Mechanism Of Action

How AMITIZA (lubiprostone) works

AMITIZA has an MOA that enhances the body's natural function by increasing intestinal fluid secretion to improve motility, which1-3:

  • Helps pass stool
  • Alleviates multiple chronic idiopathic constipation (CIC) symptoms (abdominal discomfort/bloating, stool consistency, straining, constipation severity)

AMITIZA is the first and only chloride channel-2 (CIC-2) activator for the treatment of chronic constipation1

Chloride channels in the intestinal tract help regulate fluid balance.3 AMITIZA works locally in the intestine to help activate these chloride channels.1 As a result of this activation, AMITIZA:

  • Increases fluid secretion and transit
  • Stimulates recovery of the mucosal barrier function and reduces intestinal permeability via restoration of tight junctions*
    • The MOA of AMITIZA in irritable bowel syndrome with constipation (IBS-C) is not fully understood
  • Bypasses the antisecretory effect of opioids

*Demonstrated in ex vivo studies of ischemic porcine intestine.

The role of tight junctions is unclear.

AMITIZA (lubiprostone) prescriptions

In the current chronic constipation market, AMITIZA is the branded prescription agent with the4:

  • Longest time on market (12+ years)‡4
  • Most prescriptions filled (15+ million)‡4
  • Most approved indications (CIC in adults, opioid-induced constipation (OIC) in adults with chronic, non-cancer pain, and IBS-C in adult women)

No conclusions of comparative safety or efficacy can be made from this information.

IQVIA [March 2006–October 2018]; November 2018. 
Note: This information is an estimate derived from the use of information under license from the following IQVIA information service: National Prescription Audit Monthly for the period March 2006–October 2018. IQVIA expressly reserves all rights, including rights of copying, distribution and republication.

Help patients save

The Savings Card can be used to reduce patient co-pay for cash-paying patients.


Coverage for Medicare patients

AMITIZA is covered for 89% of Medicare Part D lives.

Fingertip Formulary, September 2018.


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Important Safety Information

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AMITIZA (lubiprostone) is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction. Patients with symptoms suggestive of mechanical gastrointestinal obstruction should be thoroughly evaluated by the treating healthcare provider (HCP) to confirm the absence of such an obstruction prior to initiating AMITIZA treatment.

Patients taking AMITIZA may experience nausea. Concomitant administration of food with AMITIZA may reduce symptoms of nausea.

Avoid use of AMITIZA in patients with severe diarrhea. Patients should be aware of the possible occurrence of diarrhea during treatment. Instruct patients to discontinue AMITIZA and contact their HCP if severe diarrhea occurs.

Syncope and hypotension have been reported with AMITIZA in the postmarketing setting and a few of these adverse reactions resulted in hospitalization. Most reports occurred in patients taking 24 mcg twice daily. Patients should be aware that the risk of syncope and hypotension may be increased with concomitant diarrhea, vomiting, or use of medications known to lower blood pressure. Inform patients that syncope and hypotension may occur within an hour of the first dose or subsequent doses of AMITIZA and generally resolve prior to the next dose, but may recur with repeat dosing. Instruct patients to discontinue AMITIZA and contact their HCP if these reactions occur.

Dyspnea may occur within an hour of first dose. This symptom generally resolves within three hours, but may recur with repeat dosing. Instruct patients to contact their HCP if dyspnea occurs. Some patients have discontinued therapy because of dyspnea.

In clinical trials of AMITIZA (24 mcg twice daily vs placebo; N=1113 vs N=316, respectively) in patients with CIC, the most common adverse reactions (incidence > 4%) were nausea (29% vs 3%), diarrhea (12% vs 1%), headache (11% vs 5%), abdominal pain (8% vs 3%), abdominal distension (6% vs 2%), and flatulence (6% vs 2%).

In clinical trials of AMITIZA (24 mcg twice daily vs placebo; N=860 vs N=632, respectively) in patients with OIC, the most common adverse reactions (incidence > 4%) were nausea (11% vs 5%) and diarrhea (8% vs 2%).

In clinical trials of AMITIZA (8 mcg twice daily vs placebo; N=1011 vs N=435, respectively) in patients with IBS-C, the most common adverse reactions (incidence > 4%) were nausea (8% vs 4%), diarrhea (7% vs 4%), and abdominal pain (5% vs 5%).

Concomitant use of diphenylheptane opioids (e.g., methadone) may interfere with the efficacy of AMITIZA.

The safety of AMITIZA in pregnancy has not been evaluated in humans. Based on animal data, AMITIZA may cause fetal harm. AMITIZA should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Caution should be exercised when AMITIZA is administered to a nursing woman. Advise nursing women to monitor infants for diarrhea.

Reduce the dosage in CIC and OIC patients with moderate and severe hepatic impairment. Reduce the dosage in IBS-C patients with severe hepatic impairment.


AMITIZA (lubiprostone) 24 mcg capsules twice daily are indicated for the treatment of Chronic Idiopathic Constipation (CIC) in adults and Opioid-Induced Constipation (OIC) in adults with chronic, non-cancer pain, including chronic pain related to prior cancer or its treatment who do not require frequent (e.g. weekly) opioid dose escalation. The effectiveness in patients with OIC taking diphenylheptane opioids (e.g., methadone) has not been established. AMITIZA 8 mcg capsules twice daily are also indicated for Irritable Bowel Syndrome with Constipation (IBS-C) in women ≥ 18 years old.

Please click here for complete Prescribing Information.

  1. AMITIZA (lubiprostone) Prescribing Information. Sucampo Pharma Americas, LLC.
  2. Hall JE. Textbook of Medical Physiology. 12th ed. Philadelphia, PA: Saunders Elsevier; 2011:773-788.
  3. Keely SJ, Montrose MH, Barrett KE. In: Yamada T, Alpers DH, Kalloo AN, Kaplowitz N, Owyang C, Powell DW, eds. Textbook of Gastroenterology. 5th ed. West Sussex, England: John Wiley & Sons Ltd; 2009:330-367.
  4. Data on file. Takeda Pharmaceuticals.
  5. Johanson JF, Morton D, Geenen J, Ueno R. Am J Gastroenterol. 2008;103:170-177.
  6. Barish CF, Drossman D, Johanson JF, Ueno R. Dig Dis Sci. 2010;55:1090-1097.
  7. Data on file. Sucampo Pharma Americas, LLC.