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What Is Eluxadoline ? Uses, Dosage, Side Effects, Interactions

What Is Eluxadoline ?/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.

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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

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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.

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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.