Drugs used in Asthma Flashcards

1
Q

What is extrsinic asthma?

A
  1. allergic or classical asthma
  2. onset is early in life
  3. elevated serum IgE levels and eosinophil count
  4. driven by Th2 subset and CD4+ T cells
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2
Q

what is intrinsic asthma?

A
  1. nonimmune triggering mechanism
  2. no personal or family history of allergy
  3. serum IgE levels are normal
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3
Q

what are the main events for acute bronchoconstriction?

A
  1. IAR (30-60min)
  2. after sensitization
  3. mast cell degranulation from re-exposure to allergen
  4. smooth muscle contraction
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4
Q

what are the main events for sustained bronchoconstriction?

A
  1. LAR (4-8 hrs)
  2. caused by activation of TH2 cells and cytokine production
  3. attract/ activate eosinophils
  4. stimulate mucus hyper-secretion
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5
Q

what is the role of IgE in the pathology of extrinsic asthma?

A
  1. elevated IgE serum levels and eosinophil count
  2. acute bronchoconstriction mediated by IgE
  3. IgE production stimulated in sustained BC
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6
Q

what is the role of mast cells in the pathology of extrinsic asthma?

A
  1. in acute they are degranulated and produced LLTC/LTD, PGD2, H, tryptase
  2. after sensitization IgE binds to FceR-l on mast cells
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7
Q

what immune cells are responsible in asthma?

A

mast cells, eosinophils, Th2, B cells,NKT cells

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8
Q

what is the role of vagal (PSNS) receptors in bronchoconstriction?

A

direct stimulation provoke reflex bronchoconstriction

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9
Q

what drugs are SABAs?

A
  1. metaproterenol
  2. terbutaline
  3. albuterol
  4. pirbuterol
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10
Q

What drugs are LABAs?

A
  1. salmeterol
  2. formoterol
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11
Q

What drugs are ICS?

A
  1. triamcinolone acetonide
  2. beclomethasone dipropionate
  3. flunisolide
  4. budesonide
  5. mometasone furoate
  6. ciclesonide
  7. fluticasone propionate
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12
Q

what drugs are leukotriene pathway inhibitors?

A
  1. zileuton
  2. montelukast
  3. zafirlukast
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13
Q

what drugs are methylxanthine?

A
  1. theophylline
  2. theobromine
  3. caffeine
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14
Q

what drugs are antimuscarinic agents?

A

ipratropium

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15
Q

what drugs are mast cell stabilizers?

A
  1. cromolyn
  2. nedocromil
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16
Q

what drugs are MABs?

A
  1. omalizumab
  2. mepolizumab
  3. reslizumab
  4. benralizumab
17
Q

what meds are mostly used in asthma?

A

sympathomimetics and ICSs

18
Q

what is metaproterenol?

A
  1. resorcinol analogue of isoproterenol
  2. somewhat selective for B2 receptor
  3. least potent B2 agonist
  4. 5 min onset and 4 hr duration
  5. good bioavailability
19
Q

what is terbutaline?

A
  1. greater B2 selectivity
  2. good bioavailability
  3. 3-fold greater potency than metaproterenol at B2 receptors
  4. N-t-butyl analogue of metaproterenol
20
Q

what is albuterol?

A
  1. most widely used
  2. 5 min onset and 4-8 hr duration
  3. R isomer to levoalbuterol
    – more potent and expensive
  4. salicyl alcohol in the phenyl ring -> resistant to COMT
21
Q

what is pirbuterol?

A
  1. analogous to albuterol except pyridine ring
  2. comparable duration of action as albuterol
  3. less potent
22
Q

what is salmeterol?

A
  1. available as powder
  2. greater lipid solubility; dissolve in cellular membranes
  3. 20 min onset and 12 hr duration
23
Q

what is formoterol?

A
  1. available as powder
  2. resistant to COMT and MAO
  3. more rapid onset with comparable duration of action
24
Q

what is ciclesonide?

A

21 ester prodrug associated with less candidiasis
1. ICS

25
Q

what is zileuton?

A
  1. 5-lipoxygenase inhibitor
  2. racemic
  3. N-hydroxy essential for activity
  4. good bioavailability
  5. alternative to LABA in addition to ICS
  6. not for acute asthma attacks
  7. requires periodic monitoring of liver function
26
Q

what is montelukast?

A
  1. blocks binding of LTC4, LTD4, and LTE4 to receptor
  2. QD dosing
  3. good bioavailability
  4. little toxicity
  5. reduce frequency of asthma exacerbations
27
Q

what is theophylline, theobromine, caffeine?

A
  1. theophylline (most effective and specific for smooth muscle)
  2. used to be treatment for asthma but replaced by LABAs
  3. low cost and still used in some countries
28
Q

what is ipratropium?

A
  1. bronchodilator
  2. quaternary amine of atropine
  3. poorly absorbed after inhaled
  4. minimal bioavailability
  5. relatively free of systemic atropine-like effects
29
Q

what are cromolyn and nedocromil?

A
  1. inhibit mast cell degranulation
  2. once widely used especially in children
  3. current indication is allergic conjuntivitis in eye grops
30
Q

what is omalizumab?

A
  1. inhibit IgE binding to mast cells
  2. severe asthma/ allergic sensitization
  3. anti- IgE
    – recognize portion of IgE that binds on immune cells (FcER-l and 2)
31
Q

what is mepolizumab and reslizumab?

A
  1. anti-IL-5 MAB
  2. maintenance therapy for severe asthma in pts with eosinophilic phenotype
32
Q

what is benralizumab?

A
  • anti-IL-5 receptor MAB
  • maintenance therapy for severe asthma in pts with eosinophilic phenotype