Pharm

Lubiprostone

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Lubiprostone, Amitiza

  • Contraindications
  • Mechanism
  1. Bicyclic Fatty Acid derived from Prostaglandin E1 derivative
  2. Chloride channel activator (Secretagogue)
    1. Lubiprostone binds and activates type 2 chloride channels (CIC2) in the gastrointestinal epithelium
    2. Results in chloride release into the gastrointestinal lumen, with water following
  • Dosing
  1. General
    1. Capsules should be swallowed whole
    2. Decrease dose with moderate to severe liver dysfunction
  2. Constipation Dominant Irritable Bowel Syndrome (women age >18 years)
    1. Take 8 mcg orally twice daily
  3. Chronic Idiopathic Constipation (men and women)
    1. Take 24 mcg orally twice daily with food and water
  4. Opioid Induced Constipation (non-cancer related, in men and women)
    1. Take 24 mcg orally twice daily with food and water
  • Adverse Effects
  1. Nausea (esp. with 24 mcg dose)
    1. Decreased when taken with food
  2. Diarrhea (esp. with 24 mcg dose)
    1. Hold Lubiprostone for severe Diarrhea
  3. Abdominal Pain
  4. Chest Pain or Dyspnea
    1. Follows dose within 1 hour
    2. Resolves within 3 hours
  • Safety
  1. Pregnancy Category C
  2. Unknown safety in Lactation
  • Efficacy
  1. Low efficacy in Irritable Bowel Syndrome with Constipation (only 14% respond)
  • Drug Interactions
  1. Methadone
    1. Decreases Lubiprostone efficacy
  • References
  1. Chang (2006) Curr Treat Options Gastroenterol 9(4):314-23 [PubMed]
  2. (2021) Irritable Bowel Syndrome Drug Comparison, Presc Lett, #370305
  3. (2020) Med Lett Drugs Ther 62(1594): 41-58