Vol 12, No 4 (2018)
Review paper
Published online: 2019-01-21
The role of metabolites in morphine analgesic effects
Palliat Med Pract 2018;12(4):198-202.
Abstract
Morphine is metabolized into two main metabolites, morphine-3-glucuronide and morphine-6-glucuronide. Morphine-6-glucuronide is a potent analgesic that is responsible for up to 97% of the analgesic effect. Morphine-3-glucuronide does not bind to opioid receptors and is devoid of any analgesic effect. However, it activates the Toll-like 4 receptors initiating neurogenic inflammation in the central nervous system. This, in turn, is responsible for anti–analgesic and hyperalgesic effects. There are a number of strategies on how to inhibit this pronociceptive effect and finally improve morphine analgesia.
Palliat Med Pract 2018; 12, 4: 198–202
Keywords: painmorphine metabolismmorphine-3-glucuronidemorphine-6-glucuronideopioid receptorsanalgesiaToll-like 4 receptors
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