Cited by 267Phosphodiesterase function and regulationSexual function and dysfunction studiesPharmacogenetics and Drug Metabolism

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PHARMACOLOGY OF PHOSPHODIESTERASE‐5 INHIBITORS

Corbin, JD, Francis, SH·2002·International Journal of Clinical Practice

DOI 10.1111/j.1742-1241.2002.tb11296.x

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Abstract

SUMMARY: The clinical properties (efficacy and safety profile) of a medicine are related not only to its mode of action, but also to its selectivity for its target (usually a receptor or enzyme) and are also influenced by its pharmacokinetic properties (absorption, distribution, metabolism and elimination). The growing number of phosphodiesterase inhibitors that are selective for phosphodiesterase‐5 (PDE5) represent a promising new class of compounds that are useful for the treatment of erectile dysfunction and perhaps other disorders. Some of the basic pharmacodynamic and pharmacokinetic parameters that describe drug action are discussed with regard to the new PDE5 inhibitors. Central topics reviewed are the concentration that produces a given in vitro response, or potency (IC 50), maximum plasma concentration (C max), time to C max (T max), half‐life (t ½), area under the curve (AUC), bioavailability, onset and duration of action, and the balance to achieve optimum safety and efficacy. To illustrate these concepts, a group of inhibitors with varying selectivities and potencies for PDE5 (theophylline, IBMX, zaprinast, sildenafil, tadalafil and vardenafil) are discussed. Each drug has its own set of unique pharmacological characteristics based on its specific molecular structure, enzyme inhibition profile and pharmacokinetic properties. Each PDE5 inhibitor has a distinct selectivity that contributes to its safety profile. As with all new drugs, and especially those in a new class, careful evaluation will be necessary to ensure the optimal use of the PDE5 inhibitors.

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Authors: Corbin, J., & Francis, S.
Affiliations: Department of Molecular Physiology and Biophysics Vanderbilt University School of Medicine Nashville Tennessee USA
Venue: International Journal of Clinical Practice
Publisher: Wiley
Published: 2002-07
Volume: 56
Issue: 6
Pages: 453-459
ISSN: 1368-5031 (ISSN-L)
1742-1241
DOI: 10.1111/j.1742-1241.2002.tb11296.x
OpenAlex: W4367480699
Cited by: 260
References: 43
Citations by year: 2026: 3 · 2025: 6 · 2024: 4 · 2023: 6 · 2022: 2 · 2021: 2 · 2020: 6 · 2019: 7 · 2018: 3 · 2017: 9 · 2016: 9 · 2015: 5 · 2014: 12 · 2013: 12 · 2012: 13
FWCI: 6.81
Type: journal article
Language: en
Open access: closed
Licence: onlinelibrary.wiley.com/termsAndConditions#vor (vor)
Locations: International Journal of Clinical Practice (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Phosphodiesterase function and regulation
Health Sciences › Medicine › Psychiatry and Mental health › Sexual function and dysfunction studies
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Keywords: phosphodiesterase-5 inhibitors, sildenafil, tadalafil, vardenafil, zaprinast, theophylline, 3-isobutyl-1-methylxanthine, pharmacokinetics, pharmacodynamics, enzyme selectivity, potency, bioavailability, erectile dysfunction, drug safety, drug efficacy

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PHARMACOLOGY OF PHOSPHODIESTERASE‐5 INHIBITORS

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