Asthma drugs – Flashcards
36 test answers
Unlock all answers in this set
Unlock answers 36question
mast calls & T-lymphocytes release which mediators
answer
histamine, tryptase, PGD2, LTC4, PAF, IL-4, IL-5, GM-CSF, TNF, TGF
Unlock the answer
question
eosinophils and neutrophils release which mediators
answer
ECP, MBP, Protease, PAF
Unlock the answer
question
corticosteriods (beclomethasone, budesonide) MOA
answer
broad anti-inflammatory actions
Unlock the answer
question
methylxanthines (theophylline) MOA
answer
relaxation of bronchiole smooth muscle, effects on T-cells & eosinophils, increased mucociliary clearance (all via increase in cAMP)
Unlock the answer
question
cromolyn, nedocromil MOA
answer
inhibit release of inflammatory mediators
Unlock the answer
question
leukotriene modifiers (zafirlukast, montelukast) MOA
answer
antagonize the actions of LTs in the airways
Unlock the answer
question
muscarinic antagonists (ipratropium) MOA
answer
muscarinic blockade in airways (blocks parasympathetic bronchoconstriction)
Unlock the answer
question
monoclonal antibodies (omalizumab) MOA
answer
block IgE binding to mast cells
Unlock the answer
question
non-selective beta-agonists (3) used for asthma
answer
epinephrine, ephedrine, isoproterenol
Unlock the answer
question
epinephrine - forms, onset & DA, adv rxns
answer
injectable, aerosolinhalation: onset in 15 minduration: 60-90 minadv rxn: tachycardia, arrythmias, MI, skeletal muscle tremor
Unlock the answer
question
ephedrine for asthma (compared to epi)
answer
oral adm; longer acting; more CNS effects; less potent
Unlock the answer
question
isoproterenol for asthma (compared to epi)
answer
more potent; short onset of 5 min; 60-90 min duration
Unlock the answer
question
B2-selectives - onset, peak and DA if inhaled
answer
onset at 1-5 min; peak at 30 min; lasts for 2-6 hrs
Unlock the answer
question
B2-selectives - oral DA
answer
~ 4-8 hrs
Unlock the answer
question
B2-selective drugs
answer
albuterol (O/I), terbutaline (O/I), metaproterenol (O/I), bitolterol, pirbuterol, levalbuterol, salmeterol, formoterol
Unlock the answer
question
long-acting B2-selective drugs (12 hours or longer - useful for nocturnal symptoms)
answer
salmeterol, formoterol --> both are dry powder inhalers
Unlock the answer
question
% of dose from MDI that actually makes it into the lung
answer
2 - 10% (90% deposited in the mouth)
Unlock the answer
question
tolerance to B2-selective agents tends to develop in response to which effect
answer
tolerance to anti-inflammatory effects (mast cells and lymphocyets) more than tolerance to brochodilation
Unlock the answer
question
drug interaction with selective B2 agonists
answer
interaction b/w non-selective beta-blockers and selective B2 agonist (counteract one aother)
Unlock the answer
question
Methylxanthine drugs (4)
answer
theophylline, aminophylline, enprofylline (3-propylxanthine), and Roflumilast (newest agent in clinical trials)
Unlock the answer
question
two proposed methylxanthine MOA's (theophylline, aminophylline)
answer
Increased cAMP results in:1) inhibtion of PDE4 (requires high conc.), 2) blockade of adenosine receptors, A1 in bronchiole sm (seen at therapeutic concentrations)
Unlock the answer
question
therapeutic index/range for methylxanthine drugs (theophylline, aminophylline)
answer
10-20 micrograms/ml (SEs appear around 20-25 micrograms/ml; higher than 40 can lead to seizures or arrhythmias)
Unlock the answer
question
metabolism of methylxanthines (theophylline, aminophylline)
answer
CYP 450: 1A2 --> drug interactions
Unlock the answer
question
what's special about roflumilast
answer
newest methylxanthine in clinical trials - high specificity for PDE4 in the lungs, less AE
Unlock the answer
question
what's special about enprofylline
answer
potent bronchodilator that shows PDE4 inhibition, but no adenosine receptor antagonism
Unlock the answer
question
muscarinic antagonists for asthma (2)
answer
Ipratropium & Tiotropium: Ipratropium bromide (quaternary ammonium compound)Tiotropium (Spiriva) – new agent with 24-hr duration of action
Unlock the answer
question
muscarinic antagonists (Ipratropium & Tiotropium) - MOA
answer
blocking muscarinic receptors prevents parasympathetic bronchoconstriction - M3 receptor
Unlock the answer
question
which disease state should muscarinic antagonists be used carefully in
answer
glaucoma
Unlock the answer
question
muscarinic antagonists (Ipratropium & Tiotropium) - time to peak, DA
answer
Max effect in 30 min; duration of 3-5 hrs
Unlock the answer
question
Combivent (MDI) - 2 products
answer
albuterol (b2 selective agonist) + ipratropium (muscarinic antagonist)
Unlock the answer
question
MOA for Cromolyn (Intal) & Nedocromil (Tilade)
answer
inhibition of mast cell degranulation; inhibit mediator release from bronchial mast cells inhibition of parasympathetic & cough reflexes; not bronchodilators; no direct effects on smooth muscle
Unlock the answer
question
uses for for Cromolyn (Intal) & Nedocromil (Tilade) (mast cell degranulation inhibitors)
answer
only prophylactic use – decrease immediate & late-phase asthmatic response to antigen-, exercise-, and irritant-induced asthma; effective when given before exercise or exposure to irritants
Unlock the answer
