PMID- 16100293 OWN - NLM STAT- MEDLINE DCOM- 20060223 LR - 20151119 IS - 0091-2700 (Print) IS - 0091-2700 (Linking) VI - 45 IP - 9 DP - 2005 Sep TI - The clinical pharmacokinetics of phosphodiesterase-5 inhibitors for erectile dysfunction. PG - 987-1003 AB - 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. FAU - Gupta, Manish AU - Gupta M AD - Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 874 Union Avenue, Suite 5p, Memphis, TN 38163, USA. FAU - Kovar, Andreas AU - Kovar A FAU - Meibohm, Bernd AU - Meibohm B LA - eng PT - Comparative Study PT - Journal Article PT - Review PL - England TA - J Clin Pharmacol JT - Journal of clinical pharmacology JID - 0366372 RN - 0 (Carbolines) RN - 0 (Imidazoles) RN - 0 (Phosphodiesterase Inhibitors) RN - 0 (Piperazines) RN - 0 (Purines) RN - 0 (Sulfones) RN - 0 (Triazines) RN - 5O8R96XMH7 (Vardenafil Dihydrochloride) RN - 742SXX0ICT (Tadalafil) RN - BW9B0ZE037 (Sildenafil Citrate) RN - EC 1.14.14.1 (Cytochrome P-450 CYP3A) RN - EC 3.1.4.- (Phosphoric Diester Hydrolases) RN - EC 3.1.4.35 (3',5'-Cyclic-GMP Phosphodiesterases) RN - EC 3.1.4.35 (Cyclic Nucleotide Phosphodiesterases, Type 5) RN - EC 3.1.4.35 (PDE5A protein, human) SB - IM MH - 3',5'-Cyclic-GMP Phosphodiesterases MH - Animals MH - Biological Availability MH - Carbolines/*pharmacokinetics MH - Cyclic Nucleotide Phosphodiesterases, Type 5 MH - Cytochrome P-450 CYP3A/metabolism MH - Drug Interactions MH - Erectile Dysfunction/*drug therapy/metabolism MH - Humans MH - Imidazoles/*pharmacokinetics MH - Male MH - Metabolic Clearance Rate MH - Phosphodiesterase Inhibitors/*pharmacokinetics MH - Phosphoric Diester Hydrolases/metabolism MH - Piperazines/*pharmacokinetics MH - Purines MH - Sildenafil Citrate MH - Sulfones/pharmacokinetics MH - Tadalafil MH - Triazines/pharmacokinetics MH - Vardenafil Dihydrochloride RF - 66 EDAT- 2005/08/16 09:00 MHDA- 2006/02/24 09:00 CRDT- 2005/08/16 09:00 PHST- 2005/08/16 09:00 [pubmed] PHST- 2006/02/24 09:00 [medline] PHST- 2005/08/16 09:00 [entrez] AID - 45/9/987 [pii] AID - 10.1177/0091270005276847 [doi] PST - ppublish SO - J Clin Pharmacol. 2005 Sep;45(9):987-1003. doi: 10.1177/0091270005276847.