PDE5 inhibitors: in vitro and in vivo pharmacological profile.
PDE5 inhibitors have been clearly established as first-line therapy for the treatment of erectile dysfunction (ED). Three PDE5 inhibitors--sildenafil (Viagra), vardenafil (Levitra) and tadalafil (Cialis)--are currently approved by the FDA and the EMEA for use in ED, whereas sildenafil is also marketed under a different proprietary name (Revatio) for the treatment of pulmonary arterial hypertension (PAH). A forth PDE5 inhibitor, udenafil (Zydena), is currently marketed. In the present review the molecular basis and the mechanism of action of PDE5 inhibitors is discussed. In addition experimental and clinical data concerning their effects on different tissues, organs and systems is systematically reviewed and their possible beneficial action in numerous disorders is presented.
Department of Pharmacology, School of Medicine, Aristotle University of Thessaloniki, Greece. kouvelas@auth.gr
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Kouvelas
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Goulas
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Papazisis
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Sardeli
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Pourzitaki
D000818:Animals; D001792:Blood Platelets / Q000187:drug effects / Q000201:enzymology; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5 / Q000378:metabolism / Q000502:physiology; D041981:Gastrointestinal Tract / Q000187:drug effects; D006321:Heart / Q000187:drug effects; D006801:Humans; D007109:Immunity / Q000187:drug effects; D058986:Phosphodiesterase 5 Inhibitors; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology*; D012137:Respiratory System / Q000187:drug effects; D012140:Respiratory Tract Diseases / Q000188:drug therapy; D014553:Urinary Tract Physiological Phenomena / Q000187:drug effects; D014566:Urogenital System / Q000187:drug effects; D014570:Urologic Diseases / Q000188:drug therapy; D014785:Vision, Ocular / Q000187:drug effects
D058986:Phosphodiesterase 5 Inhibitors; D010726:Phosphodiesterase Inhibitors; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5