receptor occupancy and antagonism correspond to delirium agitation scores and EPS risk: A PBPK-PD modeling analysis.
J Psychopharmacol
January 2025
Department of Psychiatry, University of Pennsylvania Perelman School of Medicine, Philadelphia, PA, USA.
Background: Delirium 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.
View Article and Find Full Text PDFEffects of piperine-haloperidol mixture on ketamine induced schizophrenia rats and metabolism-mediated inhibitory potency: in-vivo and in-vitro evaluation.
3 Biotech
December 2024
Department of Pharmaceutical Analysis, SRM College of Pharmacy, SRMIST, Kattankulathur, Chengalpattu, Tamil Nadu 603 203 India.
Haloperidol, a conventional antipsychotic, was mixed with piperine in a ketamine-induced schizophrenia rat model to evaluate the interaction potential of this mixture through in-vitro and in-vivo analyses. Piperine, known for its CYP450 enzyme inhibitory effects, enhances the bioavailability of various drugs. Initial in-vitro assays using a high-throughput fluorometric method showed that the haloperidol-piperine mixture inhibited CYP3A4 and CYP2D6 enzymes, comparable to positive controls.
View Article and Find Full Text PDFEffects of Acute Haloperidol Treatment on Dopaminergic Markers, GAD and A Receptors in Rats with High and Low VCMs.
Neurochem Res
November 2024
Programa de Pós-Graduação em Ciências Biológicas: Bioquímica Toxicológica, Universidade Federal de Santa Maria, RS, Brazil.
Vacuous chewing movements (VCM) have been utilized as an experimental model of orofacial dyskinesia (OD) in rodents to study the underlying molecular mechanisms related to tardive dyskinesia (TD). This study aimed to investigate if the acute treatment with haloperidol can alter components of the dopaminergic synapse or its modulators such as glutamic acid decarboxylase (GAD) and adenosine 2A (A) receptor. Furthermore, to evaluate if changes in molecular markers are associated with the number of VCMs induced by haloperidol in rats it is proposing a method to classify the animals into High and Low VCM groups.
View Article and Find Full Text PDFUsing in silico methods to determine optimal tapering regimens for decanoate-based long-acting injectable psychosis drugs.
Ther Adv Psychopharmacol
September 2024
Division of Psychiatry, University College London, London, UK.
Background: Reducing the dose of psychosis drugs in a gradual hyperbolic manner may minimise withdrawal effects and risk of relapse. There is presently limited guidance on tapering decanoate-based long-acting injectable dopamine antagonists (LIDAs).
Objectives: We aimed to apply hyperbolic principles of tapering to the decanoate-based LIDAs flupentixol, zuclopenthixol and haloperidol to develop withdrawal regimens.
A Systematic Investigation of Process Parameters for Small-Volume Aqueous Suspension Production by the Use of Focused Ultrasonication.
AAPS PharmSciTech
August 2024
Department of Physics, Chemistry, and Pharmacy, University of Southern Denmark, Campusvej 55, 5230, Odense, Denmark.
Aqueous suspensions containing crystalline drug in the sub-micron range is a favorable platform for long-acting injectables where particle size can be used to obtain a desired plasma-concentration profile. Stabilizers are added to the suspensions and screened extensively to define the optimal formulation composition. In the initial formulation screening the amount of drug compound can be limited, necessitating milling methods for small-volume screening predictable for scale-up.
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