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Cerebrospinal fluid penetration of tigecycline

机译:脑脊液渗透脱癸锌素

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We report, in a clinical setting, the tigecycline concentration and area under the concentration-time curve (AUC) - both in blood and in cerebrospinal fluid (CSF) - of a patient with a ventriculo-atrial shunt infection. Tigecycline weakly penetrates CSF the CSF-to-serum concentration ratio was 0.079 and CSF-to-serum AUC_(0-12) ratio was 0.067. Tigecycline is a synthetic derivate of minocycline and belongs to the glycylcycline class of antibiotics. Tigecycline has an expanded broad-spectrum activity against Gram-positive and Gram-negative bacteria, including multidrug-resistant strains (vancomycin-resistant enterococci, methicillin-resistant staphylo-cocci, and Acinetobacter baumannii) [1]. Due to its scarce bioavailability after oral administration, the drug is usually administered as a 30-60-min intravenous (IV) infusion [2]. The half-life of tigecycline ranges between 16 and 67 h [1-3]. The drug is mainly excreted unchanged in the faeces and its dosage does not need adjustment in the case of renal failure [2]. Tigecycline is rapidly distributed into the tissues and becomes concentrated primarily in the bile and in the bowel [3,4] and, to a lesser extent, in the lungs [3]. Data regarding the ability of tigecycline to penetrate bone tissue are conflicting, especially between the murine model [5] and the human model [3]. Furthermore, easily comparable data on the ability of the drug to penetrate the central nervous system are lacking [3,4,6].
机译:我们在临床环境中报告,浓度 - 时间曲线(AUC)下的脱癸锌素浓度和面积 - 血液和脑脊液(CSF) - 患者的患者进行心室间分流感染。替代霉素弱渗透CSF CSF - 血清浓度比为0.079,CSF - 血清AUC_(0-12)的比例为0.067。脱癸锌素是米诺环素的合成衍生物,属于糖基环素类的抗生素。替霉素对革兰氏阳性和革兰氏阴性细菌具有扩展的广谱活性,包括多药抗性菌株(耐常霉素肠细胞,甲氧西林抗性葡萄球菌和血管杆菌Baumannii)[1]。由于其稀缺性生物利用度口服给药后,药物通常以30-60分钟静脉内(IV)输注[2]给药[2]。替塞霉素的半衰期范围为16至67小时[1-3]。该药主要在粪便中不变排出,其剂量在肾衰竭的情况下不需要调整[2]。将替霉素迅速分布到组织中,主要在胆汁和肠道[3,4]中浓缩,并在较小程度上浓缩[3]。关于脱癸素渗透骨组织的能力的数据是矛盾的,特别是鼠模型[5]和人模型之间[3]。此外,缺乏对药物能力渗透中枢神经系统的能力的可比数据缺乏[3,4,6]。

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