
Linaclotide, marketed as Linzess, is a guanylate cyclase-C (GC-C) agonist used to treat irritable bowel syndrome with constipation (IBS-C) in adults, chronic idiopathic constipation (CIC) in adults, and functional constipation (FC) in paediatric patients aged 6-17. It is a 14-amino acid peptide with negligible systemic absorption, acting locally on the luminal surface of intestinal epithelial cells.
Linzess is not a laxative; instead, it works directly in the intestines by calming pain-sensing nerves and accelerating bowel movements. It is a prokinetic agent, promoting intestinal motility and used for severe constipation-predominant symptoms associated with IBS-C or CIC.
Characteristics | Values |
---|---|
Drug Class | IBS Agents, Gastrointestinals, Guanylate Cyclase-C Agonists |
Generic Name | Linaclotide Capsules |
Medical Use | Treatment of irritable bowel syndrome with constipation (IBS-C) in adults, chronic idiopathic constipation (CIC) in adults, and functional constipation (FC) in pediatric patients 6 to 17 years of age |
Side Effects | Viral gastroenteritis, serious eye symptoms, serious heart symptoms, severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, tremors |
Dosage | 290 mcg orally once daily for adults with IBS-C; 145 mcg orally once daily or 72 mcg orally once daily for adults with CIC; 72 mcg orally once daily for pediatric patients with FC |
Drug Interactions | N/A |
Pregnancy and Breastfeeding | Maternal use is not expected to result in fetal exposure to the drug; linaclotide and its active metabolite were not detected in breast milk |
Description | A guanylate cyclase-C (G-CC) agonist; a 14-amino acid peptide with the chemical name: L-cysteinyl-L-cysteinyl-L-glutamyl-L-tyrosyl-Lcysteinyl-L-cysteinyl-L-asparaginyl-L-prolyl-L-alanyl-L-cysteinyl-L-threonyl-glycyl-L-cysteinyl-Ltyrosine, cyclic (1-6), (2-10), (5-13)-tris (disulfide) |
Contraindications | Patients less than 2 years of age, patients with known or suspected mechanical gastrointestinal obstruction |
Mechanism of Action | Binds to GC-C and acts locally on the luminal surface of the intestinal epithelium, increasing cyclic guanosine monophosphate (cGMP), anion secretion, fluid secretion, and intestinal transit |
Administration | On an empty stomach, at least 30 minutes prior to a meal, at approximately the same time each day |
Missed Dose | Skip the missed dose and take the next dose at the regular time |
Storage | Store at 25°C (77°F); excursions permitted between 15°C and 30°C (59°F and 86°F) |
What You'll Learn
- Linzess is a guanylate cyclase-C agonist
- Linzess treats irritable bowel syndrome with constipation (IBS-C) in adults
- Linzess treats chronic idiopathic constipation (CIC) in adults
- Linzess treats functional constipation (FC) in children and adolescents aged 6-17
- Linzess is contraindicated in patients under 2 years old
Linzess is a guanylate cyclase-C agonist
Linaclotide, or Linzess, is a 14-amino-acid synthetic peptide structurally related to the endogenous guanylin peptide family. It is a guanylate cyclase-C (GCC) receptor agonist that binds to and activates the GCC receptor on the luminal surface of the intestinal epithelium. This, in turn, stimulates the production of cyclic guanosine monophosphate (cGMP), which increases intestinal motility and fluid secretion, ultimately reducing abdominal pain.
Linaclotide is an orally available 14-residue long peptide that features three intramolecular disulfide bonds between C1–C6, C2–C10, and C5–C13. These structures improve resistance to proteolytic degradation in the gastrointestinal tract. It is prescribed to treat irritable bowel syndrome with constipation and chronic idiopathic constipation in adults.
Linzess is not a laxative and acts directly in the intestines. It works by calming pain-sensing nerves and accelerating bowel movements. It is manufactured by Ironwood Pharmaceuticals and received FDA approval in 2012 for IBS and 2017 for CIC.
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Linzess treats irritable bowel syndrome with constipation (IBS-C) in adults
Linzess (linaclotide) is a prescription medication used to treat irritable bowel syndrome with constipation (IBS-C) in adults. It is a once-daily pill that is not a laxative but a drug that works differently from other medications. It acts locally in the intestine and is thought to work in two ways: by calming pain-sensing nerves and accelerating bowel movements.
IBS-C is a chronic medical condition characterised by constipation with abdominal symptoms that return again and again. Patients typically experience constipation with abdominal pain, lumpy or hard stools, fewer than three bowel movements a week, and incomplete bowel movements. The cause of IBS-C is unknown, but researchers believe several factors may contribute to the condition. These include the colon absorbing too much fluid from stools, the muscles in the colon moving too slowly, and nerves in the intestines being extra sensitive.
Linzess is a prescription treatment that helps patients have more frequent and complete bowel movements and relieves belly pain and overall abdominal symptoms associated with IBS-C. It is a proven treatment for multiple symptoms of IBS-C and is the #1 prescribed IBS-C/CIC branded treatment. When taken daily, constipation relief is typically felt within about a week, with symptoms improving over 12 weeks. If patients stop taking Linzess, their symptoms usually return within a week.
Linzess can cause serious side effects, including diarrhea, which is the most common side effect and can sometimes be severe. Other common side effects include gas, stomach-area pain, and swelling, or a feeling of fullness or pressure in the abdomen.
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Linzess treats chronic idiopathic constipation (CIC) in adults
Chronic Idiopathic Constipation (CIC) is a common gastrointestinal disorder characterised by a reduction in bowel movements and defecatory difficulties. CIC is a complex condition with symptoms including straining at defecation, hard or lumpy stools, a sensation of incomplete evacuation, and a sensation of blockage or anorectal obstruction. CIC is defined as primary constipation when no definite cause can be demonstrated, and it is usually subdivided into normal-transit constipation, slow-transit constipation, and evacuation disorders.
Linzess (generic name: linaclotide) is a prescription medication used to treat CIC in adults and children and adolescents aged 6-17. It is a guanylate cyclase-C agonist that stimulates the GC-C receptor to increase fluid secretion, softening stools and stimulating bowel movements. It is not a laxative and is taken as a once-daily pill.
Linzess is used to treat adults with CIC, helping them to have more frequent and complete bowel movements and relieving abdominal symptoms such as pain, discomfort, and bloating. It is taken in the morning on an empty stomach, at least 30 minutes before the first meal of the day. It is important to note that Linzess should not be given to children under 2 years of age, as it may cause severe diarrhea and dehydration.
Linzess has been shown to be effective in treating CIC in adults through various clinical trials. One randomised, double-blind, placebo-controlled, multicentre phase 2 study showed that Linzess increased the overall weekly rate of spontaneous bowel movements and decreased constipation-related abdominal symptoms. Three identical phase 3 randomised trials demonstrated that Linzess significantly improved bowel and abdominal symptoms in patients with moderate-to-severe abdominal bloating.
The most common side effect of Linzess is mild to moderate diarrhea, and other common side effects include gas, stomach pain, and a feeling of fullness or pressure in the abdomen. It is important to consult a doctor if you experience unusual or severe stomach pain or bright red, bloody, or black stools.
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Linzess treats functional constipation (FC) in children and adolescents aged 6-17
Linzess (generic name: linaclotide) is a prescription medicine used to treat functional constipation (FC) in children and adolescents aged 6-17. It is the first and only FDA-approved prescription treatment for this condition.
FC is a type of constipation with no known cause. Constipation is a condition in which you may have fewer bowel movements than expected, or you may have stools that are hard, dry, lumpy, or painful or difficult to pass.
Linzess is in a different category of drugs than over-the-counter laxatives. It is not a laxative. It belongs to the class of drugs called guanylate cyclase-C agonists. The guanylate cyclase type-C (GC-C) receptor is located on the luminal surface of the intestine. Linaclotide works to treat FC by stimulating the GC-C receptor to increase fluid secretion, which softens stools and stimulates bowel movements.
The recommended dosage of Linzess for children and adolescents aged 6-17 with FC is 72 mcg orally once daily. It should be taken in the morning on an empty stomach, at least 30 minutes before the first meal. It should be taken at about the same time every day. If your child has trouble swallowing capsules, you can open the capsule and sprinkle the beads onto applesauce or into 1 oz. of water.
The efficacy of Linzess for the treatment of FC in children and adolescents aged 6-17 was established in a 12-week double-blind, placebo-controlled, randomized, multicenter clinical trial. Patients who received Linzess experienced a greater improvement in the average number of spontaneous bowel movements (SBMs) per week than patients who received a placebo.
The most common adverse reaction reported in this age group is diarrhea. Linzess contains a boxed warning that the medication should not be given to children under 2 years of age, as it can cause severe diarrhea and fatal dehydration in this age group. It should also not be taken by patients with a bowel blockage.
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Linzess is contraindicated in patients under 2 years old
Linzess (generic name: linaclotide) is a prescription drug used to treat adults with Irritable Bowel Syndrome with Constipation (IBS-C) and Chronic Idiopathic Constipation (CIC). It is also used to treat Functional Constipation (FC) in paediatric patients aged 6 to 17.
There is insufficient data available on GC-C intestinal expression in children under 2 years old to assess the risk of developing diarrhoea and its potentially serious consequences in these patients.
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Frequently asked questions
Linzess is a prescription drug used to treat irritable bowel syndrome with constipation (IBS-C) in adults, chronic idiopathic constipation (CIC) in adults, and functional constipation (FC) in paediatric patients aged 6 to 17 years.
Linzess is a guanylate cyclase-C (GC-C) agonist. It increases intestinal fluid secretion and intestinal motility, accelerating bowel movements and calming pain-sensing nerves.
The most common side effect of Linzess is diarrhoea. Other possible side effects include viral gastroenteritis, defecation urgency, and fecal incontinence.
The recommended dosage of Linzess for adults with IBS-C is 290 mcg orally once daily. For adults with CIC, the dosage is 145 mcg orally once daily, or 72 mcg orally once daily based on individual presentation or tolerability. For paediatric patients aged 6 to 17 years with FC, the dosage is 72 mcg orally once daily.