Activity of aerosol thiamphenicol glycinate acetylcysteinate in a mouse model of S. pyogenes pneumonia

Thiamphenicol glycinate acetylcysteinate (TGA, CAS 20192-91-0) is a water s oluble ester of thiamphenicol (TAP) that allows a rapid utilization by the systemic route but also a direct local action when used as aerosol. To asse ss the efficacy of aerosolized TCA in the treatment of experimental pneumon ia in mice, we compared its in vivo activity with that of thiamphenicol gly cinate hydrochloride (TG), erythromycin (ERT) and amoxicillin (AMX), the la st two compounds being more active in vitro than TAP. TGA, administered by aerosol route, showed better efficacy than the aerosolized TG, particularly as far as survival rate is concerned, and was significantly more potent th an ERT and similar to AMX either administered by oral route. No significant ly different therapeutic efficacy was observed when TGA was parenterally ad ministered. The rapid release, at the site of infection; of TAP and N-acetylcysteine an d the favourable pharmacokinetic properties of TGA accounted in large part for its high therapeutic efficacy against Streptococcus pyogenes pneumonia.