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5型磷酸二酯酶抑制剂的药代动力学、药效学及疗效

Pharmacokinetics, pharmacodynamics, and efficacy of phosphodiesterase type 5 inhibitors.

作者信息

Sussman David O

机构信息

University of Medicine and Dentistry of New Jersey--School of Osteopathic Medicine in Stratford, USA.

出版信息

J Am Osteopath Assoc. 2004 Mar;104(3 Suppl 4):S11-5.

Abstract

Clinical evidence in men with erectile dysfunction (ED) shows that the phosphodiesterase type 5 (PDE5) inhibitors sildenafil citrate, tadalafil, and vardenafil hydrochloride have favorable safety and efficacy profiles. However, as mild vasodilators, the PDE5 inhibitors are also associated with hemodynamic effects that may be clinically significant, especially when treating men with ED who have comorbid cardiovascular disease. Hemodynamic studies have shown that therapeutic dosages of the PDE5 inhibitors produce only mild and transient changes in mean systolic and diastolic blood pressure and heart rate in healthy men as well as those with ischemic heart disease or chronic stable angina. Overall, PDE5 inhibitors are safe and effective in most patient populations, including men with ischemic cardiovascular disease or those receiving anti-hypertensive agents, and men with diabetes or those who have undergone nerve-sparing retropubic radical prostatectomy. With the entry of three novel PDE5 inhibitors into the therapeutic armamentarium for ED, differentiating properties of the new agents may confer clinical benefits that physicians as well as patients and their partners should consider when selecting a PDE5 inhibitor.

摘要

勃起功能障碍(ED)男性的临床证据表明,5型磷酸二酯酶(PDE5)抑制剂西地那非柠檬酸盐、他达拉非和盐酸伐地那非具有良好的安全性和疗效。然而,作为轻度血管扩张剂,PDE5抑制剂也与血流动力学效应相关,这可能具有临床意义,尤其是在治疗患有合并心血管疾病的ED男性时。血流动力学研究表明,PDE5抑制剂的治疗剂量在健康男性以及患有缺血性心脏病或慢性稳定性心绞痛的男性中,只会引起平均收缩压、舒张压和心率的轻微和短暂变化。总体而言,PDE5抑制剂在大多数患者群体中是安全有效的,包括患有缺血性心血管疾病的男性或正在接受抗高血压药物治疗的男性,以及患有糖尿病的男性或接受保留神经的耻骨后根治性前列腺切除术的男性。随着三种新型PDE5抑制剂进入ED治疗药物库,新药物的差异化特性可能带来临床益处,医生以及患者及其伴侣在选择PDE5抑制剂时应予以考虑。

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