Mechanism and Side effects of Linaclotide

Linaclotide, (sold under the brand name Linzess in the US and Mexico, and as Constella elsewhere)is a drug used to treat irritable bowel syndrome with constipation and chronic constipation with no known cause.It has a black box warning about the risk of serious dehydration in children in the US; the most common adverse effects in others are gastrointestinal.

Uses

Linaclotide is used to treat certain types of bowel problems (irritable bowel syndrome with constipation, chronic idiopathic constipation). It works by increasing fluid in your intestines and helping speed up movement of food through the gut. 

Mechanism of action

Linaclotide is structurally related to human uroguanylin and guanylin, and is metabolized into smaller peptides and naturally occurring amino acids. Linaclotide acts on GC-C receptors throughout the upper and lower GI tract, across the entire pH range.

How to take linaclotide

Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.

Take linaclotide in the morning on an empty stomach, at least 30 minutes before your first meal.

Swallow the capsule whole and do not crush, chew, break, or open it.

If you cannot swallow a capsule whole, open it and sprinkle the medicine into a spoonful of applesauce or bottled water. Swallow the mixture right away without chewing. Do not save it for later use.

Even if you have taken this medicine with applesauce, wait at least 30 minutes before eating a full meal.

If needed, medicine from the linaclotide capsule may be given through a nasogastric (NG) or gastronomy tube.

Carefully follow instructions for mixing medicine from the capsule with applesauce or water, or giving the medicine through a feeding tube. Ask your doctor or pharmacist if you have any questions.

It may take up to 2 weeks before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve.

Store at room temperature away from moisture and heat. Keep the tablets in their original container, along with the packet or canister of moisture-absorbing preservative.

Keep this medicine out of the reach of children. Linaclotide can be fatal to a child who accidentally swallows this medicine. Seek emergency medical attention if this happens.

Side effects

The US label has a black box warning to not use linaclotide in children less than 6 years old and to avoid in people from 6 to 18 years old, due to the risk of serious dehydration.

More than 10% of people taking linaclotide have diarrhea. Between 1% and 10% of people have decreased appetite, dehydration, low potassium, dizziness when standing up too quickly, nausea, vomiting, urgent need to defecate, fecal incontinence, and bleeding in their colon, rectum, and anus