Lubiprostone

Lubiprostone Brand Name– Amitiza

What is Lubiprostone

Lubiprostone is a unique gastrointestinal agent for the treatment of constipation.

Chemically, the drug is a bicyclic fatty acid, prostaglandin E1 (PGE 1) derivative that increases intestinal fluid secretion by activating specific ClC-2 chloride channels in the luminal cells of the intestinal epithelium.

Clinically, lubiprostone alters stool consistency and promotes regular bowel movements, without altering serum electrolyte concentrations or producing tolerance, using this unique mechanism.

In comparison, fluid and electrolyte problems, as well as product dependency, have been associated with other products for constipation, such as selected laxatives.

Furthermore, other agents which effect gastrointestinal motility or inhibit visceral sensitivity (e.g., tegaserod), have not been adequately studied in the elderly suffering from chronic constipation.

Overall, lubiprostone is well tolerated in all adult populations, including in elderly patients. In clinical evaluation, statistically significant differences in the timing of the first spontaneous bowel movement (SMB) following initiation of treatment were observed in lubiprostone-treated patients compared to placebo-treated patients; approximately 60% of patients experienced an SMB within 24 hours of the first lubiprostone dose compared to roughly 35% in placebo groups.

Signs and symptoms related to constipation, including abdominal bloating, abdominal discomfort, stool consistency, and straining, as well as constipation severity ratings, were also improved in the lubiprostone group. Additionally, long-term, open-label data suggest a sustained response over a 6—12 month treatment period.

The most common side effect of lubiprostone is nausea.Lubiprostone remains under investigation for its utility in the treatment of postoperative bowel dysfunction.

Lubiprostone was approved by the FDA for chronic idiopathic constipation in adults in January 2006.

Lubiprostone was approved by FDA for constipation-predominant irritable bowel syndrome (IBS-C) in women >= 18 years of age in April 2008.

Lubiprostone was approved by FDA for opiate agonist-induced constipation (OIC) in April 2013.

Indications

  1. constipation
  2. irritable bowel syndrome
  3. opiate agonist-induced constipation

For the treatment of chronic idiopathic constipation (e.g., 6 month or longer history of less than 3 spontaneous bowel movements per week, with at least 25% of bowel movements with hard stools, sensation of incomplete evacuation, or straining)

Side Effects

  1. abdominal pain
  2. anxiety
  3. asthenia
  4. chest pain (unspecified)
  5. chills
  6. diarrhea
  7. dizziness
  8. dysgeusia
  9. dyspepsia
  10. dyspnea
  11. fatigue
  12. fecal incontinence
  13. fecal urgency
  14. flatulence
  15. flushing
  16. headache
  17. hyperhidrosis
  18. hypotension
  19. malaise
  20. nausea
  21. palpitations
  22. paresthesias
  23. peripheral edema
  24. rash
  25. syncope
  26. tremor
  27. urticaria
  28. vertigo
  29. vomiting
  30. wheezing

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • abdominal pain
  • breast-feeding
  • children
  • cholelithiasis
  • Crohn’s disease
  • diarrhea
  • diverticulitis
  • fecal impaction
  • gastric cancer
  • geriatric
  • GI disease
  • GI obstruction
  • hepatic disease
  • hypotension
  • inflammatory bowel disease
  • pregnancy
  • syncope
  • vomiting

Lubiprostone is contraindicated in any patient with a known hypersensitivity to the drug or any of its excipients

Interactions

  • Alosetron
  • Anticholinergics
  • Antidiarrheals
  • Belladonna; Opium
  • Bumetanide
  • Calcium Phosphate, Supersaturated
  • Crofelemer
  • Dichlorphenamide
  • Ethacrynic Acid
  • Furosemide
  • Lactulose
  • Loop diuretics
  • Methadone
  • Sodium Phosphate Monobasic Monohydrate; Sodium Phosphate Dibasic Anhydrous
  • Solifenacin
  • Torsemide
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