肝脏疾病对药物动力学的影响。一个更新。

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Rodighiero V

肝脏疾病对药物动力学的影响。一个更新。

Pharmacokinet。1999年11月,37 (5):399 - 431。

PubMed ID

10589374 (在PubMed

]

文摘

肝病可以修改biotransformed药物的代谢动力学的肝脏。本文更新这一领域的最新进展,特别强调细胞色素P450 (CYP)。在临床药理学CYP是一个迅速扩大的领域。目前可获得的信息对特定亚型参与药物代谢大大增加了最新多年,但知识仍然是不完整的。研究肝脏疾病的影响在特定的CYP同功酶显示一些亚型是肝脏疾病比其他人更敏感。特定的详细知识同工酶参与代谢的药物和肝脏疾病的影响,酶可以提供合理依据剂量调整患者的肝损伤。肝脏代谢药物的能力取决于肝血流和肝酶活性,可影响肝脏疾病。此外,肝衰竭可以影响药物血浆蛋白的结合。这些变化可能发生单独或结合;当他们共存药物动力学是协同效应,不仅添加剂。 The kinetics of drugs with a low hepatic extraction are sensitive to hepatic failure rather than to liver blood flow changes, but drugs having a significant first-pass effect are sensitive to alterations in hepatic blood flow. The drugs examined in this review are: cardiovascular agents (angiotensin converting enzyme inhibitors, angiotensin II receptor antagonists, calcium antagonists, ketanserin, antiarrhythmics and hypolipidaemics), diuretics (torasemide), psychoactive and anticonvulsant agents (benzodiazepines, flumazenil, antidepressants and tiagabine), antiemetics (metoclopramide and serotonin antagonists), antiulcers (acid pump inhibitors), anti-infectives and antiretroviral agents (grepafloxacin, ornidazole, pefloxacin, stavudine and zidovudine), immunosuppressants (cyclosporin and tacrolimus), naltrexone, tolcapone and toremifene. According to the available data, the kinetics of many drugs are altered by liver disease to an extent that requires dosage adjustment; the problem is to quantify the required changes. Obviously, this requires the evaluation of the degree of hepatic impairment. At present there is no satisfactory test that gives a quantitative measure of liver function and its impairment. A critical evaluation of these methods is provided. Guidelines providing a rational basis for dosage adjustment are illustrated. Finally, it is important to consider that liver disease not only affects pharmacokinetics but also pharmacodynamics. This review also examines drugs with altered pharmacodynamics.

beplay体育安全吗DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
Garenoxacin	细胞色素P450 1 a2	蛋白质	人类	没有	抑制剂	细节
Grepafloxacin	细胞色素P450 1 a2	蛋白质	人类	未知的	底物 抑制剂	细节