The Clinical Pharmacokinetics of Phosphodiesterase-5 Inhibitors for Erectile Dysfunction

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...

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Bibliographic Details
Published in:Journal of clinical pharmacology 2005-09, Vol.45 (9), p.987-1003
Main Authors: Gupta, Manish, Kovar, Andreas, Meibohm, Bernd
Format: Article
Language:English
Subjects:
3',5'-Cyclic-GMP Phosphodiesterases
Animals
Biological Availability
Carbolines - pharmacokinetics
Care and treatment
Cyclic Nucleotide Phosphodiesterases, Type 5
Cytochrome P-450 CYP3A - metabolism
Drug Interactions
erectile dysfunction
Erectile Dysfunction - drug therapy
Erectile Dysfunction - metabolism
Humans
Imidazoles - pharmacokinetics
Impotence
Male
Metabolic Clearance Rate
Pharmacokinetics
Phosphodiesterase Inhibitors - pharmacokinetics
phosphodiesterase-5
Phosphodiesterases
Phosphoric Diester Hydrolases - metabolism
Piperazines - pharmacokinetics
Purines
sildenafil
Sildenafil Citrate
Sulfones - pharmacokinetics
Tadalafil
Triazines - pharmacokinetics
vardenafil
Vardenafil Dihydrochloride
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Summary: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.
ISSN:0091-2700
1552-4604
DOI:10.1177/0091270005276847