Linaclotide (commonly sold as Linzess) is a prescription medication used to treat irritable bowel syndrome with constipation (IBS-C), chronic idiopathic constipation (CIC), and functional constipation.
Indicated in adults for the treatment of both irritable bowel syndrome with constipation and chronic idiopathic constipation.
A peptide agonist of guanylate cyclase 2C that is for use in treating abdominal pain in patients with irritable bowel syndrome (IBS) accompanied by constipation.
A peptide consisting of 14 amino acids.
Oral agent
Trade name Linzess
May be efficacious for the treatment of gastroparesis, ulcerative colitis, chronic intestinal pseudo-obstruction (CIPO), and colon inertia.
In a study of 800 patients over 12 weeks given linaclotide or a placebo in a randomized double-blind trial: 34% of those receiving linaclotide experienced relief of pain and constipation, compared to 21% of patients who had taken the placebo, 50% of those saw a significant reduction in pain, versus 37% with the placebo.
Diarrhea, the most commonly reported side effect (Ironwood et al).
Acts locally in the intestine to increase cGMP.
Decreases pain sensing nerve activity in the bowel, and increases fluid secretions and transit.
Administered as an oral capsule once daily, and taken on an empty stomach 30 minutes before the first meal of the day.
Contraindicated in pediatric patients.
Contraindicated in patients with known or suspected mechanical gastrointestinal obstruction.
Associated with diarrhea, abdominal pain and flatulence.
Binds to and activates the guanylin cyclase C receptor on the luminal surface of the intestinal epithelium.
Activation of the guanylate cyclase C generates cyclic guanosine monophosphate (cGMP) intracellularly and extracellularly.
Within intestinal epithelial cells increased cGMP triggers a signal transduction cascade activating the cystic fibrosis transmembrane conductance regulator.
This activitity causes chloride and bicarbonate secretion into the intestinal lumen and accelerates intestinal transit.
Significantly reduces bowel and abdominal symptoms in patients with chronic constipation.
It works locally in the intestines to increase fluid secretion and speed up movement.
Uses and Indications
Treat IBS-C in adults and older children. Manage chronic idiopathic constipation in adults. Relieve functional constipation in pediatric patients (ages 2 and older).
Acts as a guanylate cyclase-C (GC-C) agonist on the surface of intestinal cells.
Increases cyclic GMP levels, which triggers fluid and chloride secretion into the gut.
Softens the stool and speeds up transit time through the colon.
Dosage and Administration
Taken once daily by mouth.
Must be taken on an empty stomach, at least 30 minutes before your first meal.
Swallow whole, or open and mix with specific amounts of applesauce or water if directed.
Side Effects and Warnings
Diarrhea is the most common side effect and can occasionally be severe.
Severe dehydration risk applies to young children; never give linaclotide to children under 2 years old.
Contraindicated with known or suspected mechanical gastrointestinal obstruction.