Linaclotide
Linaclotide
Linzess
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Summary
Common uses
IBS with predominant constipation0, Chronic idiopathic constipation0, Functional constipation in pediatric patients 6-17 years0
Pharmacy
Starting dose
145 mcg PO once daily for chronic idiopathic constipation; 290 mcg daily for IBS-C; pediatric 72 mcg daily
Preparations
72, 145, 290 mcg capsules
US FDA Max
290 mcg/d
Pharmacology
Routes
Oral
Onset
Bowel movement within 1 week; abdominal pain improvement over weeks
Duration
24 hours
Half-life
Not meaningfully described (negligible systemic absorption — the drug acts locally and is degraded in the GI tract)[1]
Bioavailability
Negligible systemic absorption[1]
Pregnancy
Limited data; minimal systemic absorption likely renders fetal risk low.[citation needed]
Legal status
Purported mechanism
Linaclotide is a 14-amino-acid peptide agonist of guanylate cyclase-C (GC-C) on the luminal surface of intestinal epithelial cells; receptor activation raises intracellular and extracellular cGMP, which opens the CFTR chloride channel and increases chloride/bicarbonate secretion (and consequently water) into the gut lumen, accelerating transit.0 Extracellular cGMP separately activates submucosal sensory afferents in a way that reduces visceral pain perception, distinguishing linaclotide from purely osmotic laxatives in IBS-C. Diarrhea is the dose-limiting effect[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Linzess (linaclotide), AbbVie/Ironwood, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202811s011lbl.pdf