Amitiza 8mcg Capsules
It is used to treat constipation.It is used to treat irritable bowel syndrome with constipation (IBS-C).
Drug Class
Laxative
Pharmacologic Class
Chloride channel activator
Pregnancy Category
Category C
FDA Approved
Jan 2006
DEA Schedule
Not Controlled
Overview
What is this medicine?
Lubiprostone is a medication used to treat certain types of constipation, including chronic constipation, constipation related to irritable bowel syndrome, and constipation caused by opioid pain medications. It works by increasing the amount of fluid in your intestines, which helps to soften your stool and make it easier to pass.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most out of your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication with food and a full glass of water.
Swallow the medication whole; do not chew, break, or crush it.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it at room temperature, protected from light.
Keep it in a dry place, away from the bathroom.
Store all medications in a safe location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist.
Check with your pharmacist for guidance on the best way to dispose of medications. You may also have access to drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, follow these steps:
Take the missed dose as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and resume your regular schedule.
Do not take two doses at the same time or take extra doses to make up for the missed one.
To ensure you get the most out of your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication with food and a full glass of water.
Swallow the medication whole; do not chew, break, or crush it.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it at room temperature, protected from light.
Keep it in a dry place, away from the bathroom.
Store all medications in a safe location, out of the reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist.
Check with your pharmacist for guidance on the best way to dispose of medications. You may also have access to drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, follow these steps:
Take the missed dose as soon as you remember.
If it's close to the time for your next dose, skip the missed dose and resume your regular schedule.
Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Take with food and water to reduce nausea.
- Stay well-hydrated throughout the day.
- Maintain a balanced diet rich in fiber (unless advised otherwise by your doctor).
- Engage in regular physical activity as tolerated.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
8 mcg orally twice daily
Dose Range:
8 - 24 mg
Condition-Specific Dosing:
Chronic Idiopathic Constipation (CIC):
24 mcg orally twice daily
Irritable Bowel Syndrome with Constipation (IBS-C):
8 mcg orally twice daily
Opioid-Induced Constipation (OIC):
24 mcg orally twice daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for IBS-C or OIC. For CIC, 6-17 years: 24 mcg orally twice daily (approved for CIC in this age group, but not for 8mcg strength specifically). Not recommended for children < 6 years.
Adolescent:
Not established for IBS-C or OIC. For CIC, 6-17 years: 24 mcg orally twice daily.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
No dose adjustment needed
Dialysis:
No specific recommendations; minimal systemic absorption suggests no significant impact.
Hepatic Impairment:
Mild:
No dose adjustment needed
Moderate:
For CIC/OIC: Consider 16 mcg once daily. For IBS-C: Consider 8 mcg once daily.
Severe:
For CIC/OIC: Consider 8 mcg once daily. For IBS-C: Consider 8 mcg once daily (or less frequently if tolerated).
Pharmacology
Mechanism of Action
Lubiprostone is a bicyclic fatty acid that acts locally in the gastrointestinal tract to activate ClC-2 chloride channels on the apical membrane of gastrointestinal epithelial cells. This activation leads to an increase in intestinal fluid secretion, which softens the stool and increases motility, thereby facilitating spontaneous bowel movements.
Pharmacokinetics
Absorption:
Bioavailability:
Very low (minimal systemic absorption)
Tmax:
Not applicable for systemic absorption; local effect onset is within 24 hours.
FoodEffect:
Food does not significantly affect systemic exposure, but taking with food may reduce nausea.
Distribution:
Vd:
Not applicable (minimal systemic absorption)
ProteinBinding:
Not applicable (minimal systemic absorption)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 0.9-1.4 hours (for active metabolite M-3, parent drug not quantifiable systemically)
Clearance:
Rapid
ExcretionRoute:
Primarily via feces (60% as metabolites), with a small amount in urine (10% as metabolites).
Unchanged:
Less than 1% (not quantifiable systemically)
Pharmacodynamics
OnsetOfAction:
Within 24 hours for first spontaneous bowel movement (SBM)
PeakEffect:
Not clearly defined due to local action; continued effect with regular dosing.
DurationOfAction:
Maintained with twice-daily dosing.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Shortness of breath
Low blood pressure, which can lead to hospitalization. You are more likely to experience low blood pressure if you have diarrhea or vomiting. If you feel extremely dizzy or like you might pass out, contact your doctor immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people do not experience any side effects or only have mild ones, it is essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they bother you or do not go away:
Headache
Stomach pain or diarrhea
Gas
Bloating
Upset stomach
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Shortness of breath
Low blood pressure, which can lead to hospitalization. You are more likely to experience low blood pressure if you have diarrhea or vomiting. If you feel extremely dizzy or like you might pass out, contact your doctor immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people do not experience any side effects or only have mild ones, it is essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they bother you or do not go away:
Headache
Stomach pain or diarrhea
Gas
Bloating
Upset stomach
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe diarrhea (contact your doctor immediately)
- Severe abdominal pain or cramping
- Fainting or feeling lightheaded (syncope)
- Difficulty breathing or chest tightness (rare, transient)
- Swelling of hands, ankles, or feet
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Bowel blockage
+ Diarrhea
This list is not exhaustive, and it is crucial to discuss all your health problems with your doctor.
Additionally, provide your doctor and pharmacist with a comprehensive list of all the medications you are taking, including:
Prescription medications
Over-the-counter (OTC) medications
Natural products
Vitamins
It is vital to verify that it is safe to take this medication with all your other medications and health conditions. Never start, stop, or change the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Bowel blockage
+ Diarrhea
This list is not exhaustive, and it is crucial to discuss all your health problems with your doctor.
Additionally, provide your doctor and pharmacist with a comprehensive list of all the medications you are taking, including:
Prescription medications
Over-the-counter (OTC) medications
Natural products
Vitamins
It is vital to verify that it is safe to take this medication with all your other medications and health conditions. Never start, stop, or change the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you are pregnant, planning to become pregnant, or are breast-feeding, notify your doctor promptly. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
Overdose Information
Overdose Symptoms:
- Severe diarrhea
- Severe nausea
- Vomiting
- Abdominal pain
What to Do:
There is no specific antidote. Treatment is symptomatic and supportive. Contact your poison control center or emergency services immediately. Call 1-800-222-1222 for Poison Control.
Drug Interactions
Moderate Interactions
- Opioid antagonists (e.g., methylnaltrexone, naloxegol, naldemedine): May reduce the efficacy of lubiprostone, especially in OIC. Monitor for reduced effect.
Monitoring
Baseline Monitoring
Diagnosis of underlying condition (CIC, IBS-C, OIC)
Rationale: To ensure appropriate indication for treatment.
Timing: Prior to initiation
Routine Monitoring
Bowel movement frequency and consistency
Frequency: Daily/Weekly
Target: Improved bowel habits, reduced straining
Action Threshold: Lack of improvement or worsening symptoms after several weeks of therapy.
Adverse effects (e.g., nausea, diarrhea, abdominal pain)
Frequency: Regularly, especially during initial therapy
Target: Tolerable side effect profile
Action Threshold: Severe or persistent nausea, diarrhea, or abdominal pain requiring dose reduction or discontinuation.
Symptom Monitoring
- Nausea (especially if taken without food)
- Diarrhea (can be severe)
- Abdominal pain/distension
- Headache
- Flatulence
- Dyspnea (rare, transient, usually resolves within hours)
Special Patient Groups
Pregnancy
Lubiprostone is Pregnancy Category C. Animal studies have shown adverse effects on fetal development at doses higher than human therapeutic doses. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for developmental toxicity observed in animal studies at high doses.
Second Trimester:
Potential for developmental toxicity observed in animal studies at high doses.
Third Trimester:
Potential for developmental toxicity observed in animal studies at high doses.
Lactation
Minimal systemic absorption of lubiprostone and its active metabolite suggests that transfer into breast milk is likely to be low. However, caution should be exercised when administered to a nursing mother. Consider the benefits of breastfeeding versus the potential risks.
Infant Risk:
Low risk due to minimal systemic absorption.
Pediatric Use
Not approved for IBS-C or OIC in pediatric patients. Approved for Chronic Idiopathic Constipation (CIC) in children 6-17 years of age at 24 mcg BID. Safety and efficacy not established in children younger than 6 years for any indication.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger patients. However, elderly patients may be more susceptible to adverse reactions like diarrhea and dehydration. Monitor hydration status and electrolyte balance.
Clinical Information
Clinical Pearls
- Always take lubiprostone with food and water to minimize nausea, which is a common side effect.
- Patients should be advised that the onset of action for a spontaneous bowel movement is typically within 24 hours, but consistent relief may take longer.
- Diarrhea is a dose-dependent side effect; if severe, consider dose reduction or temporary discontinuation.
- Lubiprostone works locally in the gut with minimal systemic absorption, leading to a low potential for systemic drug interactions.
- Transient dyspnea has been reported, usually occurring within an hour of the first dose and resolving within a few hours. Patients should be informed of this possibility.
Alternative Therapies
- Linaclotide (Linzess)
- Plecanatide (Trulance)
- Tenapanor (Ibsrela)
- Osmotic laxatives (e.g., polyethylene glycol, lactulose)
- Stimulant laxatives (e.g., bisacodyl, senna) - generally for short-term use
- Fiber supplements (e.g., psyllium, methylcellulose)
- Stool softeners (e.g., docusate)
Cost & Coverage
Average Cost:
Varies widely, typically $300-$500+ per 30 capsules
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Brand), Tier 1 (Generic) depending on insurance plan
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it is a good idea to check with your pharmacist. If you have any questions or concerns about this medication, do not hesitate to discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide detailed information about the overdose, including the medication taken, the amount, and the time it occurred.