Upton R N, Ludbrook G L, Grant C, Doolette D J
Department of Anaesthesia and Intensive Care, Royal Adelaide Hospital, University of Adelaide, Adelaide, Australia.
Anesthesiology. 2000 Oct;93(4):1085-94. doi: 10.1097/00000542-200010000-00033.
Thiopental and propofol are highly lipid-soluble, and their entry into the brain often is assumed to be limited by cerebral blood flow rather than by a diffusion barrier. However, there is little direct experimental evidence for this assumption.
The cerebral kinetics of thiopental and propofol were examined over a range of cerebral blood flows using five and six chronically instrumented sheep, respectively. Using anesthesia (2.0% halothane), three steady state levels of cerebral blood flow (low, medium, and high) were achieved in random order by altering arterial carbon dioxide tension. For each flow state, 250 mg thiopental or 100 mg propofol was infused intravenously over 2 min. To quantify cerebral kinetics, arterial and sagittal sinus blood was sampled rapidly for 20 min from the start of the infusion, and 1.5 h was allowed between consecutive infusions. Various models of cerebral kinetics were examined for their ability to account for the data.
The mean baseline cerebral blood flows for the "high" flow state were over threefold greater than those for the low. For the high-flow state the normalized arteriovenous concentration difference across the brain was smaller than for the low-flow state, for both drugs. The data were better described by a model with partial membrane limitation than those with only flow limitation or dispersion.
The cerebral kinetics of thiopental and propofol after bolus injection were dependent on cerebral blood flow, despite partial diffusion limitation. Higher flows produce higher peak cerebral concentrations.
硫喷妥钠和丙泊酚具有高度脂溶性,人们通常认为它们进入脑内的过程受脑血流量限制,而非扩散屏障限制。然而,这一假设几乎没有直接的实验证据。
分别使用5只和6只长期植入监测装置的绵羊,在一系列脑血流量范围内研究硫喷妥钠和丙泊酚的脑内动力学。采用麻醉(2.0%氟烷),通过改变动脉二氧化碳分压以随机顺序实现三种稳态脑血流量水平(低、中、高)。对于每种血流状态,在2分钟内静脉输注250mg硫喷妥钠或100mg丙泊酚。为了量化脑内动力学,从输注开始迅速采集动脉血和矢状窦血20分钟,连续输注之间间隔1.5小时。研究了各种脑内动力学模型解释数据的能力。
“高”血流状态下的平均基线脑血流量比低血流状态下的高出三倍多。对于两种药物,高血流状态下全脑标准化动静脉浓度差均低于低血流状态。与仅存在血流限制或弥散的模型相比,部分膜限制模型对数据的描述更佳。
尽管存在部分扩散限制,但推注后硫喷妥钠和丙泊酚的脑内动力学仍依赖于脑血流量。血流越高,脑内峰值浓度越高。