Wells C L, Arland L A, Simmons R L, Rotstein O D
J Antimicrob Chemother. 1985 Jun;15 Suppl C:199-206. doi: 10.1093/jac/15.suppl_c.199.
Bacteroides fragilis pure-culture abscesses and Bact. fragilis-Escherichia coli mixed-culture abscesses were initiated subcutaneously in mice and intraperitoneally in rats. Within 1 h after injection of Sch 34343, the drug was present in higher concentrations in the abscesses than in the blood of infected animals. After five days of Sch 34343 therapy with either 100 or 400 mg/kg administered five times a day to mice with subcutaneous abscesses, the numbers of Bact. fragilis in pus decreased approximately three log-fold, reflecting a killing of 99.99% of the viable Bact. fragilis, while the numbers of E. coli decreased approximately 0.5 log-fold, reflecting a killing of 50% of the viable E. coli. After five days of therapy with either 50 or 150 mg/kg administered five times a day to rats with intraperitoneal fibrin clot abscesses, the viable Bact. fragilis again decreased three log-fold; the viable E. coli decreased one log-fold in rats given the higher dosages of the drug. Sch 34343 is a promising agent for the treatment of anaerobic infections because it can penetrate into anaerobic abscesses and can kill large numbers of bacteria within abscesses.
在小鼠皮下和大鼠腹腔内引发了脆弱拟杆菌纯培养脓肿以及脆弱拟杆菌 - 大肠杆菌混合培养脓肿。注射Sch 34343后1小时内,感染动物脓肿中的药物浓度高于血液中的浓度。对于患有皮下脓肿的小鼠,每天5次给予100或400mg/kg的Sch 34343进行5天治疗后,脓液中脆弱拟杆菌的数量减少了约三个对数级,这反映出99.99%的存活脆弱拟杆菌被杀死,而大肠杆菌的数量减少了约0.5个对数级,这反映出50%的存活大肠杆菌被杀死。对于患有腹腔纤维蛋白凝块脓肿的大鼠,每天5次给予50或150mg/kg的Sch 34343进行5天治疗后,存活的脆弱拟杆菌数量再次减少三个对数级;在给予较高剂量药物的大鼠中,存活的大肠杆菌数量减少了一个对数级。Sch 34343是一种有前景的治疗厌氧菌感染的药物,因为它可以渗透到厌氧脓肿中,并能杀死脓肿内的大量细菌。