Eluxan
Eluxan Uses, Dosage, Side Effects, Food Interaction and all others data.
Eluxan is a mu-opioid receptor agonist, kappa opioid receptor agonist & delta opioid receptor antagonist. Eluxan works directly in intestine to reduce peristalsis, also makes the nerves in intestine less sensitive to stimulation.
Trade Name | Eluxan |
Availability | Prescription only |
Generic | Eluxadoline |
Eluxadoline Other Names | Eluxadoline |
Related Drugs | dicyclomine, Bentyl, hyoscyamine, Amitiza, Metamucil, Lotronex |
Weight | 100mg, 75mg |
Type | Tablet |
Formula | C32H35N5O5 |
Weight | Average: 569.662 Monoisotopic: 569.263819247 |
Protein binding | 81% |
Groups | Approved, Investigational |
Therapeutic Class | Carboxylic acids and derivatives, Prokinetic drugs |
Manufacturer | Ziska Pharmaceuticals Ltd, |
Available Country | Bangladesh |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Eluxan is used for adults for the treatment of irritable bowel syndrome with diarrhea (IBS-D).
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Hepatic Impairment: It is contraused for patients with severe hepatic impairment.
Eluxan is also used to associated treatment for these conditions: Diarrhoea Predominant Irritable Bowel Syndrome
How Eluxan works
Eluxan is a mu-opioid receptor agonis, kappa opioid receptor agonist and a delta opioid receptor antagonist. Eluxan is used for diarrhea predominant IBS because it reduces intestinal contractility and normalizes stress-induced acceleration of upper GI transit. Antagonistic activity at the delta receptor minimizes the constipating effect usually seen by mu-opioid receptor agonists alone. Because of it's limited systemic bioavailability, there may be less side effects associated with the use of eluxadoline in comparison with other therapies used to treat diarrhea predominant IBS.
Dosage
Eluxan dosage
The recommended dosage in adults is 100 mg twice daily taken with food.
The recommended dosage is 75 mg twice daily taken with food in patients who:
- are unable to tolerate the 100 mg dose.
- are receiving concomitant OATP1B1 inhibitors.
- have mild or moderate hepatic impairment.
If a dose is missed, take the next dose at the regular time; do not take 2 doses at once
Side Effects
Most common adverse reactions are constipation, nausea and
abdominal pain.
Toxicity
The most common adverse reactions (>5%) are constipation, nausea and abdominal pain.
Precaution
Sphincter of Oddi spasm and Pancreatitis.
Patients who should be monitored closely-
- without a gallbladder
- with new or worsening abdominal pain
- with nausea and vomiting
- with acute biliary pain
- with liver or pancreatic enzyme elevation
Interaction
Oral Contraceptive, Cyclosporine, Probenecid, Rosuvastatin.
Food Interaction
- Avoid excessive or chronic alcohol consumption. The risk of pancreatitis is increased with excess/chronic alcohol consumption.
- Take with food.
[Major] CONTRAINDICATED: Consumption of more than 3 alcoholic beverages per day may increase the risk of acute pancreatitis during treatment with eluxadoline.
Pancreatitis has been reported rarely during clinical trials of eluxadoline, and may or may not be related to sphincter of Oddi spasm.
ADJUST DOSING INTERVAL: High-fat meals may reduce the oral bioavailability of eluxadoline.
In 28 healthy volunteers, administration of a single 100 mg dose of eluxadoline with a high-fat meal (approximately 800 to 1000 total calories, 50% from fat) decreased eluxadoline peak plasma concentration (Cmax) and systemic exposure (AUC) by 50% and 60%, respectively, compared to administration in the fasted state.
There was no significant effect on the time to peak concentration (Tmax).
The clinical relevance of this interaction is unknown.
It should be noted that phase 3 clinical trials were conducted under fed conditions.
MANAGEMENT: Chronic or acute excessive use of alcohol should be avoided during treatment with eluxadoline.
Alcoholism, alcohol abuse, alcohol addiction, and consumption of more than 3 alcoholic beverages per day are considered contraindications to the use of eluxadoline.
The product labeling recommends taking eluxadoline with food.
Patients should be advised to stop taking eluxadoline and seek medical attention if they experience potential symptoms of pancreatitis such as persistent nausea, vomiting, abdominal tenderness, and upper abdominal pain, especially that which is made worse after eating or radiates to the back or shoulders.
Eluxan Drug Interaction
Moderate: loperamide, dicyclomine, loperamideUnknown: lactobacillus acidophilus, fluticasone / salmeterol, zolpidem, testosterone, aspirin, lorazepam, moxifloxacin, cyanocobalamin, exenatide, ubiquinone, omega-3 polyunsaturated fatty acids, pregabalin, metoprolol, bifidobacterium infantis / lactobacillus acidophilus, s-adenosylmethionine, multivitamin, lisdexamfetamine
Eluxan Disease Interaction
Elimination Route
The oral absorption of eluxadoline is poor - estimated to be 1.02%, this could be attributed to poor in vitro GI permeability, and its zwitterionic nature leading to a negatively charged molecule across the GI pH range.
Half Life
The mean plasma elimination half-life ranged from 3.7 hours to 6 hours.
Elimination Route
82% excreted in feces, <1% excreted in urine.
Pregnancy & Breastfeeding use
Pregnancy: Not established.
Lactation: Not established.
Contraindication
Known or suspected biliary duct obstruction, sphincter of oddi disease or dysfunction & pancreatitis.
Storage Condition
Store in a cool & dry place, protect from light. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Eluxan
Eluxan contains Eluxadoline see full prescribing information from innovator Eluxan Monograph, Eluxan MSDS, Eluxan FDA label