Products
Tegaserod (Zelmac, Zelnorm, tablets) was approved in many countries in 2001. After showing an increased risk of ischemic cardiovascular events such as heart attack and stroke, Novartis withdrew the drug from the market in 2007 on orders from Swissmedic.
Structure and properties
Tegaserod (C16H23N5O, Mr = 301.4 g/mol) exists as tegaserodmaleate, a white crystalline powder that is sparingly soluble in water. It is an indole and -pentylcarbazimidamide derivative derived from serotonin.
Effects
Tegaserod (ATC A03AE02) has prokinetic properties. It stimulates peristalsis and intestinal secretion of water and chloride. Its effects are based on binding to 5-HT4 serotonin receptors and neurotransmitter release.
Indications
For the treatment of irritable bowel syndrome (IBS-C, constipation type) in women and for the treatment of chronic idiopathic constipation.