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The Clinical Pharmacokinetics of Phosphodiesterase‐5 Inhibitors for Erectile Dysfunction
Abstract
Differences in the clinical pharmacology of the 3 currently available oral phosphodiesterase‐5 (PDE5) inhibitors, sildenafil, vardenafil, and tadalafil, are largely determined by their clinical pharmacokinetics as well as their PDE inhibitory activity profile. This review comparatively discusses the major characteristics of the pharmacokinetic profile of all 3 PDE5 inhibitors, including bioavailability and rate of absorption, Biopharmaceutical Classification System categorization, elimination mechanisms, and metabolic profile including active metabolites, as well as the drug‐drug interaction potential and modification of pharmacokinetic properties under selected physiologic and pathophysiologic conditions. The review is aimed at providing comparative clinical pharmacology data to allow for scientifically rational, evidence‐based prescribing and dosing decisions regarding the clinical use of these medications for the treatment of erectile dysfunction.
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“The metabolism of tadalafil is via the hepatic enzyme cytochrome P450 34A (CYP34A) to a catechol metabolite, which undergoes further metabolism to its primary circulating metabolite, methylcatechol glucuronide, a 10,000-fold less potent molecule than tadalafil (Gupta et al 2005).”
From Tadalafil in the treatment of erectile dysfunction (2008) · cites this paper as Gupta et al 2005
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Cited by
Predicting Clearance Mechanism in Drug Discovery: Extended Clearance Classification System (ECCS)
Varma, M. V., Steyn, S. J., Allerton, C., & El-Kattan, A. F. (2015) · Pharmaceutical Research · doi:10.1007/s11095-015-1749-4 · Cited by 334
Tadalafil in the treatment of erectile dysfunction
Coward, R., & Carson, C. (2008) · Therapeutics and Clinical Risk Management · doi:10.2147/tcrm.s3336 · Cited by 138
Komura, H., & Iwaki, M. (2011) · Drug Metabolism Reviews · doi:10.3109/03602532.2011.597401 · Cited by 78
Metadata
- Authors
- Gupta, M., Kovar, A., & Meibohm, B.
- Venue
- The Journal of Clinical Pharmacology
- Publisher
- Wiley
- Published
- 2005-09
- Volume
- 45
- Issue
- 9
- Pages
- 987-1003
- ISSN
- 0091-2700
- 1552-4604
- Cited by
- 150
- References
- 1
- Language
- en
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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