lubiprostone (Rx)

Brand and Other Names:Amitiza
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 8mcg
  • 24mcg

Chronic Idiopathic Constipation

Indicated for treatment of chronic idiopathic constipation (CIC) in adults

24 mcg PO BID

Irritable Bowel Syndrome With Constipation

Indicated for treatment of irritable bowel syndrome with constipation (IBS-C) in women aged ≥18 years

8 mcg PO BID

Opioid-Induced Constipation

Indicated for 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

24 mcg PO BID

Limitations of use: Effectiveness in patients taking diphenylheptane opioids (eg, methadone) has not been established

Dosage Modifications

Hepatic impairment

  • Mild: No dosage adjustment required
  • Moderate (Child-Pugh B)
    • CIC or OIC: 16 mcg PO BID; if modified dose is tolerated and adequate response has not been obtained after appropriate interval, dose can be escalated to full standard dose with appropriate monitoring of patient response
    • IBS-C: No dosage adjustment required
  • Severe (Child-Pugh C)
    • CIC or OIC: 8 mcg PO BID
    • IBS-C: 8 mcg PO qDay
    • If modified dose is tolerated and adequate response has not been obtained after appropriate interval, dose can be escalated to full standard dose with appropriate monitoring of patient response

Safety and efficacy not established

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Adverse Effects

>10%

Nausea (8-29%)

Diarrhea (7-12%)

Headache (2-11%)

1-10%

Abdominal pain (4-8%)

Abdominal distension (3-6%)

Flatulence (4-6%)

Vomiting (3%)

Loose stools (3%)

Edema (1-3%)

Abdominal discomfort (1-3%)

Dizziness (3%)

Chest discomfort/pain (2%)

Dyspnea (2%)

Dyspepsia (2%)

Fatigue (2%)

Dry mouth (1%)

Postmarketing Reports

Cardiovascular: Syncope and/or hypotension, tachycardia

Gastrointestinal: Ischemic colitis

General: Asthenia

Immune system: Hypersensitivity reactions including rash, swelling, throat tightness, malaise

Musculoskeletal: Muscle cramps or muscle spasms

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Warnings

Contraindications

Hypersensitivity

Mechanical GI obstruction

Cautions

In patients with symptoms suggestive of mechanical GI obstruction, perform a thorough evaluation to confirm the absence of an obstruction prior to initiating therapy (see Contraindications)

Potential for acute dyspnea described as sensation of chest tightness and difficulty breathing within 30-60 minutes after the first dose; instruct patients to contact healthcare provider if dyspnea occurs

Avoid use in patients with severe diarrhea; instruct patients of potential for diarrhea to occur during treatment

May cause nausea and diarrhea (taking with food reduces chance of nausea); dose adjustment recommended

Syncope and hypotension reported, some of which required hospitalization; most cases occurred in patients taking 24 mcg twice daily and some occurred within hour after taking first dose or subsequent doses; patients should be aware of risk of syncope and hypotension during treatment and other adverse reactions, such as diarrhea or vomiting may increase this risk

Drug interaction overview

  • Diphenylheptane opioids (eg, methadone) have been shown in nonclinical studies to dose dependently reduce the activation of ClC-2 by lubiprostone in GI tract
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Pregnancy & Lactation

Pregnancy

Following oral administration, concentrations of lubiprostone in plasma are below the level of quantitation; however, one of the metabolites, M3, has measurable systemic concentrations

Data are not available to inform a drug associated risk of adverse developmental outcomes

Animal studies

  • Animal studies did not show an increase in structural malformations; however, a doses dependent increase in fetal loss was observed in pregnant guinea pigs at 0.2-6 times the MRHD

Lactation

No data are available on the presence in human milk of the refect on milk production

Animal studies

  • Neither lubiprostone nor its active metabolite (M3) were present in milk of lactating rats
  • When a drug is not present in animal milk, it is likely that the drug will not be present in human milk
  • If present, lubiprostone may cause diarrhea in the breastfed infant lubiprostone may cause diarrhea on effect of breastfed infants

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

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Pharmacology

Mechanism of Action

Locally acting chloride channel activator; increases intestinal fluid secretion and intestinal motility; acts locally at apical portion of intestine

Absorption

Low systemic absorption

Peak plasma time: 1 hr

Distribution

Protein binding: 94% in vitro (may be irrelevant because of low systemic absorption)

Metabolism

Probably metabolized in stomach and jejunum by carbonyl anhydrase

Elimination

Half-life: 0.9-1.4 hr

Excretion: Urine (60%), feces (trace amounts)

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Administration

Oral Administration

Administer with food and water

Swallow capsules whole and do not break apart or chew

Assess periodically the need for continuous therapy

Storage

25°C (77°F); excursions permitted to 15-30°C (59-86°F)

Protect from light and extreme temperatures

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Images

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Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.