Asthma/COPD drugs Flashcards
MOA of beta-2 agonist
Stimulate beta-2 receptors leads to increase in cAMP - activates PKA which inactivates MLCK and causes smooth muscle relaxation
Name the drugs that block the CysLT1 receptor and prevent LTC4, LTD4, and LTE4 from binding
Montelukast and Zafirulkast
Name the drug that inhibits 5-lipoxygenase and its primary effect
Zileuton - reduces leukotriene synthesis
Montelukast is preferred becuase of dosing schedule and fewer liver toxicity concerns
Name the drug that inhibits phosphodiesterase, preventing cAMP breakdown
Theophylline
Leads to bronchodilation
Also antagnoizes adeonsine receptors
Why is theophylline not commonly used?
It has a narrow therapeutic index, significant drug interactions, and serious side effects (arrhythmias, seizures, GI upset).
Name the drug class that prevents mast cell degranulation by inhibiting calcium influx, blocking histamin and leukotriene release
Mast cell stabilizers
i.e. cromoyln
Less effective that ICS and require frequent dosing
What monoclonal antibody targets IgE?
Omalizumab (anti-IgE therapy).
Which biologics target IL-5 and IL-5R for eosinophilic asthma?
Mepolizumab, Reslizumab, and Benralizumab
What is the mechanism of action of dupilumab?
It inhibits IL-4 and IL-13 signaling, reducing eosinophilic inflammation.
How does asthma treatment differ from COPD treatment?
Asthma: Primary focus is inflammation control with ICS
COPD: Bronchodilation is the mainstay, with anti-inflammatory treatment secondary.
What type of bronchodilator is more commonly used in COPD than in asthma?
Long-acting muscarinic antagonists (LAMAs) such as tiotropium.
What are examples of short-acting and long-acting muscarinic antagonists?
Short-acting (SAMA): Ipratropium
Long-acting (LAMA): Tiotropium
What receptor is target with anticholinergic Tx of asthma/COPD?
M3 receptors
Smoking cessation drugs
Bupropion: Dopamine reuptake inhibitor, reduces cravings.
Varenicline (Chantix): Partial agonist of nicotine receptors, reducing withdrawal symptoms.
What is the first-line treatment for all COPD patients?
Smoking cessation and bronchodilators (SABA or SAMA)
When should inhaled corticosteroids be used in COPD?
Only in patients with frequent exacerbations and eosinophil count >100 cells/µL
What is roflumilast and when is it used?
A PDE-4 inhibitor used in severe COPD to reduce inflammation.
Which of the following is most likely to cause dry mouth?
A. Fluticasone
B. Cromolyn
C. Ipratropium
D. Albuterol
Iptratropium
Characteristic of muscarinic antagonist
Which of the following targets IgE?
A. Dupilumab
B. Omalizumab
C. Tezepelumab
D. Benralizumab
Omalizumab
Which of the following inhibits formation of arachidonic acid?
A. Budesonide
B. Salmeterol
C. Tiotropium
D. Roflumilast
E. Aspirin
Budesonide
ICS
Which of the following is an antagonist at LT B4 receptors?
A. Zafirlukast
B. Zileuton
C. Zolpidem
D. Zaleplon
None of the above
No pharmacological agents act on LT B4 receptors
Which of the following is most likely to represent adverse effects associated with theophylline?
A. Sedation and somnolence
B. Churg Strauss syndrome
C. Tachycardia
D. Suicidal ideation
C. Tachycardia
Methyl-xanthines cause tachycardia and block adenosine receptors
Varenicline is a partial agonist of what receptor?
Nicotine receptors
Which IV drug is sometimes administered via nebulizer to decrease the viscosity of sputum in Pt’s w/ COPD?
Acetylcysteine
C. Steroids induce expression of lipocortin which inhibits phospholipase A2
What class of G-protein receptors are the leukotriene receptors?
Gq
Which drugs antagonize CysLT1 receptors?
Montelukast and zafirlukast
(Inhibit LTC4/LTD4/LTE4 - upstream)
Which of the following work, at least in part, by inhibiting phosphodiesterases III and IV?
A. Roflumilast
B. Montelukast
C. Albuterol
D. Ipratropium
E. Theophylline
F. Formoterol
G. Salmeterol
H. Tiotropium
A. Roblumilast
and
E. Theophylline