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Eluxadoline

Medically reviewed by Drugs.com. Last updated on Jul 3, 2020.

Pronunciation

(el ux AD oh leen)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Viberzi: 75 mg, 100 mg

Brand Names: U.S.

  • Viberzi

Pharmacologic Category

  • Gastrointestinal Agent, Miscellaneous

Pharmacology

Eluxadoline is a mixed mu-opioid receptor agonist, delta opioid receptor antagonist, and kappa opioid receptor agonist which acts locally to reduce abdominal pain and diarrhea in patients with IBS-D without constipating side effects.

Metabolism

Not clearly established; there is evidence that glucuronidation can occur to form an acyl glucuronide metabolite

Excretion

Feces (82.2%); urine (<1%)

Time to Peak

1.5 hours (range: 1 to 8 hours) under fed conditions; 2 hours (range: 0.5 to 6 hours) under fasting conditions

Half-Life Elimination

3.7 to 6 hours

Protein Binding

81%

Special Populations: Renal Function Impairment

Mean Cmax and AUC0-t were up to 2.4- to 5.9-fold higher, respectively, in patients with eGFR ≤30 mL/minute/m2.

Special Populations: Hepatic Function Impairment

Mean eluxadoline plasma exposure was 6-fold, 4-fold, and 16-fold higher in mild, moderate, and severe hepatically impaired subjects (Child Pugh Class A, B, C), respectively.

Use: Labeled Indications

Irritable bowel syndrome with diarrhea: Treatment of irritable bowel syndrome with diarrhea (IBS-D) in adults

Contraindications

Hypersensitivity to eluxadoline or any component of the formulation; patients without a gallbladder; known or suspected biliary duct obstruction or sphincter of Oddi disease or dysfunction; history of pancreatitis or structural diseases of the pancreas, including known or suspected pancreatic duct obstruction; alcoholism, alcohol abuse, or alcohol addiction, or in patients who drink >3 alcoholic beverages per day; severe hepatic impairment (Child-Pugh class C); history of chronic or severe constipation or sequelae from constipation; mechanical gastrointestinal obstruction (known or suspected).

Canadian labeling: Additional contraindications (not in US labeling): Mild and moderate hepatic impairment (Child-Pugh class A and B); concomitant use with potent OATP1B1 inhibitors (eg, cyclosporine).

Dosing: Adult

Irritable bowel syndrome with diarrhea: Oral: 100 mg twice daily; may decrease to 75 mg twice daily in patients unable to tolerate the 100 mg dose

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Adjustment for Toxicity

Constipation: Discontinue use in patients who develop severe constipation.

Pancreatitis or sphincter of Oddi spasms: Discontinue use in patients with symptoms of pancreatitis or sphincter of Oddi spasm; permanently discontinue use in patients who develop biliary duct obstruction or sphincter of Oddi spasm.

Administration

Administer with food.

Dietary Considerations

Take with food

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Alcohol (Ethyl): May enhance the adverse/toxic effect of Eluxadoline. Specifically, alcohol use may increase the risk of pancreatitis. Avoid combination

Alosetron: May enhance the constipating effect of Eluxadoline. Avoid combination

Alpelisib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Alpelisib. Management: Avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib due to the potential for increased alpelisib concentrations and toxicities. If coadministration cannot be avoided, closely monitor for increased alpelisib adverse reactions. Consider therapy modification

Anticholinergic Agents: May enhance the constipating effect of Eluxadoline. Avoid combination

Asunaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Asunaprevir. Avoid combination

Cladribine: BCRP/ABCG2 Inhibitors may increase the serum concentration of Cladribine. Management: Avoid concomitant use of BCRP inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider dose reduction of the BCRP inhibitor and separation in the timing of administration. Consider therapy modification

Elagolix: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix. Avoid combination

Elagolix, Estradiol, and Norethindrone: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Elagolix, Estradiol, and Norethindrone. Specifically, concentrations of elagolix may be increased. Avoid combination

Grazoprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Grazoprevir. Avoid combination

Loperamide-Loperamide Oxide: May enhance the constipating effect of Eluxadoline. Monitor therapy

Nitisinone: May increase the serum concentration of OAT1/3 Substrates. Monitor therapy

OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors: May increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with OATP1B1/1B3 inhibitors and monitor patients for increased eluxadoline effects/toxicities. Consider therapy modification

Opioid Agonists: May enhance the constipating effect of Eluxadoline. Avoid combination

Ozanimod: BCRP/ABCG2 Inhibitors may increase serum concentrations of the active metabolite(s) of Ozanimod. Avoid combination

PAZOPanib: BCRP/ABCG2 Inhibitors may increase the serum concentration of PAZOPanib. Avoid combination

Pretomanid: May increase the serum concentration of OAT1/3 Substrates. Monitor therapy

Revefenacin: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase serum concentrations of the active metabolite(s) of Revefenacin. Avoid combination

Rimegepant: BCRP/ABCG2 Inhibitors may increase the serum concentration of Rimegepant. Avoid combination

Ritonavir: May increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with ritonavir and monitor patients for increased eluxadoline effects/toxicities. Consider therapy modification

Rosuvastatin: Eluxadoline may increase the serum concentration of Rosuvastatin. Management: Use the lowest effective dose of rosuvastatin if combined with eluxadoline. Consider therapy modification

Saquinavir: May increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with saquinavir and monitor patients for increased eluxadoline effects/toxicities. Consider therapy modification

Talazoparib: BCRP/ABCG2 Inhibitors may increase the serum concentration of Talazoparib. Monitor therapy

Tipranavir: May increase the serum concentration of Eluxadoline. Management: Decrease the eluxadoline dose to 75 mg twice daily if combined with tipranavir and monitor patients for increased eluxadoline effects/toxicities. Consider therapy modification

Tolvaptan: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates. Management: Avoid concomitant use of OATP1B1/1B3 substrates in patients receiving the Jynarque brand of tolvaptant. Concentrations and effects of the OATP1B1/1B3 substrate would be expected to increase with combined use. Consider therapy modification

Tolvaptan: May increase the serum concentration of OAT1/3 Substrates. Management: Avoid concomitant use of OAT1/3 substrates in patients receiving the Jynarque brand of tolvaptan. Concentrations and effects of the OAT1/3 substrate would be expected to increase with combined use. Consider therapy modification

Topotecan: BCRP/ABCG2 Inhibitors may increase the serum concentration of Topotecan. Avoid combination

Ubrogepant: BCRP/ABCG2 Inhibitors may increase the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a BCRP inhibitor. Consider therapy modification

Voxilaprevir: OATP1B1/1B3 (SLCO1B1/1B3) Inhibitors may increase the serum concentration of Voxilaprevir. Avoid combination

Adverse Reactions

1% to 10%:

Central nervous system: Dizziness (3%), fatigue (3%), drowsiness (≤2%), euphoria (≤2%), intoxicated feeling (≤2%), sedation (≤2%)

Dermatologic: Skin rash (3%)

Gastrointestinal: Constipation (7% to 8%), nausea (7% to 8%), abdominal pain (6% to 7%), vomiting (4%), abdominal distention (3%), flatulence (3%), viral gastroenteritis (3%), gastroesophageal reflux disease (≤2%)

Hepatic: Increased serum alanine aminotransferase (2% to 3%), increased serum aspartate aminotransferase (≤2%)

Respiratory: Upper respiratory tract infection (5%), nasopharyngitis (4%), bronchitis (3%), asthma (≤2%), bronchospasm (≤2%), respiratory failure (≤2%), increased bronchial secretions (≤2%)

<1%, postmarketing, and/or case reports: Anaphylaxis, angioedema, chest pain, chest tightness, dyspnea, fecal impaction, hypersensitivity reaction, intestinal obstruction, intestinal perforation, pancreatitis, pharyngeal edema, spasm of sphincter of Oddi

Warnings/Precautions

Concerns related to adverse effects:

• Constipation: Constipation, sometimes requiring hospitalization, has been reported; severe cases with intestinal obstruction, intestinal perforation, and fecal impaction requiring intervention may also occur. Discontinue use immediately if severe constipation occurs; avoid concomitant use with drugs that may cause constipation.

• Hypersensitivity reactions: Severe hypersensitivity reactions, including anaphylaxis, have been reported during postmarketing surveillance. Some reactions occurred following the first or second dose. Discontinue immediately in patients who develop signs or symptoms of a hypersensitivity reaction.

• Pancreatitis: May cause pancreatitis, with or without sphincter of Oddi spasm, including serious cases (some fatal) requiring hospitalization. Primarily occurs in patients without a gallbladder (use is contraindicated). Most reported serious pancreatitis cases occurred within a week of starting treatment; some developed after 1 or 2 doses. Avoid chronic or acute excessive alcohol use during therapy. Monitor for signs and symptoms of pancreatitis; discontinue use if new or worsening abdominal pain that may radiate to the back or shoulder (with or without nausea/vomiting) develops.

• Sphincter of Oddi spasm: May cause sphincter of Oddi spasm resulting in pancreatitis or elevated hepatic enzymes; most reported serious cases occurred during the first week of treatment, while some developed symptoms after 1 or 2 doses. Discontinue use if patients experience symptoms of sphincter of Oddi spasm such as acute worsening of epigastric- or biliary-type abdominal pain (eg, right upper quadrant pain) that may radiate to the back or shoulder with or without nausea/vomiting, associated with elevations of pancreatic enzymes or hepatic transaminases. Permanently discontinue use in patients who develop biliary duct obstruction or sphincter of Oddi spasm.

Disease-related concerns:

• Hepatic impairment: Plasma concentrations are increased in patients with hepatic impairment; contraindicated in patients with severe hepatic impairment. Use with caution in patients with mild to moderate hepatic impairment; dosage adjustment required.

• Renal impairment: Use with caution in patients with moderate to severe renal impairment; dosage adjustment required.

Other warnings/precautions:

• Abuse potential: Current data suggest that eluxadoline has some potential for drug abuse and psychological dependence. Naloxone should be considered in the event of overdose.

Monitoring Parameters

Monitor for signs/symptoms of pancreatitis (new or worsening abdominal pain that may radiate to the back, with or without nausea/vomiting) or sphincter of Oddi spasm (eg, acute epigastric or biliary pain with hepatic or pancreatic enzyme elevations); hepatic and renal function (at baseline and when clinically indicated); impaired mental or physical abilities.

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies.

Patient Education

What is this drug used for?

• It is used to treat irritable bowel syndrome.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Common cold symptoms

• Nausea

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Pancreatitis like severe abdominal pain, severe back pain, severe nausea, or vomiting.

• Abdominal pain

• Constipation

• Abdominal pain that moves to back or shoulder with or without nausea and vomiting

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

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