Version April 2023
Chronic idiopathic constipation: Oral: 24 mcg twice daily.
Irritable bowel syndrome with constipation (females ≥18 years old; males [off label]):
Note: Reserve for patients with persistent constipation refractory to osmotic laxatives (Wald 2022).
Oral: 8 mcg twice daily; may require ≥2 months for symptom improvement (ACG [Lacy 2021]; Chey 2012; Drossman 2009).
Opioid-induced constipation: Oral: 24 mcg twice daily.
No dosage adjustment necessary.
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.
Refer to adult dosing.
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
Yes
Oral: Administer with food and water. Swallow whole; do not break or chew.
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.
Irritable bowel syndrome with constipation (male)
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)
Known or suspected mechanical gastrointestinal (GI) obstruction
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.
None known.
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
Adverse events have been observed in animal reproduction studies.
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.
Take with food and water to decrease nausea.
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
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)
Hepatic function impairment: Cmax and AUC of active metabolite M3 are increased in patients with moderate-to-severe hepatic impairment.
Capsules (Amitiza Oral)
8 mcg (per each): $7.42
24 mcg (per each): $7.42
Capsules (Lubiprostone Oral)
8 mcg (per each): $6.68 - $7.05
24 mcg (per each): $6.68 - $7.05
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