Related Experiment Video

Updated: Aug 22, 2026

A Method for Evaluating the Reinforcing Properties of Ethanol in Rats without Water Deprivation, Saccharin Fading or Extended Access Training
07:50

A Method for Evaluating the Reinforcing Properties of Ethanol in Rats without Water Deprivation, Saccharin Fading or Extended Access Training

Published on: January 29, 2017

Clinical status of methylnaltrexone, a new agent to prevent and manage opioid-induced side effects

Chun-Su Yuan1

  • 1Department of Anesthesia & Critical Care, Pritzker School of Medicine, The University of Chicago, 5841 S. Maryland Avenue, MC 4028, Chicago, IL 60637, USA. cyuan@airway.uchicago.edu

The Journal of Supportive Oncology
|August 27, 2004
PubMed

Insights

Methylnaltrexone offers a novel approach to managing opioid-induced constipation in cancer patients. This peripherally acting drug targets opioid receptors in the gut, alleviating side effects without compromising pain relief.

Area of Science:

  • Gastroenterology
  • Pharmacology
  • Oncology

Background:

  • Opioids are commonly prescribed for pain management, particularly in advanced cancer.
  • Opioid-induced constipation (OIC) is a frequent and distressing adverse effect.
  • Current treatments for OIC are limited and often ineffective.

Purpose of the Study:

  • To review the clinical data on methylnaltrexone.
  • To evaluate methylnaltrexone's efficacy in treating opioid-induced bowel dysfunction.
  • To assess methylnaltrexone's safety profile and impact on analgesia.

Main Methods:

  • Review of existing clinical trial data.
  • Focus on studies investigating methylnaltrexone's peripheral opioid receptor antagonism.
  • Analysis of outcomes related to gastrointestinal side effects and pain management.

Main Results:

  • Methylnaltrexone selectively antagonizes peripheral opioid receptors.
  • Clinical data suggest methylnaltrexone effectively alleviates OIC.
  • Methylnaltrexone does not appear to interfere with central opioid analgesia.

Conclusions:

  • Methylnaltrexone represents a promising therapeutic option for OIC.
  • Its peripheral action mechanism offers a way to manage OIC without affecting pain control.
  • Further clinical investigation is warranted to establish its role in patient care.

More Related Videos

Investigating Drivers of Antireward in Addiction Behavior with Anatomically Specific Single-Cell Gene Expression Methods09:29

Investigating Drivers of Antireward in Addiction Behavior with Anatomically Specific Single-Cell Gene Expression Methods

Published on: August 4, 2022

Related Concept Videos

Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
Analgesia and Pain Management01:25

Analgesia and Pain Management

Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
Opioid Analgesics: Morphine and Other Natural Cogeners01:20

Opioid Analgesics: Morphine and Other Natural Cogeners

Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
Opioid Receptors: Overview01:22

Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
Pharmaceutical Poisoning: Treatment Strategies01:26

Pharmaceutical Poisoning: Treatment Strategies

Treatment strategies for poisoning are a critical aspect of emergency medicine, focusing on preventing the absorption of toxins and enhancing their elimination. When a poisoning incident occurs, the first response is to halt exposure and decontaminate the patient, particularly through gastrointestinal (GI) methods if the poison was ingested.Gastrointestinal Decontamination Techniques:Activated charcoal is the cornerstone of GI decontamination. It works through adsorption, binding the toxin to...
Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

Sedatives and Hypnotics Drugs: Miscellaneous Agents

Sedatives and hypnotics encompass a wide range of substances, each with its unique mechanism of action, uses, and potential adverse effects.
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...