eluxadoline (Rx)

Brand and Other Names:Viberzi
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet: Schedule IV

  • 75mg
  • 100mg

Irritable Bowel Syndrome

Indicated for diarrhea-predominant irritable bowel syndrome (IBS-D) in adult men and women

100 mg PO BID with food

Discontinue in patients who develop severe constipation lasting >4 days

Dosage Modifications

Decrease dose to 75 mg PO BID in patients who

  • are unable to tolerate the 100-mg dose
  • are receiving concomitant OATP1B1 inhibitors
  • have mild-to-moderate hepatic impairment

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A or B): Decrease dose to 75 mg PO BID; monitor for impaired mental or physical abilities needed to perform potentially hazardous activities
  • Severe (Child-Pugh C): Contraindicated

Safety and efficacy not established

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Interactions

Interaction Checker

and eluxadoline

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Constipation (7-8%)

            Nausea (7-8%)

            Abdominal pain (6-7%)

            URT infection (3-5%)

            Vomiting (4%)

            Nasopharyngitis (3-4%)

            Abdominal distention (3%)

            Bronchitis (3%)

            Dizziness (3%)

            Flatulence (3%)

            Rash (3%)

            Increased ALT (2-3%)

            Fatigue (2-3%)

            Viral gastroenteritis (1-3%)

            ≤2%

            • Gastrointestinal: GERD
            • General disorders: Feeling drunk
            • Investigations: Increased AST
            • Nervous system: Sedation, somnolence
            • Psychiatric disorders: Euphoric mood
            • Respiratory: Asthma, bronchospasm, respiratory failure, wheezing

            <1%

            Severe constipation

            Postmarketing Reports

            Hypersensitivity: anaphylaxis, angioedema (e.g. swollen face and throat), dyspnea, throat tightness, and chest pain/tightness

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            Warnings

            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 >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

            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 risk of sphincter of Oddi spasm, resulting in pancreatitis or hepatic enzyme elevation associated with acute abdominal pain (e.g., biliary-type pain) in patients receiving therapy; instruct patients to immediately stop therapy and seek medical attention if they experience symptoms suggestive of 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 prior to 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 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 pancreatitis such as acute abdominal or epigastric pain radiating to back or shoulder associated with elevations of pancreatic enzymes with or without nausea and vomiting

            In postmarketing experience, serious hypersensitivity reactions (including anaphylaxis) reported; some of these reactions occurred after 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 health care 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
              • The majority of patients (n=44/56) received the currently recommended dosage (75 mg) for patients who do not have a gallbladder
              • Of the 56 cases in 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 systemic exposure of coadministered OATP1B1 and BCRP substrates
            • Eluxadoline may increase systemic exposure of coadministered CYP3A substrates with a narrow therapeutic index
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            Pregnancy & Lactation

            Pregnancy

            No studies in pregnant women

            Animal reproduction studies

            • Oral and SC administration of eluxadoline to rats and rabbits during organogenesis at doses approximately 51 and 115 times the human exposure after a single oral dose of 100 mg, respectively, demonstrated no teratogenic effects. In a prenatal and postnatal development study in rats
            • No adverse effects were observed in offspring with oral administration of eluxadoline at doses approximately 10 times the human exposure

            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 from the underlying maternal condition

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Mu opioid receptor agonist; it also is a delta opioid receptor antagonist and a kappa opioid receptor agonist

            The multiple opioid activity is designed to treat the symptoms of IBS-D while reducing the incidence of constipation that can occur with unopposed mu opioid receptor agonists

            Absorption

            Peak plasma time: 1.5 hr (with food); 2 hr (fasting)

            Peak plasma concentration: 2-4 ng/mL (decreased by 50% with high-fat meal)

            AUC: 12-22 ng•hr/mL (decreased by 60% with high-fat meal)

            Distribution

            Protein bound: 81%

            Metabolism

            Not clearly established; eluxadoline may decrease elimination of CYP3A, OATP1B1, and BCRP substrates

            OATP1B1 inhibitors and strong CYP inhibitors may decrease elimination of eluxadoline

            Evidence exists that glucuronidation can occur to form an acyl glucuronide metabolite

            Elimination

            Half-life: 3-7-6 hr

            Excretion: 82.2% feces; <1% urine

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            Administration

            Instructions

            Take with food

            If a dose is missed, take the next dose at the regular time; do not take 2 doses at the same time to make up for a missed dose

            Discontinue with severe constipation that lasts >4 days

            Storage

            Store at controlled room temperature (20-25°C [68-77°F]); excursions permitted to 15-30°C (59-86°F)

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            Formulary

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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