Hagen N A, Foley K M, Cerbone D J, Portenoy R K, Inturrisi C E
J Pain Symptom Manage. 1991 Apr;6(3):125-8. doi: 10.1016/0885-3924(91)90961-3.
Morphine-6-glucuronide is an active metabolite of morphine that has analgesic properties and is measurable in the plasma and cerebrospinal fluid of patients treated with this opioid. Decreased clearance of the compound has been observed in patients with renal insufficiency, and this has been associated with an increase in the ratio of morphine-6-glucuronide to morphine. Clinical effects from accumulation of morphine-6-glucuronide have not been described with the exception of case reports in which patients with renal failure were noted to develop opioid toxicity with high plasma levels of the metabolite and low levels of the parent drug. We describe a patient who experienced chronic nausea and an episode of confusion while treated with a small, stable dose of oral morphine in the setting of mild renal insufficiency. Relatively high levels of morphine-6-glucuronide were measured and all symptoms resolved promptly as the concentration of this metabolite declined. This case provides suggestive evidence that morphine-6-glucuronide can produce clinically significant effects in patients with mild renal insufficiency.
吗啡-6-葡萄糖醛酸是吗啡的一种活性代谢产物,具有镇痛特性,在接受这种阿片类药物治疗的患者的血浆和脑脊液中可检测到。在肾功能不全患者中观察到该化合物的清除率降低,这与吗啡-6-葡萄糖醛酸与吗啡的比例增加有关。除了病例报告外,尚未描述吗啡-6-葡萄糖醛酸蓄积的临床效应,在这些病例报告中,肾衰竭患者被发现随着该代谢产物血浆水平升高和母体药物水平降低而出现阿片类药物毒性。我们描述了一名在轻度肾功能不全情况下接受小剂量、稳定剂量口服吗啡治疗时出现慢性恶心和一次意识模糊发作的患者。检测到相对较高水平的吗啡-6-葡萄糖醛酸,随着该代谢产物浓度下降,所有症状迅速缓解。该病例提供了提示性证据,表明吗啡-6-葡萄糖醛酸可在轻度肾功能不全患者中产生具有临床意义的效应。