Lubiprostone !
A prostaglandin-derived drug that opens chloride channels in the gut lining, so fluid enters the bowel and stool passes more easily.
Updated 2026-11-01
Mechanism of action
Lubiprostone is a prostanoic acid derivative that acts locally. It activates ClC-2 chloride channels on the luminal membrane of intestinal cells, independent of protein kinase A. Chloride-rich fluid is secreted into the lumen without changing serum sodium or potassium; the extra fluid increases motility and eases the passage of stool. Because it acts on the epithelium, it bypasses the antisecretory effect of opioids on gut nerves.
- Activates ClC-2 chloride channels on the gut lining
- Chloride-rich fluid is secreted into the lumen
- More fluid increases motility and softens stool
Pharmacokinetics
- Absorption
- Minimal systemic absorption; acts locally on the intestinal lining
Indications
- Chronic idiopathic constipation in adults Constipation and faecal impaction →
- Opioid-induced constipation in adults with chronic non-cancer pain
- Irritable bowel syndrome with constipation in women 18 years and older Irritable bowel syndrome →
Adverse effects
Common
- Nausea (less with food)
- Diarrhoea
- Headache
- Abdominal pain, distension and flatulence
Contraindications
- Known or suspected mechanical bowel obstruction
Key interactions
- Methadone and other diphenylheptane opioids
- May reduce its activation of ClC-2 and its effect in opioid-induced constipation
What is monitored
- Bowel pattern and diarrhoea
- Nausea
- Dizziness, fainting or shortness of breath
- Periodic review of the need to continue
Administration and safety
- Capsules are swallowed whole, not opened or chewed.
- Taken with food and water to reduce nausea.
Nursing care
- Rule out symptoms of bowel obstruction before starting.
- Give with food and water.
- Teach that shortness of breath or chest tightness may occur within an hour of a dose and usually passes, but should be reported.
- Report severe diarrhoea, fainting or lightheadedness.
Pregnancy and breastfeeding
Animal data suggest possible fetal harm; it is avoided in pregnancy unless the benefit clearly outweighs the risk.
Test yourself
Think of the answer, then tap the question to see it.
Which channel does lubiprostone activate?
The ClC-2 chloride channel on the luminal membrane of intestinal cells.
How can lubiprostone help in opioid-induced constipation?
It acts directly on the epithelium, bypassing the opioid-induced suppression of secretomotor nerves.
Which opioid may reduce lubiprostone's effect?
Methadone and other diphenylheptane opioids.
What is the most common adverse effect, and how is it reduced?
Nausea; taking it with food reduces it.
Related drugs
Related conditions
← Back to the class: Laxatives
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - LUBIPROSTONE capsule (DailyMed (U.S. National Library of Medicine), 2022); Lubiprostone: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2017); Farmacología básica y clínica (Katzung), 16.ª ed., cap. 62 (McGraw Hill, 2025).
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Representative model, for educational purposes only.