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福司波佛,一种新型镇静麻醉剂,及其在围手术期的应用。

Fospropofol, a new sedative anesthetic, and its utility in the perioperative period.

机构信息

Cleveland Clinic Lerner College of Medicine of Case Western Reserve University, OH, USA.

出版信息

Curr Pharm Des. 2012;18(38):6241-52. doi: 10.2174/138161212803832308.

Abstract

Fospropofol is an intravenous sedative-anesthetic agent that is FDA-approved for monitored anesthesia care (MAC) sedation in adult patients undergoing diagnostic or therapeutic procedures. As a prodrug of propofol, fospropofol's pharmacologic activity results from its breakdown by alkaline phosphatase and release of propofol, which is the active molecule. It exhibits a longer time to peak clinical effect and a more prolonged action compared to propofol. Thus patients may exhibit smoother hemodynamic and respiratory depression compared to propofol lipid emulsion bolus. Another advantage over propofol is that it does not induce a burning sensation on IV administration. Side effects include perineal paresthesia and itching, respiratory depression, hypoxemia, hypotension, loss of consciousness, and apnea with higher IV boluses. Therefore, current recommendations call for it to be administered only by clinicians trained in general anesthesia, who are thus skilled in advanced airway management. Fospropofol has a unique dosing regimen, with a standard dose for adults 18-65 years of age, and a modified dose (75% of the standard dose) for patients > 65 years of age and for sicker adult patients whose American Society of Anesthesiologists physical status score is ≥ 3. Also, the minimum and maximun IV bolus doses are body-weight adjusted to 60 and 90 kg respectively. Available evidence demonstrates that fospropofol in MAC sedation is successful in patients undergoing esophagogastroscopy, colonoscopy and flexible bronchoscopy. The use of fospropofol is also now being explored in many other perioperative settings. In light of current shortages of many anesthetic drugs, whether forspropofol can take the place of propofol in ICUs and operating rooms remains to be determined.

摘要

福司泊酚是一种静脉镇静-麻醉剂,已获得美国食品药品监督管理局批准,可用于接受诊断或治疗程序的成年患者的监测麻醉护理(MAC)镇静。作为丙泊酚的前体药物,福司泊酚的药理活性来自其通过碱性磷酸酶的分解和丙泊酚的释放,丙泊酚是活性分子。与丙泊酚相比,它达到峰值临床效果的时间更长,作用持续时间更长。因此,与丙泊酚脂质乳剂推注相比,患者可能表现出更平稳的血液动力学和呼吸抑制。与丙泊酚相比的另一个优势是它不会在静脉给药时引起烧灼感。副作用包括会阴部感觉异常和瘙痒、呼吸抑制、低氧血症、低血压、意识丧失和呼吸暂停,与更高的静脉推注剂量有关。因此,目前的建议要求只有接受过全身麻醉培训的临床医生才能使用它,这些医生因此精通高级气道管理。福司泊酚有一个独特的剂量方案,标准剂量适用于 18-65 岁的成年人,对于>65 岁的患者和美国麻醉医师协会身体状况评分≥3 的更病重的成年患者,使用的剂量为标准剂量的 75%。此外,最小和最大静脉推注剂量分别为按体重调整至 60 和 90 公斤。现有证据表明,福司泊酚在 MAC 镇静中可成功用于接受食管胃十二指肠镜检查、结肠镜检查和纤维支气管镜检查的患者。福司泊酚的使用也正在许多其他围手术期环境中进行探索。鉴于目前许多麻醉药物短缺,福司泊酚是否可以替代 ICU 和手术室中的丙泊酚仍有待确定。

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