Lauven P M, Ebeling B J, Stoeckel H, Dierke-Dzierzon C
Anasth Intensivther Notfallmed. 1986 Dec;21(6):311-4.
The competitive benzodiazepine antagonist Ro 15-1788 proved efficacious after general anaesthesia induced by flunitrazepam. It showed a quick onset of action within 1-2 min. After antagonisation, the heart rate, blood pressure and respiratory rate remained stable. No increased demand for analgesics could be demonstrated postoperatively. A transient anxiety that could be observed in 7 of 38 patients after doses between 0.5 and 2.0 mg seemed of minor clinical importance but may indicate that Ro 15-1788 acted not only as a pure antagonist but as a partially inverse agonist as well. Recurrence of sedation could be observed in 6 out of 38 patients after 2 h of Ro 15-1788 dosage. Careful observation of the patients for at least 2 h is therefore recommended even if antagonisation seemed successful. It was possible to reverse the benzodiazepine action successfully with doses between 0.3 and 0.8 mg. After these doses the patients will awake gently and gradually and unwanted side effects will be avoided. In our experience, Ro 15-1788 is a useful improvement in benzodiazepine application after surgical anaesthesia.
竞争性苯二氮䓬拮抗剂Ro 15 - 1788在氟硝西泮诱导的全身麻醉后被证明有效。它在1 - 2分钟内起效迅速。拮抗后，心率、血压和呼吸频率保持稳定。术后未发现对镇痛药的需求增加。在38例患者中有7例在给予0.5至2.0毫克剂量后出现短暂焦虑，这似乎在临床上不太重要，但可能表明Ro 15 - 1788不仅作为一种纯粹的拮抗剂起作用，还作为一种部分反向激动剂起作用。在给予Ro 15 - 1788剂量2小时后，38例患者中有6例出现镇静复发。因此，即使拮抗似乎成功，也建议对患者进行至少2小时的仔细观察。使用0.3至0.8毫克的剂量能够成功逆转苯二氮䓬的作用。给予这些剂量后，患者将缓慢且逐渐地苏醒，并避免不必要的副作用。根据我们的经验，Ro 15 - 1788是外科麻醉后苯二氮䓬应用方面的一项有益改进。
