Linaclotide

What it is and how it works

Linaclotide is a minimally absorbed peptide that binds guanylate cyclase-C on the luminal surface of intestinal epithelium, increasing intracellular and extracellular cyclic GMP. This stimulates chloride and bicarbonate secretion into the lumen, increasing intestinal fluid and transit, and reduces visceral pain by decreasing activity of pain-sensing nerves.

Indications

Moderate to severe irritable bowel syndrome with constipation (IBS-C) in adults; in some countries also chronic idiopathic constipation.

Dosage and administration (summary)

IBS-C: 290 micrograms orally once daily, at least 30 minutes before a meal; lower doses (72–145 micrograms daily) are used for chronic idiopathic constipation where approved. Review if no improvement after 4 weeks.

Contraindications

Known or suspected mechanical gastrointestinal obstruction; hypersensitivity; not to be used in young children because of the risk of serious dehydration.

Warnings and precautions

Diarrhoea is the most common adverse effect and may be severe, leading to dehydration and electrolyte disturbance; caution in elderly patients and those at risk. Exclude organic disease before treatment; patients with inflammatory bowel disease were not studied.

Pregnancy

Avoid in pregnancy as a precaution; systemic exposure is negligible.

Storage and supply

Store below 30 °C in the original bottle with desiccant, tightly closed; use within the stated period after opening.

Source: reference summary prepared from the EU SmPC/EPAR, BNF and WHO Model Formulary. The approved product information in Iran governs.