Pharmacologic effects of naldemedine, a peripherally acting μ-opioid receptor antagonist, in in vitro and in vivo models of opioid-induced constipation.

Author: AraiTohko, ChibaHiroki, HasegawaMinoru, HoritaNarumi, KanemasaToshiyuki, KiharaTsuyoshi, KoikeKatsumi, MoriokaYasuhide, NakamuraAtsushi, OnoHiroko

Paper Details 
Original Abstract of the Article :
BACKGROUND: Naldemedine (S-297995) is a peripherally acting μ-opioid receptor antagonist developed as a once-daily oral drug for opioid-induced constipation (OIC) in adults with chronic noncancer or cancer pain. This study characterized the pharmacological effects of naldemedine in vitro and in vivo...See full text at original site
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引用元:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6850587/

データ提供:米国国立医学図書館(NLM)

Naldemedine: A New Hope for Opioid-Induced Constipation

Opioid-induced constipation (OIC) is a common and often debilitating side effect of opioid medications. This study explores the potential of naldemedine, a peripherally acting μ-opioid receptor antagonist, as a treatment for OIC, offering hope for patients seeking relief from this frustrating condition.

This study investigates the pharmacological effects of naldemedine in various in vitro and in vivo models. The research demonstrates that naldemedine effectively reduces OIC in animal models without compromising opioid analgesia, suggesting that it could be a safe and effective treatment for OIC in humans. The study also provides insights into the mechanisms of action of naldemedine, revealing its potent binding affinity to μ-, δ-, and κ-opioid receptors.

The study's findings provide compelling evidence for the potential of naldemedine as a treatment for OIC. Its targeted action, focusing on peripheral opioid receptors, suggests that it could be a safe and effective option for managing OIC without affecting the analgesic properties of opioids. This could be a significant breakthrough in addressing a common and often challenging side effect of opioid therapy.

A New Era in Opioid Management

This study marks a potential turning point in the management of OIC, a common and often debilitating side effect of opioid medications. Naldemedine, with its targeted action and promising results, could offer a new era in opioid management, allowing patients to benefit from the analgesic effects of opioids without the burden of constipation.

Relief for Opioid Users

For individuals who rely on opioid medication for pain management, constipation can be a significant source of discomfort and disruption to daily life. This research offers a beacon of hope, suggesting that naldemedine could provide a safe and effective solution for relieving OIC, potentially improving the quality of life for opioid users.

Dr. Camel's Conclusion

This study provides a promising glimpse into the potential of naldemedine as a treatment for OIC. Its targeted action and impressive results offer hope for individuals seeking relief from this common and often challenging side effect of opioid therapy. Like a camel navigating a desert oasis, we must continue our quest for better ways to manage opioid use, ensuring patient safety and well-being while maximizing the benefits of these life-saving medications.

Date :
  1. Date Completed 2020-04-13
  2. Date Revised 2022-08-16
Further Info :

Pubmed ID

30821019

DOI: Digital Object Identifier

PMC6850587

Related Literature

SNS
PICO Info
in preparation
Languages

English

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