在癌症患者大剂量的药物胃复安。

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麦戈文EM, Grevel J,布赖森SM

在癌症患者大剂量的药物胃复安。

Pharmacokinet。1986; 11 - 12月11 (6):415 - 24。doi: 10.2165 / 00003088-198611060-00001。

PubMed ID
3542335 (在PubMed
]
文摘

新的细胞毒性药物治疗方案的引入与增加有关不良反应的发生率和严重程度。这反过来又强调了需要更有效的辅助治疗。使用胃复安的恶心和呕吐的预防,在静脉注射高剂量(50至1000毫克),自1981年以来,已经建立了。脂溶性药物,胃复安有大量分布。报道后的平均值高剂量范围在2.8和4.6 L /公斤之间。全身清除半衰期和终端的平均值范围从0.31到0.69 L / kg / h和从4.5到8.8小时,分别。这些药代动力学参数的值基本上是类似后获得常规剂量(少于50毫克)。药代动力学参数似乎未受到年龄的影响,虽然没有大剂量的儿童进行了研究。体重显然与间隙。一个肾功能指标对终端半衰期和间隙的影响已被证明,这很奇怪因为肾清除率仅占总数的20%。 No thorough investigations exist which examine the influence of hepatic disease, cancer type and cytotoxic drug regimen on the disposition of metoclopramide. A relationship between dose (or concentration) and therapeutic or adverse effects of metoclopramide is outlined. The therapeutic benefit of high doses (up to 14 mg/kg) may be dependent on age, and on the combination of cytotoxic drugs. The advantages of high doses of metoclopramide are most apparent when the drug is used as protection against the adverse effects of high doses of cisplatin (greater than 60 mg/m2). Despite considerable pharmacokinetic variability, intravenous administration of high doses of metoclopramide is relatively safe due to its large therapeutic index.

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