The role of pharmacokinetics and pharmacodynamics in phosphodiesterase-5 inhibitor therapy

• Published in: International journal of impotence research Vol. 19; no. 3; pp. 253 - 264
• Main Authors: MEHROTRA, N, GUPTA, M, KOVAR, A, MEIBOHM, B
• Format: Journal Article
• Language: English
• Published: Basingstoke Nature Publishing 01.06.2007; Nature Publishing Group
• Subjects: 3',5'-Cyclic-GMP Phosphodiesterases - antagonists & inhibitors; Analysis; Biological and medical sciences; Cyclic Nucleotide Phosphodiesterases, Type 5; Drug therapy; Erectile dysfunction; Erectile Dysfunction - drug therapy; Gynecology. Andrology. Obstetrics; Health aspects; Humans; Impotence; Male; Male genital diseases; Medical sciences; Non tumoral diseases; Pharmacodynamics; Pharmacokinetics; Phosphodiesterase Inhibitors - administration & dosage; Phosphodiesterase Inhibitors - pharmacokinetics; Sildenafil; Tadalafil; United States; Andrology; Pharmacodynamics; 3',5'-Cyclic-nucleotide phosphodiesterase; Erection disorders; Enzyme; 3',5'-Cyclic-GMP phosphodiesterase; Sexual dysfunction; phosphodiesterase-5; Esterases; Phosphoric diester hydrolases; erectile dysfunction; Phosphodiesterase inhibitor; Phosphodiesterase 5 inhibitor; Treatment; pharmacotherapy; Hydrolases; Pharmacokinetics; Male genital diseases
• ISSN: 0955-9930; 1476-5489
• DOI: 10.1038/sj.ijir.3901522

Differences in clinical pharmacology of the currently marketed phosphodiesterase (PDE)5 inhibitors sildenafil, vardenafil and tadalafil are largely determined by their pharmacokinetic (PK) properties and their PDE5 inhibitory activity profile. This review outlines the basic concepts of pharmacokinetics and pharmacokinetic pharmacodynamic (PK/PD) relationships and their relevance to dose selection and applied pharmacotherapy. It is followed by a detailed comparative discussion on the pharmacokinetics and exposure-response relationship of the currently available PDE5 inhibitors, including known drug-drug interactions and dosage adjustments in special populations. The review is aimed at providing a critical assessment of the pharmacokinetics of PDE5 inhibitors, which may assist clinicians in tailoring drug and/or treatment regimens to the unique needs of each individual patient with erectile dysfunction.