The clinical pharmacology of non-sedating antihistamines

Kazuhiko Yanai, Takeo Yoshikawa*, Ai Yanai, Tadaho Nakamura, Tomomitsu Iida, Rob Leurs, Manabu Tashiro

*Corresponding author for this work

Research output: Contribution to JournalReview articleAcademicpeer-review

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We previously reported on brain H1 receptor occupancy measurements of antihistamines in human brain using [11C]doxepin and positron emission tomography (PET). We proposed the use of brain H1 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.

Original languageEnglish
Pages (from-to)148-156
Number of pages9
JournalPharmacology and Therapeutics
Early online date27 Apr 2017
Publication statusPublished - Oct 2017


  • Carnosine
  • CNS
  • Histamine
  • Histamine H1 receptor occupancy
  • Histidine
  • Impaired performance
  • Non-sedating antihistamines
  • P-glycoprotein
  • PET
  • Sedation


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