Linzela

Take orally once daily on an empty stomach, at least 30 minutes before the first meal of the day. Swallow the capsule whole. Do not chew or crush. For patients who have difficulty swallowing, the capsule may be opened and the contents mixed with applesauce or water.

Linaclotide is a guanylate cyclase-C (GC-C) agonist. It binds to GC-C receptors on the luminal surface of intestinal epithelial cells, which leads to an increase in intracellular and extracellular cyclic guanosine monophosphate (cGMP). Increased intracellular cGMP stimulates the secretion of chloride and bicarbonate into the intestinal lumen, primarily through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. Increased extracellular cGMP is thought to contribute to a decrease in visceral pain by modulating pain-sensing neurons.

• Known or suspected mechanical gastrointestinal obstruction.
• Pediatric patients less than 6 years of age.

Store at room temperature (20°C to 25°C or 68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Keep in original container. Protect from moisture.

Overdose experience with linaclotide is limited. In clinical trials, single doses of up to 2890 mcg were administered to healthy subjects without serious adverse events. If overdose occurs, treatment should be symptomatic and supportive. Hydration and electrolyte balance should be monitored, especially in cases of severe diarrhea.

Pregnancy Category C. Limited data available on use in pregnant women. Should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether linaclotide or its active metabolite are excreted in human milk. Caution should be exercised when administered to a nursing woman due to minimal systemic exposure.