Pergolizzi Joseph V, Gan Tong J, Plavin Stanford, Labhsetwar Sumedha, Taylor Robert
Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD 21205-2196, USA.
Anesthesiol Res Pract. 2011;2011:458920. doi: 10.1155/2011/458920. Epub 2011 Apr 14.
Monitored anesthesia care (MAC) is a safe, effective, and appropriate form of anesthesia for many minor surgical procedures. The proliferation of outpatient procedures has heightened interest in MAC sedation agents. Among the most commonly used MAC sedation agents today are benzodiazepines, including midazolam, and propofol. Recently approved in the United States is fospropofol, a prodrug of propofol which hydrolyzes in the body by alkaline phosphatase to liberate propofol. Propofol liberated from fospropofol has unique pharmacological properties, but recently retracted pharmacokinetic (PK) and pharmacodynamic (PD) evaluations make it difficult to formulate clear conclusions with respect to fospropofol's PK/PD properties. In safety and efficacy clinical studies, fospropofol demonstrated dose-dependent sedation with good rates of success at doses of 6.5 mg/kg along with good levels of patient and physician acceptance. Fospropofol has been associated with less pain at injection site than propofol. The most commonly reported side effects with fospropofol are paresthesia and pruritus. Fospropofol is a promising new sedation agent that appears to be well suited for MAC sedation, but further studies are needed to better understand its PK/PD properties as well its appropriate clinical role in outpatient procedures.
监测麻醉管理（MAC）对于许多小型外科手术来说是一种安全、有效且合适的麻醉方式。门诊手术的增多提高了人们对MAC镇静药物的兴趣。当今最常用的MAC镇静药物包括苯二氮䓬类药物（如咪达唑仑）和丙泊酚。在美国，丙泊酚前体药物磷丙泊酚最近获得批准，它在体内通过碱性磷酸酶水解以释放丙泊酚。从磷丙泊酚释放出的丙泊酚具有独特的药理学特性，但最近撤回的药代动力学（PK）和药效学（PD）评估使得难以就磷丙泊酚的PK/PD特性得出明确结论。在安全性和有效性临床研究中，磷丙泊酚在6.5mg/kg剂量下表现出剂量依赖性镇静，成功率良好，患者和医生的接受度也较高。与丙泊酚相比，磷丙泊酚注射部位疼痛较少。磷丙泊酚最常报告的副作用是感觉异常和瘙痒。磷丙泊酚是一种有前景的新型镇静药物，似乎非常适合MAC镇静，但需要进一步研究以更好地了解其PK/PD特性以及在门诊手术中的适当临床作用。
