(loo bi PROS tone)
- RU 0211
- SPI 0211
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Amitiza: 8 mcg
Amitiza: 24 mcg [contains fd&c red #40, fd&c yellow #10 (quinoline yellow)]
Brand Names: U.S.
- Chloride Channel Activator
- Gastrointestinal Agent, Miscellaneous
Bicyclic fatty acid that acts locally at the apical portion of the intestine as a chloride channel activator, specifically ClC-2, thereby increasing intestinal fluid secretion and intestinal motility. When used for opioid induced constipation, activation of apical ClC-2 channels bypasses the antisecretory action of opiates resulting from suppression of secretomotor neuron excitability. ClC-2 activation does not alter serum sodium or potassium concentrations.
Systemic: Parent drug: Poor (below levels of detection); Active metabolite (M3): Low
Gastrointestinal tissue; minimal beyond gastrointestinal 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 hour
M3: 0.9-1.4 hours
Special Populations: Renal Function Impairment
Special Populations: Hepatic Function Impairment
Cmax and AUC are increased in patients with moderate-to-severe hepatic impairment.
Special Populations: Gender
Use: Labeled Indications
Treatment of chronic idiopathic constipation; treatment of opioid-induced constipation with chronic non-cancer pain; treatment of irritable bowel syndrome with constipation in adult women
Known or suspected mechanical bowel obstruction
Chronic idiopathic constipation: Adults: Oral: 24 mcg twice daily
Irritable bowel syndrome with constipation: Females ≥18 years: Oral: 8 mcg twice daily
Opioid-induced constipation: Adults: Oral: 24 mcg twice daily
Dosage adjustment for renal impairment: No dosage adjustment necessary.
Dosage adjustment for hepatic impairment:
Mild hepatic impairment (Child-Pugh class A): No dosage adjustment necessary.
Moderate hepatic impairment (Child-Pugh class B):
Chronic idiopathic 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.
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.
Severe hepatic impairment (Child-Pugh class C):
Chronic idiopathic constipation: Initial: 8 mcg twice daily; may increase to 16-24 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.
Opioid-induced constipation: Initial: 8 mcg twice daily; may increase to 16-24 mcg twice daily if tolerated and an adequate response has not been obtained with lower dosage.
Administer with food and water. Swallow whole; do not break or chew.
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.
Methadone: May diminish the therapeutic effect of Lubiprostone. Monitor therapy
Central nervous system: Headache (2% to 11%)
Gastrointestinal: Nausea (8% to 29%; severe: 1% to 4%; dose related; male: 8%; elderly: 19%), diarrhea (7% to 12%; severe <1% to 2%)
1% to 10%:
Cardiovascular: Edema (3%), peripheral edema (1% to 3%), chest discomfort (2%)
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 (<1% to 3%)
<1% (Limited to important or life-threatening): Anorexia, bowel urgency, cough, decreased appetite, depression, dysgeusia, eructation, erythema, fecal incontinence, fibromyalgia syndrome, frequent bowel movements, gastritis, gastroesophageal reflux disease, gastrointestinal disease, hyperhidrosis, hypersensitivity reaction, hypokalemia, increased liver enzymes, influenza, ischemic colitis, joint swelling, muscle spasm, myalgia, pain, palpitations, pharyngolaryngeal pain, pollakiuria, rectal hemorrhage, syncope, tachycardia, urinary tract infection, weight gain
Concerns related to adverse effects:
• Dyspnea: Often described as chest tightness, dyspnea has been observed with use; generally occurs following the first dose with an acute onset (within 30-60 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.
• Diarrhea: Avoid use in patients with severe diarrhea.
• Gastrointestinal obstruction: Symptoms of mechanical gastrointestinal 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.
Concurrent drug therapy issues:
• Agents which may lower efficacy: Diphenylheptane opioids (eg, methadone) may potentially decrease the efficacy of lubiprostone in a dose-dependent manner (by decreasing the activation of ClC-2 by lubiprostone in the GI tract); efficacy of lubiprostone in the treatment of opioid-induced constipation in patients taking diphenylheptane opioids has not been established.
• Males: Not approved for use in males with irritable bowel syndrome with constipation.
Pregnancy Risk Factor
Adverse events have been observed in animal reproduction studies.
• 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, dyspepsia, diarrhea, flatulence, or bloating. Have patient report immediately to prescriber angina, significant nausea, considerable diarrhea, or dyspnea (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 healthcare 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.
More about lubiprostone
- Other brands: Amitiza