induced [1%:<1% excreted in urine. 1 Half-life 3.7 6 hours. 1 7 Stability Storage Oral Tablets 20 25 C (may be exposed to 15 30 C). 1 Actions Mixed μ-opiate receptor agonist and δ-opiate receptor antagonist. 1 2 3 4 5 6 Also exhibits agonist activity at κ-opiate receptor, but binding affinity for this receptor in humans not determined. 1 Has poor oral bioavailability and is used for its local effects at opiate receptors in the GI tract. 2 3 4 6 8 In animals, interacts with opiate receptors in the gut, 1 5 reduces contractility in intestinal tissue, and inhibits neurogenically mediated secretion in vitro; 4 5 normalizes GI transit and reduces fecal output in animal models of altered GI function. 3 4 5 6 9 Advice to Patients Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph. Advise patients to read the manufacturer's medication guide before beginning treatment and each time the prescription is refilled. 1 Advise patients without a gallbladder that they are at increased risk for sphincter of Oddi spasm. 1 Advise all patients, but especially those without a gallbladder, to discontinue the drug and seek medical attention if symptoms of sphincter of Oddi spasm or pancreatitis (e.g., unusual or severe abdominal, epigastric, or biliary pain that may radiate to the back or shoulder, with or without nausea and vomiting) develop. 1 Advise patients to inform their clinician if they cannot tolerate eluxadoline. 1 Advise patients to inform their clinician if constipation occurs and lasts >4 days. 1 Advise patients receiving eluxadoline not to use alosetron concomitantly and not to use loperamide on a chronic basis due to the potential for constipation; however, loperamide may be used occasionally for acute management of severe diarrhea. 1 Advise patients to discontinue loperamide if constipation develops. 1 Advise patients to avoid concomitant use of other drugs that may cause constipation (e.g., opiates, anticholinergics). 1 Advise patients to avoid chronic or acute excessive alcohol consumption while taking eluxadoline. 1 Advise patients that if a dose of eluxadoline is missed, to resume therapy with the next scheduled dose and to not double the dose to make up for the missed dose. 1 Advise patients with hepatic impairment not to drive, operate machinery, or perform other potentially hazardous activities until they know how eluxadoline affects them. 1 Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. 1 Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses. 1 Importance of informing patients of other important precautionary information. 1 (See Cautions.) Preparations Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details. Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations. Subject to control under the Federal Controlled Substances Act of 1970 as a schedule IV (C-IV) drug. 1 Eluxadoline Routes Dosage Forms Strengths Brand Names Manufacturer Oral Tablets, film-coated 75 mg Viberzi ( C-IV) Actavis 100 mg Viberzi ( C-IV) Actavis AHFS DI Essentials. Copyright 2017, Selected Revisions March 23, 2016. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814. References 1. Actavis Pharma, Inc. Viberzi (eluxadoline) tablets prescribing information. Parsippany, NJ; 2015 May. 2. Davenport JM, Covington P, Bonifacio L et al. Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline. J Clin Pharmacol . 2015; 55:534-42. [PubMed 25491493] 3. Fujita W, Gomes I, Dove LS et al. Molecular characterization of eluxadoline as a potential ligand targeting mu-delta opioid receptor heteromers. Biochem Pharmacol . 2014; 92:448-56. [PubMed 25261794] 4. Dove LS, Lembo A, Randall CW et al. Eluxadoline benefits patients with irritable bowel syndrome with diarrhea in a phase 2 study. Gastroenterology . 2013; 145:329-38.e1. [PubMed 23583433] 5. Garnock-Jones KP. Eluxadoline: First Global Approval. Drugs . 2015; 75:1305-10. [PubMed 26149369] 6. Hornby PJ. Drug discovery approaches to irritable bowel syndrome. Expert Opin Drug Discov . 2015; 10:809-24. [PubMed 26193876] 7. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 206940Orig1s000: Clinical pharmacology and biopharmaceutics review(s). From FDA website. 8. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 206940Orig1s000: Medical review(s). From FDA website. 9. US Food and Drug Administration. Center for Drug Evaluation and Research. Application number 206940Orig1s000: Pharmacology review(s). From FDA website. Next Interactions Print this page Add to My Med List More about eluxadoline Side Effects During Pregnancy Dosage Information Drug Interactions Support Group En Español 136 Reviews Add your own review/rating Drug class: peripheral opioid receptor mixed agonists/antagonists Consumer resources Eluxadoline Eluxadoline (Advanced Reading) Professional resources Eluxadoline (Wolters Kluwer) Other brands: Viberzi Related treatment guides Irritable Bowel Syndrome> ] FEATURED: CAR-T Cell Therapy Overview Mechanism of Action KTE-C19 Studies KTE-C19 Cancer Targets Adverse Events Manufacturing Drug Status Rx Availability Prescription only 4 CSA Schedule Some potential for abuse Approval History Drug history at FDA Drug Class Peripheral opioid receptor mixed agonists / antagonists Related Drugs Irritable Bowel Syndrome dicyclomine , Amitiza , Bentyl , Metamucil , psyllium , hyoscyamine , Levsin , Librax , lubiprostone , Donnatal , chlordiazepoxide / clidinium , Levbid , Konsyl , Anaspaz , alosetron , HyoMax , Lotronex , Levsin SL , Hyosyne , Antispasmodic , Reguloid , More... 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