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Bremazocine

An Opiate That Induces Sedation and Analgesia without Respiratory Depression

Received from the Department of Anesthesiology, University Clinics Düsseldorf, Moorenstrasse, Düsseldorf, and the Department of Central Diagnostics, University Clinics Essen, Psychiatry, Hufelandstrasse, Essen, Federal Republic of Germany.

Abstract

The benzomorphan analogue bremazocine has been shown to be a potent analgesic with a low dependence liability and with no respiratory depressant effects in preliminary pharmacologic screening. As this compound may prove to be of potential interest to anesthesiologists, it was tested in the conscious dog in increasing doses (1, 5, 10, 20, and 40 µg/kg) while blood pressure, heart rate, respiratory rate, arterial blood-gas tensions, electrical cortical activity, and somatosensory-evoked potentials (SS-EVP) were recorded. Bremazocine had no significant cardiovascular or respiratory effects. Power spectral analysis of the EEG showed a dose-related increase of power in the theta to delta band. SSEVP was characterized by a decrease in amplitude of the P₄₅ and P₇₀ waves and an increase in the latency of the P₁₀₀ peak. EEG and peak latency changes could be reversed by the kappa-specific antagonist Mr 2266 (20 µg/kg), but not by the classic opiate antagonist naloxone (20 µg/kg). It is suggested that kappa receptor sites distinct from those interacting with common opioids (µ) are responsible for the observed changes associated with bremazocine.

Key Words: ANALGESICS: bremazocine

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Anesthesia & Analgesia® is published for the International Anesthesia Research Society® by Lippincott Williams & Wilkins with the assistance of Stanford University Libraries' HighWire Press®. Copyright 2006 by the International Anesthesia Research Society. Online ISSN: 1526-7598   Print ISSN: 0003-2999