Exam 3: Drugs Flashcards
SABAs
-Metaproterenol
-Terbutaline
-Albuterol
-Pirbuterol
LABAs
-Salmeterol
-Formoterol
Inhaled Corticosteroids
-Triamcinolone acetonide
-beclomethasone dipropionate
-flunisolide
-budesonide
-mometasone furoate
-fluticasone propionate
-ciclesonide
Leukotriene pathway inhibitors
-Zileuton
-Zafirlukast
-Montelukast
Methylxanthine drugs
-Theophylline
-Theobromine
-Caffeine
Antimuscarinic agents
-Ipatropium
Mast cell stabilizers
-Cromolyn
-Nedocromil
Monoclonal antibodies
-Omalizumab
-Mepolizumab
-Reslizumab
-Benralizumab
B2 selectivity from
-bulky N substitutions
-phenyl ring substitutions (also COMT resistant)
B2 agonist risks
-tachycardia
-muscle tremors
-induction of tachyphylaxis (reduction in bronchodilator reponse)
SABA use
-PRN for acute attacks
Metaproterenol
-SABA
-least potent
-good oral bioavailability
-analog of terbutaline
Terbutaline
-SABA
-N-t-butyl analog of Metaproterenol
=greater selectivity and potency
Albuterol
-SABA
-most used
-COMT resistant
-salicyl alcohol in phenyl ring
Pirbuterol
-SABA
-pyridine version of albuterol
-less potent
Salmeterol
-LABA
-available as powder
-higher lipid solubility
Formoterol
-LABA
-available as powder
-more rapid onset
-COMT and MAO resistant
SABA tips
-5 min onset
-4-8h duration
-good oral bioavailability
-STRUCTURE
LABA tips
-available as powder
-long ass structure
-better lipid solubility
Inhaled corticosteroid use
-persistant asthma maintenance therapy
-not curative
-most effective way to minimize systemic effects
Adverse effects of ICSs
-candidiasis
-hoarseness from effect on vocal cords
-long term use may inc risk of osteoporosis and cataracts
-1 cm reduction of growth in kids only for the first year
Leukotriene pathway inhibitor tips
-improve asthma control
-reduce freq of exacerbations
-not as effective as inhlaed glucocorticoids
-effective orally, easier for kids
-reduce response to aspirin in aspirin-induced asthma
Types of leukotriene pathway inhibitors
-5-lipoxygenase inhibitor
-cysLT inhibitors
Zileuton
-5-lipoxygenase inhibitor (LT pathway inhibitor)
-N-hydroxy group
-alternative to LABA in addition to ICSs
-not for acute asthma attack
-monitor liver function
Montelukast
-LT pathway inhibitor
-blocks LTC4, LTD4, LTE4 binding to receptor
-once daily
-reduce freq of exacerbations
-little toxicity
Zafirlukast
Methylxanthine drug mech
-inhibit PDE to inc cAMP
=bronchoDILATION
=SUPPRESS histamine release
-block adenosine action (dilation and histamine)
-histone deacetylation to suppress inflammatory gene expression
methylxanthine toxicity
-nausea, vomiting, tremulousness, arrhythmias
-narrow therapeutic index
antimuscarinic mech
-inhibit action of constriction and mucus secretion
Ipratropium
-bronchodilator
-antimuscarinic
-4’ amine derivative of atropine but less effects
-minimal bioavailability (poor absorption)
-better for pts intolerant of B agonists
Cromolyn and Nedocromil
-inhibit mast cell degranulation
-daily dosing
-poorly absorbed, not as good as glucocorticoids
-used in eye drops for allergic rhinoconjuctivitis
Omalizumab
-anti-IgE mAb
-inhibits IgE binding to mast cell
-for pt w severe asthma and allergic sensitization
Mepolizumab
-anti-IL-5 mAbs
-maintenance therapy of severe asthma in pt w eosinophillic phenotype
Reslizumab
-anti-IL-5 mAbs
-maintenance therapy of severe asthma in pt w eosinophillic phenotype
Ultra-LABA
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