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systemic pharmaco > Respi - Anti-asthma Drugs > Flashcards

Respi - Anti-asthma Drugs Flashcards

1
Q

Asthma is characterized by (3)

A
  1. Hyper-responsiveness of the airway
  2. Recurrent reversible airway obstruction
  3. Chronic airway inflammation
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2
Q

Classes of anti-asthma drugs used & examples

A

Controllers (anti-inflammatory)

  1. Inhaled Corticosteroids (Fluticasone, Ciclesonide)
  2. Leukotriene Receptor Antagonist (Montelukast)
  3. Cromolyn
  4. Anti-IgE Antibody (Omalizumab)

Relievers (bronchodilators)

  1. β2 Agonists (SABA - Salbutamol, LABA - Salmeterol, ULABA - Indacaterol)
  2. Methylxanthine (Theophylline)
  3. Anti-Muscarinic (Ipratropium Bromide)
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3
Q

Mechanism of action of inhaled corticosteroids

A
  1. Binds to steroid receptors in cell cytoplasm - forms a complex that enters nucleus - binds to glucocorticoid response element (GRE) - controls protein synthesis
  2. Inhibits enzyme phospholipase A2 (arachidonic acid - inflammation) - Anti-inflammatory effects
    - DECREASED T cells, mast cells, macrophages, eosinophils in the airways; shedding of epithelial cells, macrophage phagocytosis & production of cytokines & proteases, COX2, 5-LOX, iNOS & PLA2 expression
    - INCREASED lipocortin, β2 receptors on airway smooth muscle
    - direct vasoconstriction and decreased plasma exudation/mucus secretion
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4
Q

Uses of inhaled corticosteroids (2)

A
  1. 1st line prophylactic Asthma therapy

2. Nocturnal Asthma

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5
Q

Toxicity of inhaled corticosteroids (7)

A
  1. Oropharyngeal Candidiasis - immune suppression
  2. Dysphonia - problem with vocal cords leading to hoarseness
  3. Cough/Throat Irritation
  4. Easy bruising of skin (elderly)
  5. Adrenal Suppression
  6. Posterior Subcapsular Cataracts
  7. Osteoporosis
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6
Q

Mechanism of action of leukotriene receptor antagonist

A

Blocks LTD4 in the leukotriene pathway which contributes to the pathogenesis of asthma (bronchoconstriction, inflammation)

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7
Q

Uses & toxicity of leukotriene receptor antagonists (3+1)

A
  1. Prophylaxis & chronic treatment of asthma
  2. Aspirin-induced asthma
  3. Exercise-induced asthma
  4. Eosinophilia
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8
Q

Mechanism of action of cromolyn

A
  1. Inhibits mast cell degradation induced by IgE-mediated FcεRI cross linking
  2. Alters delayed Cl channels - inhibits cellular activation
  3. Promotes secretion of Annexin A1/Lipocortin-1 - blocks histamine & eicosanoid release from mast cells
  4. Blocks release of inflammatory mediators from eosinophils, neutrophils, macrophages
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9
Q

Uses of cromolyn (2)

A
  1. Prophylactic control of Asthma
  2. Prophylactic control of Allergic Rhinitis/Conjunctivitis
    - prevents cold, dry air & exercise-induced bronchospasm
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10
Q

Toxicity of cromolyn (2)

A
  1. Throat irritation, dry mouth, coughing (preventable by first inhaling β2 agonist)
  2. Unpleasant, bitter taste
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11
Q

Mechanism of action of anti-IgE antibody

A
  1. Binds to Fc portion of IgE - decreases FcεRI expression on mast cells/basophils - prevents degranulation & asthmatic reaction
  2. Depletes free IgE levels in serum
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12
Q

Uses of anti-IgE antibody (2)

A
  1. Allergic Asthma

2. Allergic Rhinitis

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13
Q

Mechanism of action of β2 agonists

A
  1. Activates β2GPCR - activates adenylyl cyclase - increased cAMP leading to (A) decreased intracellular Ca (B) decreased MLCK (C) increased K+ conductance - leading to airway smooth muscle relaxation
  2. Mast cell stabilization, reduced microvascular leakiness, increased mucociliary clearance
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14
Q

Uses of β2 agonists (3)

A
  1. SABA - reverses constricted airways (PRN)
  2. LABA - prevents exercise-induced asthma + long term maintenance of (nocturnal) asthma
  3. ULABA - COPD
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15
Q

Toxicity of β2 agonists (6)

A
  1. Fine tremor of skeletal muscle
  2. Muscle cramps
  3. Peripheral vasodilation
  4. Palpitations & tachycardia (cross reaction with β1 receptors)
  5. Hypokalemia, Hyperglycemia
  6. Tolerance
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16
Q

Mechanism of action of theophylline

A
  1. Inhibits PDE which breaks down cAMP - increased cAMP - increased ASM relaxation
  2. Inhibits adenosine which causes SM constriction
    - Increased epinephrine release from adrenal medulla
    - Decreased microvascular leakiness
    - Increased contractility of fatigued diaphragm in COPD
17
Q

Uses of theophylline (3)

A
  1. Adjunct/add-on therapy to inhaled β2 agonists/steroids
  2. Nocturnal bronchospasm (sustained release)
  3. Improve lung function in COPD
18
Q

Toxicity of theophylline (3)

A
  1. GIT-related (nausea, vomiting, anorexia, abdominal discomfort)
  2. CNS (nervousness, tremor, anxiety, headache, seizures)
  3. CVS (arrhythmias)
19
Q

Mechanism of action of ipratropium bromide

A
  1. Inhibits M3 receptor-mediated bronchospasm (M3R is only expressed in airways)
    - reverses portion of bronchospasm & mucus secretion caused by vagal nerve
  2. Inhibits M2-nerve terminal transiently - bronchodilation
20
Q

Uses of ipratropium bromide (2)

A
  1. Adjunct/add-on therapy to inhaled steroids/β2 agonists
  2. Patients intolerant of β2 agonists
  3. COPD (more bronchodilator effect)
21
Q

Toxicity of ipratropium bromide (4)

A
  1. Unpleasant Taste
  2. Dry Mouth
  3. Urinary Retention in elderly
  4. Paradoxical Bronchospasm

systemic pharmaco (18 decks)

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