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864821-90-9 Usage

Adverse reactions

Common adverse reaction associated with Eluxadoline include constipation, nausea, abdominal pain, upper respiratory tract infection, pancreatitis, sphincter of Oddi spasm, hypersensitivity reactions, vomiting, nasopharyngitis, abdominal distention, bronchitis, dizziness, flatulence, rash, increased ALT, fatigue, viral gastroenteritis and stomach pain[4, 6, 11]. Less common adverse reactions also include gastroesophageal reflux disease, sedation, somnolence, and euphoric mood, respiration disorders such as asthma, bronchospasm, respiration failure and wheezing. Constipation was the most commonly reported adverse reaction in during the treatment by Eluxadoline. Approximately 50% of constipation events occurred within the first 2 weeks of treatment while the majority occurred within the first 3 months of therapy. Similar rates of constipation occurred between the active and placebo arms beyond 3 months of treatment. In severe cases, constipation can even lead to permanent discontinuation of drugs[11].

Indication and applications

Eluxadoline is indicated for the treatment of diarrhea-predominant irritable bowel syndrome(IBS-D). It can work directly in the intestines to slow the movement of food during digestion. Eluxadoline also makes the nerves in the intestines less sensitive to stimulation[1, 6].

References

  1. https://www.drugbank.ca/drugs/DB09272
  2. "Viberzi[eluxadoline] Tablets, for Oral Use, CIV. Full Prescribing Information". Actavis Pharma, Inc. Parsippany, NJ 07054 USA. Retrieved 26 December 2015.
  3. "Truberzi". European Medicines Agency. 29 September 2016.
  4. https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf
  5. Cash, B. D. "Eluxadoline: a promising therapy that raises many questions. " Translational Gastroenterology & Hepatology 1(2016]: 76.
  6. https://www.everydayhealth.com/drugs/eluxadoline
  7. Fujita, Wakako, et al. "Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers." Biochemical Pharmacology 92.3(2014]: 448-456.
  8. Levycooperman, N, et al. "Abuse Potential and Pharmacodynamic Characteristics of Oral and Intranasal Eluxadoline, a mixed μ- and κ-Opioid Receptor Agonist and δ-Opioid Receptor Antagonist. " Journal of Pharmacology & Experimental Therapeutics 359.3(2016]: 471-481.
  9. Chen, Hong Yu, J. J. Feng, and T. T. Song. "Eluxadoline, a new drug for treating diarrhea-predominant irritable bowel syndrome." Chinese Journal of New Drugs[2017].
  10. Davenport JM, Covington P, Bonifacio L, McIntyre G, Venitz J: Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline. J Clin Pharmacol. 2015 May; 55(5]: 534-42. doi: 10.1002/jcph.442. Epub 2015 Jan 14. 
  11. https://www.rxlist.com/viberzi-drug.htm
  12. https://www.drugs.com/viberzi.html
  13. Gawron, A. J., and K. Bielefeldt. "Risk of Pancreatitis Following Treatment of Irritable Bowel Syndrome with Eluxadoline." Clinical Gastroenterology & Hepatology the Official Clinical Practice Journal of the American Gastroenterological Association 16.3(2017].

Definition

ChEBI: 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-phenylimidazol-2-yl)ethyl]amino}methyl)ben oic acid. It has mixed opioid receptor activity and is used for treatment of irritable bowel syndrome with diarrhoea.

Overview and History

Eluxadoline is a mixed mu-opioid receptor agonist, kappa-opioid receptor agonist, and a-delta opioid receptor antagonist that can be used for the treatment of diarrhea-predominant irritable bowel syndrome(IBS-D)[1-4]. The mu-, kappa-, and delta-opioid receptors participating in regulating endogenous and exogenous opioid response in the central nervous system and peripherally in the gastrointestinal system. The 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[1, 4].
Eluxadoline is marketed under the tradename Viberzi(FDA) in US(at may 2015)[1, 2, 4, 5]. It is an antimotility agent that decreases bowel contractions, inhibits colonic transit, and reduces ?uid/ion secretion resulting in improved symptoms of abdominal pain and reductions in the Bristol Stool Scale. It is also marketed in Europe under the trade name of “Truberzi”[3].

Mode of action

Eluxadoline takes effect through acting as the antagonist of mu-opioid receptor agonis, kappa opioid receptor agonist and a delta opioid receptor[7,8]. Eluxadoline can be used for diarrhea predominant IBS because it reduces intestinal contractility and normalizes stress-induced acceleration of upper GI transit[9]. Antagonistic activity at the delta receptor minimizes the constipating effect usually seen by mu-opioid receptor agonists alone. Because of it's limited systemic bioavailability, there may be less side effects associated with the use of eluxadoline in comparison with other therapies used to treat diarrhea predominant IBS[10].

Warning and Precaution

Eluxadoline is not approved for use by anyone younger than 18 years old[6].
Eluxadoline is contradicted for administration in patients who suffer from a pancreas disorder, severe liver disease, alcoholism, and a blockage in the intestines, a gallbladder disorder, or those whose gallbladder has been removed[12].
People who are allergic to eluxadoline should also be disabled for using. In addition, it is also not allowed for patients who have a history of gallbladder, obstruction digestive problems caused by a muscle valve called the sphincter of Oddi(SFINK-ter of OD-dee), pancreas disorder, severe liver disease, a habit of drinking more than 3 alcoholic beverages per day[12, 13].
To make sure eluxadoline is safe for you; tell your doctor if you have liver disease.
It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant. It is not known whether eluxadoline passes into breast milk or if it could harm a nursing baby. Tell your doctor if you are breast-feeding a baby[12].

864821-90-9SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 14, 2017

Revision Date: Aug 14, 2017

1.Identification

1.1 GHS Product identifier

Product name eluxadoline

1.2 Other means of identification

Product number -
Other names UNII-45TPJ4MBQ1

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:864821-90-9 SDS

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