Eluxadoline is a relatively newer player in the pharmaceutical landscape, primarily used in the management of
irritable bowel syndrome with diarrhea (IBS-D). Marketed under the trade name Viberzi, Eluxadoline was developed by
Furiex Pharmaceuticals, a subsidiary of
Allergan. The drug was approved by the U.S. Food and Drug Administration (FDA) in 2015, reflecting a significant advancement in addressing gastrointestinal disorders. Eluxadoline belongs to a class of medication known as
mixed opioid receptor agonists/antagonists, which target specific receptors in the nervous system to alleviate symptoms associated with
IBS-D. This condition, characterized by
chronic abdominal pain and
frequent diarrhea, affects a significant portion of the population, and the introduction of Eluxadoline provides a much-needed therapeutic option for those who have not found relief from other treatments.
The mechanism of action of Eluxadoline is both sophisticated and targeted. The drug primarily operates through its interaction with
opioid receptors in the gut. Specifically, Eluxadoline acts as an agonist at the mu-opioid receptor and as an antagonist at the
delta-opioid receptor, while also exhibiting agonistic properties at the
kappa-opioid receptor. This multi-receptor interaction results in a dual effect: it reduces bowel contractions and motility, thereby alleviating diarrhea, and modulates
pain perception, providing relief from abdominal pain. The selective targeting of these receptors in the gastrointestinal tract, rather than the central nervous system, minimizes the risk of potential side effects commonly associated with systemic opioid use, such as
sedation and dependency.
Administering Eluxadoline is straightforward but must be approached with careful adherence to prescribed guidelines to ensure efficacy and minimize potential risks. The drug is available in tablet form and is typically taken orally twice a day, with food. This method of administration allows for consistent absorption and effectiveness. The onset of action can vary among individuals but generally occurs within a few hours after ingestion, providing relatively prompt relief from IBS-D symptoms. It's crucial for patients to follow their healthcare provider’s instructions regarding dosage and frequency, as improper use can lead to suboptimal results or increased risk of adverse effects. The standard dosage is often 100 mg twice daily; however, in cases of mild to moderate
hepatic impairment, lower dosages might be recommended to prevent accumulation of the drug in the system.
As with any medication, Eluxadoline is not without its potential side effects and contraindications, which should be thoroughly understood by both patients and healthcare providers. Common side effects of Eluxadoline include
nausea,
constipation, and abdominal pain, which can occur as the body adjusts to the medication. Less commonly, patients might experience
dizziness,
fatigue, and increased levels of liver enzymes, indicating a need for periodic monitoring of liver function during treatment. Serious but rare side effects can include
pancreatitis, which is particularly a risk in patients without a gallbladder, and
sphincter of Oddi spasm, a condition that can cause severe abdominal pain and increased liver enzymes. Consequently, Eluxadoline is contraindicated in patients with a history
of bile duct obstruction, pancreatitis, severe liver impairment, or those who consume more than three alcoholic beverages per day, as these conditions can exacerbate the risk of severe adverse reactions.
Drug interactions are another critical consideration when prescribing and taking Eluxadoline. Because the drug is metabolized primarily through hepatic pathways, concurrent use of other medications that impact liver enzymes can alter its effectiveness and safety profile. For example, strong inhibitors of the enzyme
OATP1B1, such as
cyclosporine and
gemfibrozil, can increase Eluxadoline levels in the blood, heightening the risk of adverse effects. Conversely, strong inducers of
CYP3A4, like
rifampin, can reduce the efficacy of Eluxadoline by accelerating its metabolism. Furthermore, concurrent use of other central nervous system depressants, including benzodiazepines and alcohol, can compound sedative effects and increase the risk of severe side effects. Therefore, it is imperative for patients to inform their healthcare providers of all medications and supplements they are taking to adequately assess potential drug interactions and adjust treatment plans accordingly.
In summary, Eluxadoline, marketed as Viberzi, represents an important therapeutic advancement for managing IBS-D, offering relief through its targeted action on opioid receptors in the gastrointestinal system. Its administration is straightforward but requires careful adherence to prescribed dosages and consideration of potential side effects and contraindications. Understanding and managing drug interactions is also critical to ensure the safety and effectiveness of Eluxadoline therapy. As always, ongoing communication between patients and healthcare providers is essential to optimize treatment outcomes and mitigate risks.
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