Regulation of the effect of anesthetics-relationships with intracerebral pharmacokinetics and adrenoceptors

研究了脑内肾上腺素受体对局麻药中枢神经系统毒性的影响。在清醒大鼠模型中，脑内给予普萘洛尔（一种β肾上腺素能受体拮抗剂）可显著提高利多卡因诱发惊厥的阈值。为阐明局麻药由外周血向脑内流，采用微透析方法测定局麻药在脑细胞外液中的浓度。我们发现只有不结合蛋白质的局部麻醉剂会扩散到大脑中。

Effect of intracerebral adrenoceptors on central nervous system toxicity of local anesthetics was investigated. In awake rat model, intracerebral administration of propranolol, a beta adrenoceptor antagonist, significantly increased the threshold for lidocaine-induced convulsions. For elucidating the influx of local anesthetics from peripheral blood to the brain, concentration of local anesthetics in the cerebral extracellular fluid by microdialysis method. We found that only protein-unbound fraction of local anesthetics diffuses into the brain.