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Exploration of Optimal Dosing Regimens of Haloperidol, a D2 Antagonist, via Modeling and Simulation Analysis in a D2 Receptor Occupancy Study
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Exploration of Optimal Dosing Regimens of Haloperidol, a D2 Antagonist, via Modeling and Simulation Analysis in a D2 Receptor Occupancy Study
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Exploration of Optimal Dosing Regimens of Haloperidol, a D2 Antagonist, via Modeling and Simulation Analysis in a D2 Receptor Occupancy Study
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Journal Article
Exploration of Optimal Dosing Regimens of Haloperidol, a D2 Antagonist, via Modeling and Simulation Analysis in a D2 Receptor Occupancy Study
2013
Overview
ABSTRACT
Purpose
To evaluate the potential usage of D
2
receptor occupancy (D2RO) measured by positron emission tomography (PET) in antipsychotic development.
Methods
In 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.
Results
One 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.
Conclusion
This 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.
Publisher
Springer US,Springer
Subject
/ Antipsychotic Agents - administration & dosage
/ Antipsychotic Agents - pharmacokinetics
/ Antipsychotic Agents - pharmacology
/ Biological and medical sciences
/ Biomedical and Life Sciences
/ Biomedical Engineering and Bioengineering
/ Dopamine D2 Receptor Antagonists
/ Dose-Response Relationship, Drug
/ Haloperidol - administration & dosage
/ Haloperidol - pharmacokinetics
/ Humans
/ Male
/ Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions
/ Pharmacology. Drug treatments
/ Pharmacy
/ Positron-Emission Tomography
