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西索米星与庆大霉素。抗菌及药代动力学特性比较(作者译)

[Sisomicin versus gentamicin. A comparison of antibacterial and pharmacokinetic properties (author's transl)].

作者信息

Naumann P, Rosin H, Reintjens E, Köhler M

出版信息

Dtsch Med Wochenschr. 1976 Aug 27;101(35):1277-84. doi: 10.1055/s-0028-1104256.

Abstract

In a comparison of the antibacterial in-vitro activity of sisomicin, gentamicin, and tobramycine, sisomicin showed a higher activity against E. coli, indole-positive Proteus spp. and organisms of the Klebsiella-Enterobacter-Serratia group, whereas tobramycine was superior against Pseudomonas spp. However, the differences in activity between sisomicin and gentamicin were only within one step of dilution which is hardly sufficient to guarantee a basic superiority of one or the other preparation for clinical purposes. In 12 healthy probands serum levels and renal elimination of sisomicin and gentamicin after a single intramuscular injection of 1 mg/kg body weight were investigated in a randomised change-over trial. With corresponding serum levels, almost identical elimination half-lives of 109 and 111 minutes, and recovery values of 84 and 88.4%, respectively, there were no significant differences in the pharmacokinetics of sisomicin and gentamicin. Thus in the antibacterial treatment of gentamicin-sensitive gram-negative organisms sisomicin presents an equally good alternative. With organisms only moderately sensitive or resistant to gentamicin, sisomicin, tobramycine and amikacin should be additionally tested.

摘要

在对西索米星、庆大霉素和妥布霉素的体外抗菌活性进行比较时,西索米星对大肠杆菌、吲哚阳性变形杆菌属以及克雷伯菌 - 肠杆菌 - 沙雷菌属的微生物显示出更高的活性,而妥布霉素对假单胞菌属更具优势。然而,西索米星和庆大霉素之间的活性差异仅在一个稀释度范围内,这几乎不足以保证其中一种制剂在临床应用上具有基本的优势。在一项随机交叉试验中,对12名健康受试者单次肌肉注射1mg/kg体重后西索米星和庆大霉素的血清水平及肾脏清除情况进行了研究。在相应的血清水平下,消除半衰期几乎相同,分别为109分钟和111分钟,回收率分别为84%和88.4%,西索米星和庆大霉素的药代动力学没有显著差异。因此,在对庆大霉素敏感的革兰氏阴性菌的抗菌治疗中,西索米星是一个同样好的选择。对于仅对庆大霉素中度敏感或耐药的微生物,应额外测试西索米星、妥布霉素和阿米卡星。

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