Lubiprostone


Description

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 epi...

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Pharmacology

Indication

For the treatment of chronic idiopathic constipation in the adult population. Also used for the trea... Read more

Pharmacodynamic

Chronic idiopathic constipation is generally defined by infrequent or difficult passage of stool. Th... Read more

Mechanism of action

Lubiprostone acts by specifically activating ClC-2 chloride channels, which is a normal constituent... Read more

Absorption

Lubiprostone has low systemic availability following oral administration and concentrations of lubip... Read more

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... Read more

Toxicity

In a definitive Phase 1 cardiac repolarization study, 51 patients were administered a single oral do... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Nausea US
  • adult
  • Kind: experimental
    • Percent: 17-29%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 7-12%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Headache US
    • adult
  • Kind: experimental
    • Percent: 3-11%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: 3-8%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Nausea US
    • adult
  • Kind: experimental
    • Percent: 8%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Diarrhea US
    • adult
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Abdominal distension US
    • adult
  • Kind: experimental
    • Percent: ≤6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Flatulence US
    • adult
  • Kind: experimental
    • Percent: 3-6%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Abdominal Pain US
    • adult
  • Kind: experimental
    • Percent: 5%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Edema US
    • adult
  • Kind: experimental
    • Percent: ≤3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Dizziness US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Chest Pain US
    • adult
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Chest discomfort US
    • adult
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Vomiting US
    • adult
  • Kind: experimental
    • Percent: ≤3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Loose stools US
    • adult
  • Kind: experimental
    • Percent: ≤3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Abdominal Discomfort US
    • adult
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Dyspnea US
    • adult
  • Kind: experimental
    • Percent: 2-3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Abdominal distension US
    • adult
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Fatigue US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Dyspepsia US
    • adult
  • Kind: experimental
    • Percent: ≤2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Stomach discomfort US
    • adult
  • Kind: experimental
    • Percent: ≤1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Dry Mouth US
    • adult
  • Kind: experimental
    • Percent: ≤1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Increased aspartate aminotransferase US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Eructation US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Constipation US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dry Mouth US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Increased alanine aminotransferase US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Edema US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Increased weight US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Gastritis US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Palpitations US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Dyspnea US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Gastroesophageal Reflux Disease US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Erythema US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Fecal Incontinence US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Fibromyalgia US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hard feces US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Urinary Tract Infection US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Anorexia US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Anxiety US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Depression US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Lethargy US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Rectal hemorrhage US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Pollakiuria US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Pharyngolaryngeal pain US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Hyperhidrosis US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Frequent bowel movements US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Defecation urgency US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Muscle Cramp US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial
    Fecal Incontinence US
    • adult
  • Kind: experimental
    • Percent: <1%
  • Clinical Trial

    Contraindications

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

    Food Interactions

      Information currently not available.

    Interactions

    Type in a drug name to check for interaction with Lubiprostone

    Lubiprostone may decrease the excretion rate of Abacavir which could result in a higher serum level.
    Acarbose may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    Aceclofenac may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    Acemetacin may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    Acetaminophen may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    The risk or severity of adverse effects can be increased when Acetazolamide is combined with Lubiprostone.
    Acetylsalicylic acid may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Aclidinium.
    Lubiprostone may decrease the excretion rate of Acrivastine which could result in a higher serum level.
    Acyclovir may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    Adefovir may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    Adefovir dipivoxil may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Agmatine.
    Lubiprostone may decrease the excretion rate of Albutrepenonacog alfa which could result in a higher serum level.
    Alclofenac may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Alcuronium.
    Aldesleukin may decrease the excretion rate of Lubiprostone which could result in a higher serum level.
    The therapeutic efficacy of Lubiprostone can be decreased when used in combination with Alfentanil.
    The risk or severity of adverse effects can be increased when Lubiprostone is combined with Alloin.
    Allopurinol may decrease the excretion rate of Lubiprostone which could result in a higher serum level.

    References

    • 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 . 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 . 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 . Lacy BE, Levy LC: Lubiprostone: a novel treatment for chronic constipation. Clin Interv Aging. 2008;3(2):357-64. [PubMed: 18686757]

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