Adrenergic Agonists

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Adrenergic Receptors & Classification - Receptor Rhapsody

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Catecholamines - Adrenaline's A-Team

  • IV admin (Epi IM/SC too). Rapid COMT/MAO metabolism. ADRs: Arrhythmias, HTN. ⚠️ Extravasation necrosis.

  • Epinephrine (Adrenaline): α1,α2,β1,β2 agonist.

    • Uses: Anaphylaxis (0.3-0.5mg IM/SC 1:1000; IV 1:10000 shock), cardiac arrest, septic shock.

    ⭐ Epinephrine Reversal of Dale: With α-blocker, Epi causes ↓BP (unopposed β2 vasodilation).

  • Norepinephrine (Noradrenaline): α1>β1 agonist (little β2).

    • Uses: Septic/cardiogenic shock (↑SVR, ↑MAP).
  • Isoproterenol (Isoprenaline): β1,β2 agonist (non-selective).

    • Uses: Bradycardia/heart block (↑HR, ↓SVR).
  • Dopamine: Dose-dependent:

    • Low: D1 (renal VD)
    • Med: β1 (↑inotropy, ↑HR)
    • High: α1 (VC)
    • 📌 D1→β1→α1 (↑dose).
    • Uses: Shock, bradycardia. Vasoactive Agent Receptor Profile
  • Dobutamine: Mainly β1 agonist (mild β2/α1).

    • Uses: Acute HF/cardiogenic shock (↑inotropy).

Alpha-Selective Agonists - Alpha Force

  • Alpha-1 ($\alpha_1$) Selective Agonists:
    • Drugs: Phenylephrine, Midodrine.
    • Uses:
      • Phenylephrine: Mydriasis (non-cycloplegic), nasal decongestant, ↑BP (pressor).
      • Midodrine: Orthostatic hypotension.
  • Alpha-2 ($\alpha_2$) Selective Agonists:
    • Drugs: Clonidine, Methyldopa (prodrug), Apraclonidine, Brimonidine.
    • Uses:
      • Clonidine: Hypertension, ADHD, opioid/nicotine withdrawal.
      • Methyldopa: Hypertension in pregnancy.
      • Apraclonidine, Brimonidine: Glaucoma (↓aqueous humor production).
  • Key Adverse Effects (AEs):
    • Clonidine: Sedation, dry mouth, ⚠️ rebound hypertension (abrupt withdrawal).
    • Methyldopa: Sedation, drug-induced lupus, Coombs-positive hemolytic anemia.

    ⭐ Methyldopa is a notable cause of drug-induced Coombs-positive hemolytic anemia.

Beta-Selective & Other Agonists - Beta Boosters & Mixers

  • β1-Selective Agonist
    • Dobutamine: Primarily β1 (↑inotropy, chronotropy); cross-ref Catecholamines.
  • β2-Selective Agonists
    • SABA (Short-Acting): Salbutamol (Albuterol), Terbutaline.
      • Uses: Acute asthma, COPD, hyperkalemia (Salbutamol), tocolysis (Terbutaline).
    • LABA (Long-Acting): Salmeterol, Formoterol.
      • Uses: Chronic asthma/COPD (with corticosteroids).
    • Ritodrine: Tocolytic (largely replaced).
    • AEs (common to β2 agonists): Tremor, tachycardia, palpitations, hypokalemia.
  • Indirect-Acting Sympathomimetics
    • Amphetamine, Tyramine: MOA - Release stored NE.
    • Cocaine: MOA - Inhibits NE reuptake.
  • Mixed-Acting Sympathomimetics
    • Ephedrine, Pseudoephedrine: MOA - Direct receptor agonism + release stored NE.
      • Uses: Nasal decongestion, pressor (Ephedrine). Tachyphylaxis.

⭐ Long-Acting Beta-Agonists (LABAs) like Salmeterol and Formoterol should not be used as monotherapy for asthma due to increased risk of asthma-related death; they must be used with an inhaled corticosteroid.

High-Yield Points - ⚡ Biggest Takeaways

  • Dobutamine (β1 agonist): For cardiogenic shock, acute HF; primarily ↑cardiac contractility.
  • Phenylephrine (α1 agonist): Causes vasoconstriction, mydriasis; used as nasal decongestant, raises BP.
  • Clonidine (central α2 agonist): For hypertension, opioid withdrawal. (α-methyldopa: HTN in pregnancy).
  • Salbutamol/Terbutaline (β2 agonists): For acute asthma/COPD; main side effects: tremor, tachycardia.
  • Dopamine: Dose-dependent effects: low (D1 renal), medium (β1 cardiac), high (α1 vasoconstriction).
  • Epinephrine (α & β agonist): Drug of choice for anaphylactic shock, cardiac arrest.

Practice Questions: Adrenergic Agonists

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Which sympathomimetic drug is primarily known to increase heart rate?

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Flashcards: Adrenergic Agonists

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One adverse effect associated with selective _____ adrenergic antagonists is 1st-dose orthostatic hypotension

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One adverse effect associated with selective _____ adrenergic antagonists is 1st-dose orthostatic hypotension

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