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The analgesic activity of morphine-6-glucuronide
R Osborne1, P Thompson, S Joel
1Imperial Cancer Research Fund Department of Medical Oncology, St Bartholomew's Hospital, London.
British Journal of Clinical Pharmacology
|August 1, 1992
Summary
Morphine-6-glucuronide effectively relieves cancer pain with minimal side effects. This metabolite of morphine is well-tolerated and demonstrates useful analgesic effects in most patients.
Area of Science:
- Pharmacology
- Clinical Medicine
- Pain Management
Background:
- Morphine-6-glucuronide (M6G) is a primary active metabolite of morphine.
- Understanding M6G's pharmacokinetics and effects is crucial for optimizing opioid analgesia.
Purpose of the Study:
- To evaluate the pharmacokinetics, cardio-respiratory effects, and analgesic efficacy of intravenous morphine-6-glucuronide in cancer patients.
- To assess the safety and tolerability of M6G as an analgesic agent.
Main Methods:
- Intravenous M6G was administered to 20 cancer patients at four dose levels.
- Plasma M6G concentrations, cardio-respiratory parameters, and pain relief were monitored.
- Urinary excretion of M6G and its metabolites was quantified.
Main Results:
- The mean elimination half-life of M6G was 3.2 hours, with clearance directly related to creatinine clearance.
- 17 out of 19 assessable patients experienced useful analgesia for 2-24 hours.
- No significant cardio-respiratory changes, sedation, or euphoria were observed; nausea and vomiting were absent.
Conclusions:
- Intravenous morphine-6-glucuronide is an effective and well-tolerated analgesic for cancer pain.
- M6G may be responsible for the majority of morphine's therapeutic benefits.
- Its favorable safety profile suggests M6G as a valuable option in pain management.