Alpha 1 Adrenoreceptor Antagonists


  • Richard H. Grimm, Jr MD, PhD,

    1. From Cardiolgy and Epidemiology, University of Minnesota, Minneapolis, MN;
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  • John M. Flack MD, MPH, PhD

    1. Director, Berman Center for Outcomes and Clinical Research; Division Head, Clinical Research, Hennepin County Medical Center, MMRF; Professor of Medicine and Epidemiology, University of Minnesota Medical School and School of Public Health, Minneapolis, MN
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Richard H. Grimm, Jr, MD, PhD, Cardiolgy and Epidemiology, University of Minnesota, 825 South Eight Street, Suite 440, Minneapolis, MN 55404


J Clin Hypertens (Greenwich). 2011;13:654–657. ©2011 Wiley Periodicals, Inc.

Key Points and Practical Recommendations

  •  α Antagonists lower blood pressure by selectively blocking post-synaptic α1-adrenoreceptors, which antagonizes catecholamine-induced constriction of the arterial and venous vascular beds.
  •  α1-Adrenoreceptor antagonists are not indicated for initial, first-line antihypertensive therapy; however, they can be added to most other antihypertensive drug classes in—preferably diuretic-containing—drug regimens.
  •  When used over time, these agents cause expansion of the extracellular fluid and plasma volumes that typically manifests as weight gain and an attenuation of the blood pressure–lowering efficacy in persons who are consuming usual amounts of dietary sodium.
  •  Utilization of α1-adrenoreceptor antagonists with diuretics such as chlorthalidone or hydrochlorothiazide is beneficial because these agents minimize the α antagonist–induced expansion of the extracellular and plasma volumes while providing significant incremental reductions in blood pressure.
  •  α1-Adrenoreceptor antagonists are especially useful in men with benign prostatic hypertrophy because they increase mean and peak urinary flow rates as well as reduce lower urinary tract symptoms.
  •  α1-Adrenoreceptor antagonists are contraindicated in persons with heart failure because of their aforementioned ability to expand extracellular and plasma volumes.