Most drugs used in the treatment of urinary incontinence and voiding dysfunction in women modulate neuromuscular transmission in the urethra and bladder. Pharmacotherapy is the mainstay of treatment for overactive bladder. Although several different antimuscarinic medications are available for the treatment of overactive bladder, most have similar efficacy and tolerability. Pharmacotherapy has a limited role in the management of stress incontinence and voiding dysfunction in women. Newer drugs that target different mechanisms of action are being developed for the treatment of urinary incontinence and voiding dysfunction in women.