Asthma meds Flashcards
Short Acting B2 agonists
Albuterol, Terbutaline, Metoproterenol, Pirbutol
Mech: Relax bronchial smooth muscle, inhibit mediator release (mast cells, basophils), increase mucociliary clearance, suppression of microvascular permeability
Thera: Prevent or reduce exercise-induced bronchospasms
Mild asthma
Acute exacerbations
Tox: (selectivity is lost with high doses) Musculoskeletal tremor, tachy, hyperglycemia, hypokalemia, hypomagnesemia, tolerance with chronic use, prolonged QT, lactic acidosis, paradoxical bronchospasm (downregulation of B2 receptor)
Misc: 5 minutes to take action, 4-6 hour duration, nebulizer delivers more but greater side effects
Levalbuterol is R-isomer of albuterol (S-isomer may promote inflammation and induce SEs)
Long-Acting B2 agonists
Salmeterol, Formoterol, Indacaterol
Mech: Relax bronchial smooth muscle, inhibit mediator release (mast cells, basophils), increase mucociliary clearance, suppression of microvascular permeability
Thera: Used for long-term control of asthma symptoms (always in combination with inhaled steroids)
Tox: (selectivity is lost with high doses) Musculoskeletal tremor, tachy, hyperglycemia, hypokalemia, hypomagnesemia, tolerance with chronic use, prolonged QT, lactic acidosis, paradoxical bronchospasm (downregulation of B2 receptor)
Misc: 10-15 min to take action, 6-12 hours duration, nebulizer delivers more but greater SEs; oral is least effective and most SEs; can be used for night symptoms but not ideal
Quaternary amine antimuscarinic
Ipratropium, Tiotropium, Atropine
Mech: Blocks vagal pathways and decreases vagal tone to bronchial smooth muscle; also blocks the reflex bronchoconstriction caused by inhaled irritants
Thera: First line agent for chronic COPD; status asthmaticus (with nebulized B2 agonists); no role in chronic stable asthma
Tox: Antimuscarinic effects, acute angle glaucoma, paradoxical bronchospasm
Misc: Tiotropium has anti-inflammatory (reduce neutrophil migration) properties and decreased mucus secretion and much longer halflife, more selective for M3
Atropine has much higher side effects and much more oral bioavailability
Tiotropium may have some use in chronic asthma
Aclidinium Bromide
Class: Quaternary amine antimuscarinic
Mech: Blocks vagal pathways and decreases vagal tone to bronchial smooth muscle; also blocks the reflex bronchoconstriction caused by inhaled irritants
Thera: First line agent for chronic COPD; status asthmaticus (with nebulized B2 agonists); no role in chronic stable asthma
Tox: Less systemic and CNS SEs other than antimuscarinics due to extremely short circulation half-life (metabolized in plasma)
Theophylline, theobromine, caffeine
Class: Methylxanthines
Mech: PDEi increasing cAMP and cGMP which relaxes smooth muscle (weak bronchodilator)
Thera: Reduce inflammation and bronchospasm in moderate to severe asthma, Reverse fatigue in diaphragm in COPD, night symptoms, restores corticosteroid sensitivity
Tox: CNS stimulation or seizures, tachy, anorexia, nausea, cardiac arrhythmias, GERD
Misc: Low therapeutic index, metabolized by the liver
Roflumilast
Class: Methylxanthine
Mech: Selective PDE4i which gives more anti-inflammatory agent than bronchodilator
Thera: COPD
Tox: CNS stimulation/seizures, tachy, anorexia, nausea
Corticosteroids
Budesonide, Fluticasone propionate, beclomethasone
Mech: Anti-inflammatory effects: inhibition of GF secretion, inhibition of AA and platelet activation factor, inhibition of leukocyte accumulation, decreased vascular permeability, inhibition of neuropeptide-mediated response, inhibition of mucus
Thera: Cornerstone treatment of persistent asthma, Combine with beta2 agonists, limited role in COPD
Tox: Inhaled has thrush, hoarseness, dry cough, mild adrenal suppression (high doses)
Oral has mood swings, increased appetite, Cushing
Ciclesonide
Class: Corticosteroid
Mech: Prodrug and only activated by airway esterase
Thera: Cornerstone treatment of persistent asthma, Combine with beta2 agonists, limited role in COPD
Tox: Less SEs due to on site activation
Leukotriene inhibitor
Montelukast, Pranlukast, Zafirlukast,
Mech: Leukotriene receptor antagonist
Thera: Add-on therapy in mild persistent asthma; aspirin induced asthma; prophylaxis for exercise induced bronchospasm
No role in COPD
Tox: well tolerated
Misc: Monitor liver function
Zileuton
Class: Leukotriene inhibitor
Mech: Inhibits 5-lipoxygenase and blocks leukotriene synthesis
Thera: Add-on therapy in mild persistent asthma; aspirin induced asthma; prophylaxis for exercise induced bronchospasm
No role in COPD
Tox: Liver toxicity
Sodium cromoglycate, Nedocromil sodium
Class: Anti-inflammatory agent
Mech: Prevent mast cell degranulation and mediator release from macrophage and eosinophil (altered function of delayed chloride channel)
Thera: Prophylaxis for inhibiting both early and late phase reactions; best results in mild and allergic asthma
No role in COPD
Tox: Cough and throat irritation
Omalizumab
Class: Anti-IgE mAB
Mech: Blocks IgE funciton
Thera: Poorly controlled severe asthma (reduces the requirement for oral and inhaled corticosteroids)
Reduces asthma exacerbations
Misc: Administered by subcutaneous injection every 3 weeks
