常用抗菌药物在 mrsa hap的临床应用好文档.pptVIP

* * 同样是金葡菌引起的重症菌血症与心内膜炎，我们来分析一下替考拉宁的疗效。 从这张片子我们可以看到一个很有意思的现象，对于金葡菌菌血症，同样是使用推荐剂量6mg/kg，不同的研究者得出的结果完全不同，有的可以达到100%，有的却只有21%，疗效不够稳定，而使用30mg/kg/d的大剂量时，疗效可和稳可信相当。从中反映出一个问题，即什么剂量是替考拉宁的最佳治疗剂量？很难确定。 * * 这是替考拉宁治疗金葡菌心内膜炎的临床疗效，按推荐的剂量每天6mg/kg，临床疗效很不可靠，只有剂量高达30mg/kg/d时临床有效率达到76.2%，与万古霉素相当。这说明替考拉宁按推荐剂量治疗金葡菌血内膜炎时疗效不稳定。 * * 以上的分析表明，替考拉宁虽然比稳可信晚上市30年，临床使用也少，但对葡萄球菌已经产生耐药，而目前国内尚无对稳可信耐药的葡萄球菌；另外较高的蛋白结合率（90-97%) ,使感染部位无法达到有效的的药物浓度，导致对严重感染疗效不确切，需加大剂量；常规剂量临床疗效不理想（尤其在心内膜炎），而加大剂量往往导致副反应增加，因此其始终未被美国FDA批准 ；从安全性方面看，大量研究表明，稳可信与替考拉宁在引起皮疹，肾功能障碍等副反应方面亦无统计学差异。综上所述，稳可信始终是治疗MRSA/MRSE感染的一线用药，唯一被FDA批准治疗MRSA的糖肽类抗生素。 * Mechanism of Action of 利奈唑胺 Bacterial protein synthesis involves a series of reactions that are essential for the bacterial protein translation process. These reactions include initiation, elongation, and termination. 利奈唑胺 has a unique mechanism of action.1 It is the only antibiotic that targets the formation of the initiation complex Initiation requires formation of a ternary complex consisting of N-formylmethionyl-tRNA, mRNA, and the ribosome.1,2 利奈唑胺 binds to the 50S subunit of the ribosome on a site that has not been shown to interact with other classes of antibiotics.1 As a result, 利奈唑胺 prevents the formation of a functional 70S initiation complex, which is the essential component of the bacterial translation process1,2 To date, no clinical studies have been done to confirm a lack of cross-resistance; however, the unique mechanism of action supports the contention that cross-resistance between ZYVOX? (利奈唑胺 injection, tablets, and for oral suspension) and other antibiotic classes is unlikely2,3 References: 1. Shinabarger DL, Marotti KR, Murray RW, et al. Mechanism of action of oxazolidinones: effects of 利奈唑胺 and eperezolid on translation reactions. Antimicrob Agents Chemother. 1997;41:2132-2136. 2. Swaney SM, Aoki H, Ganoza MC, et al. The oxazolidinone 利奈唑胺 inhibits initiation of protein synthesis in bacteria. Antimicrob Agents Chemother. 1998;42:3251-3255. 3. French G. 利奈唑胺.