麻培班疼痛规范化治疗.ppt

Bisphosphonates Overview * CONTIN ?控释技术保证美施康定?血药浓度相对平稳。从图中可以看出，美施康定?从口服后1h-1.5h开始显效，与即释硫酸吗啡片不同，美施康定血药浓度相对平稳，在12小时内没有明显的波峰波谷变化。而即释硫酸吗啡片血药浓度曲线呈明显的波峰波谷变化。 Bisphosphonates Overview * 美施康定的引入大大促进了我国癌痛控制事业的发展。美施康定引入的当年，即：1994年，我国医用吗啡的生产量就首次突破了100公斤。 Bisphosphonates Overview * * 如何确定初始剂量呢？ 如何进行剂量滴定呢？（如上） Bisphosphonates Overview * Significant pharmacokinetic features of oxycodone include the following: Short elimination half-life—3.2 hours for immediate-release oxycodone and 4.5 hours following the administration of OxyContin? (oxycodone HCl controlled-release) Tablets C-II—allows steady-state levels to be achieved within 24 hours to 36 hours; this facilitates prompt assessment of analgesia and dose titration.1 Oral bioavailability of 60% to 87%. Higher oral bioavailability than morphine because of less presystemic first-pass metabolism.1,40 No accumulation of oxycodone or metabolites during continuous dosing.1 Oxycodone is demethylated to oxymorphone and noroxycodone and their glucuronides, conjugated in the liver, and excreted in the urine. Its metabolites, oxymorphone and noroxycodone, do not appear to contribute to the pharmacodynamic effects of the drug. Noroxycodone is the major circulating metabolite, but is reported to be a considerably weaker analgesic than oxycodone. Oxymorphone, although possessing analgesic activity, is present in the plasma only in low concentrations. The correlation between oxymorphone concentrations and opioid effects is much less than that seen with oxycodone plasma concentrations.1 Bisphosphonates Overview * 此外，见幻灯片内容。 Bisphosphonates Overview * 奥施康定采用了全球保护的专利技术－AcroContin控释技术，即控释与即释相结合，38%的药物即释、62％的药物缓释，使羟考酮不仅能够持续延长疼痛控制时间，还能够在服药后1小时内迅速起效 Bisphosphonates Overview * 疼痛就性质来讲主要分为3类：躯体痛、内脏痛、神经病理性疼痛。 奥施康定对躯体痛的疗效与吗啡相似，下边重点介绍一下奥施康定对比较难治的神经病理性疼痛和内脏痛的疗效。 从表中我们可以看到，与其他阿片类药物相比，羟考酮对阿片受体的作用特点是：除与吗啡一样对μ 受体有非常强的作用之外，与其它常用阿片药相比，它对κ受体的亲和力更强，，而κ受体与内脏痛密切相关。 第一个吗啡控释片－美施康定所采用先进、独特的“CONTIN”控释技术 硫酸吗啡控释片（美施康定?） 薄膜包衣 蜡质颗粒 压缩成片 纤维颗粒 药物活性物质 纤维颗粒 的水合作用 蜡质