普伐他汀的临床药物动力学:药代动力学事件的机制。
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Hatanaka T
普伐他汀的临床药物动力学:药代动力学事件的机制。
Pharmacokinet。2000年12月,39 (6):397 - 412。doi: 10.2165 / 00003088-200039060-00002。
- PubMed ID
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11192473 (在PubMed]
- 文摘
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普伐他汀,3-hydroxy-3-methylglutaryl-coenzyme(β)还原酶抑制剂(他汀类药物)广泛应用于鸡蛋的管理,具有独特的药代动力学特征在这个类的成员。许多体内和体外人类和动物研究表明,主动运输机制共同作用的降胆固醇的药物动力学。普伐他汀的口服生物利用度很低,因为不完整的吸收和初步的效果。药物迅速的上半部分小肠吸收,可能通过proton-coupled carrier-mediated运输,然后被肝脏由sodium-independent胆汁酸转运体。大约一半的普伐他汀提取通过门静脉到达肝脏,肝脏,肝提取,这主要归因于胆汁排泄,是由一个主主动运输机制。化学降解产生的主要代谢物在胃里而不是在肝脏细胞色素P450-dependent新陈代谢。完整的药物及其代谢产物通过肝和肾的路线,和管状分泌肾排泄的主要机制。普伐他汀的双重途径,消除减少剂量调整如果肝脏或肾脏功能受损,并减少药物的相互作用与其他他汀类药物的可能性。这在很大程度上是通过代谢消除。低蛋白结合比其他他汀类药物减弱的倾向位移高度蛋白结合的药物。 Although all statins show a hepatoselective disposition, the mechanism for pravastatin is different from that of the others. There is high uptake of pravastatin by the liver via an active transport mechanism, but not by other tissues because of its hydrophilicity, whereas the disposition characteristics of other statins result from high hepatic extraction because of high lipophilicity. These pharmacokinetic properties of pravastatin may be the result of the drug being given in the pharmacologically active open hydroxy acid form and the fact that its hydrophilicity is markedly higher than that of other statins. The nature of the pravastatin transporters, particularly in humans, remains unknown at present. Further mechanistic studies are required to establish the pharmacokinetic-pharmacodynamic relationships of pravastatin and to provide the optimal therapeutic efficacy for various types of patients with hypercholesterolaemia.
DrugBank数据引用了这篇文章
- 药物
- 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
在您的软件的交互普伐他汀 Boceprevir 普伐他汀的血清浓度时可以增加与Boceprevir相结合。 普伐他汀 依法韦伦 普伐他汀的血清浓度时可以减少结合依法韦伦。
