fluvastatin的临床药物动力学。
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经文CD,派普农协
fluvastatin的临床药物动力学。
40 Pharmacokinet。2001; (4): 263 - 81。
- PubMed ID
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11368292 (在PubMed]
- 文摘
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Fluvastatin,第一个完全合成β-还原酶抑制剂,被证明能降低胆固醇hyperlipidaemia患者,以防止后续建立冠心病患者冠状动脉事件,并改变内皮功能和斑块稳定的动物模型。Fluvastatin相对亲水性,与半合成β-还原酶抑制剂相比,因此,它是广泛地从胃肠道吸收。吸收后,它几乎是完全提取并在肝脏新陈代谢2羟化代谢产物和N-desisopropyl代谢物,在胆汁中排出。大约有95%的剂量是粪便,恢复60%的剂量恢复3代谢物。6-hydroxy和N-desisopropyl fluvastatin代谢物完全由细胞色素P450 (CYP) 2 c9,不积累在血液里。CYP2C9 CYP3A4, CYP2C8和CYP2D6 5-hydroxy fluvastatin代谢物。由于其亲水的性质和广泛的血浆蛋白结合,fluvastatin有体积小以最小的浓度分布在肝外组织。fluvastatin的药物代谢动力学情况是不受肾功能的影响,由于其广泛的代谢和胆汁排泄;有限的数据在肝硬化患者建议口服间隙减少30%。年龄和性别不影响fluvastatin的性格。 CYP3A4 inhibitors (erythromycin, ketoconazole and itraconazole) have no effect on fluvastatin pharmacokinetics, in contrast to other HMG-CoA reductase inhibitors which are primarily metabolised by CYP3A and are subject to potential drug interactions with CYP3A inhibitors. Coadministration of fluvastatin with gastrointestinal agents such as cholestyramine, and gastric acid regulating agents (H2 receptor antagonists and proton pump inhibitors), significantly alters fluvastatin disposition by decreasing and increasing bioavailability, respectively. The nonspecific CYP inducer rifampicin (rifampin) significantly increases fluvastatin oral clearance. In addition to being a CYP2C9 substrate, fluvastatin demonstrates inhibitory effects on this isoenzyme in vitro and in vivo. In human liver microsomes, fluvastatin significantly inhibits the hydroxylation of 2 CYP2C9 substrates, tolbutamide and diclofenac. The oral clearances of the CYP2C9 substrates diclofenac, tolbutamide, glibenclamide (glyburide) and losartan are reduced by 15 to 25% when coadministered with fluvastatin. These alterations have not been shown to be clinically significant. There are inadequate data evaluating the potential interaction of fluvastatin with warfarin and phenytoin, 2 CYP2C9 substrates with a narrow therapeutic index, and caution is recommended when using fluvastatin with these agents. Fluvastatin does not appear to have a significant effect on other CYP isoenzymes or P-glycoprotein-mediated transport in vivo.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物酶
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药物 酶 类 生物 药理作用 行动 Fluvastatin 细胞色素P450 2 c8 蛋白质 人类 未知的底物抑制剂细节 Fluvastatin 细胞色素P450 2 c9 蛋白质 人类 未知的底物抑制剂细节 Fluvastatin 细胞色素P450 2 d6 蛋白质 人类 未知的底物细节 Fluvastatin 细胞色素P450 3 a4 蛋白质 人类 未知的底物抑制剂细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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药物 交互 整合药物之间
在您的软件的交互Fluvastatin 苯妥英 的血清浓度Fluvastatin时可以减少与苯妥英相结合。 Fluvastatin Fosphenytoin 的血清浓度Fluvastatin可以结合Fosphenytoin时下降。
