ELUXADOLINE

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Created Jun 2019 | Updated Nov 2020

ELUXADOLINE

  • [VIBERZI]
  • [TRUBERZI]

DEA CODE 9725: Schedule 4

Viberzi is a medication approved by the U.S. Food and Drug Administration for the treatment of diarrhea-predominant IBS in adults. Viberzi was designed to act locally on the digestive tract to help control diarrhea and alleviate abdominal pain caused by the disease. While doctors still don't fully understand what causes the recurrent symptoms of IBS (including abdominal pain, bloating, gas, diarrhea, or constipation), Viberzi is able to provide relief to sufferers who don't respond to traditional anti-diarrheal agents. Viberzi is available by prescription.

Viberzi works by activating or impeding various opioid receptors in the digestive tract. These are the receptors involved in gut motility, pain sensation, and the secretion of intestinal fluids. Viberzi is unique in that it stimulates two types of receptor and inhibits another, providing relief without constipation.

These receptors each have different and unique functions:

  • Mu receptors:
    Responsible for gut motility (the contraction of gastrointestinal muscles)
  • Kappa receptors:
    Inhibit colon contractions
  • Delta receptors:
    Are associated intestinal secretions
The addition of a delta receptor antagonist is key to avoiding constipation seen with other drugs such as Imodium (loperamide) and Lomotil (atropine/diphenoxylate) which only affect the mu and kappa receptors.

The side effects of Viberzi are typically gastrointestinal in nature but may also affect other systems due to the opioid effects. As an opioid drug, Viberzi has the potential for abuse and/or dependence. It should only be used under the supervision of a doctor. While the effects are far less profound than Oxycontin (oxycodone), it can cause euphoria if abused and lead to opioid dependence.

Background: Effective and safe treatments are needed for patients who have irritable bowel syndrome (IBS) with diarrhea. We conducted two phase 3 trials to assess the efficacy and safety of eluxadoline, a new oral agent with mixed opioid effects in patients with IBS with diarrhea.

Methods: We randomly assigned 2427 adults who had IBS with diarrhea to eluxadoline or placebo twice daily for 26 weeks or 52 weeks. The primary end point was the proportion of patients who had a composite response of decrease in abdominal pain and improvement in stool consistency on the same day for at least 50% of the days from weeks 1 through 12 and from weeks 1 through 26.

Results: For weeks 1 through 12, more patients in the eluxadoline groups (75 mg and 100 mg) than in the placebo group reached the primary end point. The most common adverse events associated with 75 mg of eluxadoline and 100 mg of eluxadoline, as compared with placebo, were nausea, constipation , and abdominal pain. Pancreatitis developed in 5 (2 in the 75-mg group and 3 in the 100-mg group) of the 1666 patients in the safety population (0.3%).

Conclusions: Eluxadoline is a new therapeutic agent that reduced symptoms of IBS with diarrhea in men and women, with sustained efficacy over 6 months in patients who received the 100-mg dose twice daily.

Eluxadoline (Truberzi): risk of pancreatitis; do not use in patients who have undergone cholecystectomy or in those with biliary disorders

Cases of pancreatitis, with or without sphincter of Oddi spasm, have been reported in patients taking eluxadoline. Some cases have resulted in hospitalisation and death, primarily in patients who have undergone cholecystectomy.


Eluxadoline normalizes gastrointestinal (GI) transit and defecation under conditions of novel environment stress or post-inflammatory altered GI function. Allergan (previously Actavis) is developing eluxadoline for the treatment of diarrhea-predominant irritable bowel syndrome. The agent was originated by Janssen Pharmaceutica. Eluxadoline has been launched in the US under trade name VIBERZI (eluxadoline) tablets, while is at the preregistration stage in the EU.

Constipation, nausea and stomach pain are the most common side effects of Viberzi, according to the drug's maker, Allergan. Because the drug's main ingredient, eluxadoline, can cause feelings of euphoria, Viberzi has abuse potential and may lead to drug dependence. People who took the drug at normal dosages reported euphoria and feeling drunk. The medication can also cause serious adverse reactions, such as pancreatitis, that may require hospitalization. In clinical trials, 8 percent of patients developed constipation when taking 100 mg of the medication twice a day. Seven percent of patients taking 75 mg twice daily experienced constipation.

Viberzi (eluxadoline tablets)
Side Effects:
  • RxList
  • Common side effects of Viberzi include:
    • constipation
    • nausea
    • abdominal pain
    • upper respiratory tract infection
    • vomiting
    • runny or stuffy nose
    • bloating
    • bronchitis
    • dizziness
    • gas
    • rash
    • fatigue

    Liver:
    Eluxadoline is associated with a low rate of serum aminotransferase elevations that appear to be due to isolated instances of sphincter of Oddi spasm and/or pancreatitis that occurs most frequently in persons without a gallbladder.

    Eluxadoline Hepatotoxicity:
    In preregistration clinical trials, serum aminotransferase elevations were uncommon during eluxadoline therapy and in pooled analyses ALT elevations above 3 times the upper limit of normal occurred in 2% to 3% of eluxadoline- vs 1% of placebo-treated subjects. More detailed analysis found rare instances of marked ALT and AST elevations with eluxadoline therapy, not seen with placebo treatment. These more marked elevations were sometimes accompanied by abdominal pain and signs of sphincter of Oddi spasm (as can occur with opioid therapy) or pancreatitis. The abnormalities also arose largely in patients without a gallbladder or with a history of pancreatitis or hepato-biliary disease. Subsequent to the approval of eluxadoline and its more widescale use, over a hundred reports of pancreatitis (including 2 deaths) were reported to the Food and Drug Administration and eluxadoline was given a "black box" warning regarding its use in persons without a gallbladder. The clinical features of these reactions have not been well described, but they typically arise within the first few weeks of treatment with severe abdominal pain and vomiting sometimes accompanied by marked ALT and AST elevations with or without increases in amylase and lipase. Jaundice is rare and the liver test abnormalities are most likely due to partial bile duct obstruction. There have been no reports of severe acute hepatitis or acute liver failure attributed to eluxadoline therapy.

    C Likelihood score: C (probable cause of acute liver injury, likely due to bile duct spasm or obstruction).


    Viberzi (eluxadoline)
    Maximum Dosage:
    Prescribers Digital Reference
    Adults:200 mg/day PO.
    Geriatric:200 mg/day PO.
    Adolescents:Safety and efficacy have not been established.
    Children:Safety and efficacy have not been established.
    Infants:Safety and efficacy have not been established.

    Precautions while using Eluxadoline:

    You should not use eluxadoline if you have a pancreas disorder, severe liver disease, alcoholism, a blockage in your intestines, a gallbladder disorder, or if your gallbladder has been removed.

    Eluxadoline may cause pancreatitis or constipation, which could be severe or lead to hospitalization. Call your doctor at once if you have severe or ongoing constipation, severe pain in your upper stomach spreading to your back (with or without nausea and vomiting).

    Avoid drinking alcohol. It may increase your risk of pancreas problems.

    Avoid taking anti-diarrhea medicine such as loperamide (Imodium) without your doctor's advice. Taking loperamide long-term while you are taking eluxadoline may cause severe constipation.

    Interactions:

    Drug Interactions (202) Alcohol/Food Interactions (1) Disease Interactions (3)


    What other drugs will affect Eluxadoline?
    Tell your doctor about all your other medicines, especially:
    • alosetron or other medications to treat irritable bowel syndrome
    • opioid pain medicine
    • medicine to treat depression, anxiety, mood disorders, or mental illness
    • cold or allergy medicine (Benadryl and others)
    • medicine to treat Parkinson's disease
    • medicine to treat stomach problems, motion sickness, or irritable bowel syndrome
    • medicine to treat overactive bladder
    • bronchodilator asthma medication
    This list is not complete. Other drugs may affect eluxadoline, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

    A total of 202 drugs are known to interact with Eluxadoline.

    • 16 major drug interactions
    • 185 moderate drug interactions
    • 1 minor drug interaction

    Pediatric:
    Appropriate studies have not been performed on the relationship of age to the effects of eluxadoline in the pediatric population.

    Safety and efficacy have not been established.

    Geriatric:
    Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of eluxadoline in the elderly. However, elderly patients are more likely to have unwanted side effects and stomach problems, which may require caution in patients receiving eluxadoline.

    Other Interactions:

    • Ethanol

    Other Medical Problems:
    Make sure you tell your doctor if you have any other medical problems, especially:

    • Alcohol abuse or addiction
    • Bowel or stomach blockage, known or suspected
    • Constipation (severe), history of
    • Gallbladder blockage, known or suspected
    • Liver disease, severe
    • Pancreas problems (eg, blockage in the pancreas)
    • Pancreatitis (inflammation of the pancreas), history of
    • Patients who drink more than 3 alcoholic beverages a day
    • Patients without a gallbladder
    • Sphincter of Oddi disease, known or suspected - Should not be used in patients with these conditions
    • Liver disease, mild to moderate - Use with caution. The effects may be increased because of slower removal of the medicine from the body

    Breastfeeding:

    Summary of Use During Lactation:
    No information is available on the use of eluxadoline during breastfeeding.

    Because it has opioid agonist activity, an alternate drug is preferred, especially while nursing a newborn or preterm infant.

    Alternate Drugs to Consider:

    • (Irritable Bowel syndrome) Alosetron
    • Cholestyramine
    • Colesevelam
    • Colestipol
    • Loperamide
    • Ondansetron
    • Rifaximin

    EMC PDF Truberzi

    TGA PDF Eluxadoline

    Scottishmedicines PDF Truberzi

    What is the most important information I should know about eluxadoline?
    You should not use eluxadoline if you have:

    Eluxadoline:
    • A medication taken by mouth
    • Used for the treatment of diarrhea and abdominal pain in individuals with diarrhea-predominant irritable bowel syndrome (IBS-D)
    • Approved for use in the United States in 2015.
    • Common adverse effects are constipation and nausea
    • Rare adverse effects: fatigue, bronchitis, viral gastroenteritis
    • Rare serious adverse effects include pancreatitis

    In March 2017, the U.S. Food and Drug Administration issued a safety alert for eluxadoline concerning an increased risk of serious pancreatitis in patients without a gallbladder.
    (https://www.fda.gov/drugs/fda-drug-safety-podcasts/fda-drug-safety-podcast-fda-warns-about-increased-risk-serious-pancreatitis-irritable-bowel-drug)

      
    Eluxadoline/Anticholinergics; Opioids Interactions - Consult your healthcare professional before taking or discontinuing any drug or commencing any course of treatment. Serious. These medicines may interact and cause very harmful effects.
    Thursday January 19, 2023 - webmd.com

    Eluxadoline/OATP1B1 Inhibitors Interactions - Consult your healthcare professional before taking or discontinuing any drug or commencing any course ... or operate machinery until you know how eluxadoline affects you. Let your doctor know ...
    Thursday February 25, 2016 - webmd.com

    Viberzi Coupon and Discount: Save on the Cost of Viberzi (Eluxadoline Coupons) - Eluxadoline, the active ingredient in Viberzi, has also been linked to dependency in animal tests, which means that after taking the drug for a long period, your body will start to crave or depend ...
    Sunday January 08, 2023 - miamiherald.com

    Efficacy of Zoledronic Acid for Chronic Low Back Pain Associated With Modic Changes in Magnetic Resonance Imaging - placebo 20% (p = 0.096), respectively. At baseline, there were no differences in self-reported use of non-steroidal anti-inflammatory drugs (NSAIDs) between the treatment groups, whereas at one ...
    Saturday December 24, 2022 - medscape.com

      
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