From the Guidelines
Lubiprostone should be used in patients with irritable bowel syndrome with constipation (IBS-C) as it has been shown to improve stool frequency and consistency, as well as reduce abdominal discomfort and bloating, according to the most recent guideline from 2022 1.
Key Points
- The typical dosage of lubiprostone is 24 mcg twice daily for chronic constipation or 8 mcg twice daily for IBS-C, taken with food and water to reduce nausea.
- Lubiprostone works by increasing fluid secretion in the small intestine, softening stool and increasing bowel movements, by activating chloride channels (specifically ClC-2) in the intestinal lining.
- Common side effects include nausea, diarrhea, headache, abdominal pain, and bloating, with nausea being the most common adverse event, typically mild or moderate, but leading to discontinuation of therapy in only 5% of individuals 2.
- The risk of nausea is dose-dependent and seems to be lower when taken with food and water.
- Systemic absorption of oral lubiprostone is negligible, and individuals with moderate or severe hepatic insufficiency should receive a lower dose (ie, 8μg twice daily) 2.
Clinical Considerations
- Lubiprostone should be avoided during pregnancy unless clearly necessary, and patients should inform their doctor if they experience severe diarrhea or nausea.
- This medication offers an alternative for patients who haven't responded well to traditional constipation treatments like fiber supplements, stool softeners, or osmotic laxatives.
- The American Gastroenterological Association (AGA) suggests using lubiprostone in patients with IBS-C, with a conditional recommendation and moderate certainty 1, 3.
From the FDA Drug Label
These highlights do not include all the information needed to use LUBIPROSTONE CAPSULES safely and effectively. Lubiprostone capsules, for oral use Initial U. S. Approval: 2006 INDICATIONS AND USAGE Lubiprostone is a chloride channel activator indicated for the treatment of: • chronic idiopathic constipation (CIC) in adults. ( 1.1) • opioid-induced constipation (OIC) in adult patients with chronic, non-cancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dosage escalation. ( 1.2) • irritable bowel syndrome with constipation (IBS-C) in women ≥ 18 years old. ( 1.3)
The main uses of Lubiprostone are for the treatment of:
- Chronic Idiopathic Constipation (CIC) in adults
- Opioid-Induced Constipation (OIC) in adult patients with chronic non-cancer pain
- Irritable Bowel Syndrome with Constipation (IBS-C) in women 18 years or older 4
From the Research
Mechanism of Action
- Lubiprostone is a synthetic bicyclic fatty acid that selectively activates type 2 chloride channels in the apical membrane of intestinal epithelial cells, stimulating chloride secretion, along with passive secretion of sodium and water, inducing peristalsis and laxation 5, 6, 7, 8, 9.
- This mechanism of action leads to increased intraluminal chloride ion secretion, resulting in a passive influx of water and sodium, and ultimately increasing intestinal peristalsis and colonic laxation with decreased intestinal stool transit time 8.
Efficacy
- Lubiprostone has been shown to be effective in the treatment of chronic idiopathic constipation and irritable bowel syndrome with constipation (IBS-C) in several randomized, double-blind, placebo-controlled trials 5, 6, 7, 8, 9.
- The medication has been approved by the US Food and Drug Administration (FDA) for the treatment of chronic constipation in men and women, and for the treatment of women with IBS-C 5, 6, 7, 8.
- Lubiprostone has also been shown to be effective in the treatment of opioid-induced constipation 8.
Dosage and Administration
- The recommended dose of lubiprostone for the treatment of chronic constipation is 24 μg twice daily 5, 6, 7, 8.
- For the treatment of IBS-C, the recommended dose is 8 μg twice daily 5, 6, 7, 8, 9.