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- W66363951 abstract "589 Objectives: Naltrexone, a mu-opioid receptor antagonist, blocks CNS reward pathways and has been used to treat opiate and alcohol dependence. The objective is to examine the dose-occupancy relationship and to determine how receptor occupancy is affected by single vs chronic naltrexone dosing. Methods: Twelve healthy, obese subjects (BMI>30 kg/m2;10M, 2F;average age 33) were randomly assigned to one of 3 chronic or 1 single dosing cohorts(chronic dosing over 7 days:16 (2×8)mg, 32 (2×16)mg, or 48 (2×24)mg; single:150mg). Subjects received two 90 minute PET scans using [11C] diprenorphine(DPN), an opioid antagonist tracer: at baseline and then 2 hours after their final dose of drug. For both scans, 20mCi of DPN was injected by IV bolus at the start of the scan. A 2-tissue compartmental model with plasma input was used for region of interest kinetic analysis to estimate tracer binding potential (BP). Percent receptor occupancy (PO) was calculated as BP(=100*(BP(baseline)-BP(naltrexone))/BP(baseline))%. Results: For the 16 mg chronic dose, naltrexone occupied 70-80% of receptors, while the PO for the 32 and 48 mg chronic and 150 mg single doses was 90%. The data from both regimens showed a smooth dose-occupancy response that reaches a saturating occupancy. When the chronic dosing data was fitted to the dose-response curve, the predicted maximal occupancy (Emax) was 90.2%, and matches the Emax of the 150 mg single dose. Conclusions: The combined data from both regimes fit a single dose-occupancy response that reaches a saturating occupancy (Fig.1). The maximal occupancy from the chronic study matches the occupancy found with the much higher single oral dose of 150 mg (Fig.1, circled). Thus, the data from the single dose and chronic doses studies show the saturation of m-opioid receptors at higher doses. This agreement between a single dose and a chronic dose study is unlike previous studies of occupancy with antipsychotics. Previous single dose studies with antipsychotics overestimate receptor occupancy (Woods, et al, 2003) when compared to chronic dose studies of the same drug (Mamo, et al, 2004)." @default.
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- W66363951 date "2007-05-01" @default.
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- W66363951 title "Receptor occupancy following chronic or single daily dosing with naltrexone" @default.
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