Publications

Publications, Books, Book Chapters and Reviews by Prof. Marcus Maurer, MD

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Brain histamine H1 receptor occupancy measured by PET after oral administration of levocetirizine, a non-sedating antihistamine

Filename 194. Hiraoka et al., Brain histamine H1 levocet.,ExpOp 2014.pdf
Filesize 486 KB
Version o.194
Date added June 6, 2020
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Category Original Work
Tags Antihistamine, histamine H1 receptor occupancy, levocetirizine, positron emission tomography, sedating side effect
Authors Hiraoka, K., Tashiro, M., Grobosch, T., Maurer, M. Oda, K., Toyohara, J., Ishii, K., Ishiwata, K., and Yanai, K.
Citation Hiraoka, K., Tashiro, M., Grobosch, T., Maurer, M. Oda, K., Toyohara, J., Ishii, K., Ishiwata, K., and Yanai, K.: Brain histamine H1 receptor occupancy measured by PET after oral administration of levocetirizine, a non-sedating antihistamine. Expert Opin. Drug. Saf. 2014: 14; 1-8.
Corresponding authors Yanai, K.
DocNum O.194
DocType PDF
Edition; Page 14; 1-8.
IF 2.91
Publisher Expert Opin. Drug. Saf.
ReleaseDate 2014

Objective: Histamine H1 receptor (H1R) antagonists often have sedative side effects, which are caused by the blockade of the neural transmission of the histaminergic neurons. We examined the brain H1R occupancy (H1RO) and the subjective sleepiness of levocetirizine, a new second-generation antihista- mine, comparing fexofenadine, another non-sedating antihistamine, as a negative active control.

Methods: Eight healthy volunteers underwent positron emission tomography (PET) imaging with [11C]doxepin, a PET tracer that specifically binds to H1Rs, after a single oral administration of levocetirizine (5 mg), fexofenadine (60 mg) or placebo in a double-blind crossover study. Binding potential ratios and H1ROs in the cerebral cortices regions were calculated using placebo. Sub- jective sleepiness was assessed with the Line Analogue Rating Scale and the Stanford Sleepiness Scale.

Results: There was no significant difference between the mean brain H1RO after levocetirizine administration (8.1%; 95% CI: -9.8 to 26.0%) and fexofe- nadine administration (-8.0%; 95% CI: -26.7 to 10.6%). Similarly, subjective sleepiness was not significantly different between the two antihistamines and placebo. Neither subjective sleepiness nor plasma concentrations was significantly correlated with the brain H1RO of the two antihistamines.

Conclusion: At therapeutic dose, levocetirizine does not bind significantly to the brain H1Rs and does not induce significant sedation.

(Last update: 08.2021)

Number of publications (original work and reviews) in peer-reviewed journals: 636
Number of original publications in peer-reviewed journals: 462
Number of reviews in peer-reviewed journals: 174
Cumulative IF of publications (original work & reviews) in peer-reviewed journals: 3834,12
Cumulative IF for original publications in peer-reviewed journals: 3043,14
Cumulative IF for reviews in peer-reviewed journals: 790,98
Citations, Hirsch index: (view on Web of Science) 26429