Background: Although initially introduced for the management of hypertension, alpha 1-adrenergic-receptorantagonists (a1-blockers) have become the standard of care for the medical management of benign prostatic hyperplasia (BPH)-related lower urinary tract symptoms (LUTS). However, these agents have the potential to produce orthostatic hypotension and other blood pressure-related adverse effects in normotensive patients and in those receiving concurrent treatment with other antihypertensive agents. As a result, more “uroselective,” less vasoactive α 1-blockers have been developed. Objective: This article reviews current information on the role of α 1-blockers in the treatment of BPH-related LUTS. The focus is on tamsulosin and alfuzosin, newer “uroselective” agents in this class that have a decreased potential for cardiovascular adverse effects. Methods: Relevant articles were identified through a search of the English-language literature indexed onMEDLINE and the proceedings of scientific meetings from 1976 to 2003. The search terms were benign prostatic hyperplasia treatment, alpha 1-adrenergic-receptor blockep uroselectivity, lower urinary tract symptoms, complications , and cardiovascular. Results: Tamsulosin has selectivity for the a α 1 and α 1d receptor subtypes. Alfuzosin, although not receptorsubtypeselective, is clinically “uroselective” and does not significantly affect vascular alpha-adrenergic receptors. Both agents are efficacious in relieving LUTS and have a decreased potential for such cardiovascular adverse effects as postural hypotension. Common adverse events with these agents include dizziness and asthenia. Conclusion: Based on the available data, “uroselective” α 1-blockers should be considered over older, morevasoactive agents for the medical management of LUTS, particularly in patients with BPH and hypertension.