Anti-inflammatory Respiratory Agents

Corticosteroids - Steroid Power Puffs

Potent anti-inflammatory; cornerstone of asthma/COPD therapy.

• MOA: Bind intracellular glucocorticoid receptors → modulate gene expression → ↓ inflammatory mediators (cytokines, PGs, LTs) & ↓ inflammatory cell activity.
• Key Examples:
  • ICS (Inhaled): Beclomethasone, Budesonide, Fluticasone.
  • Systemic: Prednisolone, Hydrocortisone.
• Major Indications:
  • Asthma: First-line controller for persistent disease.
  • COPD: Exacerbations, severe disease (often with LABA).
• Side Effects & Pearls:
  • ICS: Oral candidiasis (thrush), dysphonia. 💡 Pearl: Use spacer; rinse mouth post-ICS to prevent.
  • Systemic (long-term): Cushingoid features, osteoporosis, hyperglycemia, PUD, immunosuppression. 📌 Mnemonic for systemic effects: CUSHINGOID (multiple features).

⭐ Inhaled corticosteroids (ICS) are the most effective long-term control therapy for persistent asthma. oka

Leukotriene Modifiers - Leukotriene Block Party

• Overview: Target leukotrienes, key inflammatory mediators in asthma.
• Classes & MOA:
  • Zileuton: 5-Lipoxygenase (5-LOX) inhibitor. Blocks synthesis of all leukotrienes.
    • Indication: Chronic asthma.
    • ⚠️ Side Effect: Hepatotoxicity (monitor LFTs).
  • Montelukast, Zafirlukast: Cysteinyl Leukotriene Receptor Antagonists (LTRAs). Block CysLT1 receptors. 📌 LUKasts block LeUKotriene receptors.
    • Indications: Add-on asthma therapy, Aspirin-Exacerbated Respiratory Disease (AERD), exercise-induced bronchoconstriction.
    • ⚠️ Side Effects: Montelukast: Neuropsychiatric events. Zafirlukast: Hepatotoxicity, Churg-Strauss (rare).

⭐ Montelukast is particularly useful in patients with aspirin-exacerbated respiratory disease (AERD) due to its effect on cysteinyl leukotrienes.

Mast Cell Stabilizers & Anti-IgE - Allergy Avengers

• Mast Cell Stabilizers: Cromolyn, Nedocromil
  • MOA: Stabilize mast cells → ↓ degranulation & mediator release.
  • Use: Prophylaxis (mild asthma/allergic rhinitis). Not for acute attacks. Limited efficacy.
• Anti-IgE Antibody: Omalizumab (📌 OMA binds IgE)
  • MOA: Monoclonal Ab; binds free IgE → prevents mast cell activation.
  • Indication: Severe allergic asthma (IgE 30-700 IU/mL), ≥6 yrs.
  • Route: Subcutaneous. ⚠️ Key SE: Anaphylaxis.

⭐ Omalizumab is a monoclonal antibody that binds to free IgE, preventing its interaction with mast cells, and is used in severe, persistent allergic asthma.

PDE4 Inhibitors & Novel Agents - COPD's New Guard

• Roflumilast (PDE4 Inhibitor):
  • MOA: $↑cAMP$ in inflammatory cells.
  • Indication: Severe COPD + chronic bronchitis & exacerbations.
  • Side Effects: GI distress, weight loss, mood changes (📌 Roflumilast: Mood, Intestinal, Loss of weight).
• Novel Biologics (Anti-IL5 for Eosinophilic Asthma):
  • Mepolizumab, Reslizumab, Benralizumab.

⭐ Roflumilast: oral PDE4 inhibitor for severe COPD (chronic bronchitis, frequent exacerbations), reduces exacerbations.

High‑Yield Points - ⚡ Biggest Takeaways

• Inhaled Corticosteroids (ICS) are first-line therapy for persistent asthma control.
• Oropharyngeal candidiasis, dysphonia: key local ICS adverse effects; prevent with spacer use & mouth rinsing.
• Systemic corticosteroids are vital for acute severe asthma exacerbations, reducing airway inflammation.
• Montelukast (LTRA) is key for AERD and exercise-induced bronchoconstriction (EIB).
• Mast cell stabilizers (e.g., Cromolyn) prevent mediator release, for asthma prophylaxis only.
• Omalizumab (anti-IgE MAb) treats severe, persistent IgE-mediated allergic asthma.
• Anti-IL-5 biologics (e.g., Mepolizumab) target eosinophils in severe eosinophilic asthma.