Eli5: How do opiates cause constipation?

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My research has turned up reports that it slows bowel activity and causes too much water to be absorbed, but what does that have to do with relieving pain?

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Anonymous 0 Comments

The body produces its own opioids (“endogenous opioids”) that bind a variety of receptors (eg mu, kappa, delta receptors) to produce a number of effects. One of these effects is analgesia (reduction of pain). When we consume exogenous opioids, they’ll bind to any opioid receptor they get access to. This results not only in analgesia, but also a number of “side effects”.

Constipation is produced because opioids bind opioid receptors in the gut wall to reduce its contractions that are responsible for pushing food forwards (“peristalsis”). The more specific answer is that opioids bind mu receptors in the gut, which leads to decreased release of acetylcholine from the enteric nervous system. Acetylcholine increases gut peristalsis and secretions, so its inhibition leads to constipation.

Constipation can be problematic in patients on long term opioids for pain control (eg cancer patients). Opioids act on the central nervous system (brain & spinal cord) to cause analgesia. Opioids in such cases are often combined with opioid antagonists that cant enter the central nervous system. Thus these opioid antagonists can bind the opioid receptors on the gut, preventing opioids from causing constipation, but are unable to bind the central receptors that opioids act on to reduce pain.

Anonymous 0 Comments

The body produces its own opioids (“endogenous opioids”) that bind a variety of receptors (eg mu, kappa, delta receptors) to produce a number of effects. One of these effects is analgesia (reduction of pain). When we consume exogenous opioids, they’ll bind to any opioid receptor they get access to. This results not only in analgesia, but also a number of “side effects”.

Constipation is produced because opioids bind opioid receptors in the gut wall to reduce its contractions that are responsible for pushing food forwards (“peristalsis”). The more specific answer is that opioids bind mu receptors in the gut, which leads to decreased release of acetylcholine from the enteric nervous system. Acetylcholine increases gut peristalsis and secretions, so its inhibition leads to constipation.

Constipation can be problematic in patients on long term opioids for pain control (eg cancer patients). Opioids act on the central nervous system (brain & spinal cord) to cause analgesia. Opioids in such cases are often combined with opioid antagonists that cant enter the central nervous system. Thus these opioid antagonists can bind the opioid receptors on the gut, preventing opioids from causing constipation, but are unable to bind the central receptors that opioids act on to reduce pain.