[奥氮平:药理学、药物动力学及治疗药物监测)。

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Rao毫升,Hiemke C,鲍曼Grasmader K, P

[奥氮平:药理学、药物动力学及治疗药物监测)。

Fortschr神经Psychiatr。2001年11月,69 (11):510 - 7。doi: 10.1055 / s - 2001 - 18381。

PubMed ID

11704898 (在PubMed

]

文摘

奥氮平是一种安全有效的抗精神病药物。经典抗精神病药物的药代动力学性质相媲美。氧化过程是由细胞色素P450介导的同工酶CYP1A2和CYP2D6的轻微程度。奥氮平的主要代谢途径是通过glucuronidation。治疗剂量导致广泛的血清水平的变化;剂量和血清浓度是线性相关的。吸烟和卡马西平诱导细胞色素P450同功酶,从而降低奥氮平血清水平。抑制CYP1A2的氟伏沙明收益率增加浓度;然而,观察临床相关的CYP2D6抑制只有结合额外的性格因素,如女性的性别或年龄。一般剂量调整不是必需的,但中度肾或肝损伤要求控制血清水平提供最大安全在奥氮平治疗。 Therapeutic drug monitoring (TDM) and toxicology studies are carried out by HPLC methods using UV or MS detection. The optimal therapeutic range of olanzapine serum levels is 20 to 40 ng/ml. Concentrations of 80 ng/ml are considered threshold for the occurrence of adverse events; however, toxicological studies showed that postmortem plasma levels are higher than antemortem levels. Lethality of high olanzapine was only observed in combination with other drugs. Moderate increases of prolactin levels were detected during administration of olanzapine. In relation to olanzapine therapy, several case reports of neutropenia and agranulocytosis appeared in the literature. Weight gain in olanzapine-treated patients does not correlate with serum levels. Olanzapine response is augmented when patients' serum levels are titrated to 20 to 40 ng/ml thereby minimizing the occurrence of side effects, thus TDM is recommended for patients treated with olanzapine.

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药物酶

药物	酶	类	生物	药理作用	行动
奥氮平	细胞色素P450 2 d6	蛋白质	人类	没有	底物 抑制剂	细节