The clinical pharmacology of non-sedating antihistamines

We previously reported on brain H receptor occupancy measurements of antihistamines in human brain using [ C]doxepin and positron emission tomography (PET). We proposed the use of brain H receptor occupancy to classify antihistamines objectively into three categories of sedating, less-sedating, and...

Full description

Saved in:
Bibliographic Details
Published in:Pharmacology & therapeutics (Oxford) 2017-10, Vol.178, p.148-156
Main Authors: Yanai, Kazuhiko, Yoshikawa, Takeo, Yanai, Ai, Nakamura, Tadaho, Iida, Tomomitsu, Leurs, Rob, Tashiro, Manabu
Format: Article
Language:English
Subjects:
Animals
ATP Binding Cassette Transporter, Sub-Family B - antagonists & inhibitors
Brain - diagnostic imaging
Brain - metabolism
Gene Expression
Genes, MDR
Histamine - metabolism
Histamine H1 Antagonists, Non-Sedating - pharmacology
Humans
Positron-Emission Tomography
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:We previously reported on brain H receptor occupancy measurements of antihistamines in human brain using [ C]doxepin and positron emission tomography (PET). We proposed the use of brain H receptor occupancy to classify antihistamines objectively into three categories of sedating, less-sedating, and non-sedating antihistamines according to their sedative effects. Non-sedating antihistamines are recommended for the treatment of allergies such as pollinosis and atopic dermatitis because of their low penetration into the central nervous system. Physicians and pharmacists are responsible for fully educating patients about the risks of sedating antihistamines from pharmacological points of view. If a sedating antihistamine must be prescribed, its sedative effects should be thoroughly considered before choosing the drug. Non-sedating antihistamines should be preferentially used whenever possible as most antihistamines are equally efficacious, while adverse effects of sedating antihistamines can be serious. This review summarizes the pharmacological properties of clinically useful non-sedating antihistamines from the perspective of histamine function in the CNS.
ISSN:0163-7258
1879-016X
DOI:10.1016/j.pharmthera.2017.04.004