Ebrotidine

Description

Ebrocit was launched in Spain as a gastroprotective agent. It was prepared from 4-bromobenzenesulfonamide in two steps. Ebrocit's activity arises from its ability to antagonize histamine H₂-receptors (the first of a new generation) showing 1.5-2.5 times higher affinity than Ranitidine and 2-fold greater affinity than cimetidine which correlates to an antisecretory potency of 1 times and 4-10 times respectively. Cytoand gastroprotection arises from increased gastric mucus production, enhanced physiochemical properties (decreased permeability of H⁺), and an increase in mucin glycosylation and sulfation. It acts on gastric mucosal EGF and PDGF receptor expression. Nitric oxide was also found to be involved. Ebrocit caused enhanced mucosal blood flow with anti H.pylori activity. It has diminished P450 binding which eliminates the possibility of mutagenic nitrosoamine formation.

Originator

Ferrer (Spain)

The Uses of Ebrotidine

Ebrotidine is a H2 receptor antagonist that has shown gastroprotective properties against gastric mucosal damange.

Definition

ChEBI: Ebrotidine is a sulfonamide.

brand name

Ebrocit

References

[1]. patel s s, wilde m i. ebrotidine. drugs, 1996, 51(6): 974-80; discussion 981.
[2]. romero a, gómez f, villamayor f, et al. study of the population of enterochromaffin-like cells in mouse gastric mucosa after long-term treatment with ebrotidine. toxicologic pathology, 1996, 24(2): 160-165.