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Lubiprostone: Drug information

Lubiprostone: Drug information
(For additional information see "Lubiprostone: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Amitiza
Pharmacologic Category
  • Chloride Channel Activator;
  • Gastrointestinal Agent, Miscellaneous
Dosing: Adult
Chronic idiopathic constipation

Chronic idiopathic constipation: Oral: 24 mcg twice daily

Irritable bowel syndrome with constipation

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

Opioid-induced constipation

Opioid-induced constipation: Oral: 24 mcg twice daily

Dosing: Kidney Impairment: Adult

No dosage adjustment necessary.

Dosing: Hepatic Impairment: Adult

Mild hepatic impairment (Child-Pugh class A): No dosage adjustment necessary.

Moderate hepatic impairment (Child-Pugh class B):

Chronic idiopathic constipation or opioid-induced constipation: Initial: 16 mcg twice daily; may increase to 24 mcg twice daily if tolerated and an adequate response has not been obtained with lower dosage.

Irritable bowel syndrome with constipation: No dosage adjustment necessary.

Severe hepatic impairment (Child-Pugh class C):

Chronic idiopathic constipation or opioid-induced constipation: Initial: 8 mcg twice daily; may increase to 16 to 24 mcg twice daily if tolerated and an adequate response has not been obtained with lower dosage.

Irritable bowel syndrome with constipation: Initial: 8 mcg once daily; may increase to 8 mcg twice daily if tolerated and an adequate response has not been obtained at lower dosage.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

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 (allura red ac dye), quinoline yellow (d&c yellow #10)]

Generic: 8 mcg, 24 mcg

Generic Equivalent Available: US

Yes

Administration: Adult

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

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.

Adverse Reactions

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

>10%:

Gastrointestinal: Diarrhea (7% to 12%; severe diarrhea: ≤2%), nausea (8% to 29%, incidence lower in males; older adults: 19%; severe nausea: 1% to 4%)

Nervous system: Headache (2% to 11%)

1% to 10%:

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

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

Nervous system: Dizziness (3%), fatigue (2%)

Respiratory: Dyspnea (2% to 3%)

<1%:

Cardiovascular: Palpitations, syncope

Dermatologic: Diaphoresis, erythema of skin, hyperhidrosis

Endocrine & metabolic: Decreased serum potassium, weight gain

Gastrointestinal: Anorexia, bowel urgency, decreased appetite, dysgeusia, eructation, fecal incontinence, frequent bowel movements, gastritis, gastroesophageal reflux disease

Genitourinary: Pollakiuria, urinary tract infection

Hematologic & oncologic: Rectal hemorrhage

Hepatic: Increased serum alanine aminotransferase, increased serum aspartate aminotransferase

Infection: Influenza

Nervous system: Anxiety, depression, fibromyalgia syndrome, lethargy, pain

Neuromuscular & skeletal: Joint swelling, muscle cramps, myalgia, tremor

Respiratory: Cough, pharyngolaryngeal pain

Postmarketing:

Cardiovascular: Hypotension, tachycardia

Gastrointestinal: Bloody diarrhea (Anton 2017), ischemic colitis

Hypersensitivity: Hypersensitivity reaction

Neuromuscular & skeletal: Arthralgia (Anton 2017), asthenia, back pain (Anton 2017), muscle spasm, neck pain (Anton 2017)

Respiratory: Respiratory tract infection (Anton 2017)

Contraindications

Known or suspected mechanical gastrointestinal (GI) obstruction

Warnings/Precautions

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.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

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

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

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Breastfeeding Considerations

It is not known if lubiprostone or its active metabolite are present in breast milk. The manufacturer recommends that breastfed infants be monitored for diarrhea when administering lubiprostone to breastfeeding women. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Dietary Considerations

Take with food and water to decrease nausea.

Mechanism of Action

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.

Pharmacokinetics

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

Distribution: Minimal beyond GI tissue

Protein binding: ~94%

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

Bioavailability: Minimal

Half-life elimination: M3: 0.9 to 1.4 hours

Time to peak, plasma: M3: ~1.1 hour

Excretion: Parent drug and M3: Feces (trace amounts)

Pharmacokinetics: Additional Considerations

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

Pricing: US

Capsules (Amitiza Oral)

8 mcg (per each): $7.42

24 mcg (per each): $7.42

Capsules (Lubiprostone Oral)

8 mcg (per each): $6.68

24 mcg (per each): $6.68

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Amiprostone (EG);
  • Amitiza (BB, CH, CR, DO, GB, GT, HN, JP, NI, PA, SG, SV, TH);
  • Lubilax (BD);
  • Lubistone (BD);
  • Lubowel (IN);
  • Lupicont (EG);
  • Luprostam (EG);
  • Modulex (CO)


For country code abbreviations (show table)
  1. Amitiza (lubiprostone) [prescribing information]. Lexington, MA: Takeda Pharmaceuticals America, Inc; November 2020.
  2. Anton C. Adverse effects of laxatives: update. Wolters Kluwer Adverse Drug Reaction Bulletin. 2017;303.
  3. Johanson JF and Ueno R, “Lubiprostone, a Locally Acting Chloride Channel Activator, In Adult Patients With Chronic Constipation: A Double-Blind, Placebo-Controlled, Dose-Ranging Study to Evaluate Efficacy and Safety,” Aliment Pharmacol Ther, 2007, 25(11):1351-61. [PubMed 17509103]
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