AI Article Synopsis
- - Opioids like morphine provide pain relief (antinociception) when administered directly into the spinal space, but their hydrophilic nature can cause serious side effects, such as respiratory depression.
- - Loperamide, which is hydrophobic and less likely to spread within the spinal canal, has also shown pain relief effects when administered into specific areas of the brain and spinal cord, although its exact mechanism is not fully understood.
- - In a recent study using the formalin test, loperamide significantly reduced pain responses, and this effect was reversed by naloxone, suggesting that its pain-relieving properties are mainly due to activation of opioid receptors.
Article Abstract
Opioids like morphine produce antinociception after intrathecal administration. Being hydrophilic in nature, morphine also spreads rostrally which leads to respiratory depression. Loperamide has been reported to produce antinociception after both intracisternal and intrathecal administration. It is also hydrophobic, which could restrict its diffusion in the spinal canal. However, the mechanism of its antinociceptive action after intrathecal administration is not definitely known. In the present study, the antinociceptive effect of loperamide was evaluated by the formalin test. It significantly inhibited Phase II flinching behavior. This antinociceptive effect was reversed by pre-administration of naloxone indicating that it was predominantly due to activation of opioid receptors.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2753543 | PMC |
| http://dx.doi.org/10.1016/j.neulet.2008.10.067 | DOI Listing |
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