Mercadante S
Department of Anesthesia and Intensive Care, Pain Relief and Palliative Care, La Maddalena Clinic, Palermo, Italy.
Cancer. 1999 Nov 1;86(9):1856-66. doi: 10.1002/(sici)1097-0142(19991101)86:9<1856::aid-cncr30>3.0.co;2-g.
Some patients with cancer pain may develop uncontrolled adverse effects, including generalized myoclonus, delirium, nausea and emesis, or severe sedation before achieving adequate analgesia during opioid dose titration. Sequential therapeutic trials should be considered to determine the most favorable drug.
Recent literature was taken into account when reviewing the rationale and potential of opioid rotation.
When aggressive attempts to prevent adverse effects fail, drug rotation should be considered, because sequential therapeutic trials can be useful in identifying the most favorable drug. Different mechanisms, including receptor activity, the asymmetry in cross-tolerance among different opioids, different opioid efficacies, and accumulation of toxic metabolites can explain the differences in analgesic or adverse effect responses among opioids in a clinical setting.
When pain is relieved inadequately by opioid analgesics given in a dose that causes intolerable side effects despite routine measures to control them, treatment with the same opioid by an alternative route or with an alternative opioid administered by the same route should be considered. Opioid rotation may be useful in opening the therapeutic window and for establishing a more advantageous analgesia/toxicity relationship. By substituting opioids and using lower doses than expected according to the equivalency conversion tables, it is possible in the majority of cases to reduce or relieve the symptoms of opioid toxicity in those patients who were highly tolerant to previous opioids while improving analgesia and, as a consequence, the opioid responsiveness.
一些癌症疼痛患者在阿片类药物剂量滴定过程中,在获得充分镇痛之前可能会出现无法控制的不良反应,包括全身性肌阵挛、谵妄、恶心和呕吐,或严重镇静。应考虑进行序贯治疗试验以确定最适宜的药物。
在回顾阿片类药物轮换的基本原理和潜力时考虑了近期的文献。
当积极预防不良反应的尝试失败时,应考虑药物轮换,因为序贯治疗试验有助于确定最适宜的药物。不同的机制,包括受体活性、不同阿片类药物之间交叉耐受性的不对称性、不同的阿片类药物效力以及有毒代谢产物的蓄积,可以解释临床环境中阿片类药物在镇痛或不良反应反应方面的差异。
当给予阿片类镇痛药的剂量在采取常规措施控制副作用的情况下仍导致难以忍受的副作用,而疼痛缓解不充分时,应考虑通过替代途径使用相同的阿片类药物或通过相同途径使用替代阿片类药物进行治疗。阿片类药物轮换可能有助于打开治疗窗口并建立更有利的镇痛/毒性关系。通过替代阿片类药物并使用比等效转换表预期更低的剂量,在大多数情况下有可能减轻或缓解那些对先前阿片类药物高度耐受的患者的阿片类药物毒性症状,同时改善镇痛效果,从而提高阿片类药物的反应性。