Cullmann W, Dick W
Immun Infekt. 1984 Feb;12(1):29-34.
The induction potency of various beta-lactam compounds was studied in a clinical isolate which exhibited resistance against most beta-lactam compounds; however, spontaneous beta-lactamase production was only marginal in this strain. In general, all beta-lactam derivatives included in this study possessed induction potency independent of the nucleus of the compound. N-formimidoyl thienamycin, the penem compound Sch 29482, 6-aminopenicillanic acid, and clavulanic acid proved to be the most potent inducers. With the exception of mezlocillin and ceftazidime there was a correlation between the concentration of the compound and the induction potency. Combination of two beta-lactam antibiotics resulted in an addition of the induction potency of each one. With respect to the considerable amount of enzyme that can be induced the development of resistance even against newer compounds fairly stable against the attack of beta-lactamases can be explained.
在一株对大多数β-内酰胺类化合物耐药的临床分离株中研究了各种β-内酰胺类化合物的诱导能力;然而,该菌株中自发产生β-内酰胺酶的情况仅为微量。总体而言,本研究中包含的所有β-内酰胺衍生物都具有诱导能力,且与化合物的核心结构无关。N-甲酰亚胺基硫霉素、青霉烯化合物Sch 29482、6-氨基青霉烷酸和克拉维酸被证明是最有效的诱导剂。除美洛西林和头孢他啶外,化合物的浓度与诱导能力之间存在相关性。两种β-内酰胺类抗生素联合使用会使每种抗生素的诱导能力相加。鉴于可诱导产生大量的酶,即使是对β-内酰胺酶攻击相当稳定的新型化合物,也可能出现耐药性的产生,这一点是可以解释的。