Lubiprostone

Chronic Idiopathic Constipation

Lubiprostone® is indicated for the treatment of chronic idiopathic constipation in adults.

Opioid-induced Constipation

​Lubiprostone​ is indicated for the treatment of ​opioid​-induced constipation (OIC) in adults with chronic non-cancer pain.

​Limitations of Use:

Irritable Bowel Syndrome with Constipation

Lubiprostone is indicated for the treatment of irritable bowel syndrome with constipation (IBS-C) in women ≥ 18 years old.

Lubiprostone increases the secretion of fluid in your intestines to help make it easier to pass stools (bowel movements).

Lubiprostone is used to treat chronic constipation, or constipation caused by opioid (narcotic) pain medicine.

Lubiprostone may also be used to treat irritable bowel syndrome in women with constipation as the main symptom.

Lubiprostone is for use only in adults.

Lubiprostone may also be used for purposes not listed in this medication guide.

Take Lubiprostone orally with food and water. Swallow capsules whole and do not break apart or chew. Physicians and patients should periodically assess the need for continued therapy.

Chronic Idiopathic Constipation and Opioid-induced Constipation

The recommended dose is 24 mcg twice daily orally with food and water.

Dosage in patients with hepatic impairment

For patients with moderately impaired hepatic function (Child-Pugh Class B), the recommended starting dose is 16 mcg twice daily. For patients with severely impaired hepatic function (Child-Pugh Class C), the recommended starting dose is 8 mcg twice daily. If this dose is tolerated and an adequate response has not been obtained after an appropriate interval, doses can then be escalated to full dosing with appropriate monitoring of patient response.

Irritable Bowel Syndrome with Constipation

The recommended dose is 8 mcg twice daily orally with food and water.

Dosage in patients with h epatic impairment

For patients with severely impaired hepatic function (Child-Pugh Class C), the recommended starting dose is 8 mcg once daily. If this dose is tolerated and an adequate response has not been obtained after an appropriate interval, doses can then be escalated to full dosing with appropriate monitoring of patient response. Dosage adjustment is not required for patients with moderately impaired hepatic function (Child-Pugh Class B).

How supplied

Dosage Forms And Strengths

Lubiprostone is available as an oval, gelatin capsule containing 8 mcg or 24 mcg of Lubiprostone.

• 8 mcg capsules are pink and are printed with “SPI” on one side
• 24 mcg capsules are orange and are printed with “SPI” on one side

Storage And Handling

Lubiprostone is available as an oval, soft gelatin capsule containing 8 mcg or 24 mcg of Lubiprostone with “SPI” printed on one side. Lubiprostone is available as follows:

8 mcg pink capsule

Bottles of 60 (NDC 64764-080-60)

24 mcg orange capsule

Bottles of 60 (NDC 64764-240-60)

Bottles of 100 (NDC 64764-240-10)

Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F).

Protect from light and extreme temperatures.

Marketed by: Sucampo Pharma Americas, LLC Bethesda, MD 20814 and Takeda Pharmaceuticals America, Inc. Deerfield, IL 60015. Revised: April 2013

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What is the most important information I should know about Lubiprostone?

Lubiprostone is used to treat chronic constipation in adults. It is also used to treat irritable bowel syndrome in women with constipation as the main symptom.

Take Lubiprostone with food or milk.

Do not take Lubiprostone if you have severe diarrhea. Call your doctor for instructions.

A nursing baby could develop diarrhea if the mother takes Lubiprostone while breast-feeding. Tell your doctor if you are breast-feeding a baby, and talk with your doctor if the baby develops diarrhea.

You may have tightness in your chest or feel short of breath within 1 hour after taking Lubiprostone. This side effect should go away within 3 hours, but it may occur again when you take your next dose. Talk with your doctor if this side effect becomes bothersome.

Call your doctor at once if you have severe or ongoing nausea or diarrhea.

Use Lubiprostone as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Lubiprostone by mouth with food.
• Take Lubiprostone with a full glass (8 oz [240 mL]) of water.
• Swallow Lubiprostone whole. Do not break, crush, or chew before swallowing.
• If you miss a dose of Lubiprostone, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Lubiprostone.

Lubiprostone is used for the treatment of long-term constipation (chronic idiopathic constipation), opioid-induced constipation (OIC) in adults with chronic non-cancer pain and irritable bowel syndrome (IBS, a common disorder of the large intestine that causes abdominal pain, cramps, bloating, gas, diarrhea and constipation).

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What other drugs will affect Lubiprostone?

No in vivo drug–drug interaction studies have been performed with Lubiprostone.

Based upon the results of in vitro human microsome studies, there is low likelihood of pharmacokinetic drug–drug interactions. In vitro studies using human liver microsomes indicate that cytochrome P450 isoenzymes are not involved in the metabolism of Lubiprostone. Further in vitro studies indicate microsomal carbonyl reductase may be involved in the extensive biotransformation of Lubiprostone to the metabolite M3. Additionally, in vitro studies in human liver microsomes demonstrate that Lubiprostone does not inhibit cytochrome P450 isoforms 3A4, 2D6, 1A2, 2A6, 2B6, 2C9, 2C19, or 2E1, and in vitro studies of primary cultures of human hepatocytes show no induction of cytochrome P450 isoforms 1A2, 2B6, 2C9, and 3A4 by Lubiprostone. Based on the available information, no protein binding–mediated drug interactions of clinical significance are anticipated.

Interaction potential with diphenylheptane opioids (e.g. methadone): Non-clinical studies have shown opioids of the diphenylheptane chemical class (e.g., methadone) 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.

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What are the possible side effects of Lubiprostone?

The following adverse reactions are described below and elsewhere in labeling:

• Nausea
• Diarrhea
• Dyspnea

Clinical Studies Experience

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.

During clinical development of Lubiprostone for CIC, OIC, and IBS-C, 1234 patients were treated with Lubiprostone for 6 months and 524 patients were treated for 1 year (not mutually exclusive).

Chronic Idiopathic Constipation

Adverse reactions in dose-finding, efficacy, and long-term clinical studies: The data described below reflect exposure to Lubiprostone 24 mcg twice daily in 1113 patients with chronic idiopathic constipation over 3-or 4-week, 6-month, and 12-month treatment periods; and from 316 patients receiving placebo over short-term exposure ( ≤ 4 weeks). The placebo population (N = 316) had a mean age of 47.8 (range 21–81) years; was 87.3% female; 80.7% Caucasian, 10.1% African American, 7.3% Hispanic, 0.9% Asian; and 11.7% elderly ( ≥ 65 years of age). Of those patients treated with Lubiprostone 24 mcg twice daily (N=1113), the mean age was 50.3 (range 19-86) years; 86.9% were female; 86.1% Caucasian, 7.6% African American, 4.7% Hispanic, 1.0% Asian; and 16.7% elderly ( ≥ 65 years of age). Table 1 presents data for the adverse reactions that occurred in at least 1% of patients who received Lubiprostone 24 mcg twice daily and that occurred more frequently with study drug than placebo.

Table 1: Percent of Patients with Adverse Reactions (Chronic Idiopathic Constipation)

The most common adverse reactions (incidence > 4%) in IBS-C were nausea, diarrhea, and abdominal pain.

Nausea: Approximately 8% of patients who received Lubiprostone 8 mcg twice daily experienced nausea; 1% of patients had severe nausea and 1% of patients discontinued treatment due to nausea.

Diarrhea: Approximately 7% of patients who received Lubiprostone 8 mcg twice daily experienced diarrhea; < 1% of patients had severe diarrhea and < 1% of patients discontinued treatment due to diarrhea.

Less common adverse reactions: The following adverse reactions (assessed by investigator as probably related to treatment) occurred in less than 1% of patients receiving Lubiprostone 8 mcg twice daily in clinical studies, occurred in at least two patients, and occurred more frequently in patients receiving study drug than those receiving placebo: dyspepsia, loose stools, vomiting, fatigue, dry mouth, edema, increased alanine aminotransferase, increased aspartate aminotransferase, constipation, eructation, gastroesophageal reflux disease, dyspnea, erythema, gastritis, increased weight, palpitations, urinary tract infection, anorexia, anxiety, depression, fecal incontinence, fibromyalgia, hard feces, lethargy, rectal hemorrhage, pollakiuria.

Postmarketing Experience

The following additional adverse reactions have been identified during post-approval use of Lubiprostone. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Voluntary reports of adverse reactions occurring with the use of Lubiprostone include the following: syncope, ischemic colitis, hypersensitivity/allergic-type reactions (including rash, swelling, and throat tightness), malaise, tachycardia, muscle cramps or muscle spasms, and asthenia.

Lubiprostone is a medication used in the management of idiopathic chronic constipation. It is a bicyclic fatty acid (prostaglandin E1 derivative) which acts by specifically activating ClC-2 chloride channels on the apical aspect of gastrointestinal epithelial cells, producing a chloride-rich fluid secretion. These secretions soften the stool, increase motility, and promote spontaneous bowel movements (SBM).