TY - JOUR
T1 - Antihistamines for allergic rhinitis treatment from the viewpoint of nonsedative properties
AU - Kawauchi, Hideyuki
AU - Yanai, Kazuhiko
AU - Wang, De Yun
AU - Itahashi, Koju
AU - Okubo, Kimihiro
N1 - Funding Information:
Conflicts of Interest: The corresponding author (K.Y.) received research grants from Meiji Seika Pharma, Glaxo Smith Kline, Taiho Pharma, Sanofi, Kyorin Pharmaceutical Company. In the last three years, K.Y. had received honoraria from manufactures of 2nd generation antihistamines, including Sanofi, GlaxoSmithKline, Kyowa-Kirin, Taiho Pharma, Meiji Seika Pharma, and Mitsubishi Tanabe Pharma. Other authors have similar conflicts of interest. The contents regarding all aspects of the review were made by all academic authors without consulting with the respective pharmaceutical companies. The role of author from the pharmaceutical industry (K.I.) is the confirmation of description from the points of compilation for approved drug package information.
Funding Information:
Acknowledgments: This work was supported in part by Grants-in-Aid for Scientific Research (#26253016 and #26670117 from the Japan Society for Promotion of Science (JSPS). The publication of this review was supported by a grant from Meiji Seika Pharma.
Publisher Copyright:
© 2019 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2019/1/1
Y1 - 2019/1/1
N2 - 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 (H1 RO) 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 H1 RO. Among the non-sedating group, fexofenadine and bilastine are classified into “non-brain-penetrating antihistamines” based on the H1 RO. 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.
AB - 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 (H1 RO) 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 H1 RO. Among the non-sedating group, fexofenadine and bilastine are classified into “non-brain-penetrating antihistamines” based on the H1 RO. 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.
KW - Allergic rhinitis
KW - Antihistamine
KW - Bilastine
KW - Fexofenadine
KW - H receptor occupancy
KW - Non-brain-penetrating
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U2 - 10.3390/ijms20010213
DO - 10.3390/ijms20010213
M3 - Review article
C2 - 30626077
AN - SCOPUS:85059795832
VL - 20
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
SN - 1422-0067
IS - 1
M1 - 213
ER -