Eluxadoline Tablet /Eluxadoline is a mixed opioid receptor agonist (mu) and antagonist (delta) that is used to treat diarrhea-predominant irritable bowel disease. Eluxadoline is associated with a low rate of serum aminotransferase elevations that appear to be due to isolated instances of the sphincter of Oddi spasm and/or pancreatitis that occurs most frequently in persons without a gallbladder.
Eluxadoline is an amino acid amide obtained by the formal condensation of the carboxy group of 4-carbamoyl-2,6-dimethyl-L-phenylalanine with the secondary amino group of 2-methoxy-5-({[(1S)-1-(4-phenyl imidazole-2-yl)ethyl]amino}methyl)benzoic acid. It has mixed opioid receptor activity and is used for the treatment of irritable bowel syndrome with diarrhea. It has a role as a mu-opioid receptor agonist, a delta-opioid receptor antagonist, a kappa-opioid receptor agonist, and a gastrointestinal drug. It is a member of imidazoles, a methoxy benzoic acid, a member of benzamides, and L-phenylalanine derivative and an amino acid amide.
Eluxadoline is a mixed mu-opioid receptor agonist, kappa-opioid receptor agonist, and a-delta opioid receptor antagonist indicated for use in diarrhea-predominant irritable bowel syndrome (IBS-D). The mu-, kappa-, and delta-opioid receptors mediate endogenous and exogenous opioid response in the central nervous system and peripherally in the gastrointestinal system. Agonism of peripheral mu-opioid receptors results in reduced colonic motility, while antagonism of central delta-opioid receptors results in improved analgesia, making eluxadoline usable for the symptoms of both pain and diarrhea characteristic of IBS-D. Marketed under the tradename Viberzi (FDA), eluxadoline is an antimotility agent that decreases bowel contractions, inhibits colonic transit, and reduces fluid/ion secretion resulting in improved symptoms of abdominal pain and reductions in the Bristol Stool Scale.
Mechanism of Action of Eluxadoline
Eluxadoline is a mu-opioid receptor agonist, kappa-opioid receptor agonist, and a delta-opioid receptor antagonist. Eluxadoline is used for diarrhea-predominant IBS because it reduces intestinal contractility and normalizes stress-induced acceleration of upper GI transit. Antagonistic activity at the delta receptor minimizes the constipating effect usually seen by mu-opioid receptor agonists alone. Because of its limited systemic bioavailability, there may be fewer side effects associated with the use of eluxadoline in comparison with other therapies used to treat diarrhea-predominant IBS.
Indications of Eluxadoline
- For the treatment of irritable bowel syndrome with diarrhea (IBS-D).
- Truberzi is indicated in adults for the treatment of irritable bowel syndrome with diarrhea (IBS D).
- Eluxadoline is a mixed opioid receptor agonist (mu) and antagonist (delta) that is used to treat diarrhea-predominant irritable bowel disease.
- Drugs used for their effects on the gastrointestinal system, as to control gastric acidity, regulate gastrointestinal motility and water flow, and improve digestion.
- Diarrhoea Predominant Irritable Bowel Syndrome
Contraindications of Eluxadoline
This drug is contraindicated in case of having
- Blockage of the gallbladder or a sphincter of Oddi problem
- Problems with alcohol abuse
- Pancreatitis
- Liver problems
- Chronic or severe constipation
- are allergic to eluxadoline or any ingredients of the medication
- have or may have a biliary duct blockage
- do not have a gallbladder
- consume more than 3 alcoholic drinks daily
- are alcoholic, have an alcohol addiction, or abuse alcohol
- have a history of inflammation of the pancreas (pancreatitis)
- have decreased liver function
- have a history of chronic or severe constipation
- have or have had an obstruction of the digestive tract
Dosage of Eluxadoline
Strengths: 75 mg; 100 mg
Irritable Bowel Syndrome
- Usual dose: 100 mg orally twice a day
- Dose should be reduced to 75 mg orally twice a day for patients unable to tolerate usual dose.
- If severe constipation develops, this drug should be discontinued.
Side Effects of Eluxadoline
Most Common
- Bloating
- symptoms of pancreatitis (e.g., abdominal pain, nausea, vomiting)
- new or worsening belly pain, nausea, vomiting, or sudden pain in the upper right abdomen)
- constipation
- darkened urine
- fast heartbeat
- fever
- indigestion
- loss of appetite
- nausea
- pains in the stomach, side, or abdomen, possibly radiating to the back
- vomiting
- yellow eyes or skin
Rare
- Cough
- difficulty swallowing
- Body aches or pain
- cough producing mucus
- difficulty with breathing
- ear congestion
- excess air or gas in the stomach or bowels
- dizziness
- hives, itching, skin rash
- large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or genitals
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
- tightness in the chest
- unusual tiredness or weakness
Interactions of Eluxadoline
Elevated concentrations of eluxadoline were observed with co-administration of inhibitors of the transporter protein OATP1B1, such as
- alcohol
- Alosetron
- Anticholinergics
- Bismuth subsalicylate, potentially dangerous synergism.
- antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- atropine
- azelastine
- belladonna
- benztropine
- cyclobenzaprine
- cyclosporine
- Certain antiretrovirals
- Rifampin
- darifenacin
- disopyramide
- eltrombopag
- fesoterodine
- flavoxate
- gemfibrozil
- glycopyrrolate
- hepatitis C antivirals (e.g., dasabuvir, ombitasvir, paritaprevir, ritonavir)
- HIV protease inhibitors (e.g., atazanavir, lopinavir, ritonavir, saquinavir)
- ipratropium
- ketotifen
- loperamide
- monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
- narcotic pain relievers (e.g., codeine, fentanyl, morphine, oxycodone)
- orphenadrine
- oxybutynin
- prochlorperazine
- quinidine
- quinine
- rifampin
- rosuvastatin
- scopolamine
- solifenacin
- teriflunomide
- tiotropium
- tolterodine
- tranylcypromine
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine
- Opioids
- gemfibrozil
- HIV protease inhibitors (e.g., atazanavir, lopinavir, ritonavir, saquinavir)
- rifampin
- Eluxadoline increases the concentrations of drugs which are OATP1B1 and BCRP substrates. Also, co-administration of eluxadoline with rosuvastatin may increase the risk of rhabdomyolysis.
Pregnancy Category of Eluxadoline
US FDA Pregnancy Category – N (Not Assigned)
Pregnancy
This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.
Breast-feeding
It is not known if eluxadoline passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using this medication have not been established for children.
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