Eluxadoline is a minimally absorbed µ-opioid receptor agonist and δ-opioid
receptor antagonist. Studies have shown that when there is simultaneous µ-opioid
receptor agonism and δ-opioid receptor antagonism, patients will experience
decreased abdominal pain and diarrhea.
The dosage approved for the treatment of IBS-D is 100 mg twice daily taken with
food, but the dose is reduced to 75 mg BID in patients who are unable to tolerate 100
mg BID, have no gallbladder, have mild to moderate liver impairment, or are on
organic anion transporting polypeptides (OATP1B1) inhibitors.
with eluxadoline had better clinical response in phase 2 trials with decreased
abdominal pain and increase stool consistency without significant risk of
147 The most common side effects in patients treated with eluxadoline
include constipation, nausea, and abdominal pain.
148 The most serious known risk
associated with eluxadoline is the risk of sphincter of Oddi spasm, which can result
in pancreatitis. Eluxadoline should not be used in patients with a history of bile duct
obstruction, pancreatitis, severe liver impairment, or severe constipation, and in
patients who drink more than three alcoholic beverages daily.
counseled to avoid alosetron or loperamide in combination with eluxadoline on a
chronic basis, although it can be used on an acute as needed basis. If signs of
constipation occur, the patient must be advised to discontinue loperamide
immediately. They must discontinue eluxadoline if they experience constipation for
more than 4 days. Patients should also be advised to avoid concomitant use of
anticholinergics and other opioids with eluxadoline to avoid constipation. They
should be reminded that eluxadoline has a potential for drug abuse.
In L.K.’s case, initiation of loperamide 2 mg as needed before a stressful situation
would be a cost-effective approach to her symptoms. Should her symptoms worsen
or her current regimen lose effectiveness, eluxadoline 100 mg BID with food is an
alternative, while a course of rifaximin 550 mg TID for 14 days would be considered
an alternative strategy if she fails eluxadoline. The patient should be advised not to
combine these therapies for chronic treatment and discontinue eluxadoline if she
experiences constipation for 4 days.
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chapter, with the corresponding reference number in this chapter found in parentheses
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