Hori S, Kanemitsu K, Shimada J
Division of Clinical Pharmacology, St. Marianna University School of Medicine, Kawasaki, Japan.
J Antibiot (Tokyo). 1993 Jul;46(7):1145-8. doi: 10.7164/antibiotics.46.1145.
Cephalosporins have been well known to have potent convulsant activity. We studied the mechanism of the convulsions induced by cephalosporins. Cefazolin, cephaloridine, cefpirome and cefmetazole inhibited the receptor binding of gamma-aminobutyric acid (GABA), an inhibitory transmitter in the mammalian central nervous system. As fluoroquinolones also inhibited GABA receptor binding and this inhibition was enhanced in the presence of non-steroidal anti-inflammatory drugs (NSAIDs), we studied the effect of cephalosporins on GABA receptor binding in the presence of NSAIDs. The inhibitory activity of cephalosporins was not enhanced in the presence of NSAIDs. These results suggested that cephalosporins might induce convulsions through the inhibition of GABA receptor binding, and that concurrent administration of cephalosporins and NSAIDs might not enhance the convulsant activity of cephalosporins.
众所周知，头孢菌素具有强大的惊厥活性。我们研究了头孢菌素诱发惊厥的机制。头孢唑林、头孢噻啶、头孢匹罗和头孢美唑抑制了γ-氨基丁酸（GABA）的受体结合，GABA是哺乳动物中枢神经系统中的一种抑制性递质。由于氟喹诺酮类药物也抑制GABA受体结合，并且在非甾体抗炎药（NSAIDs）存在的情况下这种抑制作用会增强，我们研究了在NSAIDs存在的情况下头孢菌素对GABA受体结合的影响。在NSAIDs存在的情况下，头孢菌素的抑制活性并未增强。这些结果表明，头孢菌素可能通过抑制GABA受体结合来诱发惊厥，并且同时使用头孢菌素和NSAIDs可能不会增强头孢菌素的惊厥活性。
