Lower urinary tract symptoms (LUTS) are commonly associated with benign prostatic hyperplasia (BPH). The LUTS-BPH complex consists of both voiding and storage symptoms that may overlap with overactive bladder symptoms. Drug therapy for men with LUTS may include alpha1-antagonists, 5-alpha-reductase inhibitors, combination therapy, and over-the-counter phytotherapy. Anticholinergic agents are effective in relieving overactive bladder symptoms in patients without bladder outlet obstruction. However, anticholinergic therapy has historically been contraindicated in patients with LUTS associated with BPH because of concerns for developing acute urinary retention. To assess the safety and efficacy of anticholinergic therapies for LUTS associated with BPH, a MEDLINE search and a bibliographic search of the English-language literature were conducted. Two nonrandomized, open-label studies; two randomized trials that assessed anticholinergic therapy alone; and eight trials that assessed anticholinergic therapy in combination with an alpha1-antagonist were identified. Trials were of short duration (6-12 wks) and included only men with low postvoid residual volumes at baseline. Small nonsignificant changes were seen in objective measures of urinary function. Several trials demonstrated an increase in postvoid residual with anticholinergic therapy, which was statistically significant in two trials. Despite the increase in postvoid residual, rates of acute urinary retention were low and the drugs were well tolerated. Of the five trials that used a validated symptom scoring scale, two demonstrated subjective improvement in urinary function. Men with symptomatic overactive bladder and BPH who are not adequately relieved with alpha1-antagonists may benefit from the addition of an anticholinergic agent. Before starting therapy, however, a postvoid residual volume should be measured to measure to rule out baseline urinary retention.