eluxadoline

Contraindicated in:

Hypersensitivity;
Without a gallbladder (↑ risk of pancreatitis and/or sphincter of Oddi spasm);
Known/suspected biliary tract obstruction or sphincter of Oddi disease/dysfunction (↑ risk of sphincter of Oddi spasm);
Alcohol abuse/addiction or consumption of > 3 alcoholic beverages/day (↑ risk of pancreatitis);
History of pancreatitis/pancreatic disease/pancreatic duct obstruction (↑ risk of pancreatitis);
Severe hepatic impairment (Child-Pugh C);
Severe constipation/sequelae of constipation/known of suspected mechanical GI obstruction.

Use Cautiously in:

Mild or moderate hepatic impairment (↓ dosage);
Moderate or severe renal impairment or end-stage renal disease not on dialysis (↓ dosage) (eGFR <60 mL/min/1.73 m²);
Recreational opioid-experienced patients (may produce euphoria/psychological dependence);
OB: Safety not established in pregnancy;
Lactation: Use while breastfeeding only if potential maternal benefit outweighs potential risk in infant;
Pedi: Safety and effectiveness not established in children;
Geri: ↑risk of adverse reactions in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

GI: constipation, ↑liver enzymes, abdominal distention, abdominal pain, fecal impaction, flatulence, GI OBSTRUCTION/PERFORATION, nausea, PANCREATITIS, sphincter of Oddi spasm, vomiting

Neuro: dizziness, fatigue

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of OATP1B1 inhibitors, including atazanavir, cyclosporine, eltrombopag, gemfibrozil, rifampin, ritonavir, and tipranavir↑ blood levels and risk of sedation; dose ↓ recommended;
Concurrent use of strong CYP inhibitors, including bupropion, ciprofloxacin, clarithromycin, fluconazole, gemfibrozil, and paroxetine may ↑ risk of sedation; careful monitoring recommended.
Concurrent use of constipating drugs such asalosetron, anticholinergics (including loperamide), and opioids↑ risk of constipation and its sequelae; avoid concurrent use.
May ↑ levels and risk of myopathy/rhabdomyolysis with rosuvastatin; use lowest effective dose of rosuvastatin.
May ↑ levels and risk of toxicity with cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus; careful blood level/clinical monitoring recommended.

Availability ⬆ ⬇

(Generic available)

Tablets: 75 mg; 100 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 100 mg twice daily; Patients who lack a gallbladder, are unable to tolerate 100 mg twice daily or are taking concurrent OATP1B1 inhibitors: 75 mg twice daily.

Hepatic Impairment

PO (Adults ): Mild or moderate hepatic impairment (Child–Pugh Class A or B): 75 mg twice daily.

Renal Impairment

PO (Adults ): eGFR <60 mL/min/1.73 m² and not on dialysis: 75 mg twice daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Acts as a agonist at mu-opioid receptors in the GI tract.

Therapeutic effects:

↓frequency and severity of abdominal pain/diarrhea associated with IBS-d.

Classifications ⬆ ⬇

Therapeutic Classification: anti irritable bowel syndrome agents, mu-opioid receptor agonists

Pharmacokinetics ⬆ ⬇

Absorption: Some systemic absorption follows oral administration (bioavailaibility unknown).

Distribution: Unknown.

Metabolism/Excretion: Mostly metabolized by the liver; <1% excreted in urine.

Half-Life: 3.7–6 hr

Contr. Subst. Schedule ⬆ ⬇

Time/Action Profile ⬆ ⬇

(effect on GI tract)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	12 hr

Patient/Family Teaching ⬆ ⬇

Instruct patient to take eluxadoline as directed. If a dose is missed, omit and take next dose as scheduled; do not double doses.
Advise patient that eluxadoline is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed.
Advise patient to stop eluxadoline and notify health care professional if abdominal pain (acute epigastric or biliary [right upper quadrant] pain, may radiate to back or shoulder with or without nausea and vomiting), signs and symptoms of hypersensitivity reaction (swelling of face, lips, mouth or tongue; shortness of breath; wheezing; itching; rash; hives), or severe constipation occur.
Caution patient to avoid more that 3 alcoholic drinks/day.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially other medications causing constipation.
Rep: Advise female patient to notify health care professional of pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇

Contraind./Precautions ⬆ ⬇