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Medically reviewed by Last updated on Sep 26, 2020.


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Index Terms

  • RU 0211
  • SPI 0211

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Amitiza: 8 mcg

Amitiza: 24 mcg [contains fd&c red #40, fd&c yellow #10 (quinoline yellow)]

Brand Names: U.S.

  • Amitiza

Pharmacologic Category

  • Chloride Channel Activator
  • Gastrointestinal Agent, Miscellaneous


A chloride channel activator that acts locally on the apical membrane of the gastrointestinal tract to increase intestinal fluid secretion and improve fecal transit. This action bypasses the antisecretory effects of opiates, which suppress secretomotor neuron excitability.


Systemic: Parent drug: Poor (below levels of detection); Active metabolite (M3): Low


Minimal beyond GI tissue


Rapid and extensive within stomach and jejunum by carbonyl reductase to M3 (active metabolite) and others


Parent drug and M3: Feces (trace amounts)

Time to Peak

Plasma: M3: ~1.1 hour

Half-Life Elimination

M3: 0.9 to 1.4 hours

Protein Binding


Special Populations: Hepatic Function Impairment

Cmax and AUC of active metabolite M3 are increased in patients with moderate-to-severe hepatic impairment.

Use: Labeled Indications

Chronic idiopathic constipation: Treatment of chronic idiopathic constipation (CIC) in adults

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

Opioid-induced constipation: Treatment of opioid-induced constipation (OIC) in adults with chronic noncancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (eg, weekly) opioid dosage escalation.


Known or suspected mechanical gastrointestinal (GI) obstruction

Dosing: Adult

Chronic idiopathic constipation: Oral: 24 mcg twice daily

Irritable bowel syndrome with constipation: Females ≥18 years: Oral: 8 mcg twice daily

Opioid-induced constipation: Oral: 24 mcg twice daily

Dosing: Geriatric

Refer to adult dosing.


Oral: Administer with food and water. Swallow whole; do not break or chew.

Dietary Considerations

Take with food and water to decrease nausea.


Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light and extreme temperatures.

Drug Interactions

Levomethadone: May diminish the therapeutic effect of Lubiprostone. Monitor therapy

Methadone: May diminish the therapeutic effect of Lubiprostone. Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.


Central nervous system: Headache (2% to 11%)

Gastrointestinal: Nausea (8% to 29%; males: 8%; older adults: 19%), diarrhea (7% to 12%)

1% to 10%:

Cardiovascular: Edema (≤3%), chest discomfort (≤2%), chest pain (≤2%), peripheral edema (1%)

Central nervous system: Dizziness (3%), fatigue (≤2%)

Gastrointestinal: Abdominal pain (4% to 8%), flatulence (4% to 6%), abdominal distention (3% to 6%), abdominal distress (3%), loose stools (≤3%), vomiting (≤3%), dyspepsia (≤2%), xerostomia (≤1%)

Respiratory: Dyspnea (≤3%)

<1%, postmarketing, and/or case reports: Anorexia, anxiety, arthralgia (Anton 2017), asthenia, back pain (Anton 2017), bloody diarrhea (Anton 2017), bowel urgency, constipation, cough, decreased appetite, decreased serum potassium, depression, diaphoresis, dysgeusia, eructation, erythema, fecal impaction, fecal incontinence, fibromyalgia syndrome, frequent bowel movements, gastritis, gastroesophageal reflux disease, gastrointestinal disease, hyperhidrosis, hypersensitivity reaction (including skin rash, swelling, throat tightness), hypotension, increased serum alanine aminotransferase, increased serum aspartate aminotransferase, influenza, ischemic colitis, joint swelling, lethargy, malaise, muscle cramps, muscle spasm, myalgia, neck pain (Anton 2017), pain, palpitations, pharyngolaryngeal pain, pollakiuria, rectal hemorrhage, respiratory tract infection (Anton 2017), syncope, tachycardia, tremor, urinary tract infection, weight gain


Concerns related to adverse effects:

• Dyspnea: Has been observed with use; often described as chest tightness and difficulty in taking a breath; generally occurs as an acute onset (within 30 to 60 minutes following the first dose) and resolves within a few hours; however, has been frequently reported with subsequent dosing.

• Nausea: Nausea may occur; administer with food to reduce symptoms.

• Syncope/hypotension: May occur (some resulting in hospitalization) and generally resolved following discontinuation or prior to the next dose; reoccurrence has been reported with subsequent doses. Most cases occurred when taking 24 mcg twice daily, within an hour after the first dose or subsequent doses, or during concomitant use of medications known to decrease blood pressure.

Disease-related concerns:

• Diarrhea: Avoid use in patients with severe diarrhea.

• Gastrointestinal obstruction: Symptoms of mechanical GI obstruction should be evaluated before prescribing this medicine; use is contraindicated in patients with bowel obstruction.

• Hepatic impairment: Patients with moderate-to-severe hepatic impairment (Child-Pugh class B or C) have higher systemic drug exposure; dosage adjustment may be recommended, depending on the indication and severity of hepatic impairment.

Special populations:

• Males: Not approved for use in males with irritable bowel syndrome with constipation.

Other warnings/precautions:

• Appropriate use: Efficacy of lubiprostone in the treatment of opioid-induced constipation in patients taking diphenylheptane opioids (eg, methadone) has not been established.

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Patient Education

What is this drug used for?

• It is used to treat constipation.

• It is used to treat irritable bowel syndrome with constipation (IBS-C).

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Headache

• Nausea

• Abdominal pain

• Diarrhea

• Passing gas

• Bloating

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Severe dizziness

• Passing out

• Shortness of breath

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine’s uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.