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 soluble ester of thiamphenicol (TAP) that allows a rapid utilization by the systemic route but also a direct local action when used as aerosol. To assess the efficacy of aerosolized TGA in the treatment of experimental pneumonia in mice, we compared its in vivo activity with that of thiamphenicol glycinate hydrochloride (TG), erythromycin (ERT) and amoxicillin (AMX), the last 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 than ERT and similar to AMX either administered by oral route. No significantly different therapeutic efficacy was observed when TGA was parenterally administered. The rapid release, at the site of infection, of TAP and N-acetylcysteine and the favourable pharmacokinetic properties of TGA accounted in large part for its high therapeutic efficacy against Streptococcus pyogenes pneumonia.
Albini
E
E
Microbiology Laboratory, Zambon Group S.p.A, Bresso, Italy.
Arena
E
E
Belluco
G
G
Schioppacassi
G
G
Ungheri
D
D
D000111:Acetylcysteine / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D000336:Aerosols; D000658:Amoxicillin / Q000627:therapeutic use; D000818:Animals; D000900:Anti-Bacterial Agents / Q000627:therapeutic use; D004338:Drug Combinations; D004917:Erythromycin / Q000627:therapeutic use; D005260:Female; D008168:Lung / Q000378:metabolism; D051379:Mice; D008826:Microbial Sensitivity Tests; D010406:Penicillins / Q000627:therapeutic use; D018410:Pneumonia, Bacterial / Q000188:drug therapy* / Q000382:microbiology; D013290:Streptococcal Infections / Q000188:drug therapy* / Q000382:microbiology; D013297:Streptococcus pyogenes / Q000187:drug effects; D013839:Thiamphenicol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use
D000336:Aerosols; D000900:Anti-Bacterial Agents; D004338:Drug Combinations; D010406:Penicillins; D004917:Erythromycin; C028814:thiamphenicol glycinate acetylcysteinate; D000658:Amoxicillin; D013839:Thiamphenicol; D000111:Acetylcysteine