Abstract |
Preclinical data and limited studies in humans have suggested that morphine-6-glucuronide (M6G) has analgesic activity and morphine-3-glucuronide (M3G), contributes adversely to the therapeutic effect of morphine. This open point-prevalence study in 103 patients on oral morphine for cancer-related pain investigated the correlations between morphine doses, metabolites, and the degree of pain relief or toxicity. Morphine, M6G, and M3G were assayed by high-performance liquid chromatography on a single blood sample taken between two and four hours after dose. Pain, analgesia, and toxicity were recorded on numerical and visual analog scales. Patients received a median dose of 60 (range, 10 to 620) mg per day morphine, for a median of 4.1 weeks (range, 0.2 to 46.0 weeks). Ml3G:M6G ratios fell within a narrow range, with a median value of 4.39 (interquartile range, 3.78 to 6.96; range, 2.18 to 14.95). There were no significant correlations between M3G:M6G and morphine dose, or any measure of analgesia. The correlation between plasma concentration and pain score (i.e., better analgesia) was stronger for M6G (r = 0.308, p < 0.01) than morphine (r = 0.197, p = 0.05). These data suggest that M6G contributes significantly to the analgesic potency of oral morphine. No evidence was found for differences in M3G. M6G ratios contributing to analgesia or toxicity.
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Authors | Richard T Penson, Simon P Joel, Anna Gloyne, Simon Clark, Maurice L Slevin |
Journal | Journal of opioid management
(J Opioid Manag)
2005 May-Jun
Vol. 1
Issue 2
Pg. 83-90
ISSN: 1551-7489 [Print] United States |
PMID | 17319252
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Analgesics, Opioid
- Glucuronides
- Morphine
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Topics |
- Adult
- Aged
- Aged, 80 and over
- Analgesia
(methods)
- Analgesics, Opioid
(adverse effects, blood, pharmacokinetics, therapeutic use)
- Female
- Glucuronides
(blood)
- Humans
- Male
- Middle Aged
- Morphine
(adverse effects, blood, pharmacokinetics, therapeutic use)
- Neoplasms
(complications)
- Pain
(blood, drug therapy, etiology)
- Pain Measurement
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