Antihistamines for Allergic Rhinitis Treatment from the Viewpoint of Nonsedative Properties

Antihistamines targeting the histamine H₁ receptor play an important role in improving and maintaining the quality of life of patients with allergic rhinitis. For more effective and safer use of second-generation drugs, which are recommended by various guidelines, a classification based on their det...

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Bibliographic Details
Published in:International journal of molecular sciences 2019-01, Vol.20 (1), p.213
Main Authors: Kawauchi, Hideyuki, Yanai, Kazuhiko, Wang, De-Yun, Itahashi, Koju, Okubo, Kimihiro
Format: Article
Language:English
Subjects:
Allergic rhinitis
Allergies
Anesthesia
Animals
antihistamine
Antihistamines
bilastine
Binding sites
Brain - drug effects
Brain - pathology
Cetirizine
Drugs
Fexofenadine
H1 receptor occupancy
Histamine
Histamine Antagonists - chemistry
Histamine Antagonists - pharmacology
Histamine Antagonists - therapeutic use
Histamine H1 Antagonists, Non-Sedating - chemistry
Histamine H1 Antagonists, Non-Sedating - pharmacology
Histamine H1 Antagonists, Non-Sedating - therapeutic use
Humans
non-brain-penetrating
Nose
Olopatadine
Pharmaceuticals
Positron emission
Positron emission tomography
Receptors, Histamine - metabolism
Review
Rhinitis, Allergic - drug therapy
Smooth muscle
Steroid hormones
Steroids
Terfenadine
Tomography
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Summary:Antihistamines targeting the histamine H₁ receptor play an important role in improving and maintaining the quality of life of patients with allergic rhinitis. For more effective and safer use of second-generation drugs, which are recommended by various guidelines, a classification based on their detailed characteristics is necessary. Antihistamines for first-line therapy should not have central depressant/sedative activities. Sedative properties (drowsiness and impaired performance) are associated with the inhibition of central histamine neurons. Brain H₁ receptor occupancy (H₁RO) is a useful index shown to be correlated with indices based on clinical findings. Antihistamines are classified into non-sedating (
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms20010213