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Review

Antihistamines for Allergic Rhinitis Treatment from the Viewpoint of Nonsedative Properties

1
Department of Otorhinolaryngology, Shimane University, Faculty of Medicine, 89-1 Enya-cho, Izumo-shi, Shimane 693-8501, Japan
2
Department of Pharmacology, Tohoku University School of Medicine, 2-1 Seiryo-cho, Aoba-Ku, Sendai 980-8575, Japan
3
Cyclotron and Radioisotope Center, Tohoku University, 6-3 Aoba, Aramaki, Aoba-ku, Sendai 980-8578, Japan
4
Department of Otolaryngology, Yong Loo Lin School of Medicine, National University of Singapore, 1E Kent Ridge Road, Singapore 119228, Singapore
5
Medical Science Section, Pharmaceutical R&D Division, Meiji Seika Pharma Co., Ltd., Kyobashi 2-4-16, Chuo-Ku, Tokyo 104-8002, Japan
6
Department of Otorhinolaryngology, Nippon Medical School, 1-1-5 Sendagi, Bunkyo-ku, Tokyo 113-8602, Japan
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(1), 213; https://doi.org/10.3390/ijms20010213
Received: 3 December 2018 / Revised: 26 December 2018 / Accepted: 29 December 2018 / Published: 8 January 2019
(This article belongs to the Special Issue Histamine-Related Molecules as Therapeutic Targets)
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 (<20%), less-sedating (20–50%), and sedating (≥50%) groups based on H1RO. Among the non-sedating group, fexofenadine and bilastine are classified into “non-brain-penetrating antihistamines” based on the H1RO. These two drugs have many common chemical properties. However, bilastine has more potent binding affinity to the H1 receptor, and its action tends to last longer. In well-controlled studies using objective indices, bilastine does not affect psychomotor or driving performance even at twice the usual dose (20 mg). Upon selecting antihistamines for allergic rhinitis, various situations should be taken into our consideration. This review summarizes that the non-brain-penetrating antihistamines should be chosen for the first-line therapy of mild allergic rhinitis. View Full-Text
Keywords: allergic rhinitis; antihistamine; bilastine; fexofenadine; H1 receptor occupancy; non-brain-penetrating allergic rhinitis; antihistamine; bilastine; fexofenadine; H1 receptor occupancy; non-brain-penetrating
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MDPI and ACS Style

Kawauchi, H.; Yanai, K.; Wang, D.-Y.; Itahashi, K.; Okubo, K. Antihistamines for Allergic Rhinitis Treatment from the Viewpoint of Nonsedative Properties. Int. J. Mol. Sci. 2019, 20, 213. https://doi.org/10.3390/ijms20010213

AMA Style

Kawauchi H, Yanai K, Wang D-Y, Itahashi K, Okubo K. Antihistamines for Allergic Rhinitis Treatment from the Viewpoint of Nonsedative Properties. International Journal of Molecular Sciences. 2019; 20(1):213. https://doi.org/10.3390/ijms20010213

Chicago/Turabian Style

Kawauchi, Hideyuki, Kazuhiko Yanai, De-Yun Wang, Koju Itahashi, and Kimihiro Okubo. 2019. "Antihistamines for Allergic Rhinitis Treatment from the Viewpoint of Nonsedative Properties" International Journal of Molecular Sciences 20, no. 1: 213. https://doi.org/10.3390/ijms20010213

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