eluxadoline

Adult Dosing

Diarrhea-predominant irritable bowel syndrome (IBS-D)

100mg PO BID with food
75 mg PO BID with food in patients who:are without a gallbladder are unable to tolerate the dose of 100 mg are receiving OATP1B1 inhibitors simultaneously have hepatic impairment, mild (Child-Pugh Class A) or moderate (Child-Pugh Class B)

<Note>

Treatment should be discontinued in patients who develop severe constipation lasting >4 days
If the dose is missed, 2 doses should not be taken to adjust for the missed dose; the next dose should be taken at the usual time

Pediatric Dosing

[Outline]

Indications ⬆ ⬇

Contraindications ⬆ ⬇

Hypersensitivity to any of the ingredients of the product
Biliary duct obstruction, known or suspected; sphincter of Oddi disease or dysfunction
Alcoholism, alcohol abuse or addiction, or in patients who drink >3 alcoholic beverages per day
Hx of pancreatitis or structural diseases of the pancreas, including pancreatic duct obstruction, known or suspected
Severe hepatic impairment (Child-Pugh Class C)
Hx of chronic or severe constipation or sequelae from constipation; mechanical GI obstruction, known or suspected

Black Box Warnings ⬆ ⬇

Dosing Adjustment ⬆ ⬇

Renal Dose Adjustment

Hepatic Dose Adjustment

Warnings/Precautions ⬆ ⬇

Because eluxadoline is a mu opioid receptor agonist, the risk of sphincter of Oddi spasm may increase leading to pancreatitis or hepatic enzyme elevation associated with biliary-type acute abdominal pain
The patients without a gallbladder are at increased risk. Hence, alternative therapies should be considered in these patients before initiating the treatment with eluxadoline based on the risks and benefits of the therapy
Advise patients to stop eluxadoline if they experience symptoms suggestive of sphincter of Oddi spasm such as acute worsening of abdominal pain, that may radiate to the back or shoulder with or without nausea and vomiting, associated with elevations of pancreatic enzymes or liver transaminases
Do not restart eluxadoline in patients who developed biliary duct obstruction or sphincter of Oddi spasm while taking eluxadoline
Increased risk of pancreatitis not associated with sphincter of Oddi spasm has been reported; most of the cases were associated with excessive alcohol use. Chronic or acute excessive alcohol use should be avoided during the treatment with eluxadoline

Pregnancy/Breast Feeding ⬆ ⬇

Pregnancy Category:NR (Not rated)

Breastfeeding: Safety unknown.

Human data regarding the presence of eluxadoline in human milk, its effects on the breastfed infants or on milk production are not available. However, the presence of eluxadolin in rat milk has been reported

Adverse Reactions ⬆ ⬇

GI: Constipation, nausea, vomiting, abdominal pain, abdominal distension, flatulence, viral gastroenteritis, constipation
RESP: Upper respiratory tract infection, nasopharyngitis, bronchitis
CNS: Dizziness
DERM: Rash, dermatitis
MISC: Fatigue
LABTEST: Increased ALT

Clinical Pharmacology ⬆ ⬇

Mixed opioid receptor activity (mu and kappa opioid receptor agonist and delta opioid receptor antagonist): The multiple opioid activity is designed to treat the symptoms of IBS-D while reducing the incidence of constipation that can occur with unopposed mu opioid receptor agonists, however, the exact mechanism of action is not clear.
Metabolism: Glucuronidation can occur to form an acyl glucuronide metabolite.
Excretion: Excreted in feces (82.2%) and urine (<1%)
Half Life: 3.7 to 6 hours

Brands and Availability ⬆ ⬇