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Lubiprostone Description
Lubiprostone is a medication used in the management
of idiopathic chronic constipation. It was approved by
the U.S. Food and Drug Administration for this purpose
on January 31, 2006.
Lubiprostone Indications
Lubiprostone is a gastrointestinal agent used for
the treatment of idiopathic chronic constipation. It is
well-tolerated in adults, including elderly patients. As
of July 20, 2006, Lubiprostone had not been studied in
pediatric patients.
There is current research underway to determine the
efficacy of Lubiprostone in patients with
constipation-predominant IBS, postoperative bowel
dysfunction, and opioid-induced bowel dysfunction.
Lubiprostone received approval from the United States
Food and Drug Administration (FDA) on 04/29/2008 to
treat Irritable Bowel Syndrome with constipation
(IBS-C).
Lubiprostone Mode of Action
Lubiprostone is a bicyclic fatty acid (prostaglandin
E1 derivative) 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 (pain, bloating) are usually
improved within one week, and SBM may occur within one
day.
Lubiprostone Pharmacokinetics
Unlike many laxative products, Lubiprostone does not
show signs of tolerance, 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 GI 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.
Data indicate that metabolism occurs locally in the
stomach and jejunum.
Lubiprostone side effects
Stop using lubiprostone and get emergency medical
help if you have any of these signs of an allergic
reaction: hives; difficulty breathing; swelling of your
face, lips, tongue, or throat. Call your doctor at once
if you have severe vomiting or diarrhea.
Less serious side effects are more likely to occur.
Continue using lubiprostone and talk with your doctor if
you have any of these less serious side effects:
- nausea, vomiting, mild diarrhea, loss of appetite;
- stomach pain, bloating, gas,
- sore throat, cough;
- headache, dizziness;
- swelling in your hands, ankles, or feet;
- joint or muscle pain; or
- anxiety, cold sweats.
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Disclaimer:
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Information
on this page is provided for general information
purposes. You should not make a clinical treatment
decision based on information contained in this page
without consulting other references including the
package insert of the drug, textbooks and where
relevant, expert opinion. We cannot be held responsible
for any errors you make in administering drugs mentioned
on this page, nor for use of any erroneous information
contained on this page.
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