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therapeutics > Lecture 23: Asthma Drugs > Flashcards

Lecture 23: Asthma Drugs Flashcards

1
Q

Short-acting B2 agonist (SABA) use

A

-PRN for acute attacks

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2
Q

SABA drugs

A

-albuterol
-terbutaline
-metaproterenol
-pirbuterol

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3
Q

Long acting B2 agonists (LABA) uses

A

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

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4
Q

LABA black box warning

A

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

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5
Q

LABA drugs

A

-salmeterol
-formoterol

-commonly available with cortiosteroids

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6
Q

Metaproterenol

A

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

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7
Q

Terbutaline

A

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

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8
Q

Albuterol

A

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

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9
Q

Levalbuterol

A

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

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10
Q

Pirbuterol

A

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

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11
Q

Salmeterol

A

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

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12
Q

Formoterol

A

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

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13
Q

Inhaled Corticosteroids (ICSs)

A

-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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14
Q

Inhaled corticosteroids (ICSs) drugs

A

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

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15
Q

ICS adverse effects

A

-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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16
Q

Candidiasis treatment

A

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

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17
Q

Leukotrienes

A

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

18
Q

LTB4

A

-potent neutrophil chemoattractant
-leukotriene

19
Q

LTC 4 and LTD4

A

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

20
Q

Leukotriene pathway inhibitors

A

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

21
Q

Types of leukotriene pathway inhibitors

A

-5-lipoxygenase inhibitor
-cysLTI receptor ANTagonists

22
Q

5-lipoxygenase drug

A

zileuton

23
Q

cysLTI ANTagonist drugs

A

-Zafirlukast
-Montelukast

24
Q

Zileuton

A

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

25
Q

Montelukast

A

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

26
Q

Methylxanthine drugs

A

-theophylline
-theobromine
-caffeine

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

27
Q

Methylxanthine SAR

A

-6-ring next to 5 ring

28
Q

Methylxanthine drug mechanism

A

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

29
Q

Methylxanthine toxicity

A

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

30
Q

Antimuscarinic agents

A

-anticholinergics
-for pts intolerant of B agonists

31
Q

Antimuscarinic mechanism

A

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

32
Q

Antimuscarinic drug

A

Ipratropium

33
Q

Ipratropium

A

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

34
Q

Mast cell stabilizers

A

-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

35
Q

Mast cell stabilizer drugs

A

-Cromolyn
-Nedocromil

36
Q

Omalizumab

A

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

37
Q

IL-5

A

-attracts and activates eosinophils

38
Q

Anti-IL-5 mABs

A

-mepolizumab
-Reslizumab

39
Q

Anti-IL-5 receptos mABs

A

-Benralizumab

40
Q

Anti IL-5 therapy

A

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

therapeutics (78 decks)

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