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Flashcards in Pulmonary: Asthma Drugs Deck (14)
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1

Bronchoconstriction is mediated by
what two pathways?

Bronchoconstriction is mediated by
what two pathways?

  1. Inflammatory proccesses
  2. Parasympathetic tone

2

β2-agonists Drugs?

β2-agonists Drugs?

  • Albuterol (Salbutamol)
  • Salmeterol (partial agonist)
  • Formoterol (full agonist)
  • Isoproterenol
  • Metaproterenol
  • Terbutaline

3

  • β2-adrenoceptor agonists
  • Stimulates adenylate cyclase, ↑ cAMP, myosin light-chain kinase phosphorylation and inactivation
  • Relaxes Bronchial smooth muscle and bronchodilation
  • ↓ release of Leukotrienes and Histamine, ↓ airway inflammation
  • Use during acute exacerbation, Bronchospasm, Bronchitis, and COPD
  • SE: Tremor, Sinus tachycardia

Albuterol

4

  • β2-agonists
  • Long-acting agents for phrophylaxis due to high lipid solubility and hence easier entry and buildup in smooth muscle cells
  • Adverse effects are Tremor and Arrhythmia

  • Salmeterol
  • Formoterol

5

Methylxantine Drugs?

  • Theophyline (found in Tea)
  • Theobromine (found in Cocoa and Chocolate)
  • Caffeine (found in Coffee and Tea)
     
  • When taken in combination with Acetaminophen and Aspirn, can be used to treat migranes

6

  • Methylxanthine
  • Bronchodilation by inhibiting Phosphodiesterase (PDE inhibitor) → ↑ cAMP levels cause airway smooth muscle relaxation and tachycardia, 
    Due to ↓ cAMP hydrolysis (PDE4)
  • Also blocks adenosine receptors (A1 subtype of P1 Purinergic receptors) → ↑ cAMP levels
  • Usage is limited, SE: Tremor and Agitation
  • Narrow Therapeutic Index (cardiotoxicity, neurotoxicity); metabolized by cytochrome P-450

Theophyline (found in Tea)

7

  • Non-selective Muscarinic antagonists that acts on receptors found at parasympathetic effector sites
  • Derivative of atropine
  • Competitive block of muscarinic receptors
    (Macetylcholine receptors)
  • ↓ Bronchoconstriction and ↓ Bronchial secretions
  • β2-agonists > Antimuscarinics
  • 1st COPD and 2nd Asthma
  • SE: Poor absorption, Dry mouth, Sedation
  • A long-acting muscarinic antagonist

Ipratropium (Atrovent)

8

Aerosolized corticosteroids?

Aerosolized corticosteroids?

  • Beclomethasone (Vanceril, Beclovent)
  • Budesonide (Pulmicort)
  • Ciclesonide (Alvesco)
  • Flunisolide (AeroBid)
  • Fluticasone (Flovent)
  • Mometasone (Asmanex)
  • Triamcinolone (Azmacort)

9

  • Corticosteroids (glucocorticoid)
  • Inhibit synthesis of virtually all Cytokines - binds to cytosolic glucocorticoid receptor (GR) and induces GR nuclear translocation
  • Block the release of AA and syn. of Leukotrienes - blocks Phospholipase A2
  • Inhibit the infiltration of airway by Basophils, Eosinophils, and Mast cells
  • Inactivate NF-kB, the transcription factor that induces the production of TNF-α; and other inflammatory agents
  • 1st line therapy for Chronic Asthma

  • Beclomethasone (Vanceril, Beclovent)
  • Fluticasone (Flovent)

10

  • Antileukotrienes
  • LTD4 receptor blocker on Eosinophils, Mast cells, and Basophils via 5-lipoxygenase on Arachidonic Acid (AA)
  • LTB4 - neutrophil chemoattractant
  • LTC4 and LTD4 - potent bronchoconstrictors - "slow-reacting anaphylaxis" in asthma
  • Especially good for Asprin-induced Asthma (AIA) - thought to be a shift from Prostaglandins to Leukotrienes induced by Aspirin
  • SE: Churg-strauss syndrome (rare)

  • Montelukast
  • Zafirlukast

11

  • Antileukotrienes
  • 5-lipoxygenase pathway inhibitor that catalyzes the commited step in Leukotriene synthesis
  • Blocks conversion of Arachidonic acid to Leukotrienes
  • Metabolized by the CYP450 sys. and can ↑ serum concentrations of Theophylline and Warfarin
  • SE: Hepatotoxicity

Zileutron (Zyflo)

12

  • Anti-IgE Monoclonal antibody
  • Binds mostly to unbound serum IgE
  • Blocks binding of IgE to FcεRI on Mast cells and Basophils -> moderate to severe Asthma
  • Does not activate already bound IgE
  • Used in allergic asthma resistant to inhaled steroids and long-lasting β2-agonists
  • 0.2% risk of Anaphylaxis

Omalizumab (Xolair)

13

  • Non-selective Muscarinic receptor agonist
  • Inhalation agent - Challange -> excessive Bronchoconstriction via M3 receptors in Bronchial smooth muscle.
  • Used to help diagnose Asthma

Methacholine

14

  • Endothelin antagonist
  • Most potent vasoconstrictor  known
    (Smooth muscle - ET, Endothelial cells - ETB)
  • Cx: Pulmonary Arterial Hypertension (PAH)
  • Can cause ↓ levels of Warfarin
  • Competitively antagonizes endothelin-1 receptors
  • Pulmonary Vasodilation
  • Oral medication

Bosentan