Benign prostatic hyperplasia (BPH) is highly prevalent in men older than 50 years and is associated with a range of lower urinary tract symptoms that may have a negative impact on patient quality of life. Alpha1-adrenergic receptor antagonists are the first-line of pharmacologic management for lower urinary tract symptoms associated with BPH. However, many patients take multiple medications that may exacerbate age-related orthostatic hypotension. Thus, clinicians should evaluate the treatment of these patients within the context of comorbidities. The present article discusses the role of non–subtype-selective and subtype-selective α1-adrenergic receptor antagonists in the clinical management of BPH. Safety and tolerability for both non–subtype-selective and subtype-selective α1-adrenergic receptor antagonists for patients with BPH are also reviewed.