Exam 3: Drugs Flashcards by Brooke Thornburg

SABAs

-Metaproterenol
-Terbutaline
-Albuterol
-Pirbuterol

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LABAs

-Salmeterol
-Formoterol

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Inhaled Corticosteroids

-Triamcinolone acetonide
-beclomethasone dipropionate
-flunisolide
-budesonide
-mometasone furoate
-fluticasone propionate
-ciclesonide

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Leukotriene pathway inhibitors

-Zileuton
-Zafirlukast
-Montelukast

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Methylxanthine drugs

-Theophylline
-Theobromine
-Caffeine

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Antimuscarinic agents

-Ipatropium

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Mast cell stabilizers

-Cromolyn
-Nedocromil

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Monoclonal antibodies

-Omalizumab
-Mepolizumab
-Reslizumab
-Benralizumab

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B2 selectivity from

-bulky N substitutions
-phenyl ring substitutions (also COMT resistant)

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B2 agonist risks

-tachycardia
-muscle tremors
-induction of tachyphylaxis (reduction in bronchodilator reponse)

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SABA use

-PRN for acute attacks

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Metaproterenol

-SABA
-least potent
-good oral bioavailability
-analog of terbutaline

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Terbutaline

-SABA
-N-t-butyl analog of Metaproterenol
=greater selectivity and potency

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Albuterol

-SABA
-most used
-COMT resistant
-salicyl alcohol in phenyl ring

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Pirbuterol

-SABA
-pyridine version of albuterol
-less potent

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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