Oxycodone controlled release in cancer pain management.
Oxycodone controlled release in cancer pain management.
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DOI：
10.2147/tcrm.2006.2.3.229
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发表时间：
2006-09
影响因子：
2.8
通讯作者：
Biancofiore G
中科院分区：
文献类型：
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作者：
Biancofiore G
口服阿片类药物是慢性癌症疼痛的首选治疗方法。根据世界卫生组织（世卫组织）的指南，吗啡是治疗中度至重度癌症疼痛的首选强阿片类药物。世卫组织的这一建议是基于可获得性、临床医生熟悉、已确立的有效性、管理简单以及相对便宜的成本。它并不是基于已证实的治疗优于其他选择。使用一种阿片类药物后疼痛缓解不足或出现无法忍受的副作用的患者，通常可以用另一种药物或以不同途径给药的同一药物成功治疗。阿片类药物轮换，或改用替代阿片类药物，有助于一些患者更好地控制疼痛，减少相关不良反应。羟考酮是一种μ-阿片受体特异性配体，具有明显的激动剂性质。它是一种有效的阿片类药物，部分是κ受体激动剂。像吗啡和其他纯激动剂一样，羟考酮的镇痛作用没有已知的上限。羟考酮的活性代谢物（如羟吗啡酮）可能在羟考酮介导的镇痛中起重要作用。羟考酮与吗啡的主要药代动力学差异在于口服生物利用度。羟考酮的生物利用度约为60%，吗啡的生物利用度为20%。控释氧可酮以双指数方式被吸收。其中有一个快速相，平均半衰期为37 min，占剂量的38%；还有一个慢相，半衰期为6.2 h，占剩余剂量的62%。羟考酮的消除因肾功能衰竭而受损，因为分布量增加而清除率降低。大量研究证明，控释羟考酮对癌症疼痛的控制效果至少与吗啡、速释羟考酮和氢吗啡酮相当。它的毒性似乎比吗啡要好。实际上有几个例子表明中枢神经系统的副作用发生率较低。因此，有可能得出结论，羟考酮在治疗中度至重度癌症疼痛方面是吗啡的有效替代品，也可作为一线治疗。
Oral opioids are the treatment of choice for chronic cancer pain. Morphine is the strong opioid of choice for the treatment of moderate to severe cancer pain according to guidelines from the World Health Organization (WHO). This recommendation by the WHO was derived from availability, familiarity to clinicians, established effectiveness, simplicity of administration, and relative inexpensive cost. It was not based on proven therapeutic superiority over other options. Patients who experience inadequate pain relief or intolerable side effects with one opioid may often be successfully treated with another agent or with the same agent administered by a different route. Opioid rotation, or switching to an alternative opioid, helps some patients achieve better pain control with fewer associated adverse effects. Oxycodone is a μ-opioid receptor specific ligand, with clear agonist properties. It is an active potent opioid, which is in part a κ-receptor agonist. Like morphine and other pure agonists, there is no known ceiling to the analgesic effects of oxycodone. The active metabolites of oxycodone (eg, oxymorphone) could be important in oxycodone-mediated analgesia. The main pharmacokinetic difference between oxycodone and morphine is in oral bioavailability. The bioavailability of oxycodone is >60% and the bioavailability of morphine is 20%. Controlled-release oxycodone is absorbed in a bi-exponential fashion. There is a rapid phase with a mean half-life of 37 min, accounting for 38% of the dose, and a slow phase with a half-life of 6.2 h, which accounts for the residual 62%. Oxycodone elimination is impaired by renal failure because there are both an increased volume of distribution and reduced clearance. A lot of studies prove that the efficacy of controlled-release oxycodone in cancer-pain control is at least the same as morphine, immediate-release oxycodone and hydromorphone. Its toxicity profile seems better than that of morphine. There are actually several illustrations of a lower incidence of side-effects in the central nervous system. It is therefore possible to conclude that oxycodone represents a valid alternative to morphine in the management of moderate to severe cancer pain, also as first-line treatment.