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

The DOI matches its Crossref record; 43 of the 43 references it cites were found in a registry or an index.

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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Crossref · 10.1111/j.1742-1241.2002.tb11296.x

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43 of 43 references verified0 citation errors · 0 not checkable

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Citations

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Show all 43 references

Research works printed but not linked: 9

  1. Boolell M, 1996, Sildenafil: an orally active type 5 cyclic GMP‐specific phosphodiesterase inhibitor for the treatment of penile erectile dysfunction. Int, J Impot Res, 8, 47
  2. Murray KJ, 1993, Phosphodiesterase V inhibitors, Drug News Perspect, 6, 150
  3. Patterson B, 2001, The effect of intrinsic and extrinsic factors on the pharmacokinetic properties of tadalafil (IC351), Int J Impot Res, 13, S63
  4. Angulo J, 2001, IC351 enhances nitric oxide‐mediated relaxation of human arterial and trabecular penile smooth muscle, Diabetologia, 44, A295
  5. Baxendale RW, 2001, Selectivity of sildenafil citrate and other phosphodiesterase type 5 (PDE5) inhibitors against human phosphodiesterase types 7–11, J Clin Pharmacol, 41, 1015
  6. Baxendale R, 2000, Human PDE11: a distinct, dual‐substrate phosphodiesterase expressed in vascular smooth muscle and cardiac myocytes, Circulation, 102, 320
  7. 1999, Viagra® [package insert]
  8. Patterson B, 2001, Dose‐normalized pharmacokinetics of single dose tadalafil (IC351) in healthy volunteers, Int J Impot Res, 13, S63
  9. Padma‐Nathan H, 2001, Cialis (IC351) provides prompt response and extended period of responsiveness for the treatment of men with erectile dysfunction, J Urol, 165, 224

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Metadata

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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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.