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[Local anesthetic effects of morphine and naloxone]
Abstract:
The effects of both morphine (Mo) and naloxone (Nal), topically applied to the desheathed saphenous nerve, were studied in Sprague-Dawley rats during 22 min of superfusion at various concentrations (Mo: 0.086, 0.28, 0.86, 2.8, 8.6 mM/l; Nal: 0.1, 0.33, 1.0 mM/l) by recording single C-fibres. C-fibres were electrically stimulated and the latencies of action potentials were measured. Both drugs impaired nerve conduction in a dose-dependent, fully reversible manner. At high concentrations, conduction was blocked in 5 of 11 (Mo 2.8 mM/l) and 3 of 8 (Nal 1 mM/l) fibres. Mo (8.6 mM/l) instantly blocked all C-fibres investigated. Subsequent washing out of the drug resulted in complete recovery. The findings indicate that Mo and Nal also show local anaesthetic properties; a non-opiate receptor-specific mechanism is postulated. In spite of their blocking action, at present neither Mo nor Nal seems to provide distinct advantages over other agents that have been used successfully to induce reversible nerve blockade at peripheral sites. Due to the rather high dosage necessary (1-2 mg/ml), well-known side-effects of these opiates must also be taken into consideration.
Insights
Morphine and naloxone, when applied to nerves, act as local anesthetics by blocking nerve conduction. This effect is dose-dependent and reversible, suggesting a non-opioid mechanism.
Area of Science:
- Neuroscience
- Pharmacology
Context:
- The saphenous nerve in Sprague-Dawley rats was superfused with morphine and naloxone.
- Single C-fibres were recorded during electrical stimulation.
Purpose:
- To investigate the local anesthetic properties of morphine and naloxone.
- To determine the dose-dependent effects and reversibility of these drugs on nerve conduction.
Summary:
- Morphine and naloxone impaired C-fibre nerve conduction in a dose-dependent and reversible manner.
- High concentrations of morphine and naloxone blocked conduction, with morphine at 8.6 mM/l instantly blocking all tested C-fibres.
- The findings suggest a non-opiate receptor-specific mechanism for their local anesthetic effects.
Impact:
- Morphine and naloxone exhibit local anesthetic properties, though high dosages and side effects may limit clinical utility.
- Neither drug currently offers advantages over existing agents for reversible peripheral nerve blockade.