Eluxadoline

Generic name: eluxadoline
Brand name: Viberzi
Dosage form: oral tablet (100 mg; 75 mg)
Drug class: Peripheral opioid receptor mixed agonists / antagonists

Medically reviewed by  A Ras MD.

What is eluxadoline?

Eluxadoline is a prescription medicine that is used to treat irritable bowel syndrome.

Description

The active ingredient in VIBERZI is eluxadoline, a mu-opioid receptor agonist.

The full chemical name is 5-[[[(2S)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]amino]methyl]-2-methoxybenzoic acid.

Eluxadoline has a molecular weight of 569.65 and a molecular formula of C32H35N5O5. The chemical structure of eluxadoline is:

VIBERZI is available as 75 mg and 100 mg tablets for oral administration. In addition to the active ingredient, eluxadoline, each tablet contains the following inactive ingredients: silicified microcrystalline cellulose, colloidal silica, crospovidone, mannitol, magnesium stearate, and Opadry II (partially hydrolyzed polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, iron oxide yellow, and iron oxide red).

Mechanism of Action

Eluxadoline is a mu-opioid receptor agonist; eluxadoline is also a delta opioid receptor antagonist and a kappa opioid receptor agonist. The binding affinities (Ki) of eluxadoline for the human mu and delta opioid receptors are 1.8 nM and 430 nM, respectively. The binding affinity (Ki) of eluxadoline for the human kappa opioid receptor has not been determined; however, the Ki for guinea pig cerebellum kappa opioid receptor is 55 nM. In animals, eluxadoline interacts with opioid receptors in the gut.

Before taking eluxadoline, tell your doctor:

• If you are allergic to eluxadoline; any part of this medicine; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had.
• If you have any of these health problems: A problem with the part of your body that controls the flow of bile and pancreas juice to the small bowels (sphincter of Oddi), bile tract blockage, liver problems, or stomach or bowel blockage.
• If you do not have a gallbladder. The chance of very bad pancreatitis is higher in people who do not have a gallbladder. This could lead to having to go to the hospital or death.
• If you have or had problems with alcohol abuse, alcohol addiction, or drink more than 3 alcoholic drinks per day.
• If you have ever had any of these health problems: Pancreas problems like blockage in your pancreas or pancreatitis, problems caused by constipation, or very bad or long-lasting constipation.
• If you are taking any of these drugs: Alosetron; loperamide; opioid drugs like oxycodone; or oxybutynin or other drugs like it.
• If you are taking any drugs that may cause constipation. There are many drugs that can do this. Ask your doctor or pharmacist if you are not sure.

This is not a list of all drugs or health problems that interact with eluxadoline.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take eluxadoline with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some things I need to know or do while I take eluxadoline?

• Tell all of your health care providers that you take eluxadoline. This includes your doctors, nurses, pharmacists, and dentists.
• Talk with your doctor before you drink alcohol.
• If you have liver problems, avoid driving and doing other tasks or actions that call for you to be alert until you see how eluxadoline affects you.
• Severe and sometimes deadly pancreas problem (pancreatitis) has happened with eluxadoline. If you have questions, talk with the doctor.
• A problem with the part of your body that controls the flow of bile and pancreas juice to the small bowels (sphincter of Oddi) has happened with eluxadoline. Sometimes, people have had to go to the hospital.
• If you are 65 or older, use eluxadoline with care. You could have more side effects.
• Tell your doctor if you are pregnant, plan on getting pregnant, or are breast-feeding. You will need to talk about the benefits and risks to you and the baby.

How is eluxadoline best taken?

Use eluxadoline as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• Take eluxadoline with food.

What do I do if I miss a dose?

• Skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

What are the side effects of eluxadoline that I need to call my doctor about immediately?

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:

• 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.
• Signs of a pancreas problem (pancreatitis) like very bad stomach pain, very bad back pain, or very bad upset stomach or throwing up.
• Stomach pain that is new or worse.
• Stomach pain that may move to your back or shoulder, with or without upset stomach or throwing up.
• Constipation has happened with eluxadoline. Some people have had to go to the hospital. Sometimes, very bad constipation has led to other very bad health problems like bowel blockage and holes in the bowel. If you have very bad constipation, call your doctor right away.

What are some other side effects of eluxadoline?

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:

• Constipation.
• Upset stomach.
• Signs of a common cold.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-332-1088. You may also report side effects at https://www.fda.gov/medwatch.

If overdose is suspected:

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

How do I store and/or throw out eluxadoline?

• Store at room temperature in a dry place. Do not store in a bathroom.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Throw away unused or expired drugs. Do not flush down a toilet or pour down a drain unless you are told to do so. Check with your pharmacist if you have questions about the best way to throw out drugs. There may be drug take-back programs in your area.