Lubiprostone (lubiprostone)
Irritable Bowel Syndrome Agents Oral Capsule
Last reviewed · Source: First Databank (FDB) drug data
Overview
Lubiprostone, a bicyclic fatty acid that selectively activates intestinal ClC-2 chloride channels, increases intestinal fluid secretion.
Lubiprostone, a bicyclic fatty acid that selectively activates intestinal ClC-2 chloride channels, increases intestinal chloride and fluid secretion without affecting serum sodium and potassium concentrations. Lubiprostone activates the ClC-2 chloride channel which is located on the apical (luminal) membrane of the human intestinal epithelium, independent of the actions of protein kinase A.
Decreased intestinal motility is a possible cause of chronic idiopathic constipation. Lubiprostone increases intestinal motility by increasing intestinal fluid secretion, consequently increasing the passage of stool and alleviating symptoms of chronic idiopathic constipation. Activation of ClC-2 by lubiprostone also may stimulate recovery of mucosal barrier function by restoring tight junction protein complexes in the intestine.
The drug also delays gastric emptying, which may cause nausea (the most common adverse effect associated with lubiprostone therapy).
Lubiprostone has low systemic bioavailability following oral administration, and plasma concentrations of the drug are below the limit of quantitation (10 pg/mL).
Lubiprostone is rapidly and extensively metabolized, probably in the stomach and jejunum, by processes mediated by carbonyl reductase; hepatic cytochrome P-450 enzymes are not involved in the metabolism of the drug. About 60% of an orally administered dose is excreted in the urine within 24 hours, while about 30% of such dose is excreted in feces within 168 hours.
USES: This medication is used to treat certain types of constipation (chronic idiopathic constipation, irritable bowel syndrome with constipation). Chronic idiopathic constipation has an unknown cause and is not due to diet, other diseases, or drugs. Lubiprostone is also used to treat constipation caused by opioid medications in people with ongoing pain due to medical conditions other than cancer.
This medication may improve symptoms such as bloating and abdominal discomfort, improve stool texture, lessen the need to strain, and decrease the feeling of not completely relieving oneself. Lubiprostone belongs to a class of drugs known as chloride channel activators. It works by increasing the amount of fluid within your intestines, making the passage of stool easier.
Generic name: lubiprostone
Pronunciation: (loo-bi-PROST-own)
Drug class: Irritable Bowel Syndrome Agents
Therapeutic class: Gastrointestinal Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Lubiprostone
Indications
The following indications are listed for Lubiprostone:
- Chronic Idiopathic Constipation
- Constipation Predominant Irritable Bowel Syndrome
- Opioid-Induced Constipation
Also known as: Constipation Predominant Ibs.
Dosing
Clinicians and patients (with chronic idiopathic constipation or irritable bowel syndrome with constipation) should periodically assess the need for continued therapy.
No dosing information is available for this tab.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Lubiprostone 8 Mcg Capsule | Maintenance | Take 1 capsule (8 mcg) by oral route 2 times per day with food and water. |
| Lubiprostone 24 Mcg Capsule | Maintenance | Take 1 capsule (24 mcg) by oral route 2 times per day with food and water. |
| Drug label | Dosing type | Instructions |
|---|---|---|
| Lubiprostone 8 Mcg Capsule | Maintenance | Take 1 capsule (8 mcg) by oral route 2 times per day with food and water. |
| Lubiprostone 24 Mcg Capsule | Maintenance | Take 1 capsule (24 mcg) by oral route 2 times per day with food and water. |
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Laxatives/Trofinetide
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Trofinetide commonly causes diarrhea of mild to moderate severity. Laxatives may increase the incidence or severity of diarrhea.(1)
CLINICAL EFFECTS: Concurrent use of laxatives with trofinetide may increase the risk of severe diarrhea.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Patients should stop laxatives before starting trofinetide. If diarrhea occurs, consider anti-diarrheal treatment and monitor hydration status. If severe diarrhea or dehydration occurs, interrupt, reduce dose, or discontinue trofinetide.(1)
DISCUSSION: In clinical trials, 85% of patients on trofinetide developed diarrhea. Concurrent use of laxatives may increase this risk.(1)
Laxatives; Stool Softeners/Tenapanor
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Tenapanor commonly causes diarrhea of mild to moderate severity. Laxatives and stool softeners may increase the incidence or severity of diarrhea.(1)
CLINICAL EFFECTS: Concurrent use of laxatives or stool softeners with tenapanor may increase the risk of severe diarrhea.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: The US manufacturer of tenapanor states that patients should be instructed to avoid stool softeners and laxatives with tenapanor. If severe diarrhea occurs, tenapanor should be discontinued.(1)
DISCUSSION: In clinical trials, 43-53% of CKD patients on dialysis treated with tenapanor developed diarrhea. Diarrhea usually occurred soon after treatment initiation and was severe in 5% of patients.(1)
There are no moderate interactions for this drug.
Contraindications
Known hypersensitivity to lubiprostone or any ingredient in the formulation. Known or suspected mechanical GI obstruction.
- Gastrointestinal obstruction
- Severe diarrhea
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in about 2% or more of patients receiving lubiprostone for the management of chronic idiopathic constipation include nausea, diarrhea, headache, abdominal distention, abdominal pain, flatulence, vomiting, dizziness, edema, loose stools, abdominal discomfort (abdominal tenderness, abdominal rigidity, GI discomfort), dyspepsia, chest discomfort/pain, dyspnea, and fatigue.
Adverse effects reported in about 3% or more of women receiving lubiprostone for the treatment of IBS with constipation include nausea, diarrhea, abdominal pain, and abdominal distention.
Less Frequent
- Dyspnea
Rare or Very Rare
- Chest tightness
- Hypokalemia
- Hypotension
- Ischemic colitis
- Rectal bleeding
- Throat constriction
- Unconsciousness
More Frequent
- Abdominal distension
- Acute abdominal pain
- Diarrhea
- Dizziness
- Flatulence
- Headache disorder
- Nausea
Less Frequent
- Arthralgia
- Cough
- Depression
- Dyspepsia
- Fatigue
- Gastroesophageal reflux disease
- Influenza
- Loose stools
- Urinary tract infection
- Vomiting
Rare or Very Rare
- Anorexia
- Chest pain
- Constipation
- Cramps
- Dysgeusia
- Edema
- Eructation
- Fecal incontinence
- General weakness
- Hyperhidrosis
- Lethargy
- Malaise
- Muscle spasm
- Myalgia
- Palpitations
- Skin rash
- Symptoms of anxiety
- Syncope
- Tachycardia
- Tremor
- Weight gain
- Xerostomia
Precautions
No enhanced messaging available.
Safety and efficacy not established in patients younger than 18 years of age.
Category C. (See Users Guide.) (Also see Fetal/Neonatal Morbidity and Mortality under Warnings/Precautions: Warnings, in Cautions.)
Not known whether lubiprostone is distributed into human milk; discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Efficacy of lubiprostone in geriatric patients (65 years of age and older) with chronic idiopathic constipation was consistent with efficacy of the drug in the overall study population. Geriatric patients experienced a lower incidence (18 versus 29%) of associated nausea than the overall study population.
Experience in those 65 years of age or older with irritable bowel syndrome (IBS) with constipation was insufficient to determine whether they respond differently from younger adults. Safety profile of lubiprostone in these patients was consistent with the safety profile in the overall study population.
ICD codes
| Code | Type | Description |
|---|---|---|
| Chronic idiopathic constipation | ||
| K59.04 | ICD10CM | Chronic idiopathic constipation |
| Constipation predominant irritable bowel syndrome | ||
| K58.1 | ICD10CM | Irritable bowel syndrome with constipation |
| Opioid-induced constipation | ||
| K59.09 | ICD10CM | Other constipation |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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