Adrenergic Antagonists

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Alpha Blockers - Alpha's Off Switch

  • Mechanism: Block $\alpha_1$ &/or $\alpha_2$ receptors.
    • $\alpha_1$ block: Vasodilation (↓BP), relaxation of prostate & bladder neck.
  • Types & Key Drugs:
    • Non-selective ($\alpha_1 + \alpha_2$):
      • Phenoxybenzamine (Irreversible; Pheochromocytoma pre-op)
      • Phentolamine (Reversible; Pheochromocytoma, hypertensive crisis)
    • Selective $\alpha_1$ (suffix "-zosin"): Prazosin, Terazosin, Doxazosin (Hypertension, BPH); Tamsulosin, Alfuzosin, Silodosin (BPH - more uroselective).
    • Selective $\alpha_2$: Yohimbine (used for orthostatic hypotension).
  • Main Uses:
    • Hypertension (esp. with BPH)
    • Benign Prostatic Hyperplasia (BPH)
    • Pheochromocytoma
  • Key Side Effects:
    • First-dose hypotension (postural) - esp. Prazosin.
    • Reflex tachycardia.
    • Nasal congestion.
    • Retrograde ejaculation (Tamsulosin). 📌 "-ZOSIN" drugs are $\alpha_1$ selective blockers.

⭐ Phenoxybenzamine is an irreversible alpha-blocker, crucial for pre-operative blood pressure control in pheochromocytoma. oka

Beta Blockers (NS/B1) - Heart's Chill Pill

  • MoA: Block $\beta$-receptors.
    • $\beta_1$ (heart): ↓HR, ↓contractility, ↓AV conduction, ↓renin.
    • $\beta_2$ (NSBBs): Bronchoconstriction, vasoconstriction.
  • Types & Examples:
    • Non-Selective (NS: $\beta_1 + \beta_2$): Propranolol, Timolol, Nadolol, Sotalol (K+ ch. block).
    • Cardioselective ($\beta_1$ > $\beta_2$): E.g., Metoprolol, Atenolol, Nebivolol (+NO). (📌 BEMBA: Bisoprolol, Esmolol, Metoprolol, Betaxolol, Atenolol, Acebutolol, Nebivolol).
    • With ISA (Partial Agonists): Pindolol, Acebutolol (less bradycardia).
  • Key Uses: HTN, Angina, Post-MI, Arrhythmias, CHF (stable). Glaucoma (Timolol), Hyperthyroidism (symptoms), Migraine prophylaxis.
  • Side Effects: Bradycardia, AV block, hypotension. Bronchospasm (NSBBs). Fatigue, sexual dysfunction. Masks hypoglycemia (except sweating) ⚠️. Rebound on withdrawal. Beta-1 and Beta-2 Receptor Mechanism in Heart

⭐ Beta blockers are contraindicated in cocaine-induced MI due to risk of unopposed alpha-stimulation, worsening coronary vasoconstriction.

Beta Blockers (Special) & Mixed - The Dual Agents

  • With Intrinsic Sympathomimetic Activity (ISA):
    • Pindolol, Acebutolol (Partial $\beta$-agonists).
    • Mechanism: Act as partial agonists at $\beta$-receptors.
    • Effects: Less bradycardia, less adverse lipid profile changes. Preferred for bradycardia/mild asthma (use with caution).
    • 📌 Mnemonic: "Pindolol & Acebutolol are Partial Agonists".
  • Mixed $\alpha_1$ & $\beta$ Blockers (Dual Action):
    • Labetalol, Carvedilol.
    • Mechanism: Blocks $\beta_1, \beta_2$ & $\alpha_1$ receptors → vasodilation + $\beta$-blockade.
    • Labetalol:
      • $\beta:\alpha$ blockade ratio: approx. 3:1 (oral), 7:1 (IV).
      • Uses: HTN in pregnancy (DOC), hypertensive emergencies, pheochromocytoma.
    • Carvedilol:
      • Non-selective $\beta$-blocker + $\alpha_1$ blocker.
      • Additional properties: Antioxidant, anti-proliferative.
      • Uses: CHF (↓mortality/morbidity), hypertension.

      ⭐ Carvedilol shows mortality benefit in CHF due to combined $\beta + \alpha_1$ blockade & antioxidant properties.

  • Third-Generation $\beta$-Blockers (Vasodilatory via NO):
    • Nebivolol.
    • Highest $\beta_1$ selectivity among all $\beta$-blockers.
    • Mechanism: Stimulates endothelial NO synthase → ↑NO release → vasodilation.
    • Uses: Hypertension, Chronic Heart Failure.

Blocker Blueprint - Uses & Warnings

  • α-Blockers (e.g., Prazosin, Tamsulosin, Phenoxybenzamine):
    • Uses: Hypertension (α1), BPH (α1A), Pheochromocytoma (non-sel.).
    • Warnings: First-dose hypotension ⚠️, reflex tachycardia, nasal congestion.
  • β-Blockers (e.g., Propranolol, Atenolol, Carvedilol):
    • Uses: HTN, Angina, Post-MI, Arrhythmias, CHF (specific ones), Glaucoma, Hyperthyroidism symptoms, Migraine prophylaxis.
    • Warnings: Bronchoconstriction (Asthma/COPD ⚠️), bradycardia, AV block, fatigue. Mask hypoglycemia symptoms. Avoid abrupt withdrawal (rebound HTN/angina).

    ⭐ Beta-blockers (esp. non-selective) can mask hypoglycemia symptoms like tremors & palpitations, but not sweating; critical for diabetics on insulin. oka

High‑Yield Points - ⚡ Biggest Takeaways

  • Alpha-1 blockers (e.g., Prazosin) treat hypertension & BPH; risk of first-dose hypotension. Tamsulosin is uroselective for BPH.
  • Non-selective alpha-blockers (e.g., Phentolamine) are used for pheochromocytoma management.
  • Non-selective beta-blockers (e.g., Propranolol) block β1 & β2 receptors; contraindicated in asthma/COPD.
  • Cardioselective beta-blockers (e.g., Metoprolol, Atenolol) primarily target β1; safer in asthma (use cautiously).
  • Beta-blockers are key for hypertension, angina, MI, heart failure, arrhythmias.
  • Labetalol & Carvedilol are mixed α & β blockers, used in hypertensive emergencies & heart failure.
  • Common β-blocker side effects: bradycardia, fatigue, bronchospasm (non-selective), masking of hypoglycemia symptoms.

Practice Questions: Adrenergic Antagonists

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Effects of beta blockers on the heart are all of the following except:

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Flashcards: Adrenergic Antagonists

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Prior to removal of a pheochromocytoma, irreversible _____, such as phenoxybenzamine are administered, followed by beta-blockers

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Prior to removal of a pheochromocytoma, irreversible _____, such as phenoxybenzamine are administered, followed by beta-blockers

alpha-antagonists

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