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
Main Authors: Tzoumas, Nikolaos, Farrah, Tariq E., Dhaun, Neeraj, Webb, David J.
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
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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.
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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PublicationDate December 2020
PublicationDateYYYYMMDD 2020-12-01
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  year: 2020
  text: December 2020
PublicationDecade 2020
PublicationPlace England
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PublicationTitle British journal of pharmacology
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Publisher Blackwell Publishing Ltd
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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
URI https://onlinelibrary.wiley.com/doi/abs/10.1111%2Fbph.14920
https://www.ncbi.nlm.nih.gov/pubmed/31721165
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https://pubmed.ncbi.nlm.nih.gov/PMC7707100
Volume 177
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