碱化丁卡因溶液尿道粘膜表面麻醉的临床观察和药代动力学研究

Alkalized tetracaine as a topical anaesthetic for urethra

１６例接受膀胱镜检的患者分为临床碱化组和临床对照组；将２０只家兔匀分为动物碱化组和动物对照组。碱化组均给予ｐＨ７．１５的１％丁卡因溶液，对照组给予ｐＨ５．１的１％丁卡因溶液。结果，临床碱化组麻醉效果优于临床对照组（Ｐ＜０．０５）。但临床对照组药液在血液中达峰时间（Ｔｐｅａｋ）快；峰浓度（Ｃｍａｘ）及血药浓度的各个时点均高于临床碱化组（Ｐ均＜０．０１）。两组中分布半衰期，消除半衰期无显著性差异。表现分布容积（Ｖｄ），药时曲线下面积（ＡＵＣ）和清除率（ＣＬ）有显著性差异（Ｐ均＜０．０１）。动物碱化组丁卡因在血中浓度低，而在膀胱组织中浓度高（Ｐ均＜０．０１）。认为碱化丁卡因具有效果好，毒性低和清除快的优点，用于临床尿道粘膜表面麻醉安全有效。

Urethroscopy was undertaken for 8 patients under topical anaesthesia with 1% alkalized tetracaine(1.2mg/kg,PH 7.15).8 patients,served as controls,received the same dosage of tetracaine but with a PH of 5. 1.The anaesthesia effect of alkalized tetracaine was significantly better(P<0.05)while the plasma peak time was longer and the concentration peak was lower as compared with the controls(P<0.01).Alkalized tetracaine(pH 7.15)was safe and effective as a topical anaesthetic for urethra.