Trial reportPharmaceutical research2013
Exploration of optimal dosing regimens of haloperidol, a D2 Antagonist, via modeling and simulation analysis in a D2 receptor occupancy study.
Trial report in Pharmaceutical research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
9 citing papers in PubMed, 21 citations in OpenAlex.
- The sense and nonsense of antipsychotic combinations: A model for dopamine DTranslational psychiatry · 2025Article
- Pharmacological Modulation of Dopamine Receptors Reveals Distinct Brain-Wide Networks Associated with Learning and Motivation in Nonhuman Primates.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2025Article
- Population Pharmacokinetic and Pharmacodynamic Modeling Analysis of rhIL-7-hyFc, a Hybrid Fc-Fused Long-Acting Interleukin-7, to Support Optimal Dosing Regimens in Patients with Solid Cancer.Drug design, development and therapy · 2025Article
- Pharmacological modulation of dopamine receptors reveals distinct brain-wide networks associated with learning and motivation in non-human primates.bioRxiv : the preprint server for biology · 2024Article
- Nonlinear Mixed-Effects Modeling Approach for Simplified Reference Tissue Model.IEEE transactions on bio-medical engineering · 2024Article
- Nonlinear Mixed-Effects Models for PET Data.IEEE transactions on bio-medical engineering · 2019Article
- Do doctors agree on doses of antipsychotic medications?Therapeutic advances in psychopharmacology · 2016Article
- Secondary parkinsonism induced by hydrocephalus after subarachnoid and intraventricular hemorrhage.Neural regeneration research · 2016Article
- Integration of PKPD relationships into benefit-risk analysis.British journal of clinical pharmacology · 2015Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo evaluate the potential usage of D(2) receptor occupancy (D2RO) measured by positron emission tomography (PET) in antipsychotic development.
methodsIn this randomized, parallel group study, eight healthy male volunteers received oral doses of 0.5 (n = 3), 1 (n = 2), or 3 mg (n = 3) of haloperidol once daily for 7 days. PET's were scanned before haloperidol, and on days 8, 12, with serial pharmacokinetic sampling on day 7. Pharmacokinetics and binding potential to D(2) receptor in putamen and caudate nucleus over time were analyzed using NONMEM, and simulations for the profiles of D2RO over time on various regimens of haloperidol were conducted to find the optimal dosing regimens.
resultsOne compartment model with a saturable binding compartment, and inhibitory E(max) model in the effect compartment best described the data. Plasma haloperidol concentrations at half-maximal inhibition were 0.791 and 0.650 ng/ml, in putamen and caudate nucleus. Simulation suggested haloperidol 2 mg every 12 h is near the optimal dose.
conclusionThis study showed that sparse D2RO measurements in steady state pharmacodynamic design after multiple dosing could reveal the possibility of treatment effect of D(2) antagonist, and could identify the potential optimal doses for later clinical studies by modeling and simulation.
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