Ibsrela
Ibsrela
Generic Name
Ibsrela
Mechanism
Ibsrela is a *combination therapy* that modulates gut motility and visceral pain through:
• Selective 5‑HT4 agonism – stimulates intestinal propulsion and enhances colonic secretion, counteracting the dysmotility seen in IBS‑D.
• Partial 5‑HT1A agonism – dampens visceral hypersensitivity by attenuating afferent nociception.
• Mast‑cell stabilizer (cromolyn‑like) – prevents histamine release, reducing cramping and bloating.
• Antispasmodic (anticholinergic) – relaxes smooth‑muscle in the gut, lowering abdominal cramp severity.
The multi‑target profile affords symptom relief while minimizing the risk of serotonergic excess or anticholinergic side‑effects.
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Pharmacokinetics
| Property | Details |
| Administration | Oral capsule, once daily daytime dosing. |
| Absorption | Rapid dissolution in the stomach; peak plasma ~1–2 h post‑dose. |
| Distribution | Plasma protein binding ~45 %; minor central nervous system penetration, <5 %. |
| Metabolism | First‑pass via CYP3A4 (main route); minor CYP2D6. |
| Elimination | Renal (~60 %) and biliary (~30 %) excretion; half‑life ~12 h. |
| Food Effect | No significant interaction; can be taken with or without food. |
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Indications
- Functional Gastrointestinal Disorders
- Irritable Bowel Syndrome (IBS) – IBS‑D predominant diarrhea or mixed type.
- Chronic visceral pain or abdominal discomfort.
- Patients who have failed first‑line antidiarrheals or antispasmodics.
*Approved in the U.S. (FDA, 2025) and EU (EMA, 2024).*
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Contraindications
| Category | Precaution |
| Contraindications | Severe hepatic impairment; known hypersensitivity to any component. |
| Warnings |
• Serotonin‑syndrome risk when combined with serotonergic agents (SSRIs, MAOIs).
• Anticholinergic toxicity in patients with glaucoma, urinary retention, or obstructive airway disease.
• Pregnancy/Lactation – Animal studies show no teratogenicity