What are the reinforcing and analgesic effects of opioid receptor agonists?

Expert Solution

The analgesic and reinforcing effects of opioids are primarily mediated by mu-opioid receptors (MORs), which are widely-expressed in the central and peripheral nervous systems and in the gastrointestinal tract.Medically, opioids are used for pain relief, but chronic use and abuse can lead to physical dependence.
Generally, opioid analgesics used in the clinic are ? agonists. These compounds show strongest efficacy in the treatment of severe acute pain, but their activity remains variable in situations of chronic pain.
In rhesus monkeys, cannabinoids fail to enhance and often decrease self-administration of the mu opioid receptor agonist heroin, suggesting that opioid/cannabinoid mixtures do not have greater reinforcing effects (abuse potential) compared with opioids alone.
Opioids are potent analgesics for nonvisceral as well as visceral pain. However, µ-opioid receptor agonists commonly cause gastrointestinal side effects such as nausea, vomiting, and constipation. Especially in patients with gastrointestinal disorders, these unwanted effects may become dose limiting.

Hayet Jeridi answered 6 months ago

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