title: Analysis of disease-dependent sedative profiles of H(1)-antihistamines by large-scale surveillance using the visual analog scale.
abstract: Sedation is the most frequent side effect of H(1)-antihistamines, and, sometimes, it may be life-threatening for patients. Evaluation of the sedative properties of H(1)-antihistamines is important to improve the patients' quality of life (QOL). Therefore, we carried out a large-scale surveillance quantified through a questionnaire using visual analog scale (VAS) from 1,742 patients. The results showed that the degree of sleepiness caused by some nonsedative second-generation antihistamines, including fexofenadine, olopatadine and cetirizine, was disease dependent. In atopic dermatitis, an unexpectedly low VAS score of sleepiness was obtained for the first-generation antihistamine d-chlorpheniramine, which is similar to those obtained for bepotastine and epinastine. d-Chlorpheniramine also showed a high VAS score in efficacy. Meanwhile, fexofenadine showed a higher VAS score of sleepiness in atopic dermatitis than those obtained in the other allergic diseases including allergic rhinitis, urticaria and asthma. In asthma, a higher VAS score of sleepiness was found for olopatadine, ebastine and cetirizine, when compared with d-chlorpheniramine. On the other hand, bepotastine showed the lowest VAS score for sleepiness. Our findings suggest the existence of unknown factors influencing the sedative properties of H(1)-antihistamines. Therefore, appropriate H(1)-antihistamines may need to be selected, depending on allergic diseases, to improve patients' QOL.
authors.affiliation: Department of Molecular Pharmacology, Institute of Health Biosciences, University of Tokushima Graduate School, Tokushima, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Izumi
authors.forename: H
authors.initials: H
authors.lastname: Mizuguchi
authors.forename: H
authors.initials: H
authors.lastname: Umehara
authors.forename: S
authors.initials: S
authors.lastname: Ogino
authors.forename: H
authors.initials: H
authors.lastname: Fukui
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D001249:Asthma / Q000188:drug therapy; D002090:Butyrophenones / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D017332:Cetirizine / Q000494:pharmacology / Q000627:therapeutic use; D002648:Child; D002744:Chlorpheniramine / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D003876:Dermatitis, Atopic / Q000188:drug therapy; D003984:Dibenzazepines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D003990:Dibenzoxepins / Q000494:pharmacology / Q000627:therapeutic use; D005260:Female; D006634:Histamine H1 Antagonists / Q000009:adverse effects* / Q000494:pharmacology* / Q000627:therapeutic use; D039563:Histamine H1 Antagonists, Non-Sedating / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007093:Imidazoles / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D007564:Japan / Q000453:epidemiology; D008297:Male; D008875:Middle Aged; D000069605:Olopatadine Hydrochloride; D010147:Pain Measurement; D010880:Piperidines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D011159:Population Surveillance; D011597:Psychomotor Performance / Q000187:drug effects; D011725:Pyridines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D011788:Quality of Life; D012221:Rhinitis, Allergic, Perennial / Q000188:drug therapy; D006255:Rhinitis, Allergic, Seasonal / Q000188:drug therapy; D012894:Sleep Stages / Q000187:drug effects*; D011795:Surveys and Questionnaires; D016593:Terfenadine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D014581:Urticaria / Q000188:drug therapy
chemical_list: D002090:Butyrophenones; D003984:Dibenzazepines; D003990:Dibenzoxepins; D006634:Histamine H1 Antagonists; D039563:Histamine H1 Antagonists, Non-Sedating; D007093:Imidazoles; D010880:Piperidines; D011725:Pyridines; D000069605:Olopatadine Hydrochloride; D002744:Chlorpheniramine; C511534:bepotastine besilate; D016593:Terfenadine; C093230:fexofenadine; C053090:epinastine; C058249:ebastine; D017332:Cetirizine