期刊
EUROPEAN JOURNAL OF PHARMACOLOGY
卷 765, 期 -, 页码 100-106出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejphar.2015.08.016
关键词
H-1-antihistamine; P-glycoprotein; MDR1; Sedative effect; Minimally sedating
H-1-antihistamines are widely used in treating allergic disorders, e.g., conjunctivitis, urticaria, dermatitis and asthma. The first-generation H-1-antihistamines have a much greater sedative effect than the second-generation H-1-antihistamines. Researchers could not offer a satisfactory explanations until late 1990s when studies showed that second-generation H-1-antihistamines were substrates of P-glycoprotein. P-glycoprotein, expressed in the blood-brain barrier, acts as an efflux pump to decrease the concentration of H-1-antihistamines in the brain, which minimizes drug effects on the central nervous system and results in less sedation. P-glycoprotein is found in the apical side of the epithelium. It consists of transmembrane domains that bind substrates/drugs and nucleotide-binding domains that bind and hydrolyze ATP to generate energy for the drug efflux. This review mainly discusses interactions between P-glycoprotein and commonly used second-generation H-1-antihistamines. In addition, it describes other possible determining factors of minimal sedating properties of second-generation H-1-antihistamines. (C) 2015 Elsevier B.V. All rights reserved.
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