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

Hiroyuki Kamei, Ami Isaji, Yukihiro Noda, Kazuhiro Ishikawa, Koji Senzaki, Kiyofumi Yamada, Kazumitsu Sugiura, Yasushi Tomita, Toshitaka Nabeshima

Research output: Contribution to journalArticle

12 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)263-272
Number of pages10
JournalArchives of Dermatological Research
Volume304
Issue number4
DOIs
Publication statusPublished - 01-05-2012
Externally publishedYes

Fingerprint

fexofenadine
Promethazine
Therapeutic Uses
Histamine
Healthy Volunteers
Placebos
Histamine Antagonists
Non-Sedating Histamine H1 Antagonists
Psychomotor Disorders
Hypnotics and Sedatives
Central Nervous System
Flicker Fusion
Actigraphy
Olopatadine Hydrochloride
Wrist
Automatic Data Processing
Cross-Over Studies
Reaction Time

All Science Journal Classification (ASJC) codes

  • Dermatology

Cite this

@article{0587c1b2ba4c42de8912636c5f0d83f7,
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.",
author = "Hiroyuki Kamei and Ami Isaji and Yukihiro Noda and Kazuhiro Ishikawa and Koji Senzaki and Kiyofumi Yamada and Kazumitsu Sugiura and Yasushi Tomita and Toshitaka Nabeshima",
year = "2012",
month = "5",
day = "1",
doi = "10.1007/s00403-011-1192-2",
language = "English",
volume = "304",
pages = "263--272",
journal = "Archives of Dermatological Research",
issn = "0340-3696",
publisher = "Springer Verlag",
number = "4",

}

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. / Kamei, Hiroyuki; Isaji, Ami; Noda, Yukihiro; Ishikawa, Kazuhiro; Senzaki, Koji; Yamada, Kiyofumi; Sugiura, Kazumitsu; Tomita, Yasushi; Nabeshima, Toshitaka.

In: Archives of Dermatological Research, Vol. 304, No. 4, 01.05.2012, p. 263-272.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Effects of single therapeutic doses of promethazine, fexofenadine and olopatadine on psychomotor function and histamine-induced wheal- and flare-responses

T2 - A randomized double-blind, placebo-controlled study in healthy volunteers

AU - Kamei, Hiroyuki

AU - Isaji, Ami

AU - Noda, Yukihiro

AU - Ishikawa, Kazuhiro

AU - Senzaki, Koji

AU - Yamada, Kiyofumi

AU - Sugiura, Kazumitsu

AU - Tomita, Yasushi

AU - Nabeshima, Toshitaka

PY - 2012/5/1

Y1 - 2012/5/1

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=84862892212&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84862892212&partnerID=8YFLogxK

U2 - 10.1007/s00403-011-1192-2

DO - 10.1007/s00403-011-1192-2

M3 - Article

VL - 304

SP - 263

EP - 272

JO - Archives of Dermatological Research

JF - Archives of Dermatological Research

SN - 0340-3696

IS - 4

ER -