Pharmacokinetics of granisetron in adults and children with malignant diseases.
Pharmacokinetics of granisetron in adults and children with malignant diseases.
复制标题
格拉司琼在成人和儿童恶性疾病中的药代动力学。
DOI：
--
复制
发表时间：
2001
影响因子：
2
通讯作者：
K. Hirano
中科院分区：
文献类型：
--
作者：
I. Wada;T. Takeda;M. Sato;H. Saitoh;T. Nakabayashi;K. Miño;T. Honma;M. Takada;K. Hirano
格拉司琼（GRN）广泛用于各种癌症患者化疗引起的呕吐和恶心。然而，GRN的药代动力学在这些患者中尚未得到充分评价，其给药方案仍有争议。在这项研究中，我们测定了肺癌患者和癌症儿童静脉输注后血清和尿液中的GRN水平。在肺癌患者中，t（1/2 β）、浓度-时间曲线下面积（AUC）和Vd（β）的个体间差异相对小于先前健康受试者报告的预期，而健康受试者中的t（1/2 β）延长超过5倍。肺癌患者尿中原型GRN的排泄量约为1000 mg/kg。15%的剂量，与以前的报告一致，一个人表现出更高的尿排泄（约。45%）。GRN在儿童癌症患者中的药代动力学参数在个体之间存在显著差异，并且一些儿童患者的t（1/2 β）小于成人患者。在这些情况下，GRN应该以较短的间隔施用。这些结果表明，GRN的药代动力学研究是必要的，规划剂量方案和管理化疗引起的呕吐和恶心。
Granisetron (GRN) is widely used for patients with various cancers who suffer from chemotherapy-induced vomiting and nausea. The, pharmacokinetics of GRN has not been fully evaluated in such patients, however, and its dosage regimen is still controversial. In this study, we determined GRN levels in serum and urine from lung cancer patients and children suffering from cancer after intravenous infusion. In lung cancer patients, the interindividual variations in t(1/2beta), area under the concentration-time curve (AUC), and Vd(beta) were relatively smaller than expected from previous reports on healthy subjects, while t(1/2beta) was prolonged more than 5-fold in healthy subjects. Urinary excretion of unchanged GRN in lung cancer patients was ca. 15% of dose, consistent with previous reports, and one individual demonstrated an even higher urinary excretion (ca. 45%). The pharmacokinetic parameters of GRN in child cancer patients varied markedly among individuals, and some child patients had smaller t(1/2beta) than adult patients. In these cases, GRN should be administered at shorter intervals. These results suggested that a pharmacokinetic study of GRN was necessary for planning a dosage regimen and managing chemotherapy-induced vomiting and nausea.