Lecture 23: Asthma Drugs Flashcards by Brooke Thornburg

Short-acting B2 agonist (SABA) use

-PRN for acute attacks

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SABA drugs

-albuterol
-terbutaline
-metaproterenol
-pirbuterol

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Long acting B2 agonists (LABA) uses

-additional therapy in pts using inhaled glucocotricoids
-daily use
-not for acute attacks

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LABA black box warning

-not an anti-inflammatory
-should NOT be used as monotherapy for asthma

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LABA drugs

-salmeterol
-formoterol

-commonly available with cortiosteroids

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Metaproterenol

-SABA
-4 hour
-analog of isoproterenol
-least potent B2 agonist
-good oral availability

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Terbutaline

-SABA
-N-t-butyl analog of metaproterenol
-greater B2 selectivity
-3x more potent than metaproterenol
-good oral availability

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Albuterol

-SABA
-most used
-4-8hour
-salicyl alcohol in phenyl = COMT resistant

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Levalbuterol

-R-isomer or albuterol
-greater potency
-more expensive

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Pirbuterol

-SABA
-analogous to albuterol except the pyridine ring
-similar duration but less potent than albuterol

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Salmeterol

-LABA
-available as powder
-greater lipid solubility;dissolve in cell membranes
-12 hour

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Formoterol

-LABA
-available as powder
-more rapid onset but similar duration to salmeterol
-resistant to COMT and MAO

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Inhaled Corticosteroids (ICSs)

-maintenance therapy for persistant asthma
-not curative (effective only when taken)
-systemic/oral admin for severe cases only
-most effective way to minimize systemic effects

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Inhaled corticosteroids (ICSs) drugs

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

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ICS adverse effects

-candidiasis
-hoarseness (effect on vocal cords)
-long-term inc risk of osteoporosis and cataracts
-1 cm reduction of growth of children in the first year

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Candidiasis treatment

-clotrimazole
-reduced by gargling water after each use
-ciclesonide (21-ester prodrug) associated w less effects

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Leukotrienes

-produced from arachidonic acid by 5-lipoxygenase
-involved in inflammatory diseases and anaphylaxis

LTB4

-potent neutrophil chemoattractant
-leukotriene

LTC 4 and LTD4

-bronchoconstriction
-inc bronchial reactivity
-mucosal edema
-mucus hypersecretion

Leukotriene pathway inhibitors

-improve asthma control
-reduce freq of exacerbations
-not as effective as ICSs
-effective orally
-reduce response to aspirin in aspirin-induced asthma

Types of leukotriene pathway inhibitors

-5-lipoxygenase inhibitor
-cysLTI receptor ANTagonists

5-lipoxygenase drug

zileuton

cysLTI ANTagonist drugs

-Zafirlukast
-Montelukast

Zileuton

-5-lipoxygenase inhibitor
-good oral availability
-alternative to LABA in addition to ICSs
-NOT for acute attack
-requires periodic monitoring of liver function

Montelukast

-blocks binding of LTC, LTD, LTE4 to receptor -once daily -good oral bioavailability -reduces frequency of asthma exacerbations -little toxicity

Methylxanthine drugs

-theophylline -theobromine -caffeine -replaced by B2 agonists but used in some countries bc it cheap

Methylxanthine SAR

-6-ring next to 5 ring

Methylxanthine drug mechanism

-inhibit phosphodiesterase -inc cAMP -bronchodilation -suppress histamine release -block adenosine action (constriction and H release) -histone deacetylation (suppresses inflammatory genes)

Methylxanthine toxicity

-nausea -vomiting -tremulousness -arrhythmias -narrow therapuetic index

Antimuscarinic agents

-anticholinergics -for pts intolerant of B agonists

Antimuscarinic mechanism

-inhibit acetylcholine at muscarinic receptors -doesn't allow bronchoconstriction and mucus secretion

Antimuscarinic drug

Ipratropium

-bronchodilator -4' amine derivative of atropine -poorly absorbed into circulation after inhaled -minimal oral bioavailability -relatively free of systemic atropine-like effects

Mast cell stabilizers

-inhibit mast cell degranulation -no direct action, use daily -poorly absorbed -little toxicity -not a potent or effective as glucocorticoids -currently used for allergic rhinoconjuctivitis eye drops

Mast cell stabilizer drugs

-Cromolyn -Nedocromil

Omalizumab

-inhibits IgE binding to mast cells -reserved for patients w severe asthma and allergic sensitization

IL-5

-attracts and activates eosinophils

Anti-IL-5 mABs

-mepolizumab -Reslizumab

Anti-IL-5 receptos mABs

-Benralizumab

Anti IL-5 therapy

-used as maintenance therapy of severe asthma in pats w eosinophillic phenotype