羟考酮:药理和临床检查。

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德加利西亚语,冈萨雷斯男爵M, Espinosa Arranz E

羟考酮:药理和临床检查。

中国Transl杂志。2007;9 (5):298 - 307。

PubMed ID

17525040 (在PubMed

]

文摘

羟考酮是一种半合成的阿片类药物与受体激动剂活动μ,卡帕和δ受体。等价对吗啡是1:2。其效果开始一小时后管理和持续12 h缓释制剂。血浆半衰期是3 - 5 h(吗啡的一半)和稳定的等离子体水平达到24 h内吗啡(2天)。口服生物利用度范围从60到87%,血浆蛋白结合是45%。大部分的药物在肝脏代谢,其余由肾脏排泄及其代谢物。两个主要代谢物羟吗啡酮——这也是一个非常有效的镇痛noroxycodone,虚弱的止痛剂。羟考酮代谢比吗啡更可预测,因此滴定是容易。羟考酮具有相同的作用机制与其他阿片类药物:绑定一个受体,抑制adenylyl-cyclase hyperpolarisation神经元,兴奋性下降。这些机制还在依赖的发病中发挥作用和宽容。 The clinical efficacy of oxycodone is similar to that of morphine, with a ratio of 1/1.5-2 for the treatment of cancer pain. Long-term administration may be associated with less toxicity in comparison with morphine. In the future, both opioids could be used simultaneously at low doses to reduce toxicity. It does not appear that there are any differences between immediate and slow-release oxycodone, except their half-life is 3-4 h, and 12 h, respectively. In Spain, controlled-release oxycodone (OxyContin) is marketed as 10-, 20-, 40- or 80-mg tablets for b.i.d. administration. Tablets must be taken whole and must not be broken, chewed or crushed. There is no food interference. The initial dose is 10 mg b.i.d. for new treatments and no dose reduction is needed in the elderly or in cases of moderate hepatic or renal failure. Immediate-release oxycodone (OxyNorm) is also available in capsules and oral solution. Side effects are those common to opioids: mainly nausea, constipation and drowsiness. Vomiting, pruritus and dizziness are less common. The intensity of these side effects tends to decrease over the course of time. Oxycodone causes somewhat less nausea, hallucinations and pruritus than morphine.

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药物靶点

药物	目标	类	生物	药理作用	行动
羟考酮	三角洲类型阿片受体	蛋白质	人类	是的	受体激动剂	细节
羟考酮	Kappa-type阿片受体	蛋白质	人类	是的	受体激动剂	细节
羟考酮	Mu-type阿片受体	蛋白质	人类	是的	受体激动剂	细节