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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
what is zileuton?
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
what is montelukast?
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
what is theophylline, theobromine, caffeine?
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
what is ipratropium?
1. bronchodilator 2. quaternary amine of atropine 3. poorly absorbed after inhaled 4. minimal bioavailability 5. relatively free of systemic atropine-like effects
29
what are cromolyn and nedocromil?
1. inhibit mast cell degranulation 2. once widely used especially in children 3. current indication is allergic conjuntivitis in eye grops
30
what is omalizumab?
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
what is mepolizumab and reslizumab?
1. anti-IL-5 MAB 2. maintenance therapy for severe asthma in pts with eosinophilic phenotype
32
what is benralizumab?
- anti-IL-5 receptor MAB - maintenance therapy for severe asthma in pts with eosinophilic phenotype

Asthma/COPD Exam 3 (9 decks)

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