Purpose

Single doses of gentamicin have demonstrated clinical efficacy in the treatment of urogenital gonorrhea, but lower cure rates for oropharyngeal and anorectal gonorrhea. Formulations selectively enriched in specific gentamicin C congeners have been proposed as a less toxic alternative to gentamicin, potentially permitting higher dosing to result in increased plasma exposures at the extragenital sites of infection. The purpose of the present study was to compare the antibacterial activity of individual gentamicin C congeners against Neisseria gonorrhoeae to that of other aminoglycoside antibiotics.

Methods

Antimicrobial susceptibility of three N. gonorrhoeae reference strains and 152 clinical isolates was assessed using standard disk diffusion, agar dilution, and epsilometer tests.

Results

Gentamicin C1, C2, C1a, and C2a demonstrated similar activity against N. gonorrhoeae. Interestingly, susceptibility to the 1-N-ethylated aminoglycosides etimicin and netilmicin was significantly higher than the susceptibility to their parent compounds gentamicin C1a and sisomicin, and to any other of the 25 aminoglycosides assessed in this study. Propylamycin, a 4’-propylated paromomycin analogue, was significantly more active against N. gonorrhoeae than its parent compound, too.

Conclusion

Selectively enriched gentamicin formulations hold promise for a less toxic but equally efficacious alternative to gentamicin. Our study warrants additional consideration of the clinically established netilmicin and etimicin for treatment of genital and perhaps extragenital gonorrhea. Additional studies are required to elucidate the mechanism behind the advantage of alkylated aminoglycosides.

中文翻译：

---

与庆大霉素和其他氨基糖苷类药物相比，淋病奈瑟菌对奈替米星和依替米星的体外敏感性

目的

单剂量庆大霉素在治疗泌尿生殖淋病方面已显示出临床疗效，但对口咽和肛门直肠淋病的治愈率较低。选择性富含特定庆大霉素 C 同系物的制剂已被提议作为庆大霉素毒性较小的替代品，可能允许更高的剂量，从而导致生殖器外感染部位的血浆暴露增加。本研究的目的是比较单个庆大霉素 C 同系物与其他氨基糖苷类抗生素对淋病奈瑟菌的抗菌活性。

方法

使用标准纸片扩散、琼脂稀释和 esilometer 测试评估了3 种淋病奈瑟菌参考菌株和 152 种临床分离株的抗菌敏感性。

结果

庆大霉素 C1、C2、C1a 和 C2a 对淋病奈瑟菌具有相似的活性。有趣的是，对 1- N-乙基化氨基糖苷类依替米星和奈替米星的敏感性显着高于对其母体化合物庆大霉素 C1a 和西索米星以及本研究中评估的 25 种氨基糖苷类中任何其他药物的敏感性。丙霉素（Propylamycin）是一种 4'-丙基化巴龙霉素类似物，对淋病奈瑟菌的活性也显着高于其母体化合物。

结论

选择性浓缩庆大霉素制剂有望成为毒性较小但同样有效的庆大霉素替代品。我们的研究需要额外考虑临床上确定的奈替米星和依替米星用于治疗生殖器和可能的生殖器外淋病。需要进一步的研究来阐明烷基化氨基糖苷类优势背后的机制。