Alpha-Adrenergic Receptor Blockers Classification, Key differences, Clinical uses, Side Effects

Alpha-Adrenergic Receptor Blockers Classification, Key differences, Clinical uses, Side Effects

Find out the notes on Alpha-Adrenergic Receptor Blockers

Alpha-Adrenergic Receptor Blockers

These drugs block alpha-adrenergic receptors, leading to vasodilation and reduced blood pressure.


🔹 Classification of Alpha Blockers

1. Non-selective Alpha Blockers

Block both α₁ and α₂ receptors

  • Examples:

    • Phentolamine (reversible)

    • Phenoxybenzamine (irreversible)

2. Selective α₁ Blockers

Block only α₁ receptors → vasodilation without increased NE release

  • Examples:

    • Prazosin

    • Terazosin

    • Doxazosin

    • Tamsulosin (uroselective – α₁A selective)

3. Selective α₂ Blockers

Rare; mainly experimental or research use


🔹 Key Differences

Feature Non-selective Selective α₁
Action Blocks α₁ & α₂ Blocks only α₁
Reflex Tachycardia ↑↑ (due to α₂ block) Less
Duration Phentolamine (short) < Phenoxybenzamine (long) Moderate to long
Use in Pheochromocytoma Yes No (not preferred)

🔹 Important Clinical Uses

Drug Use
Phenoxybenzamine Pheochromocytoma (pre-op)
Phentolamine Hypertensive crisis (e.g., MAOI + tyramine), diagnosis of pheochromocytoma
Prazosin, Terazosin, Doxazosin Hypertension, BPH
Tamsulosin, Alfuzosin BPH (selective for prostate, fewer BP effects)

🔹 Adverse Effects

  • Orthostatic hypotension (especially first-dose effect in α₁ blockers)

  • Reflex tachycardia (notably with non-selective)

  • Nasal congestion

  • Dizziness, headache


🔹 Important Points to Remember

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  • First-dose phenomenon: Sudden hypotension — start with low dose at bedtime (esp. Prazosin).

  • Phenoxybenzamine is irreversible — useful in long-term blockade (pheochromocytoma).

  • Tamsulosin is α₁A-selective — fewer cardiovascular side effects.

  • Blocking α₂ receptors increases norepinephrine release → reflex tachycardia.

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