title: Effects of single therapeutic doses of promethazine, fexofenadine and olopatadine on psychomotor function and histamine-induced wheal- and flare-responses: a randomized double-blind, placebo-controlled study in healthy volunteers.
abstract: Since most first-generation antihistamines have undesirable sedative effects on the central nervous systems (CNS), newer (second-generation) antihistamines have been developed to improve patients' quality of life. However, there are few reports that directly compare the antihistaminic efficacy and impairment of psychomotor functions. We designed a double-blind, placebo controlled, crossover study to concurrently compare the clinical effectiveness of promethazine, a first-generation antihistamine, and fexofenadine and olopatadine, second-generation antihistamines, by measuring their potency as peripheral inhibitors of histamine-induced wheal and flare. Further, we investigated their sedative effects on the CNS using a battery of psychomotor tests. When single therapeutic doses of fexofenadine (60 mg), olopatadine (5 mg) and promethazine (25 mg) were given in a double-blind manner to 24 healthy volunteers, all antihistamines produced a significant reduction in the wheal and flare responses induced by histamine. In the comparison among antihistamines, olopatadine showed a rapid inhibitory effect compared with fexofenadine and promethazine, and had a potent effect compared with promethazine. In a battery of psychomotor assessments using critical flicker fusion, choice reaction time, compensatory tracking, rapid visual information processing and a line analogue rating scale as a subjective assessment of sedation, promethazine significantly impaired psychomotor function. Fexofenadine and olopatadine had no significant effect in any of the psychomotor tests. Promethazine, fexofenadine and olopatadine did not affect behavioral activity, as measured by wrist actigraphy. These results suggest that olopatadine at a therapeutic dose has greater antihistaminergic activity than promethazine, and olopatadine and fexofenadine did not cause cognitive or psychomotor impairment.
authors: Department of Clinical Pharmacy Practice and Health Care Management, Meijo University, Nagoya, Japan.
authors: Hiroyuki
authors: H
authors: Kamei
authors: Ami
authors: A
authors: Isaji
authors: Yukihiro
authors: Y
authors: Noda
authors: Kazuhiro
authors: K
authors: Ishikawa
authors: Koji
authors: K
authors: Senzaki
authors: Kiyofumi
authors: K
authors: Yamada
authors: Kazumitsu
authors: K
authors: Sugiura
authors: Yasushi
authors: Y
authors: Tomita
authors: Toshitaka
authors: T
authors: Nabeshima
mesh_terms: D000293:Adolescent; D003990:Dibenzoxepins / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D004311:Double-Blind Method; D005260:Female; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000627:therapeutic use*; D006801:Humans; D008297:Male; D000069605:Olopatadine Hydrochloride; D011398:Promethazine / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D011537:Pruritus / Q000188:drug therapy; D011597:Psychomotor Performance / Q000187:drug effects*; D006255:Rhinitis, Allergic, Seasonal / Q000188:drug therapy; D016593:Terfenadine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000627:therapeutic use; D014581:Urticaria / Q000188:drug therapy*; D055815:Young Adult
chemical_list: D003990:Dibenzoxepins; D006634:Histamine H1 Antagonists; D000069605:Olopatadine Hydrochloride; D016593:Terfenadine; C093230:fexofenadine; D011398:Promethazine