Bronchodilators

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Bronchodilators: Overview & Classes - Airway Openers 101

  • Drugs that dilate bronchi & bronchioles, decreasing airway resistance and improving airflow to the lungs.
  • Mechanism: Primarily act by relaxing airway smooth muscle; some also modulate inflammation.
  • Key indications: Asthma, Chronic Obstructive Pulmonary Disease (COPD).
  • Major Classes:
    • β2-Adrenergic Agonists (e.g., Salbutamol, Formoterol)
    • Muscarinic Antagonists (e.g., Ipratropium, Tiotropium)
    • Methylxanthines (e.g., Theophylline) Bronchial smooth muscle relaxation pathways diagram

⭐ β2-agonists are the most effective bronchodilators; they activate adenylyl cyclase, leading to increased intracellular cAMP, which causes bronchial smooth muscle relaxation. 📌 Remember "BAM" for Bronchodilator classes: Beta-agonists, Anticholinergics, Methylxanthines for quick recall during exams!

Beta-2 Agonists - Speedy Relief Crew

  • MOA: Activate $\beta_2$ adrenergic receptors → $↑cAMP$ → bronchial smooth muscle relaxation & bronchodilation. Beta-2 adrenergic receptor signaling short and long term
  • Types & Uses:
    FeatureSABA (Short-Acting)LABA (Long-Acting)Ultra-LABA
    DrugsSalbutamol, Levosalbutamol, TerbutalineSalmeterol, FormoterolIndacaterol, Olodaterol, Vilanterol
    Onset<5 minSal: 20 min, For: 2-3 min5-15 min
    Duration4-6 hrs>12 hrs>24 hrs
    RoleRescue (acute asthma/COPD)Maintenance (Asthma with ICS, COPD)Maintenance (COPD, Asthma)
  • 📌 Mnemonic (SABA): "Salbutamol Alleviates Breathlessness Acutely."
  • Key Side Effects: Tachycardia, palpitations, tremor, hypokalemia (monitor K+), headache.

Exam Favourite: Formoterol (LABA) has rapid onset (2-3 min), like SABAs, suiting reliever/maintenance (SMART therapy).

Antimuscarinics (Anticholinergics) - Block That Squeeze

  • Mechanism: Block M3 receptors in airway smooth muscle → bronchodilation by ↓ vagal tone.

  • Primary use: COPD (maintenance/relief). Adjunct in severe asthma.

  • Comparison:

    FeatureSAMA (e.g., Ipratropium)LAMA (e.g., Tiotropium)
    Onset15-30 min~30 min
    Duration4-6 hrs12-24 hrs (Tio: 24h)
    UseAcute relief (COPD/asthma)Maintenance (COPD, asthma)
  • Key Drugs:

    • SAMA: Ipratropium bromide, Oxitropium bromide.
    • LAMA: Tiotropium, Glycopyrronium, Aclidinium, Umeclidinium.
  • Side Effects: Dry mouth (common), metallic taste. Systemic effects (blurred vision, urinary retention) rare with inhaled quaternary amines.

  • Caution: Narrow-angle glaucoma, BPH. ACh effects on airways: bronchoconstriction, inflammation

⭐ Ipratropium, a quaternary amine, has minimal systemic absorption, enhancing safety.

Methylxanthines - Old School Power

  • Examples: Theophylline, Aminophylline (IV).
  • MOA: Non-selective PDE inhibition (↑cAMP, ↑cGMP); Adenosine receptor antagonism; ↑HDAC activity (anti-inflammatory).
  • Therapeutic Range: 10-20 mcg/mL (narrow).
  • AEs: Tachycardia, arrhythmias, N/V, CNS stimulation, seizures (toxic).
    • 📌 THEO: Tremors/Tachycardia, Hyperthermia/Headache, Emesis, Overdose (seizures, arrhythmias).
  • Interactions: CYP450 metabolism (many drugs affect levels; smoking ↓ levels).

    ⭐ Theophylline toxicity is precipitated by macrolides (e.g., erythromycin) and quinolones (e.g., ciprofloxacin) due to CYP1A2 inhibition.

Bronchodilator Clinical Strategy - Pick Your Player

  • SABA (Salbutamol): Acute relief (SOS).
  • LABA (Salmeterol, Formoterol): Chronic asthma (with ICS), COPD.
  • SAMA (Ipratropium): Acute asthma/COPD (adjunct).
  • LAMA (Tiotropium): COPD (mainstay), severe asthma.
  • Methylxanthines (Theophylline): 3rd line, monitor levels.

⭐ Formoterol: a LABA with rapid onset, suitable for SMART therapy (Single Maintenance And Reliever Therapy) in asthma.

High‑Yield Points - ⚡ Biggest Takeaways

  • SABA (e.g., Salbutamol) are first-line rescue for acute asthma attacks.
  • LABA (e.g., Salmeterol) for asthma maintenance, always combined with ICS.
  • Anticholinergics (e.g., Ipratropium, Tiotropium) are first-line for COPD; Ipratropium in severe acute asthma.
  • Theophylline: narrow therapeutic index; watch for seizures and arrhythmias.
  • Leukotriene antagonists (e.g., Montelukast) for aspirin-exacerbated respiratory disease & exercise-induced asthma.
  • Omalizumab (Anti-IgE monoclonal antibody) for severe, persistent allergic asthma.
  • Roflumilast (PDE-4 inhibitor) reduces COPD exacerbations in severe cases_._

Practice Questions: Bronchodilators

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Aminophylline inhibits which of the following enzymes?

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Flashcards: Bronchodilators

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Paradoxical bronchoconstriction with ipratropium bromide is seen with a _____tonic nebulizer solution

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Paradoxical bronchoconstriction with ipratropium bromide is seen with a _____tonic nebulizer solution

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