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Lubiprostone (Monograph)

Brand name: Amitiza
Drug class: Chloride Channel Activators

Medically reviewed by Drugs.com on May 10, 2024. Written by ASHP.

Introduction

Bicyclic fatty acid; selectively activates intestinal ClC-2 chloride channels and increases intestinal fluid secretion.

Uses for Lubiprostone

Chronic Idiopathic Constipation

Management of chronic idiopathic constipation in adults.

Irritable Bowel Syndrome with Constipation in Women

Treatment of irritable bowel syndrome (IBS) with constipation in women ≥18 years of age.

Lubiprostone Dosage and Administration

Administration

Oral Administration

Administer orally with food and water.

Dosage

Adults

Periodically assess need for continued therapy.

Chronic Idiopathic Constipation
Oral

24 mcg twice daily.

May reduce dosage to 24 mcg daily in patients experiencing severe nausea.

Irritable Bowel Syndrome with Constipation in Women
Oral

8 mcg twice daily.

Special Populations

No special population recommendations at this time.

Cautions for Lubiprostone

Contraindications

Warnings/Precautions

Warnings

GI Obstruction

Thoroughly evaluate patients with symptoms suggestive of mechanical GI obstruction to confirm absence of such obstruction prior to initiating lubiprostone therapy. (See Contraindications under Cautions.)

Fetal/Neonatal Morbidity and Mortality

Women of childbearing potential should have a negative pregnancy test prior to receiving lubiprostone and should use an effective method of contraception during therapy with the drug.

General Precautions

GI Effects

Dose-dependent nausea may occur. Symptoms may be reduced by coadministration with food and water.

Possible diarrhea (may be severe).

Do not prescribe lubiprostone to patients with severe diarrhea.

Respiratory Effects

Possible dyspnea (may result in discontinuance of the drug).

Onset of symptoms (e.g., sensation of chest tightness, difficulty in breathing) generally occurs within 30–60 minutes after taking the first dose. Symptoms usually resolve within a few hours; however, frequently recur with subsequent doses.

Specific Populations

Pregnancy

Category C. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Not known whether distributed into human milk. Discontinue nursing or the drug.

Pediatric Use

Safety and efficacy not established in pediatric patients <18 years of age.

Geriatric Use

Geriatric patients with chronic idiopathic constipation experienced a lower incidence (18 versus 29%) of associated nausea than the overall study population.

Experience in those ≥65 years of age with IBS with constipation was insufficient to determine whether they respond differently from younger adults.

Hepatic Impairment

Not studied in patients with hepatic impairment.

Renal Impairment

Not studied in patients with renal impairment.

Common Adverse Effects

Chronic idiopathic constipation: Nausea, diarrhea, headache, abdominal distention, abdominal pain, flatulence, vomiting, dizziness, edema, loose stools, abdominal discomfort (including abdominal tenderness, abdominal rigidity, GI discomfort), dyspepsia, chest discomfort/pain, dyspnea, fatigue.

IBS with constipation in women: Nausea, diarrhea, abdominal pain, abdominal distention.

Drug Interactions

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Does not inhibit CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 in vitro. Does not induce CYP1A2, CYP2B6, CYP2C9, or CYP3A4 in vitro. Pharmacokinetic interactions unlikely with drugs metabolized by these CYP isoenzymes.

Not metabolized by isoenzymes.

Highly Protein-bound Drugs

Pharmacokinetic interaction unlikely.

Lubiprostone Pharmacokinetics

Absorption

Bioavailability

Low systemic bioavailability following oral administration with peak plasma concentrations usually attained within 1.1 hours.

Food

High-fat meal may reduce peak plasma concentration but does not affect extent of absorption (AUC).

Distribution

Extent

Minimal distribution beyond GI tissues.

Lubiprostone crosses the placenta in animals; not known whether crosses the placenta in humans.

Not known whether distributed into human milk.

Plasma Protein Binding

Approximately 94%.

Elimination

Metabolism

Rapidly and extensively metabolized, probably in the stomach and jejunum, by processes mediated by carbonyl reductase. CYP isoenzymes not involved in metabolism of the drug.

Elimination Route

Excreted in the urine (about 60%) within 24 hours and in feces (about 30%) within 168 hours.

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).

Actions

Advice to Patients

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Lubiprostone

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

8 mcg

Amitiza

Sucampo

24 mcg

Amitiza

Sucampo

AHFS DI Essentials™. © Copyright 2024, Selected Revisions May 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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