Lecture 3 Asthma/COPD drugs

Question 1

3 components influencing bronchoconstriction in asthma:

which are more important in non-atopic forms?

Answer 1

activation of mast cells

local inflammation, vagal stimulation (these 2)

Question 2

3 categories of things that mast cells release:

Answer 2

histamine, leukotrienes, eosinophil chemotactic factors

Question 3

in the timing of asthma, bronchoconstriction occurs ____, and airway inflammation occurs ____ due ____

Answer 3

early;

late, cell infiltrate (ie eosiniophils)

Question 4

bronchoconstriction:
ATP/cAMP ______ it;
cGMP/GTP _____ it

Answer 4

inhibits (ie bronchodilation), increases

Question 5

Gq receptors involved in bronchoconstriction: (3)

these (increase or inhibit bronchoconstriction)

Answer 5

histamine H1, muscarinic M1, leukotriene CYS-LT1;

increase

Question 6

Gi receceptor involved in bronchoconstriction:

this decreases _____, resulting in _____

Answer 6

Muscarinic M2, cAMP, bronchoconstriction

Question 7

Gs receptor involved in bronchoconstriction:

this increases ___, resulting in ____

Answer 7

B2;

cAMP, bronchodilation

Question 8

bronchodilators cause an (increase or decrease) in intracellular cAMP

Answer 8

increase

Question 9

3 old sympathomimetics that are no longer really used (except for one in particular instances):

Answer 9

epinephrine (used in emergency), ephedrine, isoproterenol

Question 10

2 SABAs (Short acting B2 agonists) most often used:

Answer 10

albuterol, terbutaline (also pirbuterol)

Question 11

how long do SABA’s typically last? any side effects?

Answer 11

3-4 hours;

few, but some with oral forms ie jittery, nervousness

Question 12

in theory, b2 agonists may act on pulmonary vascular beds resulting in vaso____. this causes an increase in _____ mismatches and ______ oxygenation. what kind of patient is this an issue in?

Answer 12

dilation;
V/Q, decreased;
COPD

Question 13

2 long acting beta agonists:

why are these longer lasting?

Answer 13

salmeterol, formoterol;
high lipid solubility

DON’T USE ALONE

Question 14

antimuscarinics reverse the ____ contribution to bronchoconstriction. they have greater effectiveness in ____ conditions such as ____

Answer 14

vagal;

non-allergic, COPD

Question 15

2 antimuscarinics used:

which is longer lasting?

Answer 15

iptraropium,

tiotropium (is longer lasting)

Question 16

_____ such as ____ and caffeine are inhibitors of phosphodiesterase. these cause an increase in levels of _____

Answer 16

methylxanthines, theophylline;

cAMP

Question 17

do methylxanthines cause bronchodilation, inhibit inflammatory cell action, or both?

Answer 17

both

Question 18

two issues with methylxanthines:

Answer 18

wide variation in blood levels, narrow therapeutic window

Question 19

at low doses, main side effect of theophylline is ____ and nervousness. high doses can cause ____ and ____ effects

Answer 19

tremor;

cardiac (ie Tachy, arrythmia), CNS (ie vomiting, anxiety)

Question 20

the binding of ____ to _____ receptors triggers mast cell degranulation

Answer 20

IgE, FcER1

Question 21

similar to bronchoconstriction, increased ____ stimulates mast cell secretion while increased ____ inhibits it

Answer 21

GTP, ATP (eg caused by epinephrine)

Question 22

____ is a monoclonal antibody that targets the ___ portion of IgE, preventing attachment to mast cells and basophils

Answer 22

omalizumab, Fc

Question 23

omalizumab decreases circulating levels of ___. it is best used in patients with ____ asthma

Answer 23

IgE;

allergic (ie have high levels of IgE in serum)

Question 24

mechanism of action of cromolyn sodium/nedocromil sodium?

Answer 24

inhibit mast cell degranulation by membrane stabilization

Question 25

cromolyn sodium has no effect on _____. is dr. kreisle a fan?

Answer 25

bronchoconstriction;

hell no

Question 26

anti-histamines should be used _____, especially for ____ asthma

Answer 26

prophylactically, allergic

Question 27

leukotrienes:
cause bronchoconstriction that is (Slower or faster) and (more or less persistent) than histamine;
potentiate bronchial reactivity to ____;
increase mucosal edema and cause ____ of mucus

Answer 27

slower, more persistent;
histamine;
hypersecretion

Question 28

zileuton mechanism of action:

side effect?

Answer 28

inhibits 5-lipoxygenase;

hepatotoxicity

Question 29

zafirlukast and montelukast mechanism of action:

Answer 29

block leukotriene receptor (CysLT1)

Question 30

leukotriene modifiers are particularly effective in what kind of asthma?

Answer 30

aspirin induced

Question 31

mainstay of anti-inflammatory meds in asthma is (systemic or inhaled) _____

Answer 31

inhaled corticosteroids

Question 32

steroids inactivate ____. they decrease ____ ____ reactancts

Answer 32

NF-kB;

late phase

Question 33

2 issues (general) with systemic steroids

Answer 33

immunosuppression, adrenal suppressant

Question 34

side effect mentioned in sketchy/her notes of inhaled steroids:
how to prevent?

Answer 34

oropharyngeal candidiasis;

spacer/gargling

Question 35

2 general endings of steroids:

Answer 35

“-one” or “-ide”

Question 36

3 examples of steroids mentioned in sketchy/FA:

Answer 36

fluticasone, budesonide, beclomethasone