Pharmacokinetic-pharmacodynamic后果和临床相关性的细胞色素P450 3 a4抑制。
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梳妆台g·斯彭斯JD,贝利DG
Pharmacokinetic-pharmacodynamic后果和临床相关性的细胞色素P450 3 a4抑制。
Pharmacokinet。2000年1月,38 (1):41-57。
- PubMed ID
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10668858 (在PubMed]
- 文摘
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药物相互作用时的疗效或毒性药物改变另一种物质的管理。药代动力学的相互作用通常发生由于药物代谢的变化。细胞色素P450 (CYP) 3 a4氧化广泛的药物的代谢过程。CYP3A4的位置在小肠和肝脏许可presystemic和系统性药物代谢产生影响。还可能涉及到一些交互CYP3A4抑制剂抑制22。临床上重要的CYP3A4抑制剂包括伊曲康唑、酮康唑,克拉霉素、红霉素、奈法唑酮,例如和柚子汁。带条de同构,危及生命的心室性心律失常与QT延长,可以发生在这些抑制剂与terfenadine coadministered,阿司咪唑、cisapride或哌咪清。横纹肌溶解有关联的共同服用一些3-hydroxy-3-methylglutaryl-coenzyme还原酶抑制剂(他汀类药物)和CYP3A4抑制剂。症状性低血压可能发生当CYP3A4抑制剂给出一些dihydropyridine钙拮抗剂,与磷酸二酯酶抑制剂西地那非。政府过度镇静会导致原有的苯二氮(咪达唑仑、三唑仑、阿普唑仑或安定)或nonbenzodiazepine (zopiclone和丁螺环酮)hypnosedatives CYP3A4抑制剂。 Ataxia can occur with carbamazepine, and ergotism with ergotamine, following the addition of a CYP3A4 inhibitor. Beneficial drug interactions can occur. Administration of a CYP3A4 inhibitor with cyclosporin may allow reduction of the dosage and cost of the immunosuppressant. Certain HIV protease inhibitors, e.g. saquinavir, have low oral bioavailability that can be profoundly increased by the addition of ritonavir. The clinical importance of any drug interaction depends on factors that are drug-, patient- and administration-related. Generally, a doubling or more in plasma drug concentration has the potential for enhanced adverse or beneficial drug response. Less pronounced pharmacokinetic interactions may still be clinically important for drugs with a steep concentration-response relationship or narrow therapeutic index. In most cases, the extent of drug interaction varies markedly among individuals; this is likely to be dependent on interindividual differences in CYP3A4 tissue content, pre-existing medical conditions and, possibly, age. Interactions may occur under single dose conditions or only at steady state. The pharmacodynamic consequences may or may not closely follow pharmacokinetic changes. Drug interactions may be most apparent when patients are stabilised on the affected drug and the CYP3A4 inhibitor is then added to the regimen. Temporal relationships between the administration of the drug and CYP3A4 inhibitor may be important in determining the extent of the interaction.
DrugBank数据引用了这篇文章
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药物 酶 类 生物 药理作用 行动 Clorazepic酸 细胞色素P450 3 a4 蛋白质 人类 未知的底物细节 伊曲康唑 细胞色素P450 3 a4 蛋白质 人类 没有底物抑制剂细节 - 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Acalabrutinib 甲硫咪唑 的新陈代谢时可以减少Acalabrutinib结合甲巯基咪唑。 Acalabrutinib Amprenavir 的新陈代谢Acalabrutinib结合Amprenavir时可以减少。 Acalabrutinib Telithromycin 的新陈代谢Acalabrutinib结合Telithromycin时可以减少。 Acalabrutinib 克拉霉素 的新陈代谢时可以减少Acalabrutinib结合克拉霉素。 Acalabrutinib Telaprevir 的新陈代谢Acalabrutinib结合Telaprevir时可以减少。 Acalabrutinib Boceprevir 的新陈代谢Acalabrutinib结合Boceprevir时可以减少。 Acalabrutinib Cobicistat 的新陈代谢Acalabrutinib结合Cobicistat时可以减少。 Acalabrutinib Atazanavir 的新陈代谢Acalabrutinib结合Atazanavir时可以减少。 Acalabrutinib 胺碘酮 的新陈代谢Acalabrutinib时可以减少与胺碘酮相结合。 Acalabrutinib Ribociclib 的新陈代谢Acalabrutinib结合Ribociclib时可以减少。
