Alvimopan is a μ-opioid receptor antagonist approved in
the U.S. in May 2008 for the treatment of post-operative
ileus (POI) – a temporary dysfunction of the gastrointestines.
Alvimopan does not penetrate the central nervous system
(CNS) and acts as a peripheral antagonist. The molecule inhibits
the negative effects of opioids on the gastrointestinal
(GI) system without inhibiting the desired analgesic effects
of CNS penetrant opioids.
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Treatment of opioid-induced bowel dysfunction, opioidinduced
nausea and vomiting, postoperative ileus, idiopathic
constipation, and irritable bowel syndrome (peripherally
restricted mu opioid receptor antagonist).