Tzoumas Nikolaos, Farrah Tariq E, Dhaun Neeraj, Webb David J
British Heart Foundation/University Centre for Cardiovascular Science, Queen's Medical Research Institute, University of Edinburgh, Edinburgh, UK.
Institute of Genetic Medicine, Newcastle University, Newcastle Upon Tyne, UK.
Br J Pharmacol. 2020 Dec;177(24):5467-5488. doi: 10.1111/bph.14920. Epub 2020 Feb 4.
PDE type 5 inhibitors (PDE5Is), such as sildenafil, tadalafil and vardenafil, are a class of drugs used to prolong the physiological effects of NO/cGMP signalling in tissues through the inhibition of cGMP degradation. Although these agents were originally developed for the treatment of hypertension and angina, unanticipated side effects led to advances in the treatment of erectile dysfunction and, later, pulmonary arterial hypertension. In the last decade, accumulating evidence suggests that PDE5Is may confer a wider range of clinical benefits than was previously recognised. This has led to a broader interest in the cardiovascular therapeutic potential of PDE5Is, in conditions such as hypertension, myocardial infarction, stroke, peripheral arterial disease, chronic kidney disease and diabetes mellitus. Here, we review the pharmacological properties and established licensed uses of this class of drug, along with emerging therapeutic developments and possible future indications.
5型磷酸二酯酶抑制剂(PDE5Is),如西地那非、他达拉非和伐地那非,是一类通过抑制环磷酸鸟苷(cGMP)降解来延长组织中一氧化氮(NO)/cGMP信号生理效应的药物。尽管这些药物最初是为治疗高血压和心绞痛而研发的,但意外的副作用推动了勃起功能障碍治疗的进展,随后又用于肺动脉高压的治疗。在过去十年中,越来越多的证据表明,PDE5Is可能带来比以往认识到的更广泛的临床益处。这引发了人们对PDE5Is在高血压、心肌梗死、中风、外周动脉疾病、慢性肾病和糖尿病等病症中的心血管治疗潜力产生更广泛的兴趣。在此,我们综述这类药物的药理特性、已获批的用途,以及新出现的治疗进展和可能的未来适应症。