Davey P G, Jacobus N V, Tally F P
Department of Clinical Pharmacology, Ninewells Hospital and Medical School, Dundee, Scotland.
J Antimicrob Chemother. 1987 Nov;20(5):705-12. doi: 10.1093/jac/20.5.705.
Spiramycin, a macrolide antibiotic, has inferior in-vitro activity to erythromycin, but superior tissue penetration. Recent publications have suggested that the in-vivo activity of spiramycin should be re-assessed. The efficacy of clindamycin, erythromycin and spiramycin was compared against Staphylococcus aureus infections in the rat croton oil pouch model. The concentration of spiramycin in the pouch fluid was lower than the concentration of clindamycin or erythromycin after single or multiple intraperitoneal injections. In contrast, the concentration of spiramycin in the pouch wall (73.3 +/- 14.5 micrograms/g) was markedly higher than that of erythromycin (less than 7.5 micrograms/g). Multiple doses of spiramycin had no significant effect upon bacterial growth in the pouch, whereas clindamycin and erythromycin had a significant bactericidal effect. The results suggest that spiramycin is bound to tissues, diffuses poorly into tissue fluid and may therefore be ineffective against infections in large collections of tissue fluid.
螺旋霉素是一种大环内酯类抗生素,其体外活性不如红霉素,但组织穿透力更强。近期的出版物表明,螺旋霉素的体内活性应重新评估。在大鼠巴豆油袋模型中,比较了克林霉素、红霉素和螺旋霉素对金黄色葡萄球菌感染的疗效。单次或多次腹腔注射后,袋液中螺旋霉素的浓度低于克林霉素或红霉素的浓度。相比之下,袋壁中螺旋霉素的浓度(73.3±14.5微克/克)明显高于红霉素(低于7.5微克/克)。多次给药的螺旋霉素对袋内细菌生长无显著影响,而克林霉素和红霉素有显著的杀菌作用。结果表明,螺旋霉素与组织结合,向组织液中的扩散较差,因此可能对大量组织液中的感染无效。