Neuropharmacology is a rapidly expanding field due to the regular discovery of new neurotransmitters or neuroreceptors. Hopes have now been raised for the treatment of vesicosphincteric disorders by developing molecules with a potential selective clinical action on the detrusor or the urethra. After a brief review of the neuroanatomy and general neuropharmacology of the sympathetic nervous system, the current indications for alpha agonists are reviewed and discussed. These indications include the treatment of priapism, retrograde ejaculation, and incontinence due to sphincter incompetence. The more recent use of agents with a central mechanism of action is also discussed (detrusor hyperactivity of spinal cord injury patients). The authors review the current indications and note that, although the use of these drugs is very specific and limited in the field of urology, it is nevertheless based on an interesting concept. Like molecules at the stage of clinical trials for peripheral or central targets, the mechanism of action of these molecules on the sympathetic adrenergic system needs to be more fully elucidated. Their adverse effects remain the limiting factor for use on peripheral targets.