Chair and Department of Palliative Medicine, Poznan University of Medical Sciences, Poznan, Poland.
Pharmacology. 2011;87(5-6):274-85. doi: 10.1159/000326085. Epub 2011 Apr 15.
In most cancer patients, pain is successfully treated with pharmacological measures using opioid analgesics for moderate to severe pain (strong opioids) alone or in combination with adjuvant analgesics (coanalgesics). Opioids for mild to moderate pain (weak opioids) are usually recommended in the treatment of cancer pain of mild to moderate intensity. There is a debate whether the second step of the WHO analgesic ladder comprising weak opioids such as tramadol, codeine and dihydrocodeine is still needed for the treatment of cancer and chronic pain since low doses of strong opioids show similar efficacy. However, many patients with mild, moderate and in some cases strong pain intensity are still successfully treated with weak opioids. All these drugs are metabolized through CYP2D6, an important enzyme for approximately 25% of all drugs administered in clinical practice. The aim of this review is to summarize data on the impact of CYP2D6 polymorphism on pharmacokinetics, pharmacodynamics and adverse effects of weak opioids.
在大多数癌症患者中，疼痛可以通过使用阿片类镇痛药进行药物治疗来成功控制，对于中重度疼痛（强阿片类药物），单独使用或联合辅助镇痛药物（协同镇痛药）均可；对于轻至中度疼痛（弱阿片类药物），通常建议在治疗轻至中度强度的癌症疼痛时使用。关于是否仍需要使用包括曲马多、可待因和二氢可待因在内的弱阿片类药物作为世界卫生组织镇痛阶梯的第二步来治疗癌症和慢性疼痛存在争议，因为低剂量的强阿片类药物显示出相似的疗效。然而，许多轻、中、重度疼痛强度的患者仍能成功地使用弱阿片类药物进行治疗。所有这些药物都通过 CYP2D6 代谢，CYP2D6 是大约 25%在临床实践中使用的药物的重要酶。本综述的目的是总结 CYP2D6 多态性对弱阿片类药物药代动力学、药效学和不良反应的影响数据。
