Capsaicin and related compounds can exert a therapeutic benefit in patients with neurogenic bladder hyper-reflexia and other micturition disturbances. Modulation can be achieved by drugs acting at several levels of the micturition pathway. At the peripheral level, drugs might modulate sensory inputs arising from the bladder by acting directly not only on afferent neurons but also on other kinds of cells. Sensory modulation can be achieved through drugs acting on receptors or ion channels. Targeting either can be effective strategies to treat bladder overactivity.