BRODIMOPRIM CONCENTRATIONS IN BRONCHIAL-MUCOSA, BRONCHIAL-SECRETIONS AND MIDDLE-EAR EFFUSIONS

Brodimoprim, a structural analogue of trimethoprim, is a long acting b road spectrum antibacterial agent characterized by a good pharmacokine tic profile, allowing once daily (OD) administration, The aim of this study was to investigate the penetration of brodimoprim into bronchial mucose, bronchial secretion and middle ear effusion, in order to eval uate the efficacy of the antibiotic in respiratory tract infections. T he study was performed in patients affected by chronic bronchitis havi ng to undergo diagnostic bronchoscopy (n=26), in patients affected by exacerbation of chronic bronchitis with purulent or mucopurulent secre tions (n=10), and in patients affected by otitis media with eardrum pe rforation (n=28). Patients were orally treated with 400 mg of brodimop rim (single dose), Samples of serum, bronchial mucose, bronchial secre tion and middle ear effusion were collected in the separate series of patients above mentioned, at different times after drug administration . Brodimoprim determinations were performed by a microbiological metho d using Bacillus subtilis ATCC 6633 as test microorganism. Brodimoprim reached the highest concentration in serum 4 h after administration a nd was still detectable at 24th hour. In bronchial mucose and in bronc hial secretion the peaks were reached at 8th hour (9.7+/-5.3 mg/kg and 4.57+/-1 mg/l respectively) while in middle car effusion were reached at 4th hour (4.8+/-2.5 mg/l). The drug was still detectable at antiba cterial concentrations, both in infected fluids and in tissue samples, 24 hours after administration (4.3+/-1.8 mg/kg in bronchial mucosa; 3 .5+/-0.66 mg/l in bronchial secretions; 3+/-0.6 mg/l in middle ear eff usion). These data indicate that brodimoprim, administered OD is able to reach effective concentrations in respiratory tract tissues and flu ids.