Gales Ana C, Jones Ronald N, Andrade Soraya S, Pereira Andrea S, Sader Hélio S
Department of Medicine, Division of Infectious Diseases, University of São Paulo, Rua Leandro Dupret 188, São Paulo, Brazil.
Braz J Infect Dis. 2005 Oct;9(5):348-56. doi: 10.1590/s1413-86702005000500001. Epub 2006 Jan 6.
The in vitro activity of tigecycline (former GAR-936), a new semisynthetic tetracycline, was evaluated in comparison with tetracycline and other antimicrobial agents.
A total of 1,326 contemporary clinical isolates collected from the Latin American region were collected in 2000-2002 period and tested with microdilution broth according to the CLSI guidelines. The bacterial pathogens evaluated included Staphylococcus aureus (505), Streptococcus pneumoniae (269), coagulase-negative staphylococci (CoNS; 227), Haemophilus influenzae (129), Enterococcus spp. (80), Moraxella catarrhalis (54), beta-haemolytic streptococci (28), viridans group streptococci (26), and Neisseria meningitidis (8)
Tigecycline demonstrated excellent activity against all Gram-positive cocci, with 90% of penicillin-resistant S. pneumoniae strains being inhibited at 0.12 microg/mL, while the same isolates had an MIC90 of > 16 microg/mL for tetracycline. All Enterococcus spp. were inhibited at 0.25 microg/mL of tigecycline. Tigecycline (MIC50, 0.25 microg/mL) was eight-fold more potent than minocycline (MIC50, 2 microg/mL) against oxacillin-resistant S. aureus (ORSA); all ORSA were inhibited at < 2 microg/mL of tigecycline. Tigecycline demonstrated excellent activity (MIC50, 0.5 microg/mL) against CoNS with reduced susceptibility to teicoplanin (MIC, 16 microg/mL). Tigecycline also showed high potency against respiratory pathogens such as M. catarrhalis (MIC50, 0.12 microg/mL) and H. influenzae (MIC50, 0.5 microg/mL). No tigecycline resistant isolates were detected when the proposed susceptible breakpoints (< 4 microg/mL) was applied.
This results indicate that tigecycline has potent in vitro activity against clinically important pathogenic bacteria, including Gram-positive isolates resistant to both tetracycline and minocycline.
评价了新型半合成四环素替加环素(原GAR-936)与四环素及其他抗菌药物相比的体外活性。
2000 - 2002年期间从拉丁美洲地区收集了总共1326株当代临床分离株,并根据CLSI指南用微量稀释肉汤进行检测。评估的细菌病原体包括金黄色葡萄球菌(505株)、肺炎链球菌(269株)、凝固酶阴性葡萄球菌(CoNS;227株)、流感嗜血杆菌(129株)、肠球菌属(80株)、卡他莫拉菌(54株)、β溶血性链球菌(28株)、草绿色链球菌(26株)和脑膜炎奈瑟菌(8株)。
替加环素对所有革兰氏阳性球菌均表现出优异的活性,90%的耐青霉素肺炎链球菌菌株在0.12μg/mL时被抑制,而相同分离株对四环素的MIC90>16μg/mL。所有肠球菌属在替加环素浓度为0.25μg/mL时被抑制。替加环素(MIC50,0.25μg/mL)对耐氧西林金黄色葡萄球菌(ORSA)的活性比米诺环素(MIC50,2μg/mL)高8倍;所有ORSA在替加环素浓度<2μg/mL时被抑制。替加环素对凝固酶阴性葡萄球菌表现出优异的活性(MIC50,0.5μg/mL),这些菌株对替考拉宁的敏感性降低(MIC,16μg/mL)。替加环素对呼吸道病原体如卡他莫拉菌(MIC50,0.12μg/mL)和流感嗜血杆菌(MIC50,0.5μg/mL)也显示出高效力。当应用建议的敏感折点(<4μg/mL)时,未检测到替加环素耐药分离株。
这些结果表明替加环素对临床上重要的病原菌具有强大的体外活性,包括对四环素和米诺环素均耐药的革兰氏阳性分离株。