Description

Simple

A laxative that improves constipation by increasing the amount of fluid in the gastrointestinal tract.

Clinical

A prostaglandin derivative used to treat constipation caused by irritable bowel syndrome and opioid-use.

Overview

Lubiprostone is a medication used in the management of idiopathic chronic constipation. A prostaglandin E1 derivative, lubiprostone is a bicyclic fatty acid that activates ClC-2 chloride channels located on the apical side of the gastrointestinal epithelial cells. Activation of these channels promotes the secretion of a chloride-rich fluid that soften the stool, increase gastrointestinal motility, and induce spontaneous bowel movements (SBM).

Pharmacology

Indication

For the treatment of chronic idiopathic constipation in the adult population. Also used for the treatment of irritable bowel syndrome with constipation in women who are 18 years of age or older.

Pharmacodynamic

Chronic idiopathic constipation is generally defined by infrequent or difficult passage of stool. The signs and symptoms associated with chronic idiopathic constipation (i.e., abdominal pain or discomfort, bloating, straining, and hard or lumpy stools) may be the result of abnormal colonic motility... Read more

Mechanism of action

Lubiprostone acts by specifically activating ClC-2 chloride channels, which is a normal constituent of the apical membrane of the human intestine, in a protein kinase A action independent fashion. Activation of ClC-2 chloride channels causes an efflux of chloride ions into the lumen, which in turn l... Read more

Absorption

Lubiprostone has low systemic availability following oral administration and concentrations of lubiprostone in plasma are below the level of quantitation (10 pg/mL).

Protein binding

94%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

0.9 to 1.4 hours

Route of elimination

Peak plasma concentration was shown to be around 1.14 hours, with a majority of the drug excreted in the urine within 48 hours. Lubiprostone and M3 are only detected in trace amounts in human feces.

Toxicity

In a definitive Phase 1 cardiac repolarization study, 51 patients were administered a single oral dose of 144 mcg of lubiprostone, which is 6 times the normal single administration dose. Thirty-nine (39) of the 51 patients experienced an adverse event. The adverse events reported in >1% of this grou... Read more

Adverse Effects

Contraindications

  • Hypersensitivity:
    • false
  • Regions: US
  • Regions: US
  • Patient Conditions:
      • Name: Mechanical gastrointestinal obstruction
      • Drugbank Id: DBCOND0107884

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Abacavir
Lubiprostone may decrease the excretion rate of Abacavir which could result in a higher serum level.
Acarbose
Acarbose may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Acetaminophen
Acetaminophen may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Acetazolamide
The risk or severity of adverse effects can be increased when Acetazolamide is combined with Lubiprostone.
Acetylsalicylic acid
Acetylsalicylic acid may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Aclidinium
Aclidinium may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Acrivastine
Lubiprostone may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Adefovir
Adefovir may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Adefovir dipivoxil
Adefovir dipivoxil may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Agmatine
The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Agmatine.
Albutrepenonacog alfa
Lubiprostone may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
Alclofenac
Alclofenac may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Alcuronium
The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Alcuronium.
Aldesleukin
Aldesleukin may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
Alfentanil
The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Alfentanil.
Alloin
The risk or severity of adverse effects can be increased when Lubiprostone is combined with Alloin.
Allopurinol
Allopurinol may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
4 References
  1. 1 . Crowell MD, Harris LA, DiBaise JK, Olden KW: Activation of type-2 chloride channels: a novel therapeutic target for the treatment of chronic constipation. Curr Opin Investig Drugs. 2007 Jan;8(1):66-70.PubMed: 17263187
  2. 2 . Lacy BE, Chey WD: Lubiprostone: chronic constipation and irritable bowel syndrome with constipation. Expert Opin Pharmacother. 2009 Jan;10(1):143-52. doi: 10.1517/14656560802631319 .PubMed: 19236188
  3. 3 . Ambizas EM, Ginzburg R: Lubiprostone: a chloride channel activator for treatment of chronic constipation. Ann Pharmacother. 2007 Jun;41(6):957-64. Epub 2007 May 22.PubMed: 17519292
  4. 4 . Lacy BE, Levy LC: Lubiprostone: a novel treatment for chronic constipation. Clin Interv Aging. 2008;3(2):357-64.PubMed: 18686757