Eluxan100 mg

Eluxan is indicated for the treatment of irritable bowel syndrome with diarrhea (IBS-D) in adults. This is its only FDA-approved indication, supported by randomized controlled clinical trials.

• Established/approved use: Reduction of abdominal pain and improvement of stool consistency in adults with IBS-D.
• Not approved for: Other forms of IBS (such as IBS with constipation), general diarrhea, or infectious diarrhea.
• Off-label use: No commonly accepted off-label indications exist; use outside IBS-D is not recommended.

Eluxan should only be used in patients in whom the diagnosis of IBS-D has been confirmed and other causes of diarrhea have been excluded.

Each film-coated tablet contains Eluxadoline INN 75 mg or 100 mg as the active ingredient, along with pharmaceutically inert excipients.

Eluxan is an orally administered, locally acting mixed opioid receptor modulator developed specifically for irritable bowel syndrome with diarrhea (IBS-D). It combines mu-opioid receptor agonism with delta-opioid receptor antagonism to slow gastrointestinal transit and reduce visceral hypersensitivity while limiting the constipating and central opioid-type effects seen with pure mu-agonists.

Eluxan is available as film-coated oral tablets in 75 mg and 100 mg strengths and is intended for long-term, physician-supervised management of IBS-D symptoms rather than short-term or as-needed use.

Mixed opioid receptor agonist/antagonist (gastrointestinal motility modifier) - Eluxan acts as a mu-opioid receptor agonist and delta-opioid receptor antagonist, used specifically for IBS-D.

Eluxadoline acts locally within the gastrointestinal tract as a mixed mu-opioid receptor (OP3) agonist and delta-opioid receptor (OP1) antagonist, with minimal binding at kappa-opioid receptors.

• Mu-opioid receptor agonism reduces gastrointestinal motility and visceral pain sensitivity, decreasing diarrhea and abdominal pain associated with IBS-D.
• Delta-opioid receptor antagonism counteracts the constipating and tolerance-promoting effects that would otherwise result from unopposed mu-agonism, aiming for a more balanced effect on bowel function.

Pharmacokinetics: Eluxadoline has low and variable oral bioavailability, is a substrate of the OATP1B1 hepatic uptake transporter, undergoes minimal hepatic metabolism, and is eliminated predominantly unchanged in the feces via biliary excretion, with a small renal component. Food increases systemic exposure, which is why it must be taken with food.

Take Eluxan tablets by mouth exactly as prescribed, twice daily, always with food (not on an empty stomach). Swallow the tablet whole with water; do not crush, split, or chew it unless advised otherwise by a physician. Take at approximately the same times each day.

The following interactions with Eluxan are clinically significant and well documented:

• OATP1B1 inhibitors (e.g., cyclosporine, gemfibrozil): significantly increase Eluxan blood levels, raising the risk of adverse effects; the Eluxan dose should be reduced to 75 mg twice daily when co-administered.
• Constipating medicines (opioid analgesics, anticholinergics, and agents such as alosetron): concomitant use with Eluxan increases the risk of severe constipation and its complications; avoid combining unless directed by a physician.
• Alcohol: heavy alcohol use increases the risk of pancreatitis in patients taking Eluxan (see Contraindications) and should be avoided.
• OATP1B1 substrate statins (e.g., rosuvastatin): Eluxan can increase statin blood levels; use the lowest effective statin dose and monitor for statin-related adverse effects.
• CNS depressants: may add to sedative or CNS-depressant effects; use with caution.

The most common side effects of Eluxan (occurring in more than 5% of patients) are:

• Constipation (can occasionally be severe enough to require hospitalization - see Precautions and Warnings)
• Nausea
• Abdominal pain

Less common side effects include vomiting, flatulence, upper respiratory tract infection, fatigue, and mild increases in liver enzymes.

Serious but uncommon reactions include pancreatitis with or without sphincter of Oddi spasm, and hypersensitivity reactions including anaphylaxis (see Precautions and Warnings for details and contraindications).

Pregnancy: There are no adequate, well-controlled human studies of Eluxan in pregnant women. Animal reproduction studies have not shown evidence of harm to the fetus at clinically relevant exposures, but this does not guarantee safety in humans. Eluxan should be used during pregnancy only if clearly needed and if the potential benefit to the mother justifies the potential risk to the fetus; a physician should always be consulted before use in pregnancy.

Lactation: It is not known whether Eluxan passes into human breast milk. Because many drugs are excreted in breast milk and the effects on a nursing infant are unknown, a physician should be consulted to weigh the benefits of treatment against any potential risk before using Eluxan while breastfeeding.

Boxed warning: Eluxan is contraindicated in patients without a gallbladder because of a significantly increased risk of serious, potentially fatal pancreatitis from sphincter of Oddi spasm (see Contraindications).

• Pancreatitis and sphincter of Oddi spasm: Can occur even in patients with an intact gallbladder, though the risk is markedly higher without one. Watch for new or worsening severe abdominal pain, especially if it radiates to the back or shoulder, with or without nausea and vomiting or elevated liver/pancreatic enzymes. Discontinue Eluxan immediately and seek medical attention if this is suspected.
• Hypersensitivity reactions: Anaphylaxis and other hypersensitivity reactions have been reported, sometimes after only one or two doses. Discontinue immediately if signs occur (rash, swelling, difficulty breathing) and seek urgent care.
• Severe constipation: Discontinue Eluxan if severe constipation develops; avoid use with other constipating agents.
• Abuse and dependence potential: Because of its mu-opioid agonist activity, Eluxan has some potential for abuse and is subject to controlled-substance scheduling in some countries; use with caution in patients with a history of substance use disorder and store securely.
• Not recommended in patients who do not have a confirmed diagnosis of IBS-D, or in whom other structural or biliary/pancreatic disease has not been excluded.

There is limited clinical experience with Eluxan overdose. Suspected overdose may increase the risk of pancreatitis, sphincter of Oddi spasm, severe constipation, or opioid-type adverse effects.

If an overdose of Eluxan is suspected, seek immediate medical attention or contact a poison control center/emergency services right away. Treatment should be supportive and managed by qualified medical personnel; there is no specific antidote, and unsupervised home treatment is not advised.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

• Hepatic impairment: Use Eluxan at 75 mg twice daily in mild-to-moderate impairment (Child-Pugh A/B); contraindicated in severe impairment (Child-Pugh C).
• Renal impairment: Use Eluxan at 75 mg twice daily in moderate-to-severe renal impairment or end-stage renal disease not yet on dialysis.
• Elderly patients: Higher rates of adverse effects have been observed in patients 65 years and older taking Eluxan; use with routine clinical monitoring.
• Pediatric patients: Safety and efficacy of Eluxan have not been established in children; its use is not recommended in this population.
• Pregnancy and lactation: See Pregnancy and Lactation section above.

The duration of treatment with Eluxan should be determined by the prescribing physician based on symptom response. It is generally used for long-term maintenance of IBS-D symptom control. If no improvement in symptoms is seen after about 3-4 months, the physician should reassess whether continued treatment with Eluxan is appropriate.

Eluxadoline belongs to the class of mixed opioid receptor agonists/antagonists (mu-opioid receptor agonist and delta-opioid receptor antagonist) used as gastrointestinal motility modifiers for IBS-D.

Eluxadoline works locally in the gut wall by simultaneously activating mu-opioid receptors (slowing transit and reducing pain signaling) and blocking delta-opioid receptors (limiting the excessive constipation and tolerance associated with pure mu-opioid agonism), producing a net reduction in diarrhea and abdominal pain in IBS-D without the full opioid-type bowel-slowing seen with conventional opioids.

The safety and efficacy of Eluxan have not been established in pediatric patients. It is not approved and not recommended for use in children or adolescents; IBS-D in pediatric patients should be evaluated and managed by a pediatric specialist using age-appropriate therapies.