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    Subjects/Pharmacology/Pharmacodynamics and Receptor Theory
    Pharmacodynamics and Receptor Theory
    easy
    pill Pharmacology

    A 68-year-old woman with chronic obstructive pulmonary disease (COPD) and acute exacerbation presents with severe bronchospasm. Which beta-2 adrenergic agonist is the drug of choice for acute relief in this setting?

    A. Salbutamol
    B. Vilanterol
    C. Salmeterol
    D. Formoterol

    Explanation

    Beta-2 Agonist Selection in Acute Bronchospasm

    Key Point
    Salbutamol (albuterol) is the gold-standard short-acting beta-2 agonist (SABA) for acute bronchospasm due to its rapid onset and short duration of action.
    Pharmacodynamic Properties Required for Acute Relief
    Table
    PropertyRequirementSalbutamolSalmeterolFormoterolVilanterol
    Onset of actionRapid (< 5 min)5–15 min10–20 min1–3 min1–3 min
    DurationShort (4–6 hrs)4–6 hrs12 hrs12 hrs24 hrs
    Receptor selectivityβ2 >> β1ExcellentExcellentExcellentExcellent
    IndicationAcute reliefYesNoNoNo
    IndicationMaintenanceNoYesYesYes
    High-YieldNEET PG
    SABA = Short-Acting Beta-2 Agonist for acute symptoms. LABA = Long-Acting Beta-2 Agonist for maintenance. Never use LABA monotherapy in COPD (increased mortality risk).
    Why Salbutamol is Preferred in Acute Exacerbation
    1. 1.
      Rapid onset: Begins working within 5–15 minutes via β2-mediated smooth muscle relaxation
    2. 2.
      Short duration: Allows frequent dosing (every 4–6 hours) without accumulation
    3. 3.
      Reversible binding: Quickly dissociates from receptor, permitting dose titration
    4. 4.
      Inhaled route: Delivers high local concentration to airways with minimal systemic effects
    Clinical Pearl
    In acute exacerbation, salbutamol can be given via nebulizer (2.5–5 mg) or MDI (100 mcg/puff) every 15–30 minutes for the first hour, then every 4–6 hours. This flexibility is unique to SABAs.
    Mnemonic
    SABA-LABA rule — Short-acting for Acute, Long-acting for Long-term (maintenance).

    KD Tripathi 8e Ch 27

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