|Trade names||Amitiza, others|
|Main uses||Chronic constipation of unknown cause, irritable bowel syndrome associated constipation|
|Side effects||Nausea, diarrhea, abdominal pain, swelling, tiredness|
|Typical dose||8 to 24 mcg BID|
|Metabolism||Extensive, CYP not involved|
|Elimination half-life||Unknown (lubiprostone)|
0.9–1.4 hours (main metabolite)
|Excretion||Kidney (60%) and fecal (30%)|
|Chemical and physical data|
|Molar mass||390.468 g·mol−1|
|3D model (JSmol)|
Lubiprostone, sold under the trade name Amitiza among others, is a medication used to treat chronic constipation of unknown cause and irritable bowel syndrome associated constipation. It is taken by mouth.
Common side effects include nausea, diarrhea, abdominal pain, swelling, and tiredness. Other side effects may include shortness of breath. Safety in pregnancy is unclear. It works by activating certain chloride channels in the intestines which increases fluid release.
Lubiprostone was approved for medical use in the United States in 2006 and Canada in 2015. In the United States a month of medication costs about 290 USD as of 2021. A generic version was approved in 2021 in the USA. It is not commercially available in the United Kingdom.
Lubiprostone is approved to treat chronic idiopathic constipation (CIC) in adults.
Lubiprostone is also approved to treat opioid-induced constipation, in adults with chronic non-cancer pain. The effectiveness of lubiprostone has not been established in patients who are taking a diphenylheptane opioid (e.g., methadone).
Lubiprostone is approved to treat irritable bowel syndrome with constipation (IBS-C) in women 18 years of age and older.
It is used at a dose of 8 mcg twice per day in IBS and 24 mcg twice per day in constipation of unknown cause.
Common side event include nausea (31%). Other adverse events (≥5% of patients) included diarrhea (13%), headache (13%), abdominal distension (5%), abdominal pain (5%), flatulence (6%), sinusitis (5%), vomiting (5%), and fecal incontinence (1%).
There is no current data on use in people with liver or kidney complications. The effects on pregnancy have not been studied in humans but testing in guinea pigs resulted in fetal loss.
Mechanism of action
Lubiprostone is a bicyclic fatty acid derived from prostaglandin E1 that acts by specifically activating ClC-2 chloride channels on the apical aspect of gastrointestinal epithelial cells, producing a chloride-rich fluid secretion. These secretions soften the stool, increase motility, and promote spontaneous bowel movements (SBM).
Symptoms of constipation such as pain and bloating are usually improved within one week, and SBM may occur within one day.
Unlike many laxative products, lubiprostone does not show signs of drug tolerance, chemical dependency, or altered serum electrolyte concentration. There was no rebound effect following withdrawal of treatment, but a gradual return to pre-treatment bowel movement frequency should be expected.
Minimal distribution of the drug occurs beyond the immediate gastrointestinal tissues. Lubiprostone is rapidly metabolized by reduction/oxidation, mediated by carbonyl reductase. There is no metabolic involvement of the hepatic cytochrome P450 system. The measurable metabolite, M3, exists in very low levels in plasma and makes up less than 10% of the total administered dose.
Society and culture
The medication is at a cost in the U.S. of $290 (USD) for 60 capsules (8 mcg)
The drug is available in the United States, Japan, Switzerland, India, and Canada.
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