Yu Q H, Kitazumi K, Kamei C, Tasaka K
J Pharmacobiodyn. 1984 Aug;7(8):586-92. doi: 10.1248/bpb1978.7.586.
Epileptogenic activity induced by intravenous injection of certain cephalosporin derivatives was studied. Ceftezole provided the most potent epileptogenic activity among the drugs tested. Changes in seizure patterns on electroencephalogram (EEG) tracings and behavioral signs after administration of cefotiam and cefazolin were similar to those seen after ceftezole, though the intensity and duration were less than those of ceftezole. Cephacetrile and cephaloridine elicited the spiking activity in the frontal cortex and the other regions without apparent behavioral changes. Latamoxef and cefmenoxime displayed a weak epileptogenic activity at a dose of 1000 mg/kg. On the other hand, cephapirin, cefmetazole and cefoxitin did not evoke any changes in EEG nor in behavior. Penicillin G at a dose of 200 mg/kg affected spike or spike-and-wave complex in a few cases, but at a dose of 500 mg/kg the animals died of dyspnea almost immediately after injection without showing apparent epileptogenic signs. These results suggest that some of cephalosporins such as ceftezole, cefotiam, cephacetrile and cefazolin provide epileptogenic activity at higher doses.
研究了静脉注射某些头孢菌素衍生物所诱导的致痫活性。在受试药物中，头孢替唑具有最强的致痫活性。注射头孢替安和头孢唑林后，脑电图（EEG）描记图上的癫痫发作模式变化及行为体征与注射头孢替唑后所见相似，不过强度和持续时间低于头孢替唑。头孢乙腈和头孢噻啶在前额叶皮质及其他区域引发了棘波活动，但无明显行为变化。拉氧头孢和头孢甲肟在剂量为1000mg/kg时表现出较弱的致痫活性。另一方面，头孢匹林、头孢美唑和头孢西丁未引起脑电图及行为的任何变化。剂量为200mg/kg的青霉素G在少数情况下影响棘波或棘慢复合波，但剂量为500mg/kg时，动物在注射后几乎立即死于呼吸困难，未表现出明显的致痫体征。这些结果表明，某些头孢菌素如头孢替唑、头孢替安、头孢乙腈和头孢唑林在较高剂量时具有致痫活性。
