anti irritable bowel syndrome agents
mu-opioid receptor agonists
Controlled Substance Schedule: IV
Treatment of diarrhea – predominant irritable bowel syndrome (IBS-d).
Acts as a agonist at mu-opioid receptors in the GI tract.
↓ frequency and severity of abdominal pain/diarrhea associated with IBS-d.
Absorption: Some systemic absorption follows oral administration (bioavailaibility unknown).
Metabolism and Excretion: Mostly metabolized by the liver; <1% excreted in urine.
Half-life: 3.7–6 hr
TIME/ACTION PROFILE (effect on GI tract)
- 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-moderate hepatic impairment (dose reduction recommended)
- Recreational opioid-experienced patients (may produce euphoria/psychological dependence)
- Geri: ↑ risk of adverse reactions;
- OB: Pregnancy (effects unknown)
- Lactation: Consider maternal need for eluxadoline and potential risks of adverse effects on infant;
- Pedi: Safety and effectiveness not established.
Adverse Reactions/Side Effects
CNS: dizziness, fatigue
GI: PANCREATITIS, constipation, abdominal distention, abdominal pain, flatulence, ↑ liver enzymes, nausea, sphincter of Oddi spasm, vomiting
Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- Concurrent use of OATP1B1 inhibitors including atazanavir, cyclosporine, eltrombopag, gemfibrozil, rifampin, ritonavir, saquinavir and tipranavir ↑ blood levels and risk of sedation; dose reduction 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 chronic concurrent use.
- May ↑ levels and risk of myopathy/rhabdomyolysis with rosuvastatin; use lowest effective dose of rosuvastatin.
- May ↑ levels and risk of toxicity with alfentanil, cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus; careful blood level/clinical monitoring recommended.
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
(Adults) Mild-moderate hepatic impairment–75 mg twice daily.
Tablets: 75 mg, 100 mg
- Assess bowel function (quality and quantity of stools) periodically during therapy. Discontinue eluxadoline if constipation last more than 4 days.
- PO Administer twice daily with food.
- 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) 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.
- Advise female patient to notify health care professional of pregnancy is planned or suspected or if breastfeeding.
Reduction of abdominal pain/diarrhea in patients with irritable bowel syndrome.
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