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The Clinical Pharmacokinetics of Phosphodiesterase-5 Inhibitors for Erectile Dysfunction

From the Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis (Dr Gupta, Dr Meibohm), and Clinical Pharmacology & Pharmacokinetics, Merck KGaA, Darmstadt, Germany (Dr Kovar).

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.

Key Words: Pharmacokinetics • sildenafil • vardenafil • tadalafil • phosphodiesterase-5 • erectile dysfunction

Address for reprints: Bernd Meibohm, PhD, FCP, Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 874 Union Avenue, Suite 5p, Memphis, TN 38163.

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