lubiprostone

Action and Spectrum

Actions and spectrum: 

lubiprostone is a medication used to treat certain gastrointestinal disorders. It acts as a type-2 chloride channel activator and increases intestinal fluid secretion, which helps in softening stool and promoting bowel movements. It is primarily used to treat chronic idiopathic constipation and irritable bowel syndrome with constipation.

It helps to relieve symptoms such as bloating, abdominal discomfort, and infrequent bowel movements. The drug’s action is focused on the gastrointestinal system, and it is not used for a broader spectrum of conditions. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

abdominal distension (3-6%) 

Vomiting (3%) 

Edema (1-3%) 

Dizziness (3%) 

Dyspnea (2%) 

Fatigue (2%) 

Abdominal pain (4-8%) 

Flatulence (4-6%) 

Loose stools (3%) 

Abdominal discomfort (1-3%) 

Chest discomfort/pain (2%) 

Dyspepsia (2%) 

Dry mouth (1%)  

>10% 

Diarrhea (7-12%) 

Nausea (8-29%) 

Headache (2-11%) 

Post marketing Reports 

Gastrointestinal: Ischemic colitis 

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

Cardiovascular: tachycardia, hypotension, or Syncope 

General: Asthenia 

Musculoskeletal: muscle spasms or Muscle cramps 

Black Box Warning

Black Box Warning: 

There were no black box warnings associated with lubiprostone. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Known hypersensitivity: lubiprostone should not be used in individuals with a known hypersensitivity or allergy to the drug or any of its components. 
• Bowel obstruction: lubiprostone is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction. It is not suitable for use in individuals with conditions that can cause a blockage in the digestive tract. 
• Severe diarrhoea: lubiprostone should not be used in patients with severe diarrhea. It is not recommended for those experiencing excessive loose stools.

Caution: 

• Gastrointestinal disorders: Patients with a history of gastrointestinal disorders, such as inflammatory bowel disease or diverticulitis, should use lubiprostone with caution. It may exacerbate certain conditions, and its use should be closely monitored in these individuals. 
• Nausea and vomiting: lubiprostone may cause nausea, vomiting, or dizziness in some patients. If these symptoms occur, medical attention should be sought, and the medication may need to be discontinued or adjusted. 
• Electrolyte imbalances: lubiprostone can alter electrolyte levels in the body, particularly chloride and bicarbonate levels. Patients with a history of electrolyte imbalances or those taking other medications that may affect electrolyte levels should use lubiprostone with caution. 
• Drug interactions: lubiprostone may interact with other medications, including certain antifungal medications and antibiotics. It is essential to inform the healthcare professional about all the medications, supplements, and herbal products being taken to avoid potential drug interactions. 
• Swallowing disorders: For patients with swallowing disorders or difficulty swallowing capsules, lubiprostone capsules should be avoided, as it may pose a choking hazard. 
• Pediatric use: The safety and efficacy of lubiprostone in children have not been established, and its use in pediatric patients should be approached with caution.

Comorbidities: 

• Gastrointestinal disorders: lubiprostone may be used cautiously in patients with a history of gastrointestinal disorders, such as inflammatory bowel disease, diverticulitis, or gastrointestinal obstruction. 
• Kidney or liver impairment: Patients with severe kidney or liver impairment may require dosage adjustments or close monitoring when using lubiprostone. 
• Cardiac disorders: lubiprostone has been associated with an increased incidence of chest pain in clinical trials. Therefore, it should be used with caution in patients with a history of cardiac disorders or those at risk for cardiovascular events. 
• History of swallowing disorders: Patients with a history of swallowing disorders or difficulty swallowing capsules should avoid lubiprostone capsules due to the risk of choking. 
• Electrolyte imbalances: lubiprostone may alter electrolyte levels, particularly chloride and bicarbonate. Patients with a history of electrolyte imbalances should be monitored closely during treatment. 
• Pregnancy and lactation: The use of lubiprostone during pregnancy and lactation should be carefully considered, and its potential benefits and risks should be discussed with a healthcare professional. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: C 

Lactation: Excreted into human milk: Unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

lubiprostone is a prostone, a synthetic prostaglandin E1 analog, that selectively activates specific chloride channels (ClC-2) in the gastrointestinal (GI) tract. 

• Intestinal Secretion: lubiprostone enhances chloride secretion into the lumen of the GI tract, leading to increased fluid secretion. This helps to soften the stool and improve bowel movement, making it beneficial for the treatment of constipation. 
• Intestinal Motility: lubiprostone also activates enteric nerves in the intestinal smooth muscle, which helps to enhance peristalsis, the coordinated muscular contractions that propel stool through the gut. This effect can aid in relieving constipation by promoting bowel movements.

Pharmacodynamics: 

• Increase in Intestinal Fluid Secretion: lubiprostone stimulates chloride secretion into the lumen of the GI tract, resulting in an increase in the secretion of fluid into the intestines. This increased fluid content in the intestines helps to soften the stool and facilitates its passage through the gut. 
• Enhanced Intestinal Motility: lubiprostone also activates enteric nerves in the intestinal smooth muscle, leading to increased intestinal motility. This enhancement of peristalsis (coordinated muscular contractions) helps propel the stool forward and promotes regular bowel movements. 
• Mucus Production: lubiprostone may increase mucus production in the GI tract, which can have a protective effect on the intestinal lining and potentially help with lubrication during bowel movements.

Pharmacokinetics: 

Absorption 

lubiprostone is taken orally as a capsule. After ingestion, it undergoes minimal absorption in the gastrointestinal (GI) tract due to its high molecular weight and poor water solubility. The drug primarily acts locally in the GI tract, where it stimulates chloride channels and enhances intestinal fluid secretion. 

Distribution 

lubiprostone does not extensively distribute throughout the body because of its limited absorption. As a result, its effects are mostly localized in the GI tract. The drug does not significantly bind to plasma proteins. 

Metabolism 

lubiprostone undergoes minimal metabolism in the body. It is primarily metabolized by fatty acid amide hydrolase in the gut wall to form its active metabolite, M3. This metabolite retains similar pharmacological effects as the parent compound and is responsible for most of lubiprostone’s activity. 

Elimination and excretion 

After metabolism, the metabolites of lubiprostone are eliminated primarily through the feces, with a lesser extent through urine. The drug and its metabolites are eliminated slowly, allowing for extended duration of action. 

Adminstartion

Administration: 

• Swallow the capsule whole: Do not crush, chew, or break the capsule, as it is designed to release the medication slowly in the gastrointestinal tract. 
• Take it with food: lubiprostone is usually taken with food to enhance its absorption and reduce the risk of gastrointestinal side effects. 
• Stay hydrated: Drink a glass of water with the medication to ensure proper swallowing and to prevent dehydration, especially if experiencing diarrhea as a side effect. 
• Follow the prescribed dosage: Adhere to the recommended dose and dosing schedule provided by your healthcare provider.  
• Take it regularly: For the medication to be effective, it is crucial to take lubiprostone consistently as prescribed. 
• If you miss a dose: If you forget to take a dose, take it as soon as you remember. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: lubiprostone 

Pronounced: (loo-bi-PROS-tone)  

Why do we use lubiprostone? 

lubiprostone is a medication used for various gastrointestinal conditions. Its main use is for the treatment of chronic idiopathic constipation (CIC) in adults, which refers to infrequent and difficult bowel movements without a known underlying cause. lubiprostone helps to increase the fluid secretion in the intestines, which facilitates the passage of stool and relieves constipation. 

Additionally, lubiprostone is also used to treat irritable bowel syndrome with constipation (IBS-C) in adult women who have not responded well to other treatments. IBS-C is a common digestive disorder characterized by bloating, abdominal pain, and bowel changes, including constipation.