帕罗西汀(R)稳态浓度增加美沙酮CYP2D6在广泛但不可怜的代谢。

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Begre年代,冯Bardeleben U, Ladewig D, Jaquet-Rochat年代,Cosendai-Savary L,戈利KP, Kosel M,鲍曼P Eap CB

帕罗西汀(R)稳态浓度增加美沙酮CYP2D6在广泛但不可怜的代谢。

中国Psychopharmacol。2002年4月,22 (2):211 - 5。

PubMed ID

11910269 (在PubMed

]

文摘

稳态血药浓度(R) -美沙酮(即。活动形式),(S)美沙酮和(R, S)美沙酮测量之前和之后引入帕罗西汀20毫克/天平均12天期间10成瘾者在美沙酮维持治疗病人。8个病人CYP2D6基因分型为纯合子的广泛的代谢(EMs)和两个病人的代谢一样贫穷(PMs)。帕罗西汀显著增加的两种对映体的美沙酮浓度在整个集团(意味着增加(R)美沙酮+ / - SD, 26 + / - 32%;范围内,-14% + 83%,p = 0.032;对美沙酮,49 + / - 51%;范围内,-29% + 137%,p = 0.028;美沙酮(R, S), 35 + / - 41%;范围,-20% + 112%,p = 0.032)和八国集团EMs(意味着增加32%,p = 0.036;53%,p = 0.028; and 42%, p = 0.036, for (R)-methadone, (S)-methadone, and (R,S)-methadone, respectively). On the other hand, in the two PMs, (S)-methadone but not (R)-methadone concentrations were increased by paroxetine (mean increases of 36% and 3%, respectively). Paroxetine is a strong CYP2D6 inhibitor, and these results confirm previous studies showing an involvement of CYP2D6 in methadone metabolism with a stereoselectivity toward the (R)-enantiomer. Because paroxetine is a mild inhibitor of CYP1A2, CYP2C9, CYP2C19, and CYP3A4, increase of (S)-methadone concentrations in both EMs and PMs could be mediated by inhibition of any of these isozymes.

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药物酶

药物	酶	类	生物	药理作用	行动
帕罗西汀	细胞色素P450 1 a2	蛋白质	人类	未知的	底物 抑制剂	细节
干扰素alfa-2a	细胞色素P450 1 a2	蛋白质	人类	未知的	抑制剂	细节