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西地那非作为肺动脉高压治疗的药代动力学评价。

Pharmacokinetic evaluation of sildenafil as a pulmonary hypertension treatment.

机构信息

Université Paris-Sud, Faculté de Pharmacie, Chatenay-Malabry, France.

出版信息

Expert Opin Drug Metab Toxicol. 2013 Sep;9(9):1193-205. doi: 10.1517/17425255.2013.804063. Epub 2013 Jun 12.

DOI:10.1517/17425255.2013.804063
PMID:23944387
Abstract

INTRODUCTION

Sildenafil citrate is a potent, selective phosphodiesterase type 5 inhibitor approved for the treatment of pulmonary arterial hypertension (PAH) and plays an important role in the management of the disease.

AREAS COVERED

In this review, we focus on the current available information on the pharmacokinetics, pharmacodynamics, clinical efficacy and safety of sildenafil citrate in PAH through a MEDLINE literature search. Comparison of sildenafil citrate with tadalafil, another phosphodiesterase type 5 inhibitor was also performed.

EXPERT OPINION

In the last few years, considerable progress has been made in the understanding and treatment of PAH. Sildenafil citrate has multiple advantages and whether it is first-line treatment alone or in combination for the mild form of the disease, it is one of the treatments of choice. In terms of its future use, more studies are still needed to better evaluate the benefit/risk balance of sildenafil citrate in pediatric populations.

摘要

简介

枸橼酸西地那非是一种有效的、选择性的磷酸二酯酶 5 抑制剂,已被批准用于治疗肺动脉高压(PAH),并在疾病管理中发挥重要作用。

涵盖领域

在这篇综述中,我们通过 MEDLINE 文献检索,重点关注目前关于枸橼酸西地那非在 PAH 中的药代动力学、药效学、临床疗效和安全性的现有信息。还比较了枸橼酸西地那非与另一种磷酸二酯酶 5 抑制剂他达拉非。

专家意见

在过去的几年中,人们对 PAH 的认识和治疗取得了相当大的进展。枸橼酸西地那非具有多种优势,无论是作为轻度疾病的单一治疗药物还是联合治疗药物,它都是治疗选择之一。就其未来的用途而言,仍需要更多的研究来更好地评估枸橼酸西地那非在儿科人群中的获益/风险平衡。

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Combination of Sildenafil and Ba at a Low Concentration Show a Significant Synergistic Inhibition of Inward Rectifier Potassium Current Resulting in Action Potential Prolongation.低浓度西地那非和Ba的组合显示出对内向整流钾电流的显著协同抑制作用,导致动作电位延长。
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Therapeutic Targeting of PDEs and PI3K in Heart Failure with Preserved Ejection Fraction (HFpEF).射血分数保留的心力衰竭(HFpEF)中磷酸二酯酶(PDEs)和磷脂酰肌醇-3-激酶(PI3K)的治疗靶点
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