Phosphodiesterases as Drug Targets

Volume 204 of the series Handbook of Experimental Pharmacology pp 307-322


Treatment of Erectile Dysfunction and Lower Urinary Tract Symptoms by Phosphodiesterase Inhibitors

  • Stefan ÜckertAffiliated withDivision of Surgery, Department of Urology and Urological Oncology, Hannover Medical SchoolUrological Research Unit, Institute for Biochemical Research and Analysis Email author 
  • , Christian G. StiefAffiliated withFaculty of Medicine, Department of Urology, Ludwig-Maximilians-University, University Hospital Grosshadern

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To date, it is widely accepted that several disorders of the male and female urogenital tract, such as erectile dysfunction, bladder overactivity, urinary stone disease, the benign prostatic syndrome, as well as symptoms of female sexual arousal and orgasmic dysfunctions, can be therapeutically approached by influencing the function of the smooth musculature of the respective organs. To achieve a pronounced drug effect without significant adverse events, a certain degree of tissue selectivity is mandatory. Selective intervention in intracellular pathways regulating smooth muscle tone has become the most promising strategy to modulate tissue and organ function. Since the concept of taking a pill to relieve symptoms of lower urinary tract dysfunction is now widely accepted following the successes of phosphodiesterase 5 (PDE5) inhibitor treatment of erectile dysfunction, the treatment of urological diseases has focused on orally available drugs acting via influencing intracellular signaling pathways, thereby combining a high response rate with the advantage of an on-demand intake. Specifically, the use of isoenzyme-selective PDE inhibitors offers great opportunities in the medical treatment of various genitourinary diseases. These agents are regarded to be safe and to be efficacious, i.e., having a fast onset of drug action and an improved effect-to-side-effect ratio. As experience with this class of compounds and their use in urology is rapidly growing, basic and clinical research in this field will most likely expand the pharmacological armamentarium of innovative treatment options in the next few years. The purpose of this review is to summarize current, as well as potential, upcoming indications for the use of PDE inhibitors in the pharmacotherapy of male erectile dysfunction and lower urinary tract symptoms.


Lower urinary tract symptoms Male erectile dysfunction Oral pharmacotherapy Phosphodiesterase (PDE) inhibitors