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Suicide attempt with an overdose of imatinib

机译:用过量伊马替尼自杀未遂

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Imatinib is approved for the treatment of chronic myelog-enous leukaemia (CIVIL) as well as gastrointestinal stromal tumour (GIST), both of which show dysregulated imatinib-sensitive tyrosine kinase activity. Imatinib is rapidly absorbed after oral administration (bioavailability 86%) and is mainly metabolized by the CYP3A4 and CYP3A5 isoenzymes of the liver [1]. Although the drug is usually well-tolerated, grade 1-2 adverse effects, such as muscu-loskeletal events, are frequently observed [2-4]. In a phase I clinical trial in patients with CIVIL, the minimum therapeutic dose of imatinib required to obtain an optimal therapeutic response was determined to be 300 mg day~(-1). However, the maximum tolerated dose has not yet been defined. In addition, there have been few case reports of imatinib overdose [5]. We herein report the results of a vpharmacokinetic analysis in a patient with CIVIL who took 2000 mg of imatinib as a single dose together with broti-zolam and triazolam in an attempt to commit suicide.
机译:伊马替尼被批准用于治疗慢性骨髓性白血病(CIVIL)和胃肠道间质瘤(GIST),两者均显示出对伊马替尼敏感的酪氨酸激酶活性失调。口服给药后伊马替尼迅速吸收(生物利用度为86%),主要通过肝脏的CYP3A4和CYP3A5同工酶代谢[1]。尽管该药物通常具有良好的耐受性,但经常观察到1-2级不良反应,例如肌肉骨骼疾病[2-4]。在一项针对CIVIL患者的I期临床试验中,获得最佳治疗反应所需的伊马替尼的最小治疗剂量确定为300 mg day〜(-1)。但是,最大耐受剂量尚未确定。此外,很少有伊马替尼用药过量的病例报道[5]。我们在此报告了一名CIVIL患者的v药代动力学分析结果,该患者服用2000 mg伊马替尼单剂量以及broti-zolam和triazolam以自杀。

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