Slover Christine M, Rodvold Keith A, Danziger Larry H
Department of Pharmacy Practice, University of Illinois at Chicago, Chicago, IL 60612, USA.
Ann Pharmacother. 2007 Jun;41(6):965-72. doi: 10.1345/aph.1H543. Epub 2007 May 22.
To review the literature on tigecycline, a novel antibiotic.
References were identified through MEDLINE (1966-February 2007) and International Pharmaceutical Abstracts (1970-February 2007) databases, using the key words tigecycline, glycylcycline, complicated skin and skin structure infections (cSSSI), complicated intraabdominal infections (cIAI), and in vitro. Additional articles for this review were identified by reviewing the bibliographies of articles cited. The package insert was also used as a reference.
In vitro, clinical, and pharmacokinetic studies evaluating tigecycline's safety and efficacy were selected.
A tigecycline 100 mg intravenous loading dose followed by an intravenous infusion of 50 mg every 12 hours was shown in clinical trials to be as effective as comparator antibiotics in treating cSSSI and cIAI. Tigecycline has a broad spectrum of activity that includes many resistant bacteria with few treatment options, such as methicillin-resistant Staphylococcus aureus and extended-spectrum beta-lactamase-producing bacteria such as Escherichia coli and Klebsiella pneumoniae. In cSSSI studies, tigecycline was found to be noninferior to vancomycin plus aztreonam with test-of-cure rates of 86.5% and 88.6%, respectively. Tigecycline was also found to be noninferior to imipenem/cilastatin in cIAI studies; clinical cure rates were 86.1% and 86.2%, respectively. In vitro activity has been demonstrated against other multidrug-resistant microorganisms of concern, such as Acinetobacter spp. Although it has a broad spectrum of activity, tigecycline has inadequate activity against Pseudomonas spp. Nausea and vomiting were the most frequently reported adverse effects.
Tigecycline is approved for the treatment of cSSSI and cIAI infections. To date, little resistance to tigecycline has been reported; however, with widespread use of the drug, resistance will likely occur. Since published studies have not dealt with seriously ill patients, it is recommended that, until further studies have been completed, other agents be used in the treatment of these patients unless no option other than tigecycline exists.
综述关于新型抗生素替加环素的文献。
通过MEDLINE（1966年 - 2007年2月）和国际药学文摘数据库（1970年 - 2007年2月）检索参考文献，使用关键词替加环素、甘氨酰环素、复杂性皮肤和皮肤结构感染（cSSSI）、复杂性腹腔内感染（cIAI）以及体外研究。通过查阅所引用文章的参考文献确定了本综述的其他文章。药品说明书也用作参考。
选择评估替加环素安全性和有效性的体外、临床和药代动力学研究。
临床试验表明，替加环素静脉注射100mg负荷剂量，随后每12小时静脉输注50mg，在治疗cSSSI和cIAI方面与对照抗生素疗效相当。替加环素具有广泛的抗菌活性，包括许多耐药菌，如耐甲氧西林金黄色葡萄球菌以及产超广谱β - 内酰胺酶的细菌，如大肠杆菌和肺炎克雷伯菌，而针对这些细菌的治疗选择较少。在cSSSI研究中，发现替加环素不劣于万古霉素加氨曲南，治愈率分别为86.5%和88.6%。在cIAI研究中，替加环素也不劣于亚胺培南/西司他丁；临床治愈率分别为86.1%和86.2%。体外研究已证明其对其他引起关注的多重耐药微生物具有活性，如不动杆菌属。尽管替加环素具有广泛的抗菌活性，但对铜绿假单胞菌活性不足。恶心和呕吐是最常报告的不良反应。
替加环素已被批准用于治疗cSSSI和cIAI感染。迄今为止，几乎没有关于替加环素耐药性的报道；然而，随着该药物的广泛使用，耐药性可能会出现。由于已发表的研究未涉及重症患者，建议在完成进一步研究之前，除非除替加环素外别无选择，否则在治疗这些患者时应使用其他药物。
