Linaclotide

Linaclotide is a prescription medication used for the treatment of irritable bowel syndrome and chronic idiopathic constipation.

• Linaclotide is available under the following different brand names: Linzess
• Chronic idiopathic constipation (CIC) in adults
• Functional constipation (FC) in pediatric patients 6 to 17 years of  age

Adult dosage

Capsule

• 72mcg
• 145mcg
• 290mcg

Irritable Bowel Syndrome

Adult dosage

• 290 mcg orally every day 

Chronic Idiopathic Constipation 

Adult dosage

• 145 mcg orally every day
• 72 mcg orally every day may be used based on individual presentation

Functional constipation

Pediatric dosage

• Children aged below 2 years: Contraindicated
• Children aged below 6 years: Safety and efficacy not established
• Children aged 6 to 17 years of age: 72 mcg orally once daily

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

Common side effects of Linaclotide include:

• diarrhea,
• stomach pain,
• gas, and
• bloating or feeling full in the stomach 

Serious side effects of Linaclotide include:

• severe or ongoing diarrhea,
• diarrhea with dizziness,
• lightheadedness,
• increased thirst or urination,
• leg cramps,
• mood changes,
• confusion,
• feeling unsteady,
• irregular heartbeats,
• fluttering in the chest,
• muscle weakness,
• limp feeling,
• severe stomach pain, and
• black, bloody, or tarry stools

 Rare side effects of Linaclotide include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Linaclotide has no noted severe interactions with any other drugs.
• Linaclotide has no noted serious interactions with any other drugs.
• Linaclotide has no noted moderate interactions with any other drugs.
• Linaclotide has no noted minor interactions with any other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns.

Contraindications

• Patients aged below 2 years due to risk of serious dehydration
• Known or suspected mechanical gastrointestinal obstruction 

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Linaclotide?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Linaclotide?”

Cautions

• Pediatric risk
  • Contraindicated in patients below 2 years of age
  • In neonatal mice, fluid secretion increased because of GC-C agonism resulting in mortality within the first 24 hr due to dehydration
  • There was no age-dependent trend in GC-C intestinal expression in a clinical study of children 2 to 19 years of age; there are insufficient data available on GC-C intestinal expression in children aged below 2 years to assess the risk of developing diarrhea and its potentially serious consequences in these patients
  • Safety and efficacy in patients aged below 18 years not established
• Diarrhea
  • Diarrhea was the most common adverse reaction in clinical trials
  • Diarrhea has also been reported in pediatric patients 6 to 17 years of age with FC treated with  linaclotide. In a double-blind placebo-controlled trial, diarrhea was the most common adverse  reaction and was reported in 4% of pediatric patients 6 to 17 years of age treated with  linaclotide 72 mcg once daily. Severe diarrhea was reported in one linaclotide-treated patient 
  • In postmarketing reports, severe diarrhea associated with dizziness, syncope, hypotension, and electrolyte abnormalities (hypokalemia and hyponatremia) requiring hospitalization or IV fluid administration has been reported
  • If severe diarrhea occurs, suspend dosing, and rehydrate 

Pregnancy and Lactation

• Linaclotide and its active metabolite are negligibly absorbed systemically following oral administration, and maternal use is not expected to result in fetal exposure
• Insufficient data available data on use in pregnant women to inform any drug-associated risk for major birth defects and miscarriage
• Lactation
  • Linaclotide and its active metabolite were not detected in the milk of lactating women; in adults, concentrations of linaclotide and its active metabolite were below the limit of quantitation in plasma following multiple doses of the drug
  • Maternal use of the drug is not expected to result in exposure to the drug or its active metabolite in breastfed infants; there is no information on effects on milk production; consider developmental and health benefits of breastfeeding along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition
  • No lactation studies in animals have been conducted
  • Unknown whether negligible systemic absorption of linaclotide by adults will result in a clinically relevant exposure to breastfed infants