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Lubiprostone (Monograph)

Brand name: Amitiza
Drug class: GI Drugs, Miscellaneous
VA class: GA900
Chemical name: (–)-7-[(2R,4aR,5R,7aR)-2-(1,1-difluoropentyl)-2-hydroxy-6-oxooctahydrocyclopenta[b]pyran-5-yl]heptanoic acid
Molecular formula: C20H32F2O5
CAS number: 136790-76-6

Medically reviewed by on Feb 20, 2023. Written by ASHP.


Bicyclic fatty acid; selectively activates intestinal ClC-2 chloride channels and increases intestinal fluid secretion.

Uses for Lubiprostone

Chronic Idiopathic Constipation

Management of chronic idiopathic constipation in adults.

Irritable Bowel Syndrome with Constipation in Women

Treatment of irritable bowel syndrome (IBS) with constipation in women ≥18 years of age.

Lubiprostone Dosage and Administration


Oral Administration

Administer orally with food and water.



Periodically assess need for continued therapy.

Chronic Idiopathic Constipation

24 mcg twice daily.

May reduce dosage to 24 mcg daily in patients experiencing severe nausea.

Irritable Bowel Syndrome with Constipation in Women

8 mcg twice daily.

Special Populations

No special population recommendations at this time.

Cautions for Lubiprostone


  • Known hypersensitivity to lubiprostone or any ingredient in the formulation.

  • Known or suspected mechanical GI obstruction.



GI Obstruction

Thoroughly evaluate patients with symptoms suggestive of mechanical GI obstruction to confirm absence of such obstruction prior to initiating lubiprostone therapy. (See Contraindications under Cautions.)

Fetal/Neonatal Morbidity and Mortality

Women of childbearing potential should have a negative pregnancy test prior to receiving lubiprostone and should use an effective method of contraception during therapy with the drug.

General Precautions

GI Effects

Dose-dependent nausea may occur. Symptoms may be reduced by coadministration with food and water.

Possible diarrhea (may be severe).

Do not prescribe lubiprostone to patients with severe diarrhea.

Respiratory Effects

Possible dyspnea (may result in discontinuance of the drug).

Onset of symptoms (e.g., sensation of chest tightness, difficulty in breathing) generally occurs within 30–60 minutes after taking the first dose. Symptoms usually resolve within a few hours; however, frequently recur with subsequent doses.

Specific Populations


Category C. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)


Not known whether distributed into human milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.

Geriatric Use

Geriatric patients with chronic idiopathic constipation experienced a lower incidence (18 versus 29%) of associated nausea than the overall study population.

Experience in those ≥65 years of age with IBS with constipation was insufficient to determine whether they respond differently from younger adults.

Hepatic Impairment

Not studied in patients with hepatic impairment.

Renal Impairment

Not studied in patients with renal impairment.

Common Adverse Effects

Chronic idiopathic constipation: Nausea, diarrhea, headache, abdominal distention, abdominal pain, flatulence, vomiting, dizziness, edema, loose stools, abdominal discomfort (including abdominal tenderness, abdominal rigidity, GI discomfort), dyspepsia, chest discomfort/pain, dyspnea, fatigue.

IBS with constipation in women: Nausea, diarrhea, abdominal pain, abdominal distention.

Interactions for Lubiprostone

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Does not inhibit CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 in vitro. Does not induce CYP1A2, CYP2B6, CYP2C9, or CYP3A4 in vitro. Pharmacokinetic interactions unlikely with drugs metabolized by these CYP isoenzymes.

Not metabolized by isoenzymes.

Highly Protein-bound Drugs

Pharmacokinetic interaction unlikely.

Lubiprostone Pharmacokinetics



Low systemic bioavailability following oral administration with peak plasma concentrations usually attained within 1.1 hours.


High-fat meal may reduce peak plasma concentration but does not affect extent of absorption (AUC).



Minimal distribution beyond GI tissues.

Lubiprostone crosses the placenta in animals; not known whether crosses the placenta in humans.

Not known whether distributed into human milk.

Plasma Protein Binding

Approximately 94%.



Rapidly and extensively metabolized, probably in the stomach and jejunum, by processes mediated by carbonyl reductase. CYP isoenzymes not involved in metabolism of the drug.

Elimination Route

Excreted in the urine (about 60%) within 24 hours and in feces (about 30%) within 168 hours.





25°C (may be exposed to 15–30°C).


  • Bicyclic fatty acid; selectively activates intestinal ClC-2 chloride channels; increases intestinal chloride and fluid secretion without affecting serum sodium and potassium concentrations. Activates the ClC-2 chloride channel which is located on the apical (luminal) membrane of the human intestinal epithelium, independent of the actions of protein kinase A.

  • Increases intestinal motility by increasing intestinal fluid secretion, consequently increasing the passage of stool and alleviating symptoms of chronic idiopathic constipation.

  • May stimulate recovery of mucosal barrier function by restoring tight junction protein complexes in the intestine.

  • Delays gastric emptying, which may result in nausea.

Advice to Patients

  • Advise patients to take the drug twice daily (morning and evening) with food and water.

  • Importance of advising patients to swallow capsules whole without chewing or breaking apart.

  • Importance of advising patients that nausea may occur; administer with food and water to reduce nausea. Advise patients to contact a clinician if nausea becomes severe.

  • Clinicians and patients periodically should assess the need for continued treatment.

  • Importance of advising patients that diarrhea may occur. Advise patients to notify a clinician and not to take lubiprostone if they experience severe diarrhea.

  • Importance of advising patients that dyspnea may occur; advise patients to notify clinician if dyspnea becomes severe.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed. Advise pregnant women of risk to the fetus. Importance of using effective method of contraception.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

  • Importance of informing patients of other important precautionary information. (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.



Dosage Forms


Brand Names




8 mcg



24 mcg



AHFS DI Essentials™. © Copyright 2023, Selected Revisions March 1, 2009. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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