Takahashi Masahiko, Ohara Takeshi, Yamanaka Hiroyuki, Shimada Akira, Nakaho Toshimichi, Makoto Yamamuro
Division of Pain Control, Department of Anesthesiology and Emergency Medicine, Tohoku University Postgraduate Medical School, 1-1 Seiryo, Aoba-ku, Sendai 980-8574, Japan.
Palliat Med. 2003 Dec;17(8):673-8. doi: 10.1191/0269216303pm824oa.
To provide additional pharmacokinetic evidence for the oral-to-parenteral relative potency ratio of 1:2 to 1:3 for chronic morphine use in a palliative care setting, we determined the plasma concentrations of morphine and its major metabolites, morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G), in hospitalized advanced cancer patients maintained on long-term oral or intravenous morphine. There were significant linear correlations between daily doses of morphine and plasma concentrations (molar base) of morphine, M3G and M6G for both routes of administration. The oral-to-intravenous relative ratios of the regression coefficients were 2.9 for morphine and 1.8 for morphine + M6G. The morphine kinetic variables were not significantly influenced by any hepato-renal biochemical markers. These results support the commonly used oral-to-intravenous relative potency ratio of 1:2 to 1:3 in patients with cancer pain receiving chronic morphine treatment.
为了提供更多药代动力学证据,以支持在姑息治疗环境中慢性使用吗啡时口服与胃肠外给药的相对效价比为1:2至1:3,我们测定了长期口服或静脉注射吗啡的住院晚期癌症患者体内吗啡及其主要代谢产物吗啡-3-葡萄糖醛酸苷(M3G)和吗啡-6-葡萄糖醛酸苷(M6G)的血浆浓度。两种给药途径下,吗啡的每日剂量与吗啡、M3G和M6G的血浆浓度(摩尔碱)之间均存在显著的线性相关性。回归系数的口服与静脉相对比,吗啡为2.9,吗啡+M6G为1.8。吗啡动力学变量未受到任何肝肾生化指标的显著影响。这些结果支持了在接受慢性吗啡治疗的癌症疼痛患者中常用的口服与静脉相对效价比为1:2至1:3。