scholarly journals Dyspepsia and Opioid–Induced Bowel Dysfunction: The Role of Opioid Receptor Antagonists

10.5772/56624 ◽  
2013 ◽  
Author(s):  
Wojciech Leppert
Keyword(s):  
Opioid Receptor ◽  
Bowel Dysfunction ◽  
Receptor Antagonists ◽  
Opioid Receptor Antagonists

scholarly journals S1277 The Role of Peripherally Acting µ-Opioid Receptor Antagonists (PAMORA) in Pediatric Opioid-Induced Bowel Dysfunction

2021 ◽  
Vol 116 (1) ◽  
pp. S586-S587
Author(s):  
Thu Pham ◽  
James Noel ◽  
Robert Noel ◽  
Lucile McLoughlin ◽  
Chris Moreau ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Bowel Dysfunction ◽  
Receptor Antagonists ◽  
Opioid Receptor Antagonists

scholarly journals Peripherally Acting μ-Opioid Receptor Antagonists for the Treatment of Opioid-Related Side Effects: Mechanism of Action and Clinical Implications

2017 ◽  
Vol 31 (6) ◽  
pp. 658-669 ◽  
Author(s):  
John M. Streicher ◽  
Edward J. Bilsky
Keyword(s):  
Side Effects ◽  
Opioid Receptor ◽  
Opioid Receptors ◽  
Mechanism Of Action ◽  
Bowel Dysfunction ◽  
Cardiac Risk ◽  
Common Side Effect ◽  
Receptor Antagonists ◽  
Opioid Receptor Antagonists ◽  
Opioid Administration

Opioid receptors are distributed throughout the central and peripheral nervous systems and on many nonneuronal cells. Therefore, opioid administration induces effects beyond analgesia. In the enteric nervous system (ENS), stimulation of µ-opioid receptors triggers several inhibitory responses that can culminate in opioid-induced bowel dysfunction (OBD) and its most common side effect, opioid-induced constipation (OIC). OIC negatively affects patients’ quality of life (QOL), ability to work, and pain management. Although laxatives are a common first-line OIC therapy, most have limited efficacy and do not directly antagonize opioid effects on the ENS. Peripherally acting µ-opioid receptor antagonists (PAMORAs) with limited ability to cross the blood-brain barrier have been developed. The PAMORAs approved by the U S Food and Drug Administration for OIC are subcutaneous and oral methylnaltrexone, oral naloxegol, and oral naldemedine. Although questions of cost-effectiveness and relative efficacy versus laxatives remain, PAMORAs can mitigate OIC and improve patient QOL. PAMORAS may also have applications beyond OIC, including reducing the increased cardiac risk or potential tumorigenic effects of opioids. This review discusses the burden of OIC and OBD, reviews the mechanism of action of new OIC therapies, and highlights other potential opioid-related side effects mediated by peripheral opioid receptors in the context of new OIC therapies.

Role of spacer and address components in peptidomimetic .delta.-opioid receptor antagonists related to naltrindole

1991 ◽  
Vol 34 (5) ◽  
pp. 1715-1720 ◽  
Author(s):  
P. S. Portoghese ◽  
H. Nagase ◽  
K. E. MaloneyHuss ◽  
C. E. Lin ◽  
A. E. Takemori
Keyword(s):  
Opioid Receptor ◽  
Delta Opioid Receptor ◽  
Receptor Antagonists ◽  
Opioid Receptor Antagonists

The opioid bowel syndrome: A review of pathophysiology and treatment

2005 ◽  
Vol 1 (3) ◽  
pp. 153 ◽  
Author(s):  
Mellar P. Davis, MD, FCCP
Keyword(s):  
Opioid Receptor ◽  
Terminally Ill ◽  
Bowel Dysfunction ◽  
Receptor Antagonists ◽  
Specific Therapy ◽  
Terminally Ill Patients ◽  
Opioid Receptor Antagonists

Opioids are responsible for 25 percent of constipation in terminally ill patients. Patients in pain require prophylaxis to prevent opioid bowel syndrome (OBS). Laxatives are the treatment of choice, but are marginally effective. The development of quaternary opioid receptor antagonists is a step toward target-specific therapy for opioidinduced bowel dysfunction. This review will discuss the pathophysiology and management of OBS.

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