阿片类药物的Pharmacokinetic-pharmacodynamic建模。

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Lotsch J

阿片类药物的Pharmacokinetic-pharmacodynamic建模。

J疼痛症状管理。2005年5月,29(生理):s90 - 103。doi: 10.1016 / j.jpainsymman.2005.01.012。

PubMed ID

15907650 (在PubMed

]

文摘

阿片类药物的影响通常平行但血浆浓度时间转变。这时间转变阿片类药物之间的不同。它很小alfentanil或remifentanil和很长的吗啡的活性代谢物,morphine-6-glucuronide (M6G)。数学建模与实验技术这些pharmacokinetic-pharmacodynamic (PK / PD)是1970年代末开发的关系。等离子体浓度和效果之间的延迟是由室引入假设的影响,与等离子体室由一阶传递函数与速率常数k (e0)。然后与浓度的影响在影响站点等标准的药效学模型乙状结肠(E (max))模型或权力模型,根据实际效果的措施。这些原则首次应用于阿片类药物芬太尼,1985年alfentanil。从那时起,阿片类药物的PK / PD反复评估,使用脑电图派生参数,瞳孔大小,实验和临床疼痛效果的措施。阿片类药物的芬太尼集团、美沙酮、吗啡,和piritramid今天特点对他们的PK / PD特性。Alfentanil和remifentanil很快等离子体和效果之间的平衡和平衡阿片类药物半衰期约1分钟。beplayapp They are followed by fentanyl and sufentanil, each with equilibration half-lives of about 6 min. Methadone equilibrates with a half-life of about 8 min. Morphine, in contrast, equilibrates with a half-life of 2-3 h. The slowest opioid with respect to plasma-effect site transfer is M6G, with an equilibration half-life of about 7 h. PK/PD modeling has advanced the understanding of the time course of the clinical effects of opioids after various dosing regimens. It may provide a rational basis for the selection of opioids in clinical circumstances. PK/PD modeling of opioids may also be employed for the design and the interpretation of experiments addressing clinical effects of opioids.

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药物

吗啡