Antinociceptive interaction between alprazolam and opioids

Chaim G. Pick*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

25 Scopus citations

Abstract

Alprazolam is a triazolobenzodiasapine, with a potent anxiolytic action and a short half-life. Alprazolam analgesia was measured, using the radiant heat tailflick assay in mice, which was administered alone or in combination with opioids. Intrathecally administered alprazolam produced a dose-response increase in the tailflick latency with an ED50 of 34 μg (19.4-72.5, 95% CL). There were almost no effects after intracerebroventricular injections. Naloxone almost completely abolished the analgesia response mediated by alprazolam. This sensitivity to naloxone indicates that at least some of the analgesic effects of alprazolam are mediated by an opioid mechanism of action. When administered together with various antagonists of opioid receptor subtypes, we found that the μ antagonists, but not the δ and κ1 subtypes inhibited alprazolam analgesia significantly. No effect was found when alprazolam was coadministrated with κ3 opioid agonists. In addition, we found a supra-additivity (synergistic) increase in analgesia when alprazolam was given with morphine. Competition binding assays show the highest affinity of alprazolam to the μ1 subtype. In summary, we conclude that alprazolam mediates its analgesic effect, most probably via an μ opiate mechanism of action.

Original languageEnglish
Pages (from-to)239-243
Number of pages5
JournalBrain Research Bulletin
Volume42
Issue number3
DOIs
StatePublished - 1997

Funding

FundersFunder number
V. Schreiber Foundation of the Tel Aviv University

    Keywords

    • Alprazolam
    • Analgesia
    • Mice
    • Opioid receptors
    • Receptor binding
    • Tailflick

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