Lecture 3 Asthma/COPD drugs Flashcards
3 components influencing bronchoconstriction in asthma:
which are more important in non-atopic forms?
activation of mast cells
local inflammation, vagal stimulation (these 2)
3 categories of things that mast cells release:
histamine, leukotrienes, eosinophil chemotactic factors
in the timing of asthma, bronchoconstriction occurs ____, and airway inflammation occurs ____ due ____
early;
late, cell infiltrate (ie eosiniophils)
bronchoconstriction:
ATP/cAMP ______ it;
cGMP/GTP _____ it
inhibits (ie bronchodilation), increases
Gq receptors involved in bronchoconstriction: (3)
these (increase or inhibit bronchoconstriction)
histamine H1, muscarinic M1, leukotriene CYS-LT1;
increase
Gi receceptor involved in bronchoconstriction:
this decreases _____, resulting in _____
Muscarinic M2, cAMP, bronchoconstriction
Gs receptor involved in bronchoconstriction:
this increases ___, resulting in ____
B2;
cAMP, bronchodilation
bronchodilators cause an (increase or decrease) in intracellular cAMP
increase
3 old sympathomimetics that are no longer really used (except for one in particular instances):
epinephrine (used in emergency), ephedrine, isoproterenol
2 SABAs (Short acting B2 agonists) most often used:
albuterol, terbutaline (also pirbuterol)
how long do SABA’s typically last? any side effects?
3-4 hours;
few, but some with oral forms ie jittery, nervousness
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?
dilation;
V/Q, decreased;
COPD
2 long acting beta agonists:
why are these longer lasting?
salmeterol, formoterol;
high lipid solubility
DON’T USE ALONE
antimuscarinics reverse the ____ contribution to bronchoconstriction. they have greater effectiveness in ____ conditions such as ____
vagal;
non-allergic, COPD
2 antimuscarinics used:
which is longer lasting?
iptraropium,
tiotropium (is longer lasting)
_____ such as ____ and caffeine are inhibitors of phosphodiesterase. these cause an increase in levels of _____
methylxanthines, theophylline;
cAMP
do methylxanthines cause bronchodilation, inhibit inflammatory cell action, or both?
both
two issues with methylxanthines:
wide variation in blood levels, narrow therapeutic window
at low doses, main side effect of theophylline is ____ and nervousness. high doses can cause ____ and ____ effects
tremor;
cardiac (ie Tachy, arrythmia), CNS (ie vomiting, anxiety)
the binding of ____ to _____ receptors triggers mast cell degranulation
IgE, FcER1
similar to bronchoconstriction, increased ____ stimulates mast cell secretion while increased ____ inhibits it
GTP, ATP (eg caused by epinephrine)
____ is a monoclonal antibody that targets the ___ portion of IgE, preventing attachment to mast cells and basophils
omalizumab, Fc
omalizumab decreases circulating levels of ___. it is best used in patients with ____ asthma
IgE;
allergic (ie have high levels of IgE in serum)
mechanism of action of cromolyn sodium/nedocromil sodium?
inhibit mast cell degranulation by membrane stabilization
