Marchese A, Debbia E A, Tonoli E, Gualco L, Schito A M
Institute of Microbiology, University of Genoa, Italy.
J Chemother. 2002 Dec;14(6):554-61. doi: 10.1179/joc.2002.14.6.554.
Thiamphenicol is a derivative of chloramphenicol characterized by a spectrum comparable to that of the parent compound against multiresistant pathogens but showing satisfactory tolerability. The in vitro activity of thiamphenicol and of 11 comparative drugs against 397 recently isolated antibiotic-resistant and/or invasive pneumococci and 52 multiply-resistant MRSA including 2 VISA strains was determined. Bactericidal activity against Haemophilus influenzae and the post-antibiotic effect on Streptococcus pneumoniae, H. influenzae, Staphylococcus aureus and Escherichia coli were also assessed. Against invasive pneumococci, thiamphenicol and chloramphenicol were the most potent non-beta-lactam molecules together with vancomycin and rifampin. Against high-level penicillin-resistant strains phenicol activities were superior to those of cefotaxime, ceftriaxone and imipenem. Against MRSA thiamphenicol and chloramphenicol were second only to the glycopetides and also inhibited the VISA strains. Thiamphenicol showed a significant PAE (0.33 to 2.9h) on all pathogens studied and a powerful bactericidal effect against beta-lactamase-positive and -negative H. influenzae. These results indicate a good in vitro activity of thiamphenicol against difficult-to-treat multiply resistant pathogens.
甲砜霉素是氯霉素的衍生物,其抗菌谱与母体化合物相当,对多重耐药病原体有效,且耐受性良好。测定了甲砜霉素和11种对照药物对397株近期分离出的耐抗生素和/或侵袭性肺炎球菌以及52株多重耐药的耐甲氧西林金黄色葡萄球菌(包括2株万古霉素中度敏感金黄色葡萄球菌菌株)的体外活性。还评估了对流感嗜血杆菌的杀菌活性以及对肺炎链球菌、流感嗜血杆菌、金黄色葡萄球菌和大肠杆菌的抗生素后效应。对于侵袭性肺炎球菌,甲砜霉素和氯霉素是与万古霉素和利福平一起最有效的非β-内酰胺类分子。对于高水平耐青霉素菌株,甲砜霉素的活性优于头孢噻肟、头孢曲松和亚胺培南。对于耐甲氧西林金黄色葡萄球菌,甲砜霉素和氯霉素仅次于糖肽类药物,并且也能抑制万古霉素中度敏感金黄色葡萄球菌菌株。甲砜霉素对所有研究的病原体均显示出显著的抗生素后效应(0.33至2.9小时),并且对β-内酰胺酶阳性和阴性流感嗜血杆菌具有强大的杀菌作用。这些结果表明甲砜霉素对难以治疗的多重耐药病原体具有良好的体外活性。