Alosetron
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Alosetron
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| Systematic (IUPAC) name | |
| 5-methyl-2-[(4-methyl-1H-imidazol-5-yl)methyl]- 3,4-dihydro-2H-pyrido[4,3-b]indol-1(5H)-one |
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| Identifiers | |
| CAS number | 122852-42-0 |
| ATC code | A03AE01 |
| PubChem | 2099 |
| DrugBank | APRD00580 |
| Chemical data | |
| Formula | C17H18N4O |
| Mol. weight | 294.351 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 50–60% |
| Protein binding | 82% |
| Metabolism | Hepatic (including CYP2C9, CYP3A4 and CYP1A2) |
| Half life | 1.5–1.7 hours |
| Excretion | Renal 73%, faecal 24% |
| Therapeutic considerations | |
| Pregnancy cat. |
B (U.S.) |
| Legal status |
℞-only (U.S.) |
| Routes | Oral |
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 It was withdrawn from the market in 2000 owing to the occurrence of serious life-threatening gastrointestinal adverse effects, but was reintroduced in 2002 with availability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.
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[edit] Mode of action
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.
[edit] Serious adverse effects
Alosetron was withdrawn in 2000 following the association of alosetron with serious life-threatening gastrointestinal adverse effects.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.[1]
[edit] References
- ^ GlaxoSmithKline plc. Lotronex (U.S. Prescribing Information). Brentford: GlaxoSmithKline; 2002.
