Eluxadoline

Eluxadoline is a prescription medication used to treat the symptoms of irritable bowel syndrome (IBS). 

• Eluxadoline is available under the following different brand names: Viberzi

Common side effects of Eluxadoline include:

• Constipation,
• Nausea,
• Vomiting,
• Abdominal pain, and
• Drowsiness

Serious side effects of Eluxadoline include:

• Hives,
• Difficulty breathing,
• Swelling of your face, lips, tongue, or throat,
• Suddenly worsening stomach pain that moves to your back or shoulder,
• Persistent nausea or vomiting, and
• Dizziness

Rare side effects of Eluxadoline include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Tablet: Schedule IV

• 75 mg
• 100 mg

Irritable Bowel Syndrome

Adult dosage

• 100 mg orally two times a day with food
• Discontinue in patients who develop severe constipation lasting over 4 days

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Eluxadoline has severe interactions with no other drugs.
• Eluxadoline has serious interactions with at least 82 other drugs.
• Eluxadoline has moderate interactions with at least 114 other drugs.
• Eluxadoline has minor interactions with the following drug
  • voclosporin

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Documented hypersensitivity to drug or components of the formulation
• Patients who do not have a gallbladder
• Known or suspected gallbladder obstruction, biliary duct obstruction, or sphincter of Oddi disease or dysfunction; increased risk for sphincter of Oddi spasm
• Alcoholism, alcohol abuse, alcohol addiction, or in patients who drink above 3 alcoholic beverages/day: increased risk of pancreatitis
• History of pancreatitis, pancreatic duct obstruction, or structural diseases of the pancreas; increased risk of acute pancreatitis
• Severe hepatic impairment (Child-Pugh C); risk of significantly increased eluxadoline plasma concentrations
• History of chronic or severe constipation or sequelae from constipation, or known mechanical GI obstruction; increased risk of bowel obstruction

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Eluxadoline?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Eluxadoline?”

Cautions

• Eluxadoline is a mu-opioid receptor agonist; because of this mechanism of action, the potential for increased risk of sphincter of Oddi spasm exists, resulting in pancreatitis or hepatic enzyme elevation associated with acute abdominal pain (see Contraindications)
• There is a risk of sphincter of Oddi spasm, resulting in pancreatitis or hepatic enzyme elevation associated with acute abdominal pain (. g., biliary-type pain) in patients receiving therapy; instruct patients to immediately stop therapy and seek medical attention if they experience symptoms suggestive of the sphincter of Oddi spasm such as acute worsening of abdominal pain
• Increased risk of pancreatitis not associated with sphincter of Oddi spasm reported; most cases were associated with excessive alcohol use
• In patients with a gallbladder, evaluate a patient’s alcohol intake before starting therapy; instruct patients to avoid chronic or acute excessive alcohol use while in therapy; monitor for new or worsening abdominal pain that may radiate to the back or shoulder, with or without nausea and vomiting; instruct patients to immediately stop therapy and seek medical attention if they experience symptoms suggestive of pancreatitides such as acute abdominal or epigastric pain radiating to back or shoulder associated with elevations of pancreatic enzymes with or without nausea and vomiting
• Constipation requiring hospitalization reported; severe cases with development of intestinal obstruction, intestinal perforation, and fecal impaction, requiring intervention, also reported; instruct patients to stop therapy and immediately contact their healthcare provider if they experience severe constipation; avoid the use of other drugs that may cause constipation
• In post-marketing experience, serious hypersensitivity reactions (including anaphylaxis) were reported; some of these reactions occurred after the first one or two doses of treatment; instruct patients to immediately stop therapy and seek medical attention if they experience symptoms suggestive of a hypersensitivity reaction
• Patients who do not have a gallbladder
  • Monitor patients without a gallbladder for new or worsening abdominal pain, with or without nausea and vomiting, or acute biliary pain with liver or pancreatic enzyme elevations
  • Discontinue therapy and seek medical attention if symptoms develop
  • March 2017: An FDA review found patients who do not have a gallbladder are at increased risk of developing serious pancreatitis that could result in hospitalization or death
• Symptoms of pancreatitis have occurred with just 1 or 2 doses of eluxadoline at the recommended dosage for patients who do not have a gallbladder (75 mg) and who do not consume alcohol
• Pancreatitis, with or without sphincter of Oddi spasm, reported in patients taking either the 75 mg or 100 mg dosage, including serious cases resulting in hospitalization, primarily in patients without a gallbladder; fatal cases also reported in patients without a gallbladder
• The FDA is recommending the following
  • Physicians should not prescribe eluxadoline to patients without a gallbladder
  • Patients taking eluxadoline who do not have a gallbladder should talk to their healthcare professional to consider other treatment options
• Data summary
  • From May 2015 through February 2017, the FDA received reports of 120 serious cases of pancreatitis or death; 76 of these cases resulted in hospitalization, of which 2 patients died
  • Among the 68 cases that reported gallbladder status, 56 cases of pancreatitis or death occurred in patients who do not have a gallbladder
  • Many patients (n=44/56) received the currently recommended dosage (75 mg) for patients who do not have a gallbladder
  • Of the 56 cases of patients who do not have a gallbladder, 21 reported that the patient did not abuse alcohol, and 35 did not report alcohol use status
• Drug interaction overview
  • OATP1B1 inhibitors may increase systemic exposure to eluxadoline
  • Strong CYP inhibitors may increase systemic exposure to eluxadoline
  • Risk of constipation increased when coadministered with other drugs that cause constipation
  • Eluxadoline may increase the systemic exposure of coadministered OATP1B1 and BCRP substrates
  • Eluxadoline may increase systemic exposure to coadministered CYP3A substrates with a narrow therapeutic index

Pregnancy and Lactation

• No studies on pregnant women
• Lactation
  • Unknown if distributed in human breast milk
  • Secreted in rat milk
  • Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed infant from the drug or the underlying maternal condition