Established and emerging therapeutic uses of PDE type 5 inhibitors in cardiovascular disease
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...
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| Published in: | British journal of pharmacology Vol. 177; no. 24; pp. 5467 - 5488 |
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| Main Authors: | , , , |
| Format: | Journal Article |
| Language: | English |
| Published: |
England
Blackwell Publishing Ltd
01.12.2020
John Wiley and Sons Inc |
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| ISSN: | 0007-1188, 1476-5381, 1476-5381 |
| Online Access: | Get full text |
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| Abstract | 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. |
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| AbstractList | 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. 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.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. |
| Author | Farrah, Tariq E. Dhaun, Neeraj Webb, David J. Tzoumas, Nikolaos |
| AuthorAffiliation | 2 Institute of Genetic Medicine Newcastle University Newcastle Upon Tyne UK 1 British Heart Foundation/University Centre for Cardiovascular Science, Queen's Medical Research Institute University of Edinburgh Edinburgh UK |
| AuthorAffiliation_xml | – name: 1 British Heart Foundation/University Centre for Cardiovascular Science, Queen's Medical Research Institute University of Edinburgh Edinburgh UK – name: 2 Institute of Genetic Medicine Newcastle University Newcastle Upon Tyne UK |
| Author_xml | – sequence: 1 givenname: Nikolaos orcidid: 0000-0003-2081-6042 surname: Tzoumas fullname: Tzoumas, Nikolaos organization: Newcastle University – sequence: 2 givenname: Tariq E. surname: Farrah fullname: Farrah, Tariq E. organization: University of Edinburgh – sequence: 3 givenname: Neeraj surname: Dhaun fullname: Dhaun, Neeraj organization: University of Edinburgh – sequence: 4 givenname: David J. surname: Webb fullname: Webb, David J. email: d.j.webb@ed.ac.uk organization: University of Edinburgh |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/31721165$$D View this record in MEDLINE/PubMed |
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| Snippet | 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... |
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| SubjectTerms | Angina Cardiovascular diseases Cerebral infarction Cyclic GMP Diabetes mellitus Erectile dysfunction Hypertension Kidney diseases Myocardial infarction Review Sildenafil TARGETING THE NITRIC OXIDE (NO)‐cGMP PATHWAY: THERAPEUTIC OPPORTUNITIES IN THE 21ST CENTURY |
| Title | Established and emerging therapeutic uses of PDE type 5 inhibitors in cardiovascular disease |
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