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Effects of three narcotic antagonists (naltrexone, diprenorphine, and S-20682) on blood pressure, heart rate and electrical cortical activity.

Abstract
Three narcotic antagonist drugs (EN-1639 or naltrexone, M-5050 or diprenorphine and the 6-oxo analogue of oxilorphan, S-20682) were evaluated in increasing doses (1-80 micrograms/kg) in the unanaesthetised dog for possible effects on blood pressure, heart rate, respiratory rate, arterial blood gases, and convulsive EEG changes. Compared to the control-awake situation, diprenorphine and S-20682 induced hypotension (maximum fall 15%), bradycardia (maximum 12%) and bradypnoea (maximum 25%). These effects were not increased at doses higher than 20 micrograms/kg. Despite the induced bradypnoea, there were no significant changes in arterial pO2 and pCO2. Simultaneously, with the cardio-respiratory changes, EEG activity shifted from high frequency, low amplitudes of the awake state, to low frequency, high amplitudes of a sleep-like state. Convulsive EEG changes were never recorded with any of the tested compounds. It is suggested that the observed cardiovascular changes are due to a reduced state of vigilance, since auditory stimuli induced an arousal reaction with a reversal of the depressed variables. In contrast, naltrexone induced only bradycardia in the observed dose range (maximum 25%). There were no effects on blood pressure, respiratory rate, arterial blood gases and EEG.
AuthorsE Freye, E Hartung, G K Schenk
JournalPharmacology (Pharmacology) Vol. 26 Issue 2 Pg. 110-6 ( 1983) ISSN: 0031-7012 [Print] Switzerland
PMID6133288 (Publication Type: Journal Article)
Chemical References
  • 20682-S
  • Morphinans
  • Narcotic Antagonists
  • Carbon Dioxide
  • Diprenorphine
  • Naltrexone
Topics
  • Animals
  • Blood Pressure (drug effects)
  • Carbon Dioxide (metabolism)
  • Cerebral Cortex (drug effects)
  • Diprenorphine (pharmacology)
  • Dogs
  • Electroencephalography
  • Electrophysiology
  • Heart Rate (drug effects)
  • Morphinans (analogs & derivatives, pharmacology)
  • Naltrexone (pharmacology)
  • Narcotic Antagonists (pharmacology)
  • Respiration (drug effects)

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