为什么aztreonam是如何工作的。

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为什么aztreonam是如何工作的。

杂志Gynecol。。1990; 171年增刊:南港。

PubMed ID

2244291 (在PubMed

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文摘

Aztreonam是第一个单环beta-lactam抗生素(monobactam)临床试验。其合成结构决定了特定区域的活动,包括增强的活动对假单胞菌的物种,特殊活动对革兰氏阴性细菌,稳定beta-lactamases和缺乏活动对革兰氏阳性细菌——所有这些都可以直接与它的化学成分有关。Aztreonam具有高度的亲和力此种蛋白3 (PBP-3)的需氧革兰氏阴性细菌。大多数这些生物的抑制和杀死了在低浓度的药物。Aztreonam结合差PBP网站的需氧革兰氏阳性和厌氧细菌,因此对这些细菌有相对贫穷的抑制效应。在体外,最低抑制浓度(MIC)值对几乎所有的肠杆菌科和脑膜炎和嗜血杆菌菌株通常低于1微克/毫升。MIC值对铜绿假单胞菌8毫克每毫升与其他类似antipseudomonal beta-lactams acylureidopenicillins。与amino-glycosides联合治疗,aztreonam行为协同作用对铜绿假单胞菌、不动杆菌和革兰氏阴性杆菌gentamicin-resistant。Aztreonam是广泛分布于人体组织和体液,和平均消除半衰期1.7小时。肌内剂量导致血清水平峰值大约一个小时,虽然静脉给药结果在五分钟内最高水平。 After a 2 gram dose given intravenously, MIC90 values for most of the Enterobacteriaceae are exceeded for eight hours, and those for P. aeruginosa, for almost six hours. The steady-state volume of distribution is approximately 0.18 liter per kilogram. Concentrations above the MIC90 for most gram-negative bacteria are also present within bone, prostate and cerebrospinal fluid. Between 60 and 70 per cent of the drug is excreted unchanged in the urine, resulting in concentrations approximating 3,000 micrograms per milliliter two hours after a 1 gram dose given intravenously. Serum clearance of aztreonam is directly proportional to creatinine clearance. Dosage adjustment must, therefore, be made in the presence of reduced clearance. Dosing varies between 0.5 and 2.0 grams every six to 12 hours, depending on the severity of the infection. The characteristics of aztreonam suggest that it is a useful nonnephrotoxic drug for treatment of aerobic gram-negative infection.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
Aztreonam	Penicillin-binding蛋白3	蛋白质	枯草芽孢杆菌(168株)	是的	抑制剂	细节