Linzess 145mcg Capsules
WARNING: This drug is not for use in all ages of children. If your child is younger than 6 years old, talk with your child's doctor. @ COMMON USES: It is used to treat irritable bowel syndrome with constipation (IBS-C).It is used to treat constipation.
Drug Class
Guanylate Cyclase-C (GC-C) Agonist
Pharmacologic Class
Guanylate Cyclase-C (GC-C) Agonist
Pregnancy Category
Not available
FDA Approved
Aug 2012
DEA Schedule
Not Controlled
Overview
What is this medicine?
Linzess is a medication used to treat chronic constipation and irritable bowel syndrome with constipation. It works by increasing the amount of fluid in your intestines, which helps to soften your stool and make it easier to pass. It also helps reduce abdominal pain in IBS-C.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from 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 on an empty stomach, at least 30 minutes before a meal.
Take your medication at the same time every day to establish a routine.
Swallow the capsule whole; do not chew, break, or crush it.
If you have trouble swallowing the capsule, you may open it and mix the contents with applesauce or water, following the instructions provided or as directed in the package insert. If you are unsure, consult your doctor or pharmacist.
If you mix the medication with applesauce or water, swallow the mixture immediately; do not store it for later use. Also, do not chew the mixture.
If you have a feeding tube, you can use this medication as directed. After administering the medication, flush the feeding tube.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom.
Keep your medication in its original container, and do not remove the antimoisture cube or packet.
What to Do If You Miss a Dose
If you miss a dose, skip it and return to your regular schedule.
Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from 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 on an empty stomach, at least 30 minutes before a meal.
Take your medication at the same time every day to establish a routine.
Swallow the capsule whole; do not chew, break, or crush it.
If you have trouble swallowing the capsule, you may open it and mix the contents with applesauce or water, following the instructions provided or as directed in the package insert. If you are unsure, consult your doctor or pharmacist.
If you mix the medication with applesauce or water, swallow the mixture immediately; do not store it for later use. Also, do not chew the mixture.
If you have a feeding tube, you can use this medication as directed. After administering the medication, flush the feeding tube.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom.
Keep your medication in its original container, and do not remove the antimoisture cube or packet.
What to Do If You Miss a Dose
If you miss a dose, skip it and return to 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 Linzess on an empty stomach, at least 30 minutes before your first meal of the day.
- Swallow the capsule whole. Do not chew, break, or crush the capsule.
- If you miss a dose, skip the missed dose and take your next dose at the regular time. Do not take two doses at once.
- Stay well-hydrated, especially if you experience diarrhea.
- Maintain a balanced diet rich in fiber (unless advised otherwise by your doctor) and engage in regular physical activity to support bowel regularity.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
145 mcg orally once daily (for Chronic Idiopathic Constipation - CIC)
Dose Range:
145 - 290 mg
Condition-Specific Dosing:
Chronic Idiopathic Constipation (CIC):
145 mcg orally once daily
Irritable Bowel Syndrome with Constipation (IBS-C):
290 mcg orally once daily
Pediatric Dosing
Neonatal:
Contraindicated
Infant:
Contraindicated
Child:
Contraindicated in patients less than 6 years of age. Not recommended in patients 6 years to less than 18 years of age.
Adolescent:
Not recommended
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
No dose adjustment needed
Dialysis:
No dose adjustment needed; minimal systemic absorption
Hepatic Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
No dose adjustment needed
Pharmacology
Mechanism of Action
Linaclotide is a guanylate cyclase-C (GC-C) agonist. It binds to GC-C receptors on the luminal surface of intestinal epithelial cells. This binding activates GC-C, leading to an increase in intracellular and extracellular cyclic guanosine monophosphate (cGMP). Increased intracellular cGMP stimulates chloride and bicarbonate secretion into the intestinal lumen, primarily through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, which increases intestinal fluid and accelerates transit. Increased extracellular cGMP is thought to decrease visceral pain by reducing the activity of pain-sensing nerves.
Pharmacokinetics
Absorption:
Bioavailability:
Negligible (<0.1%)
Tmax:
Not applicable (minimal systemic absorption)
FoodEffect:
Taking with food can increase stool frequency and looseness. Should be taken at least 30 minutes before the first meal of the day.
Distribution:
Vd:
Not applicable (minimal systemic absorption)
ProteinBinding:
High (>92%) for the small amount that might be absorbed
CnssPenetration:
Minimal
Elimination:
HalfLife:
Not applicable (minimal systemic absorption)
Clearance:
Not applicable (minimal systemic absorption)
ExcretionRoute:
Fecal
Unchanged:
Not applicable (minimal systemic absorption)
Pharmacodynamics
OnsetOfAction:
Within 24 hours (for bowel movement)
PeakEffect:
Not precisely defined for systemic effects due to minimal absorption; clinical effect (bowel movements) seen within days to weeks.
DurationOfAction:
Approximately 24 hours (once daily dosing)
Safety & Warnings
BLACK BOX WARNING
Risk of Serious Dehydration in Pediatric Patients: LINZESS is contraindicated in patients less than 6 years of age. The safety and effectiveness of LINZESS in patients less than 18 years of age have not been established. In nonclinical studies, deaths occurred in young juvenile mice due to dehydration secondary to diarrhea. Avoid use of LINZESS in patients 6 years to less than 18 years of age.
Side Effects
Serious Side Effects: Seek Medical Attention Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. 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
Black, tarry, or bloody stools
Swelling of the abdomen
Bloating
Severe diarrhea that requires hospitalization
Signs of dehydration, including:
+ Severe dizziness or fainting
+ Inability to pass urine or changes in urine output
+ Feeling extremely tired
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's 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 persist or bother you:
Stomach pain or diarrhea
Gas
* Symptoms of a common cold
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 for medical advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. 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
Black, tarry, or bloody stools
Swelling of the abdomen
Bloating
Severe diarrhea that requires hospitalization
Signs of dehydration, including:
+ Severe dizziness or fainting
+ Inability to pass urine or changes in urine output
+ Feeling extremely tired
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's 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 persist or bother you:
Stomach pain or diarrhea
Gas
* Symptoms of a common cold
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 for medical advice. 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 or persistent diarrhea (more than 7 days)
- Dizziness or lightheadedness
- Signs of dehydration (e.g., excessive thirst, dry mouth, decreased urination, dark urine)
- New or worsening severe abdominal pain
- Rectal bleeding
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 symptoms you experienced.
If you have a bowel blockage, as this may affect the use of this medication.
This is not an exhaustive list of potential interactions. Therefore, it is crucial to discuss all of your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. This will help ensure that it is safe to take this medication in conjunction with your other treatments. Never start, stop, or modify 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 symptoms you experienced.
If you have a bowel blockage, as this may affect the use of this medication.
This is not an exhaustive list of potential interactions. Therefore, it is crucial to discuss all of your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. This will help ensure that it is safe to take this medication in conjunction with your other treatments. Never start, stop, or modify 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 experience diarrhea while taking this drug, it is crucial to prevent dehydration by drinking plenty of fluids and monitoring your weight. If you notice any weight loss or concerns, discuss them with your doctor.
If a child, especially those under 2 years of age, accidentally ingests this medication, they may be at risk of severe side effects, including severe diarrhea and dehydration. In such cases, seek immediate medical attention.
Before taking this medication, inform your doctor if you are pregnant, planning to become pregnant, or are breast-feeding. Your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby to ensure informed decision-making.
If a child, especially those under 2 years of age, accidentally ingests this medication, they may be at risk of severe side effects, including severe diarrhea and dehydration. In such cases, seek immediate medical attention.
Before taking this medication, inform your doctor if you are pregnant, planning to become pregnant, or are breast-feeding. Your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby to ensure informed decision-making.
Overdose Information
Overdose Symptoms:
- Severe diarrhea
- Dehydration
- Electrolyte imbalances (e.g., low potassium)
What to Do:
Contact your doctor or poison control center immediately (Call 1-800-222-1222 in the US). Management is supportive, focusing on fluid and electrolyte replacement.
Drug Interactions
Monitoring
Baseline Monitoring
Diagnosis of CIC or IBS-C
Rationale: Confirm appropriate indication for therapy.
Timing: Prior to initiation
Baseline bowel habits and symptoms
Rationale: Establish a baseline for assessing treatment efficacy.
Timing: Prior to initiation
Routine Monitoring
Frequency and consistency of bowel movements
Frequency: Daily/Weekly
Target: Improved bowel habits (e.g., increased frequency, softer stools)
Action Threshold: Lack of improvement after several weeks, or worsening symptoms.
Occurrence and severity of diarrhea
Frequency: Daily
Target: Absence or mild, manageable diarrhea
Action Threshold: Severe or persistent diarrhea, leading to dehydration or electrolyte imbalance.
Abdominal pain and discomfort
Frequency: Daily/Weekly
Target: Reduction in pain/discomfort (for IBS-C)
Action Threshold: Worsening or new onset of severe abdominal pain.
Signs and symptoms of dehydration (e.g., dizziness, lightheadedness, decreased urination)
Frequency: As needed, especially with diarrhea
Target: Normal hydration status
Action Threshold: Presence of any signs of dehydration.
Symptom Monitoring
- Severe or persistent diarrhea
- Dizziness
- Lightheadedness
- Signs of dehydration (e.g., decreased urination, excessive thirst, dry mouth)
- Worsening abdominal pain
Special Patient Groups
Pregnancy
Linaclotide has minimal systemic absorption, and therefore, maternal use is not expected to result in fetal exposure to the drug. Based on animal data, linaclotide may cause adverse developmental outcomes, but the relevance to humans is low due to negligible systemic exposure. Use only if the potential benefit justifies the potential risk.
Trimester-Specific Risks:
First Trimester:
Low risk due to minimal systemic absorption.
Second Trimester:
Low risk due to minimal systemic absorption.
Third Trimester:
Low risk due to minimal systemic absorption.
Lactation
Linaclotide has minimal systemic absorption, and therefore, maternal use is not expected to result in exposure of the breastfed infant to the drug. No data are available on the presence of linaclotide in human milk, the effects on the breastfed infant, or the effects on milk production. Considered low risk.
Infant Risk:
Low risk (L3 - Moderately Safe, based on negligible systemic absorption)
Pediatric Use
Contraindicated in patients less than 6 years of age due to the risk of serious dehydration. Not recommended in patients 6 years to less than 18 years of age due to lack of established safety and effectiveness and the potential for serious dehydration.
Geriatric Use
No dose adjustment is necessary. However, elderly patients may be more susceptible to the effects of dehydration, so monitor carefully for diarrhea and signs of dehydration.
Clinical Information
Clinical Pearls
- Linzess is a locally acting drug with minimal systemic absorption, which contributes to its favorable safety profile regarding systemic drug interactions.
- The most common and dose-limiting side effect is diarrhea. Patients should be counseled on managing diarrhea and recognizing signs of dehydration.
- It is crucial to take Linzess on an empty stomach, at least 30 minutes before the first meal, as food can increase the risk of diarrhea.
- Linzess is contraindicated in children under 6 years due to the risk of serious dehydration, and generally not recommended for those under 18.
- Improvement in symptoms may take several weeks, especially for abdominal pain in IBS-C.
Alternative Therapies
- Plecanatide (Trulance) - another GC-C agonist
- Lubiprostone (Amitiza) - chloride channel activator
- Tegaserod (Zelnorm) - 5-HT4 agonist (for IBS-C in women <65 with no history of cardiovascular disease)
- Prucalopride (Motegrity) - 5-HT4 agonist (for CIC)
- Laxatives (e.g., polyethylene glycol, magnesium hydroxide, stimulant laxatives)
- Fiber supplements
- Dietary modifications (e.g., FODMAP diet for IBS-C)
Cost & Coverage
Average Cost:
Varies, typically $400-$600 per 30 capsules
Insurance Coverage:
Tier 2 or Tier 3 (Specialty/Non-Preferred Brand)
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. This medication is accompanied by a Medication Guide, which provides crucial information for patients. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, we encourage you to discuss them with your doctor, 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 reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.