Treatment of opioid-induced gut dysfunction

  title={Treatment of opioid-induced gut dysfunction},
  author={Peter Holzer},
  journal={Expert Opinion on Investigational Drugs},
  pages={181 - 194}
  • P. Holzer
  • Published 24 January 2007
  • Medicine, Biology
  • Expert Opinion on Investigational Drugs
Opioid analgesics are the mainstay in the treatment of moderate-to-severe pain, yet their use is frequently associated with adverse effects, the most common and debilitating being constipation. Opioid-induced motor stasis results from blockade of gastrointestinal peristalsis and fluid secretion, and reflects the action of the endogenous opioid system in the gut. Methylnaltrexone and alvimopan are new investigational drugs that selectively target peripheral μ-opioid receptors because they are… 

The impact of opioid analgesics on the gastrointestinal tract function and the current management possibilities

The aim of this article is to review the pathomechanism and possible treatment strategies of OIBD and target opioid receptors in the gut that seem to be the main source of O IBD.

Treatment of Opioid-induced Constipation: A Therapeutic Update

A step-wise approach to treating OIC should be considered which includes life style modifications, administration of laxatives and stool-softeners, and if necessary, pharmacologic agents to enhance bowel motility and antagonize peripheral μ-opioid receptors.

The Novel Role of Opioid μ-receptors in Gastroenterology

It is meaningful that a novel target is provided for handling of OIC in cancer patients receiving chronic opioid therapy and the activation of opioid μ-2 receptors seems associated with OIC induced by opioid analgesics.

Clinical potential of naloxegol in the management of opioid-induced bowel dysfunction

As naloxegol is administered orally once daily, has proven efficacious compared to placebo, has an acceptable safety profile, and can be used as add-on to existing pain treatment, it is a welcoming addition to the targeted treatment possibilities for OIBD.

Opioid-Induced Bowel Dysfunction

Multiple agents currently in development show promise in treating OIC without significant impact on analgesia or precipitation of withdrawal symptoms, and the approval and availability of such medications would represent a significant improvement in the management of OIC and OIBD in patients with chronic pain.

Opioid antagonists for prevention and treatment of opioid-induced gastrointestinal effects

  • P. Holzer
  • Medicine, Biology
    Current opinion in anaesthesiology
  • 2010
The availability of opioid receptor antagonists with restricted access to the central nervous system provides a novel opportunity to specifically control opioid-induced constipation and other peripheral adverse effects of opioid analgesics.

Opioid receptors in the gastrointestinal tract

  • P. Holzer
  • Biology, Medicine
    Regulatory Peptides
  • 2009

Opioid-Induced Bowel Dysfunction

Traditional laxatives are normally prescribed but they are often insufficient to alleviate symptoms, especially those from the upper gastrointestinal tract, and new prokinetics, such as prucalopride and lubiprostone, may be more effective in alleviate OIBD.

Methylnaltrexone for the management of unwanted peripheral opioid effects

Clinical trials have shown methylnaltrexone to be of benefit in opioid-induced constipation, postoperative ileus and urinary retention, while analgesia remains unabated, and holds great promise in freeing opioid therapy of some of its most-feared adverse aspects.



Assessment of nalmefene glucuronide as a selective gut opioid antagonist.

Management of Opioid‐Induced Gastrointestinal Effects in Patients Receiving Palliative Care

A strong understanding of the pathophysiology of the sequelae is therefore paramount, and many pharmacotherapeutic agents available with which to prevent or treat these side effects are examined.


Alvimopan, a selective peripherally acting μ‐opioid antagonist *

  • M. Camilleri
  • Medicine
    Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society
  • 2005
A review of the basic and applied pharmacology and current evidence for the use of the medication, alvimopan, in clinical gastroenterology addresses the clinical need for effective medications for the treatment of postoperative ileus and opiate‐induced constipation and other motility disorders.

Methylnaltrexone, a novel peripheral opioid receptor antagonist for the treatment of opioid side effects

This article reviews preclinical studies and clinical opioid bowel dysfunction trial data, and briefly discusses other potential roles of this compound in clinical practice.

The central and peripheral influences of opioids on gastrointestinal propulsion.

This article represents an effort to lay out a framework against which to assess the relative roles of central and peripheral opioid-specific mechanisms affecting gastrointestinal propulsion.

Endogenous nitric oxide modulates morphine-induced constipation.