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Pharmacology Antihypertensive Drugs

Alpha-receptor Blockers

Topic overview

Start with the big picture

α₁-blockers such as prazosin, terazosin, and doxazosin lower systemic vascular resistance and venous return, with little long-term change in heart rate. Some agents, including tamsulosin and alfuzosin, are more uroselective and are used for BPH symptoms. Other applications include pheochromocytoma-related blood-pressure control, Raynaud phenomenon, and prazosin for PTSD nightmares. A key safety issue is first-dose orthostatic hypotension or syncope; low-dose initiation, bedtime administration, and monitoring supine and standing blood pressure are emphasized. Dizziness and other adverse effects, potential additive hypotension with PDE-5 inhibitors, and caution in volume depletion or severe heart failure also matter. Because outcome evidence found higher heart-failure risk than with thiazides, these drugs are generally positioned as adjuncts for hypertension.

Learning objectives

What you'll learn

  • Explain how α₁-receptor blockade changes vascular tone, systemic resistance, and preload.
  • Distinguish selective α₁-blockers from non-selective agents and identify their clinical roles.
  • Recognize first-dose hypotension and other important adverse effects and precautions.
  • Describe monitoring and counseling during α₁-blocker titration.
  • Summarize why α₁-blockers have an adjunctive role in hypertension.
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