Shimada J, Hori S, Kanemitsu K, Shoji Y, Nakashio S, Yanagawa A
Division of Clinical Pharmacology, St. Marianna University School of Medicine, Kawasaki, Japan.
Drugs Exp Clin Res. 1992;18(9):377-81.
Beta-lactams are well known to have potent convulsant activity. Imipenem, the first carbapenem antibiotic introduced in the clinical field, has been reported to induce convulsions. The neurochemical mechanism of the convulsions induced by carbapenems and cephalosporins were studied. Intraventricular injection of cefazolin, cephaloridine and imipenem, and of panipenem (a new carbapenem), induced convulsions in a dose-dependent manner in mice. They inhibited the receptor binding of gamma-aminobutyric acid (GABA), an inhibitory transmitter in the mammalian central nervous system. These in-vitro and in-vivo results suggest that carbapenems and cephalosporins might induce convulsions through the inhibition of GABA receptor binding when they are accumulated in the central nervous system.
众所周知，β-内酰胺类药物具有强大的惊厥活性。亚胺培南是临床领域引入的首个碳青霉烯类抗生素，据报道可诱发惊厥。对碳青霉烯类和头孢菌素类药物诱发惊厥的神经化学机制进行了研究。向小鼠脑室内注射头孢唑林、头孢噻啶、亚胺培南以及帕尼培南（一种新型碳青霉烯类药物），均可剂量依赖性地诱发惊厥。它们抑制了γ-氨基丁酸（GABA，哺乳动物中枢神经系统中的一种抑制性递质）的受体结合。这些体外和体内研究结果表明，碳青霉烯类和头孢菌素类药物在中枢神经系统中蓄积时，可能通过抑制GABA受体结合而诱发惊厥。
