Alosetron is a 5-HT₃ antagonist used for the management of severe diarrhoea-predominant irritable bowel syndrome (IBS) in women only. It was withdrawn from the market in 2000 owing to the occurrence of serious life-threatening gastrointestinal adverse effects, but was reintroduced in 2002 with availability and use restricted. It is currently marketed by GlaxoSmithKline under the trade name Lotronex.

Mode of action

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Alosetron, while being a 5-HT₃ antagonist like ondansetron, is not an antiemetic. Alosetron has an antagonist action on the 5-HT₃ receptors of the enteric nervous system of the gastrointestinal tract.

Serious adverse effects

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Alosetron was withdrawn in 2000 following the association of alosetron with serious life-threatening gastrointestinal adverse effects.

The cumulative incidence of ischaemic colitis was 2 in 1000, while serious complications arising from constipation (obstruction, perforation, impaction, toxic megacolon, secondary colonic ischaemia, death) was 1 in 1000.GlaxoSmithKline plc. Lotronex (U.S. Prescribing Information). Brentford: GlaxoSmithKline; 2002.

References

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See also

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• Irritable bowel syndrome

5-HT3 antagonists

Alosétron