的临床药物动力学vinorelbine (Navelbine)。

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Wargin佤邦,卢卡斯VS

的临床药物动力学vinorelbine (Navelbine)。

Semin 10月杂志。1994;21(生理10):21-7。

PubMed ID

7973765 (在PubMed

]

文摘

Vinorelbine (Navelbine;伯勒斯威康公司Research Triangle Park,数控;皮埃尔·法布尔药剂,法国巴黎)是一种半合成长春花生物碱剂的结构修改catharanthine核上的传授亲油性增加。因此,vinorelbine似乎拥有一个更高的治疗指数和药代动力学性质不同于其他销售长春花生物碱。Vinorelbine一直在量化生物测量矩阵的总辐射、放射免疫检定法和高效液相色谱法。因为它是特定的父药物,高效液相色谱法生成的最可靠的药代动力学数据。Vinorelbine高度绑定到血小板和淋巴细胞,也必将α1-acid糖蛋白,白蛋白和脂蛋白。药物经历重大通过肝脏代谢和消除,代谢产物主要是分泌胆汁。两个可能vinorelbine代谢物,vinorelbine N-oxide deacetylvinorelbine,已经被分离出来并识别在人类尿液和非常低的浓度出现在等离子体。尿排泄的药物占不到20%不变的静脉注射剂量,与粪便消除占一个额外的30%到60%。 The pharmacokinetic profile of vinorelbine after intravenous bolus or infusion is characterized by triexponential decay. Initial rapid decay is due primarily to distribution into tissues in the peripheral compartments. There is a prolonged terminal phase due to relatively slow efflux of the drug from peripheral compartments, which results in a long terminal phase half-life, with average values ranging from 27.7 to 43.6 hours. Plasma clearance of vinorelbine is high, approaching hepatic blood flow in humans, and its volume of distribution is large, indicating extensive extravascular distribution. In comparison to vinblastine or vincristine, vinorelbine has a higher clearance and a larger volume of distribution than either drug, and a half-life shorter than vinblastine but longer than vincristine. There is no relationship between the age of the patient and the pharmacokinetic parameters of vinorelbine, and coadministration of cisplatin does not appear to influence the pharmacokinetics of vinorelbine. Vinorelbine is the first vinca alkaloid to show promising efficacy following oral administration, and this has led to the development of a liquid-filled, soft-gelatin capsule dosage form. The absolute bioavailability of vinorelbine from this dosage form was 27% when intravenous doses of 30 mg/m2 were compared with oral doses of 100 mg/m2.

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药物

Vinorelbine