Development of Peripheral Opioid Antagonists: New Insights Into Opioid Effects

Moss, Jonathan; Rosow, Carl E.
October 2008
Mayo Clinic Proceedings;Oct2008, Vol. 83 Issue 10, p1116
Academic Journal
The recent approval by the US Food and Drug Administration of 2 medications—methylnaltrexone and alvimopan—introduces a new class of therapeutic entitles to clinicians. These peripherally acting μ-oploid receptor antagonists selectively reverse oploid actions mediated by receptors outside the central nervous system, while preserving centrally mediated analgesia. Methyl-naitrexone, administered subcutaneously, has been approved in the United States, Europe, and Canada. In the United States, it is indicated for the treatment of oploid-induced constipation in patients with advanced illness (eg, cancer, AIDS) who are receiving palliative care, when response to laxative therapy has not been sufficient. Alvimopan, an orally administered medication, has been approved in the United States to facilitate recovery of gastrointestinal function after bowel resection and primary anastomosis. Clinical and laboratory studies performed during the development of these drugs have indicated that peripheral receptors mediate other oploid effects, including decreased gastric emptying, nausea and vomiting, pruritus, and urinary retention. Laboratory investigations with these compounds suggest that oploids affect fundamental cellular processes through mechanisms that were previously unknown. These mechanisms include modifications of human immunodeficiency virus penetration, tumor angiogenesis, vascular permeability, and bacterial virulence.


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