Brilacidin
Brilacidin 是一种称为多肽模拟物或防御素模拟物的新型抗生素。目前正作为单剂药物开发,对革兰氏阳性和革兰氏阴性菌均有抗菌活性,包括 MRSA 等耐药微生物。预期 Brilacidin 不久会进入 III 期试验。
达巴万星
达巴万星是一类抑制细胞壁合成的脂糖肽类抗生素,对MRSA有体外抗菌活性。因其半衰期长达6-10天,所以可一周静脉用药一次。[35]Drew RH. Emerging options for treatment of invasive, multidrug-resistant Staphylococcus aureus infections. Pharmacotherapy. 2007;27:227-249.http://www.ncbi.nlm.nih.gov/pubmed/17253914?tool=bestpractice.com[28]Micek ST. Alternatives to vancomycin for the treatment of methicillin-resistant Staphylococcus aureus infections. Clin Infect Dis. 2007;45(suppl 3):S184-S190.http://www.ncbi.nlm.nih.gov/pubmed/17712745?tool=bestpractice.com美国FDA已批准将达巴万星用于治疗甲氧西林敏感或耐药的金黄色葡萄球菌引起的急性细菌性皮肤和皮肤结构感染(ABSSI)。[39]Boucher HW, Wilcox M, Talbot GH, et al. Once-weekly dalbavancin versus daily conventional therapy for skin infection.N Engl J Med. 2014;370:2169-2179.http://www.ncbi.nlm.nih.gov/pubmed/24897082?tool=bestpractice.com
泰地唑胺
泰地唑胺是FDA推荐的一种新的恶唑烷酮类抗生素,用于治疗甲氧西林敏感或耐药的金黄色葡萄球菌引起的急性细菌性皮肤和皮肤结构感染。[40]Kisgen JJ, Mansour H, Unger NR, et al. Tedizolid: a new oxazolidinone antimicrobial. Am J Health-Sys Pharm. 2014;71:621-633.http://www.ncbi.nlm.nih.gov/pubmed/24688035?tool=bestpractice.com泰地唑胺采用每日一次方式给药,与利奈唑胺相比,在不良反应方面可能具有更好的结果。
奥利万星
奥利万星是一种糖肽类抗生素,可破坏细胞膜跨膜电位,目前正在开发中。[35]Drew RH. Emerging options for treatment of invasive, multidrug-resistant Staphylococcus aureus infections. Pharmacotherapy. 2007;27:227-249.http://www.ncbi.nlm.nih.gov/pubmed/17253914?tool=bestpractice.com[28]Micek ST. Alternatives to vancomycin for the treatment of methicillin-resistant Staphylococcus aureus infections. Clin Infect Dis. 2007;45(suppl 3):S184-S190.http://www.ncbi.nlm.nih.gov/pubmed/17712745?tool=bestpractice.com静脉使用,单次给药。
头孢吡普
头孢吡普是头孢菌素类抗生素,它是第一个对 MRSA 有抗菌活性的β-内酰胺类抗生素。其用药方法为一天两次静脉给药。
头孢洛林
头孢洛林是一种对有抗MRSA活性的头孢菌素。[28]Micek ST. Alternatives to vancomycin for the treatment of methicillin-resistant Staphylococcus aureus infections. Clin Infect Dis. 2007;45(suppl 3):S184-S190.http://www.ncbi.nlm.nih.gov/pubmed/17712745?tool=bestpractice.com[41]Zhanel GG, Sniezek G, Schweizer F, et al. Ceftaroline: a novel broad-spectrum cephalosporin with activity against methicillin-resistant Staphylococcus aureus. Drugs. 2009;69:809-831.http://www.ncbi.nlm.nih.gov/pubmed/19441869?tool=bestpractice.com[42]Nannini EC, Stryjewski ME, Corey GR. Ceftaroline for complicated skin and skin-structure infections. Expert Opin Pharmacother. 2010;11:1197-1206.http://www.ncbi.nlm.nih.gov/pubmed/20402556?tool=bestpractice.com研究发现,头孢洛林可达到很高的临床治愈率,对于MRSA或其它常见病原体导致的复杂性皮肤和皮肤结构感染有效,且其耐受性好,安全性与其它头孢菌素相似。它有望单药治疗复杂性皮肤和皮肤结构感染。[43]Corey GR, Wilcox M, Talbot GH, et al. Integrated analysis of CANVAS 1 and 2: phase 3, multicenter, randomized, double-blind studies to evaluate the safety and efficacy of ceftaroline versus vancomycin plus aztreonam in complicated skin and skin-structure infection. Clin Infect Dis. 2010;51:641-650.http://www.ncbi.nlm.nih.gov/pubmed/20695801?tool=bestpractice.com[44]Corey GR, Wilcox MH, Talbot GH, et al. CANVAS 1: the first phase III, randomized, double-blind study evaluating ceftaroline fosamil for the treatment of patients with complicated skin and skin structure infections. J Antimicrob Chemother. 2010;65(suppl 4):iv41-iv51.http://www.ncbi.nlm.nih.gov/pubmed/21115454?tool=bestpractice.com[45]Corrado ML. Integrated safety summary of CANVAS 1 and 2 trials: phase III, randomized, double-blind studies evaluating ceftaroline fosamil for the treatment of patients with complicated skin and skin structure infections. J Antimicrob Chemother. 2010;65(suppl 4):iv67-iv71.http://www.ncbi.nlm.nih.gov/pubmed/21115456?tool=bestpractice.com头孢洛林已于2010年10月获得FDA批准[46]Jorgenson MR, DePestel DD, Carver PL, et al. Ceftaroline fosamil: a novel broad-spectrum cephalosporin with activity against methicillin-resistant Staphylococcus aureus. Ann Pharmacother. 2011;45:1384-1398.http://www.ncbi.nlm.nih.gov/pubmed/22009993?tool=bestpractice.com
艾拉普林
艾拉普林是一种二氨基嘧啶类药物,其作用为抑制二氢叶酸还原酶。前期试验数据显示该药有抗MRSA的活性。[28]Micek ST. Alternatives to vancomycin for the treatment of methicillin-resistant Staphylococcus aureus infections. Clin Infect Dis. 2007;45(suppl 3):S184-S190.http://www.ncbi.nlm.nih.gov/pubmed/17712745?tool=bestpractice.com[35]Drew RH. Emerging options for treatment of invasive, multidrug-resistant Staphylococcus aureus infections. Pharmacotherapy. 2007;27:227-249.http://www.ncbi.nlm.nih.gov/pubmed/17253914?tool=bestpractice.com
法罗培南
法罗培南是一种碳青霉烯类抗菌药物,用于治疗皮肤感染。其用法为每天口服给药两次。对MRSA具有体外抗菌活性。[28]Micek ST. Alternatives to vancomycin for the treatment of methicillin-resistant Staphylococcus aureus infections. Clin Infect Dis. 2007;45(suppl 3):S184-S190.http://www.ncbi.nlm.nih.gov/pubmed/17712745?tool=bestpractice.com[35]Drew RH. Emerging options for treatment of invasive, multidrug-resistant Staphylococcus aureus infections. Pharmacotherapy. 2007;27:227-249.http://www.ncbi.nlm.nih.gov/pubmed/17253914?tool=bestpractice.com
磷霉素
临床数据显示,磷霉素主要在联合治疗方案中使用,对于甲氧西林耐药性金黄色葡萄球菌的磷霉素敏感分离株,磷霉素的临床成功率是 28/29 (96.6%)(主要疾病是肺炎、菌血症和脑膜炎)。但磷霉素在治疗高度耐药的革兰阳性球菌感染中的作用,尚需进一步研究。[47]Falagas ME, Roussos N, Gkegkes ID, et al. Fosfomycin for the treatment of infections caused by Gram-positive cocci with advanced antimicrobial drug resistance: a review of microbiological, animal and clinical studies. Expert Opin Investig Drugs. 2009;18:921-944.http://www.ncbi.nlm.nih.gov/pubmed/19548851?tool=bestpractice.com
替考拉宁
这是一种糖肽类药物。在治疗有较高急性肾损伤风险的MRSA病人时,前景优于万古霉素。替考拉宁尚未获得FDA批准应用,但已在其它国家得以应用。[48]Cavalcanti AB, Goncalves AR, Almeida CS et al. Teicoplanin versus vancomycin for proven or suspected infection. Cochrane Database Syst Rev. 2010;(6):CD007022.http://onlinelibrary.wiley.com/doi/10.1002/14651858.CD007022.pub2/fullhttp://www.ncbi.nlm.nih.gov/pubmed/20556772?tool=bestpractice.com
Omadacycline
Omadacycline是一类氨甲环素类抗生素,可治疗MRSA皮肤软组织感染,且与利奈唑胺相比耐受性更好。[49]Noel GJ, Draper MP, Hait H, et al. A randomized, evaluator-blind, phase 2 study comparing the safety and efficacy of omadacycline to those of linezolid for treatment of complicated skin and skin structure infections. Antimicrob Agents Chemother. 2012;56:5650-5654.http://aac.asm.org/content/56/11/5650.longhttp://www.ncbi.nlm.nih.gov/pubmed/22908151?tool=bestpractice.com