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头孢羟氨苄、头孢氨苄和头孢拉定在体外药代动力学模型中的杀菌活性。

Bactericidal activity of cefadroxil, cephalexin, and cephradine in an in vitro pharmacokinetic model.

作者信息

Leitner F, Goodhines R A, Buck R E, Price K E

出版信息

J Antibiot (Tokyo). 1979 Jul;32(7):718-26. doi: 10.7164/antibiotics.32.718.

Abstract

Cefadroxil (Duricef, Mead Johnson and Company), resembles cephalexin and cephradine in spectrum of antibacterial activity but differs in human pharmacokinetic properties. Whether the latter are likely to affect activity in vivo was assessed by determining bactericidal activity against clinical isolates under conditions simulating the variation of drug concentration in the blood stream after an oral dose of 500 mg to adults. In this kinetic model, cefadroxil was more active than cephalexin or cephradine against Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, Proteus mirabilis, Haemophilus influenzae and one of two strains of Escherichia coli. The other strain of E. coli was virtually unaffected by the cephalosporins. S. pyogenes was equally susceptible to all three cephalosporins. Analysis of the results suggest that the pharmocokinetic properties of an antibiotic affect its activity in the blood stream, provided the susceptibility of the infecting organism is concentration-dependent within the range of drug concentration occurring in serum.

摘要

头孢羟氨苄(杜里辛,美赞臣公司),其抗菌活性谱与头孢氨苄和头孢拉定相似,但人体药代动力学特性有所不同。通过测定口服500毫克剂量给成人后,模拟血流中药物浓度变化条件下对临床分离株的杀菌活性,评估了后者是否可能影响体内活性。在这个动力学模型中,头孢羟氨苄对金黄色葡萄球菌、肺炎链球菌、肺炎克雷伯菌、奇异变形杆菌、流感嗜血杆菌以及两株大肠杆菌中的一株,比头孢氨苄或头孢拉定更具活性。另一株大肠杆菌实际上不受头孢菌素影响。化脓性链球菌对所有三种头孢菌素同样敏感。结果分析表明,只要感染菌的敏感性在血清中出现的药物浓度范围内是浓度依赖性的,抗生素的药代动力学特性就会影响其在血流中的活性。

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