Lubiprostone

Generic Name: lubiprostone

Chloride Channel Activator [EPC]Over-the-Counter (OTC)

Brand Names:

Lubiprostone

11 DESCRIPTION Lubiprostone is a chloride channel activator for oral use. The chemical name for lubiprostone is (–)-7-[(2 R ,4a R ,5 R ,7a R )-2-(1,1-difluoropentyl)-2-hydroxy-6-oxooctahydrocyclopenta[ b ]pyran-5-yl]heptanoic acid.

Overview

11 DESCRIPTION Lubiprostone is a chloride channel activator for oral use. The chemical name for lubiprostone is (–)-7-[(2 R ,4a R ,5 R ,7a R )-2-(1,1-difluoropentyl)-2-hydroxy-6-oxooctahydrocyclopenta[ b ]pyran-5-yl]heptanoic acid.

Uses

1 INDICATIONS AND USAGE Lubiprostone capsules are a chloride channel activator indicated for the treatment of: chronic idiopathic constipation (CIC) in adults. (1.1) opioid-induced constipation (OIC) in adult patients with chronic, non-cancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dosage escalation. (1.2) Limitations of Use: Effectiveness of lubiprostone capsules in the treatment of OIC in patients taking diphenylheptane opioids (e.g., methadone) has not been established. (1.2 , 7.1) irritable bowel syndrome with constipation (IBS-C) in women ≥18 years old.

Dosage

2 DOSAGE AND ADMINISTRATION Recommended Dosage (2.1) CIC and OIC: 24 mcg twice daily. IBS-C: 8 mcg twice daily. See full prescribing information for dosage adjustment by indication and degree of hepatic impairment. Administration Instructions (2.2) Swallow capsules whole and do not break apart or chew, Take capsules with food and water, Assess periodically the need for continuous therapy. 2.1 Recommended Dosage The recommended oral dosage of lubiprostone capsules by indication and adjustments for patients with moderate (Child Pugh Class B) and severe (Child Pugh Class C) hepatic impairment are shown in Table 1. Table 1.

Side Effects

6 ADVERSE REACTIONS The following adverse reactions are described below and elsewhere in labeling: Nausea [see Warnings and Precautions (5.1) ] Diarrhea [see Warnings and Precautions (5.2) ] Syncope and Hypotension [see Warnings and Precautions (5.3 ] Dyspnea [see Warnings and Precautions (5.4) ] Most common adverse reactions (>4%) are: CIC: nausea, diarrhea, headache, abdominal pain, abdominal distension, and flatulence. (6.1) OIC: nausea and diarrhea. (6.1) IBS-C: nausea, diarrhea, and abdominal pain. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Teva at 1-888-838-2872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Interactions

7 DRUG INTERACTIONS 7.1 Methadone Diphenylheptane opioids (e.g., methadone) have been shown in nonclinical studies to dose-dependently reduce the activation of ClC-2 by lubiprostone in the gastrointestinal tract. There is a possibility of a dose-dependent decrease in the efficacy of lubiprostone in patients using diphenylheptane opioids. No in vivo interaction studies have been conducted. The effectiveness of lubiprostone in the treatment of OIC in patients taking diphenylhepatane opioids (e.g., methadone) has not been established [see Indications and Usage (1.2) ] .

Warnings

5 WARNINGS AND PRECAUTIONS Nausea : Patients may experience nausea; concomitant administration of food may reduce this symptom. (2.2 , 5.1) Diarrhea : Avoid use in patients with severe diarrhea. Instruct patients to discontinue lubiprostone and contact their healthcare provider if severe diarrhea occurs during treatment. (5.2) Syncope and Hypotension : May occur after taking the first dose or with subsequent doses. Generally resolves prior to the next dose, but may recur with repeat dosing. Instruct patients to discontinue lubiprostone and contact their healthcare provider if symptoms occur. (5.3) Dyspnea : May occur within an hour of first dose. Generally resolves within 3 hours, but may recur with repeat dosing. Instruct patients to contact their healthcare provider if symptoms occur. 4 CONTRAINDICATIONS Lubiprostone is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction [see Warnings and Precautions (5.5) ]. Patients with known or suspected mechanical gastrointestinal obstruction. (4 , 5.5)

Pregnancy

8.1 Pregnancy Risk Summary Following oral administration, concentrations of lubiprostone in plasma are below the level of quantitation; however, one of the metabolites, M3, has measurable systemic concentrations [see Clinical Pharmacology (12.3) ] . Limited available data with lubiprostone use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes. Animal reproduction studies did not show an increase in structural malformations.

Storage

16 HOW SUPPLIED/STORAGE AND HANDLING Lubiprostone capsules are available as follows: 8 mcg – Oval, opaque pink soft gelatin capsule printed with A08 on the outer shell in black ink, in: Unit dose packages of 20 (5 x 4) NDC 60687-816-32 24 mcg – Oval, clear orange soft gelatin capsule printed with A04 on the outer shell in black ink, in: Unit dose packages of 20 (5 x 4) NDC 60687-827-32 Store at 20...

Frequently Asked Questions

What is Lubiprostone used for?

1 INDICATIONS AND USAGE Lubiprostone capsules are a chloride channel activator indicated for the treatment of: chronic idiopathic constipation (CIC) in adults. (1.1) opioid-induced constipation (OIC) in adult patients with chronic, non-cancer pain, including patients with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dosage escalation. (1.2) Limitations of Use: Effectiveness of lubiprostone capsules in the treatment of OIC in patients taking diphenylheptane opioids (e.g., methadone) has not been established. (1.2 , 7.1) irritable bowel syndrome with constipation (IBS-C) in women ≥18 years old.

What are the side effects of Lubiprostone?

6 ADVERSE REACTIONS The following adverse reactions are described below and elsewhere in labeling: Nausea [see Warnings and Precautions (5.1) ] Diarrhea [see Warnings and Precautions (5.2) ] Syncope and Hypotension [see Warnings and Precautions (5.3 ] Dyspnea [see Warnings and Precautions (5.4) ] Most common adverse reactions (>4%) are: CIC: nausea, diarrhea, headache, abdominal pain, abdominal distension, and flatulence. (6.1) OIC: nausea and diarrhea. (6.1) IBS-C: nausea, diarrhea, and abdominal pain. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Teva at 1-888-838-2872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Can I take Lubiprostone during pregnancy?

8.1 Pregnancy Risk Summary Following oral administration, concentrations of lubiprostone in plasma are below the level of quantitation; however, one of the metabolites, M3, has measurable systemic concentrations [see Clinical Pharmacology (12.3) ] . Limited available data with lubiprostone use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes. Animal reproduction studies did not show an increase in structural malformations.

What are the important warnings for Lubiprostone?

5 WARNINGS AND PRECAUTIONS Nausea : Patients may experience nausea; concomitant administration of food may reduce this symptom. (2.2 , 5.1) Diarrhea : Avoid use in patients with severe diarrhea. Instruct patients to discontinue lubiprostone and contact their healthcare provider if severe diarrhea occurs during treatment. (5.2) Syncope and Hypotension : May occur after taking the first dose or with subsequent doses. Generally resolves prior to the next dose, but may recur with repeat dosing. Instruct patients to discontinue lubiprostone and contact their healthcare provider if symptoms occur. (5.3) Dyspnea : May occur within an hour of first dose. Generally resolves within 3 hours, but may recur with repeat dosing. Instruct patients to contact their healthcare provider if symptoms occur. 4 CONTRAINDICATIONS Lubiprostone is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction [see Warnings and Precautions (5.5) ]. Patients with known or suspected mechanical gastrointestinal obstruction. (4 , 5.5)

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Medical Disclaimer

This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.