Williams P D, Bennett D B, Comereski C R
Department of Experimental Toxicology, Bristol-Myers Company, Syracuse, New York 13221-4755.
Antimicrob Agents Chemother. 1988 May;32(5):758-60. doi: 10.1128/AAC.32.5.758.
The beta-lactam antibiotics imipenem-cilastatin, BMY-26225, and cefazolin significantly lowered the convulsive threshold of pentylenetetrazole in mice. In addition, imipenem-cilastatin and cefazolin were found to inhibit 3H-labeled gamma-aminobutyric acid binding to synaptic membranes from rat brains. Our results suggest that the pentylenetetrazole convulsive model may be useful in evaluating the proconvulsive liabilities of new carbapenems and other beta-lactam antibiotics and that the mechanism of imipenem-cilastatin and cefazolin toxicity may involve interaction with gamma-aminobutyric acid receptors.
β-内酰胺类抗生素亚胺培南-西司他丁、BMY-26225和头孢唑林可显著降低小鼠戊四氮的惊厥阈值。此外，还发现亚胺培南-西司他丁和头孢唑林可抑制3H标记的γ-氨基丁酸与大鼠脑突触膜的结合。我们的结果表明，戊四氮惊厥模型可能有助于评估新型碳青霉烯类和其他β-内酰胺类抗生素的促惊厥风险，且亚胺培南-西司他丁和头孢唑林的毒性机制可能涉及与γ-氨基丁酸受体的相互作用。
