Trulance is trade name.

A drug approved for the treatment of chronic idiopathic constipation (CIC) in adults.

An agonist of guanylate cyclase-C.

It increases intestinal transit and fluid through a buildup of cGMP.

Oral agent.

Rome III diagnostic criteria for chronic constipation requires that the patient meet stool frequency, stool consistency, incomplete evacuation, and straining requirements in addition to not being a likely candidate for irritable bowel syndrome.

The symptoms should also have been present for at least three of the last six months to establish the chronic nature of the condition before treatment with this drug is indicated.

Presently contraindicated in children and in persons who are suspected of having a mechanical gastrointestinal obstruction.

A 16 amino acid peptide with the amino acid sequence, that is nearly structurally identical to human uroguanylin, apart from the substitution of Asp3 with Glu3.

Optimal activity of Plecanatide occurs at pH 5, making it suitable for targeting cells within the proximal intestine, which has a pH of between 5 and 6.

Works as a laxative by drawing water in to the gastrointestinal tract thereby softening stool and encouraging its natural passage.

Activates guanylate cyclase-C on endothelial cells within the gastrointestinal tract.

The activation of guanylate cyclase-C catalyses the production of the second messenger guanosine 3’,5’-cyclic monophosphate (cGMP).

Guanosine 3′,5′-cyclic monophoshate leads to the protein kinase A (PKA) and protein kinase G II (PKGII)-mediated phosphorylation of the cystic fibrosis transmembrane conductance regulator (CFTR) protein.

Transmembrane conductance regulator (CFTR) protein is an anion channel and when activated secretes negatively charged ions, particularly chloride (Cl−) and bicarbonate (HCO3−) in to the GI tract lumen.

By disrupting the electrochemical gradient, it is partly rectified by the passive secretion of positively charged sodium ions in to the lumen and water follows by osmosis.

It acts on receptors present on the apical side of endothelial cells lining the gastrointestinal tract, and its effect occurs without ever entering circulation.

It is degraded by intestinal enzymes and so very little of the active drug enters systemic circulation.

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