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.

我们先前曾报道使用[ ¹¹ C] doxepin和正电子发射断层扫描（PET）对人脑中抗组胺药的脑H ₁受体占有率进行测量。我们建议使用脑H ₁根据抗组胺药的镇静作用，可将受体抗组胺药客观地分为镇静剂，镇静剂和非镇静剂三类。非镇静抗组胺药由于对中枢神经系统的渗透性低，因此建议用于治疗过敏症，例如花粉症和特应性皮炎。医师和药剂师负责从药理学角度全面教育患者镇静抗组胺药的风险。如果必须开具镇静抗组胺药，则在选择药物之前应彻底考虑其镇静作用。由于大多数抗组胺药同样有效，因此应尽可能使用非镇静性抗组胺药，而镇静性抗组胺药的不良反应可能很严重。