Alosetron



Alosetron
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
Identifiers
CAS number 122852-42-0
ATC code A03AE01
PubChem 2099
DrugBank APRD00580
Chemical data
O 
Mol. mass 294.351 g/mol
Pharmacokinetic data
Bioavailability 50–60%
Protein binding 82%
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 GlaxoSmithKline under the trade name Lotronex.

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.

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Alosetron was withdrawn in 2000 following the association of alosetron with serious life-threatening gastrointestinal adverse effects.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

References

  1. ^ GlaxoSmithKline plc. Lotronex (U.S. Prescribing Information). Brentford: GlaxoSmithKline; 2002.

See also

  • Irritable bowel syndrome
v • d • e
Drugs for functional gastrointestinal disorders (Propantheline

papaverine and derivatives: Drotaverine - Moxaverine

acting on Tegaserod)

other: Clebopride
 
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