What is the mechanism of Eluxadoline?

Eluxadoline is a medication primarily used in the treatment of irritable bowel syndrome with diarrhea (IBS-D). Understanding the mechanism of Eluxadoline requires a closer look at its pharmacological properties and how it interacts with the body to exert its therapeutic effects.

Eluxadoline is a mixed opioid receptor agonist and antagonist. Specifically, it acts as an agonist at the mu (μ) and kappa (κ) opioid receptors and as an antagonist at the delta (δ) opioid receptor. This unique combination of actions at different opioid receptors underlies its effectiveness in managing IBS-D symptoms.

The mu and kappa opioid receptors are primarily involved in modulating pain and gastrointestinal motility. When Eluxadoline activates these receptors, it helps to reduce the bowel movements and abdominal pain associated with IBS-D. By slowing down gut motility, Eluxadoline can help alleviate diarrhea, which is a hallmark symptom of IBS-D.

On the other hand, the antagonistic action of Eluxadoline at the delta opioid receptors serves to mitigate potential adverse effects associated with opioid agonism, such as constipation and central nervous system side effects. Blocking the delta receptors helps balance the overall effect, making Eluxadoline more tolerable for long-term use.

The combination of these receptor interactions results in a reduction of abdominal pain and diarrhea without causing significant constipation, a common side effect of many other opioid-based treatments. This balance is particularly important in managing IBS-D, where both excessive bowel movements and abdominal discomfort need to be addressed.

One of the key advantages of Eluxadoline is its minimal absorption into the bloodstream, which limits its systemic side effects. Most of the drug’s action is localized within the gastrointestinal tract, allowing for effective symptom control without widespread opioid-related side effects.

In conclusion, Eluxadoline’s mechanism of action involves a dual role as an agonist at mu and kappa opioid receptors and an antagonist at delta opioid receptors. This combination helps to reduce the symptoms of IBS-D, such as diarrhea and abdominal pain, while minimizing adverse effects like constipation. Its localized action within the gastrointestinal tract ensures effective management of IBS-D symptoms with a favorable safety profile.