Borowicz K, Kozicka M, Kleinrok Z, Czuczwar S J
Department of Pharmacology, Lublin Medical School, Poland.
J Neural Transm Gen Sect. 1993;93(2):157-63. doi: 10.1007/BF01245345.
Aminophylline (theophylline2.ethylenediamine) in the dose of 12.5 mg/kg (i.p.) was ineffective upon all antiepileptic drugs studied and at the higher dose of 25 mg/kg, impaired the anticonvulsant action of phenobarbital and valproate against maximal electroshock in mice. The protection offered by diphenylhydantoin was diminished by aminophylline at 50 mg/kg (0.238 mmol of anhydrous theophylline/kg). In contrast, 8-(p-sulfophenyl)theophylline (a theophylline derivative unable to cross the blood-brain barrier) in the dose of 80 mg/kg (0.238 mmol/kg) did not influence the protective activity of diphenylhydantoin, phenobarbital, and valproate. It might be concluded that the aminophylline-induced impairment of the anticonvulsant action of common antiepileptic drugs results from the central effects of this methylxanthine.
氨茶碱（茶碱乙二胺）腹腔注射剂量为12.5毫克/千克时，对所研究的所有抗癫痫药物均无作用；剂量增至25毫克/千克时，会削弱苯巴比妥和丙戊酸盐对小鼠最大电休克的抗惊厥作用。剂量为50毫克/千克（0.238毫摩尔无水茶碱/千克）的氨茶碱会降低苯妥英的保护作用。相比之下，剂量为80毫克/千克（0.238毫摩尔/千克）的8-（对-磺苯基）茶碱（一种无法穿过血脑屏障的茶碱衍生物）不会影响苯妥英、苯巴比妥和丙戊酸盐的保护活性。可以得出结论，氨茶碱引起的常见抗癫痫药物抗惊厥作用受损是由这种甲基黄嘌呤的中枢作用所致。
