Linzess 290mcg 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 agonist
Pharmacologic Class
Chloride channel activator
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 fluid in your intestines and speeding up the movement of stool, which helps relieve constipation. It also helps reduce abdominal pain associated with IBS-C.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your medication and follow the instructions closely.
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 by your doctor or pharmacist.
If you mix the medication with applesauce or water, swallow the mixture immediately; do not store it for later use.
Do not chew the mixture.
If you have a feeding tube, you can use this medication as directed by your healthcare provider. After administering the medication through the feeding tube, flush the tube with water.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from 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 take your next dose at the usual time.
* Do not take two doses at the same time or take extra doses to make up for a missed dose.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your medication and follow the instructions closely.
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 by your doctor or pharmacist.
If you mix the medication with applesauce or water, swallow the mixture immediately; do not store it for later use.
Do not chew the mixture.
If you have a feeding tube, you can use this medication as directed by your healthcare provider. After administering the medication through the feeding tube, flush the tube with water.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from 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 take your next dose at the usual time.
* Do not take two doses at the same time or take extra doses to make up for a missed dose.
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 or crush it.
- If you have trouble swallowing, the capsule can be opened and the beads mixed with applesauce or water.
- Maintain adequate hydration, especially if experiencing diarrhea.
- Discuss dietary changes (e.g., fiber intake) with your healthcare provider.
- Regular physical activity may also help with constipation.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
290 mcg orally once daily
Dose Range:
72 - 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:
Not established (Contraindicated in patients less than 6 years of age)
Infant:
Not established (Contraindicated in patients less than 6 years of age)
Child:
Not established (Contraindicated in patients less than 6 years of age); Safety and efficacy not established in pediatric patients 6 to 17 years of age.
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary
Moderate:
No dosage adjustment necessary
Severe:
No dosage adjustment necessary
Dialysis:
No dosage adjustment necessary; Linaclotide is minimally absorbed systemically.
Hepatic Impairment:
Mild:
No dosage adjustment necessary
Moderate:
No dosage adjustment necessary
Severe:
No dosage adjustment necessary
Pharmacology
Mechanism of Action
Linaclotide is a guanylate cyclase-C (GC-C) agonist. It binds to the GC-C receptor on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Increased intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, primarily through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, which results in increased intestinal fluid and accelerated transit. Increased extracellular cGMP is thought to decrease visceral pain by reducing the activity of pain-sensing nerves.
Pharmacokinetics
Absorption:
Bioavailability:
Minimal systemic absorption (<0.1%)
Tmax:
Not applicable (minimal systemic absorption)
FoodEffect:
Administration with a high-fat breakfast resulted in softer stools and more frequent bowel movements compared to administration in a fasted state. It is recommended to take Linzess on an empty stomach at least 30 minutes before the first meal of the day.
Distribution:
Vd:
Not applicable (minimal systemic absorption)
ProteinBinding:
Not applicable (minimal systemic absorption)
CnssPenetration:
No
Elimination:
HalfLife:
Not applicable (minimal systemic absorption)
Clearance:
Not applicable (minimal systemic absorption)
ExcretionRoute:
Fecal
Unchanged:
Not applicable (minimal systemic absorption)
Pharmacodynamics
OnsetOfAction:
Within 1 week for increased bowel movement frequency; pain reduction may take longer.
PeakEffect:
Typically within 1-2 weeks for full therapeutic effect.
DurationOfAction:
Daily dosing required to maintain effect.
Safety & Warnings
BLACK BOX WARNING
Risk of Serious Dehydration in Pediatric Patients: LINZESS is contraindicated in patients less than 6 years of age. In nonclinical studies, linaclotide caused deaths due to dehydration in young juvenile mice. Avoid use of LINZESS in patients 6 years to less than 18 years of age.
Side Effects
Serious Side Effects: Seek Medical Help Right Away
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 attention immediately:
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 urinate 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:
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, 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 attention immediately:
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 urinate 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:
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, 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 or persistent diarrhea
- Dizziness or lightheadedness
- Excessive thirst
- Decreased urination
- 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 as a result of the allergy.
If you have a bowel blockage, as this may affect the use of this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication in conjunction with your other treatments and health issues.
Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor to ensure your safety.
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 as a result of the allergy.
If you have a bowel blockage, as this may affect the use of this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication in conjunction with your other treatments and health issues.
Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor to ensure your safety.
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 significant changes, consult your doctor promptly.
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 discuss the potential benefits and risks of this medication to both you and your baby, allowing you to make an informed decision.
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 discuss the potential benefits and risks of this medication to both you and your baby, allowing you to make an informed decision.
Overdose Information
Overdose Symptoms:
- Severe diarrhea
- Dehydration
What to Do:
Discontinue Linzess and initiate supportive therapy, including rehydration. Call 1-800-222-1222 (Poison Control) or seek immediate medical attention.
Drug Interactions
Monitoring
Routine Monitoring
Bowel movement frequency and consistency (Bristol Stool Scale)
Frequency: Regularly, especially during initial treatment
Target: Improved frequency and consistency, reduced straining
Action Threshold: Persistent severe diarrhea, signs of dehydration
Abdominal pain/discomfort
Frequency: Regularly
Target: Reduction in pain
Action Threshold: Worsening or new severe abdominal pain
Symptom Monitoring
- Diarrhea (especially severe or persistent)
- Abdominal pain or cramping
- Bloating
- Gas
- Signs of dehydration (dizziness, lightheadedness, excessive thirst, decreased urination)
Special Patient Groups
Pregnancy
Minimal systemic absorption suggests low risk of fetal exposure. Use only if clearly needed and potential benefits outweigh potential risks. Consult with healthcare provider.
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
Minimal systemic absorption makes infant exposure unlikely. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for Linzess and any potential adverse effects on the breastfed infant from Linzess or from the underlying maternal condition.
Infant Risk:
Low risk (L3 - no human data, but drug properties suggest low risk).
Pediatric Use
Contraindicated in patients less than 6 years of age due to risk of serious dehydration. Avoid use in patients 6 years to less than 18 years of age due to potential risk of serious dehydration. Safety and efficacy have not been established in pediatric patients.
Geriatric Use
No dosage adjustment is necessary. Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, no overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients. Due to the minimal systemic absorption, age-related differences in pharmacokinetics are not expected.
Clinical Information
Clinical Pearls
- Linzess should be taken on an empty stomach, at least 30 minutes before the first meal of the day, to optimize efficacy and minimize potential for adverse effects like diarrhea.
- The 290 mcg dose is typically for IBS-C, while 145 mcg is for CIC. Ensure correct dosing for the indication.
- Diarrhea is the most common adverse effect; patients should be advised on hydration and when to contact their healthcare provider.
- Due to the black box warning, Linzess is contraindicated in children under 6 years old and generally avoided in those under 18.
- If a dose is missed, patients should be advised to skip the missed dose and take the next dose at the regular time. Do not take two doses at once.
Alternative Therapies
- Lubiprostone (Amitiza) - chloride channel activator
- Plecanatide (Trulance) - guanylate cyclase-C agonist
- Prucalopride (Motegrity) - serotonin 5-HT4 receptor agonist
- Tegaserod (Zelnorm) - serotonin 5-HT4 receptor agonist (for IBS-C in women <65 without cardiovascular risk factors)
- Laxatives (e.g., polyethylene glycol, magnesium hydroxide, stimulant laxatives) for CIC
- Dietary fiber, osmotic laxatives for general constipation
Cost & Coverage
Average Cost:
$500 - $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 promptly. To ensure safe use, 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, consult 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 quantity, and the time it occurred.