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- W2100348528 abstract "Aims The strength of sedation due to antihistamines can be evaluated using positron emission tomography (PET). The purpose of the present study is to measure histamine H1 receptor (H1R) occupancy following oral administration of cetirizine (10 and 20 mg) in order to examine dose dependency. Methods Fifteen healthy male volunteers (age range, 20–35 years) were divided into 3 subgroups and were studied following single oral administration of cetirizine at 10 mg (n = 5) and 20 mg (n = 5) or hydroxyzine at 30 mg (n = 5) using PET with 11C-doxepin. Each subject was scanned also following the administration of placebo. Binding potential and H1RO values were calculated in the prefrontal and anterior cingulate cortices. Subjective sleepiness was also measured, and the correlation to H1RO was examined for each antihistamine. Results The averaged H1ROs of cetirizine 10 mg, 20 mg, and hydroxyzine 30 mg in the prefrontal and cingulate cortices was 12.6%, 25.2%, and 67.6%, respectively. The H1RO of hydroxyzine 30 mg correlated well with subjective sleepiness (p < 0.001); however, those of cetirizine 10 and 20 mg showed no correlation with subjective sleepiness. Conclusion It was demonstrated that the brain penetration of orally administered cetirizine was dose-dependent. Cetirizine 10 mg, with its low H1RO and thus minimal sedation, could be more safely used than cetirizine 20 mg for the treatment of various allergic disorders. Copyright © 2009 John Wiley & Sons, Ltd." @default.
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- W2100348528 date "2009-10-01" @default.
- W2100348528 modified "2023-10-17" @default.
- W2100348528 title "Dose dependency of brain histamine H1 receptor occupancy following oral administration of cetirizine hydrochloride measured using PET with [<sup>11</sup>C]doxepin" @default.
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- W2100348528 doi "https://doi.org/10.1002/hup.1051" @default.
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