The mechanism responsible for the drowsiness caused by first generation H1 antagonists on the EEG pattern

Y. Kaneko, K. Shimada, K. Saitou, Yukio Sugimoto, Chiaki Kamei

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20 Citations (Scopus)

Abstract

The present study was performed to clarify the mechanism responsible for the drowsiness caused by first generation H1 antagonists according to electroencephalogram activity. All H1 antagonists used in the present study caused the EEG-recorded drowsiness pattern, i.e., increases in EEG power spectra of the δ and θ bands at the frontal cortex in rats. The potency of cyproheptadine was greater than those of diphenhydramine and promethazine, while that of pyrilamine was less than those of the other drugs examined. The increase in EEG power spectra in the δ band induced by H1 antagonists was antagonized by pretreatment with both histidine and physostigmine. The effect of pyrilamine was more potently antagonized by histidine and less potently antagonized by physostigmine as compared to diphenhydramine, promethazine and cyproheptadine. The increases in EEG power spectra induced by H1 antagonists were neither antagonized nor potentiated by 5-hydroxytryptophan. These results clearly indicate that the increases in EEG power spectra in the δ and θ bands at the frontal cortex in rats induced by first generation H1 antagonists are responsible for both histaminergic and cholinergic mechanisms. (C) 2000 Prous Science.

Original languageEnglish
Pages (from-to)163-168
Number of pages6
JournalMethods and Findings in Experimental and Clinical Pharmacology
Volume22
Issue number3
Publication statusPublished - 2000

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Keywords

  • Cyproheptadine
  • Diphenhydramine
  • Electroencephalogram power spectra
  • Promethazine
  • Pyrilamine

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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