Unit 4-Asthma Flashcards
Albuterol; Terbutaline; Metoproterenol; Pirbutal
Drug class
Bronchodilator - short-acting β2 agonist)
Albuterol; Terbutaline; Metoproterenol; Pirbutal
Mechanism
Relax bronchial smooth muscle, inhibit mediator release (mast cells, basophils), increase mucociliary clearance, suppression of microvascular permeability
Albuterol; Terbutaline; Metoproterenol; Pirbutal
Uses
Prevent or reduce exercise-induced bronhospasms; mild asthma & acute exacerbations
Albuterol; Terbutaline; Metoproterenol; Pirbutal
Side effects
Musculoskeletal tremor, Tachycardia, hyperglycemia, hypokalemia, hypomagnesemia
Tolerance with chronic use, Prolonged QTc, lactic acidosis, paradoxical bronchospasm
5 minutes to take action, 4-6 hours duration; nebulizer delivers more, but greater side effects. Note: Levalbuterol is R-isomer of albuterol.
Salmeterol (Serevent); Formoterol; Indacaterol
Drug class
Bronchodilator - long-acting β2 agonist
Salmeterol (Serevent); Formoterol; Indacaterol
Uses
used for long-term control of asthma symptoms (always in comination with inhaled steroids)
Salmeterol (Serevent); Formoterol; Indacaterol
Side effects
Salmeterol (Serevent); Formoterol; Indacaterol
Mechanism
Relax bronchial smooth muscle, inhibit mediator release (mast cells, basophils), increase mucociliary clearance, suppression of microvascular permeability
Salmeterol (Serevent); Formoterol; Indacaterol
Side effects
Musculoskeletal tremor, Tachycardia, hyperglycemia, hypokalemia, hypomagnesemia
Tolerance with chronic use, Prolonged QTc, lactic acidosis, paradoxical bronchospasm
10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal
Theophylline (Theolair); Theobromine; Caffeine
Drug class
Bronchodilator (Methylxanthine)
Theophylline (Theolair); Theobromine; Caffeine
Mechanism
Phosphodiesterase inhibition and enhanced signalling via increased cAMP and cGMP; relax bronchial smooth muscle
Theophylline (Theolair); Theobromine; Caffeine
Uses
Reduce inflammation and bronchospasm in moderate to severe asthma, night symptoms
Theophylline (Theolair); Theobromine; Caffeine
Side effects
CNS stimulation or seizures, tachycardia/arrythmias, anorexia, nausea
Low therapeutic index! Metabolized by liver; cimetidine and quinoline increase blood levels
Roflumilast
Drug class
Methylxanthine
Roflumilast
Mechanism
Selective PDE4 inhibitor; more of an anti-inflammatory agent than bronchodilator
Roflumilast
Uses
COPD
Roflumilast
Side effects
CNS stimulation or seizures, tachycardia/arrythmias, anorexia, nausea
Ipratropium (Atrovent); Tiotropium; Atropine
Drug class
Quarternary amine antimuscarinic
Ipratropium (Atrovent); Tiotropium; Atropine
Mechanism
Blocks vagal pathways and decreases vagal tone to bronchial smooth muscle; also blocks the reflex bronchoconstriction caused by inhaled irritants
Note: tiotropium has anti-inflammatory properties and decreases mucus secretion.
Ipratropium (Atrovent); Tiotropium; Atropine
Uses
First-line agent for chronic COPD; status asthmaticus (w/ nebulized β2-agonists); no role in chronic stable asthma
Ipratropium (Atrovent); Tiotropium; Atropine
Side effects
Typical antimuscarinic effects; acute angle glaucoma; paradoxical bronchospasm
Aclidinium Bromide
Drug class
Quarternary amine antimuscarinic
Aclidinium Bromide
Mechanism
Blocks vagal pathways and decreases vagal tone to bronchial smooth muscle; also blocks the reflex bronchoconstriction caused by inhaled irritants
Aclidinium Bromide
Uses
Functionally similar to tiotropium
Aclidinium Bromide
Side effects
Less systemic & CNS side effects than other antimuscarinics due to extremely short circulation half-life.
Budesonide; Fluticasone propionate; beclomethasone
Drug class
Corticosteroid - anti-inflammatory agent
Budesonide; Fluticasone propionate; beclomethasone
Mechanism
Anti-inflammatory effects: inhibition of growth factor secretion, inhibition of arachidonic acid metabolites and platelet activation factor, inhibition of leukocyte accumulation, decreased vascular permeability, inhibition of neuropeptide-mediated responses, inhibition of mucous glycoprotein secretion
Budesonide; Fluticasone propionate; beclomethasone
Uses
Cornerstone treatment of persistent asthma; beneficial combination with beta-2 agonist; limited role in COPD
Budesonide; Fluticasone propionate; beclomethasone
Side effects
Inhaled has thrush, hoarseness, dry cough, mild adrenal suppression (higher doses); oral has mood-swings, increased appetite, and suppression of adrenocorticotropic hormone secretion (Cushing’s Syndrome)
Ciclesonide
Drug class
Corticosteroid - anti-inflammatory agent
Ciclesonide
Mechanism
Same as other corticosteroids, but is a prodrug and only activated by airway esterase.
Ciclesonide
Uses
Cornerstone treatment of persistent asthma; beneficial combination with beta-2 agonist; limited role in COPD
Ciclesonide
Side effects
Less side effects than other corticosteroids (on site activation required)
Sodium cromoglycate; Nedocromil sodium
Drug class
Anti-inflammatory agent
Sodium cromoglycate; Nedocromil sodium
Mechanism
Prevent mast cell degranulation and mediator release from mast cells
Sodium cromoglycate; Nedocromil sodium
Uses
Prophylaxis for inhibiting both early and late phase reactions; best results in mild and allergic asthma
Sodium cromoglycate; Nedocromil sodium
Side effects
Minimal local side effect (cough & throat irritation)
Montelukast (Singulair); Pranlukast (Azlaire); Zafirlukast (Accolate)
Drug class
Leukotriene inhibitor
Montelukast (Singulair); Pranlukast (Azlaire); Zafirlukast (Accolate)
Mechanism
Leukotriene receptor antagonist
Montelukast (Singulair); Pranlukast (Azlaire); Zafirlukast (Accolate)
Uses
Add-on therapy in mild persistent asthma; aspirin-induced asthma; prophylaxis for exercise-induced bronchospasm
Montelukast (Singulair); Pranlukast (Azlaire); Zafirlukast (Accolate)
Side effects
Well tolerated
Must monitor liver function test.
Zileuton
Drug class
Leukotriene inhibitor
Zileuton
Mechanism
Inhibits 5-lipoxygenase and blocks leukotriene synthesis
Zileuton
Uses
Add-on therapy in mild persistent asthma; aspirin-induced asthma; prophylaxis for exercise-induced bronchospasm
Zileuton
Side effects
Liver toxicity
Omalizumab
Drug class
Anti-IgE mAB
Omalizumab
Mechanism
Blocks IgE function.
Omalizumab
Uses
Poorly controlled severe asthma
Administered by subQ injection every 3 weeks