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 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.
Gupta
Manish
M
Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 874 Union Avenue, Suite 5p, Memphis, TN 38163, USA.
Kovar
Andreas
A
Meibohm
Bernd
B
D015106:3',5'-Cyclic-GMP Phosphodiesterases; D000818:Animals; D001682:Biological Availability; D002243:Carbolines / Q000493:pharmacokinetics*; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism; D004347:Drug Interactions; D007172:Erectile Dysfunction / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D007093:Imidazoles / Q000493:pharmacokinetics*; D008297:Male; D008657:Metabolic Clearance Rate; D010726:Phosphodiesterase Inhibitors / Q000493:pharmacokinetics*; D010727:Phosphoric Diester Hydrolases / Q000378:metabolism; D010879:Piperazines / Q000493:pharmacokinetics*; D011687:Purines; D000068677:Sildenafil Citrate; D013450:Sulfones / Q000493:pharmacokinetics; D000068581:Tadalafil; D014227:Triazines / Q000493:pharmacokinetics; D000069058:Vardenafil Dihydrochloride
D002243:Carbolines; D007093:Imidazoles; D010726:Phosphodiesterase Inhibitors; D010879:Piperazines; D011687:Purines; D013450:Sulfones; D014227:Triazines; D000069058:Vardenafil Dihydrochloride; D000068581:Tadalafil; D000068677:Sildenafil Citrate; D051544:Cytochrome P-450 CYP3A; D010727:Phosphoric Diester Hydrolases; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; C517381:PDE5A protein, human