title: Phosphodiesterase type 5 inhibitors: back and forward from cardiac indications.
abstract: PDE5 inhibitors (PDE5i) are widely known as treatment for erectile dysfunction (ED). This favorable action has emerged as a "side effect" from pioneering studies when PDE5i have been originally proposed as treatment for coronary artery disease (CAD). PDE5i showed marginal benefits for CAD treatment; although disappointing for that indication, they improved systemic and pulmonary vasodilation and ameliorated general endothelial function. Therefore, PDE5i have been approved and licensed also for pulmonary artery hypertension (PAH), besides ED. Nowadays, fine-tuned biomolecular mechanisms of PDE5i are well recognized to be beneficial onto myocardial contractility and geometry, to reduce tissue fibrosis, hypertrophy and apoptosis. PDE5i consistently exert benefits on heart failure, infarct, cardiomyopathy. The concept that PDE5i likely blunt Th1-driven inflammatory processes, which shift the homeostatic balance from health to disease, has emerged; PDE5i seem to decrease the release of active biomolecules from cells to tissues interested by inflammation. In this view, following clinical and basic research progresses, PDE5i can be undoubtedly "re-allocated" for cardiac indications and, hopefully, they could be approved as therapeutic tools to treat and prevent heart disease. This review aims to summarize PDE5i different clinical applications, from past to present and future, focusing on their potential power as treatment for cardiac diseases.
authors.affiliation: Department of Movement, Human and Health Sciences, Section of Health Science, Unit of Endocrinology, University of Rome "Foro Italico", Rome, Italy.
authors.forename: C
authors.initials: C
authors.lastname: Corinaldesi
authors.affiliation: Department of Movement, Human and Health Sciences, Section of Health Science, Unit of Endocrinology, University of Rome "Foro Italico", Rome, Italy.
authors.forename: L
authors.initials: L
authors.lastname: Di Luigi
authors.affiliation: Department of Experimental Medicine, Sapienza University of Rome, Rome, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Lenzi
authors.affiliation: Department of Movement, Human and Health Sciences, Section of Health Science, Unit of Endocrinology, University of Rome "Foro Italico", Rome, Italy. clara.crescioli@uniroma4.it.
authors.forename: C
authors.initials: C
authors.lastname: Crescioli
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D002317:Cardiovascular Agents / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000276:immunology / Q000378:metabolism / Q000503:physiopathology; D003324:Coronary Artery Disease / Q000188:drug therapy / Q000276:immunology / Q000378:metabolism / Q000503:physiopathology; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5 / Q000737:chemistry / Q000378:metabolism; D004730:Endothelium, Vascular / Q000187:drug effects / Q000276:immunology / Q000378:metabolism / Q000503:physiopathology; D019317:Evidence-Based Medicine; D006321:Heart / Q000187:drug effects* / Q000503:physiopathology; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy / Q000378:metabolism / Q000503:physiopathology; D009206:Myocardium / Q000201:enzymology / Q000276:immunology / Q000378:metabolism; D058986:Phosphodiesterase 5 Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D014665:Vasodilator Agents / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002317:Cardiovascular Agents; D058986:Phosphodiesterase 5 Inhibitors; D014665:Vasodilator Agents; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5
keywords: Cardioprotection; Inflammation; PDE5 inhibitors