sitaxentan在西地那非的影响在健康受试者药代学和药效学。

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达沃F,克莱默,威尔金斯先生

sitaxentan在西地那非的影响在健康受试者药代学和药效学。

Br中国新药杂志。2010年1月,69 (1):23-6。doi: 10.1111 / j.1365-2125.2009.03541.x。

PubMed ID

20078609 (在PubMed

]

文摘

这个话题已经知道是什么:* Endothelin-A受体拮抗剂(ETRAs)和phosphodiesterase-type 5抑制剂单一药物治疗肺动脉高血压的批准;结合代理从这两个药物类可能是有益的。*有一个重要的药代动力学(PK)之间的交互应用波生坦ETRA phosphodiesterase-type 5抑制剂西地那非。*本研究评估是否ETRA sitaxentan同样影响西地那非的PK。这个研究补充道:*这项研究表明sitaxentan对西地那非PK和药效学的影响不大,不需要调整剂量或代理在与sitaxentan合并施打西地那非。目的:本研究评估sitaxentan在药效学的影响[系统性血压(BP)]和西地那非在健康志愿者的药代动力学(PK)参数。方法:健康受试者(60年,n = 24)随机分成两组序列。组1收到sitaxentan钠100毫克每日(7天),紧随其后的是安慰剂(7天)。第二组接受安慰剂(7天),其次是sitaxentan钠100毫克(7天)。7天的治疗期间,参与者收到了西地那非100毫克。 PK parameters and BP were analysed on day 7 in each treatment period. RESULTS: Sildenafil exposure was slightly higher [AUC(infinity) geometric mean ratio (GMR), 128%] when co-administered with sitaxentan 100 mg vs. placebo, demonstrating a weak, but statistically significant interaction (90% confidence interval 115.5%, 141.2%). The mean maximum positive (E(max)+) and maximum negative (E(max)-) changes from baseline in both systolic and diastolic BP were comparable for sitaxentan and placebo (range 4.8-7.3 mmHg) with three of four geometric mean ratios falling within the equivalence window, suggesting that the drug interaction was not clinically significant. Adverse events were similar between sitaxentan 100 mg (39%) and placebo (30%). No deaths or serious adverse events occurred during the study. CONCLUSION: The dose of sildenafil does not need to be adjusted when co-administered with sitaxentan.

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
Sitaxentan	细胞色素P450 3 a4	蛋白质	人类	未知的	抑制剂	细节