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Lubiprostone

Pronunciation

(loo bi PROS tone)

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

Pharmacology

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.

Absorption

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

Distribution

Minimal beyond GI tissue

Metabolism

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

Excretion

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

~94%

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 in adults

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

Opioid-induced constipation: Treatment of opioid-induced constipation in adults with chronic noncancer pain

Contraindications

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.

Dosing: Renal Impairment

No dosage adjustment necessary.

Dosing: Hepatic Impairment

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.

Administration

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

Dietary Considerations

Take with food and water to decrease nausea.

Storage

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

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

Adverse Reactions

>10%:

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

Gastrointestinal: Nausea (8% to 29%; dose related; 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% (Limited to important or life-threatening): Anorexia, anxiety, 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 ALT, increased serum AST, influenza, ischemic colitis, joint swelling, lethargy, malaise, muscle cramps, muscle spasm, myalgia, pain, palpitations, pharyngolaryngeal pain, pollakiuria, rectal hemorrhage, syncope, tachycardia, tremor, urinary tract infection, weakness, weight gain

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 has not been established.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events have been observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache, nausea, abdominal pain, flatulence, or bloating. Have patient report immediately to prescriber angina, severe diarrhea, severe dizziness, passing out, or shortness of breath (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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