Harper P B
Clin Ther. 1984;6(4):411-24.
Ceftazidime is an aminothiazolyl cephalosporin that exhibits a high level of broad-spectrum activity, with particularly good activity against Pseudomonas sp. Although activity in vitro against staphylococci is moderate, the majority of enterobacteria are susceptible, with MIC50 values in the range from 0.06 to 4 micrograms/ml. This cephalosporin is also highly active against indole-positive Proteus sp, Providencia sp, Citrobacter sp, and Serratia sp, with MIC50 values ranging from less than or equal to 0.06 to 0.13 microgram/ml. Good activity against Pseudomonas sp is a notable feature, with MIC90 values in the range of 4 to 8 micrograms/ml. Ceftazidime is bactericidal at concentrations identical or close to the MIC. Antibiotic performance in vitro appears to be unaffected by the presence of body fluids. Good stability to hydrolysis by a range of the prevalent beta-lactamases, good penetration into the intact bacterium, and a high affinity for the essential penicillin-binding proteins combine to account for the broad spectrum and high activity of ceftazidime. Comparative in vitro studies have shown ceftazidime to be as active and sometimes more active than available aminoglycoside antibiotics. Since the mode of action of ceftazidime differs fundamentally from that of the aminoglycosides, high activity is maintained against the majority of aminoglycoside-resistant isolates. Ceftazidime should therefore represent a viable and potentially safer alternative to aminoglycoside antibiotics.
头孢他啶是一种氨噻唑基头孢菌素,具有高度广谱活性,对假单胞菌属尤其具有良好活性。尽管其对葡萄球菌的体外活性中等,但大多数肠杆菌都敏感,其MIC50值在0.06至4微克/毫升范围内。这种头孢菌素对吲哚阳性变形杆菌属、普罗威登斯菌属、柠檬酸杆菌属和沙雷菌属也具有高度活性,其MIC50值范围为小于或等于0.06至0.13微克/毫升。对假单胞菌属的良好活性是一个显著特征,其MIC90值在4至8微克/毫升范围内。头孢他啶在等于或接近MIC的浓度下具有杀菌作用。体外抗生素性能似乎不受体液存在的影响。对多种常见β-内酰胺酶水解具有良好稳定性、对完整细菌具有良好穿透力以及对必需青霉素结合蛋白具有高亲和力,这些因素共同促成了头孢他啶的广谱和高活性。体外比较研究表明,头孢他啶与现有的氨基糖苷类抗生素活性相当,有时甚至更具活性。由于头孢他啶的作用方式与氨基糖苷类药物根本不同,因此对大多数耐氨基糖苷类分离株仍保持高活性。因此,头孢他啶应该是氨基糖苷类抗生素的一种可行且可能更安全的替代品。