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首页> 外文期刊>Journal of pharmaceutical sciences. >Cerebral kinetics of oxycodone in conscious sheep.
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Cerebral kinetics of oxycodone in conscious sheep.

机译：羟考酮在有意识的绵羊中的脑动力学。

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Oxycodone is an opioid analgesic that is administered orally or parenterally. The time-course of opioid action is a function of the systemic kinetics of the opioid, and the rate and extent of its entry into the brain and central nervous system. The latter is incompletely understood for oxycodone. Therefore, the cerebral kinetics of oxycodone was quantified using a conscious chronically instrumented sheep preparation. Five sheep were administered oxycodone as intravenous infusions (30 mg over 4 min). Using hybrid physiologically based kinetic models, cerebral kinetics was estimated from arterio-sagittal sinus concentration gradients and cerebral blood flow (CBF). A two-compartment membrane-limited model best described the data. The volume of the first brain compartment was 35.4 mL with a half-life of equilibrium of 0.6 min. The brain:blood equilibration of oxycodone was relatively slow (half-life of 7.2 min), with a large deep cerebral distribution volume (222.8 mL) for the second compartment and a moderate membrane permeability of 54.8 mL/min, which exceeded the nominal CBF (40 mL/min). Drug retention in the brain was 1.3% after 45 min. In conclusion, pharmacokinetic modelling of oxycodone showed a delayed equilibration between brain and blood of a nature that would be affected by changes in both CBF and blood brain barrier permeability.
机译：羟考酮是口服或胃肠外给药的阿片类镇痛药。阿片类药物作用的时程是阿片类药物的全身动力学以及其进入大脑和中枢神经系统的速率和程度的函数。对于羟考酮，后者的理解不完全。因此，使用有意识的慢性仪器化绵羊制剂对羟考酮的脑动力学进行了定量。给五只绵羊静脉注射羟考酮（30分钟内4分钟）。使用基于混合生理学的动力学模型，从动脉矢状窦浓度梯度和脑血流量（CBF）估算脑动力学。两室膜限制模型最能描述数据。第一脑室的体积为35.4 mL，平衡的半衰期为0.6分钟。羟考酮的脑：血平衡相对较慢（半衰期为7.2分钟），第二部分的大深度大脑分布体积（222.8 mL）和中等的膜通透性为54.8 mL / min，超过了标称CBF （40 mL / min）。 45分钟后，大脑中的药物保留率为1.3％。总之，羟考酮的药代动力学模型显示大脑和血液之间的平衡延迟，这种平衡受CBF和血脑屏障通透性的变化影响。

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