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Published on: July 29, 2014
Peripheral opioid receptor agonists for analgesia: a comprehensive review
Nalini Vadivelu1, Sukanya Mitra, Roberta L Hines
1Department of Anesthesiology, Yale University School of Medicine, New Haven, Connecticut, USA.
Journal of Opioid Management
|March 26, 2011
Summary
Peripheral opioid receptors offer pain relief without central side effects. Research is advancing peripherally acting opioid agonists for potential clinical use.
Area of Science:
- Neuroscience
- Pharmacology
- Pain Management
Background:
- Opioid receptors are found in the dorsal root ganglia and primary afferent neuron terminals.
- Peripheral terminals of afferent nerves can modulate nociception (pain perception).
- Opioid analgesia can be mediated by peripheral opioid receptors.
Purpose of the Study:
- To describe the peripheral opioidergic system.
- To review the development of peripherally active opioid receptor agonists.
- To discuss their potential clinical applications.
Main Methods:
- Conducted online and manual literature searches.
- Used keywords: peripheral opioid receptors, peripherally restricted opioid agonists.
- Reviewed full-text articles and cross-referenced findings.
Main Results:
- Peripherally acting opioids may provide analgesia without central adverse effects.
- Several peripherally restricted opioid agonists are in development, with some in clinical trials.
- Existing drugs like loperamide show variable analgesic effects peripherally.
Conclusions:
- Peripheral opioid analgesia is a promising research area for basic and clinical science.
- Ongoing research aims to enhance peripheral opioid analgesia.
- Further development of peripherally acting opioid agonists is anticipated.
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