E2: Asthma and COPD Flashcards
What class of drugs are the most effective bronchodilators?
B2 agonists
Aside from being a B2 agonists, what are the other MOAs of the B2 agonist class? (4)
Activate adenylate cyclase
Increase cAMP
Relax smooth muscles
Stabilize mast cells
What is the first line tx for asthma?
Short acting beta agonists (SABA)
What are the SABAs? (2)
Albuterol
Levalbuterol
Why are SABAs used to stop an asthma attack in progress?
Fast-acting!
Last ~4-8 hours
How are SABAs/LABAs administered?
Inhaled
What are the long acting beta agonists? (3)
Salmeterol
Formoterol
Vilanterol
*Often combined w/ Fluticasone
How long does it take for LABAs to start working? How long do they last? How does this effect the way they are used?
Take 20-30 minutes to start working
Last for ~12 hours
***Therefore not used as a rescue inhaler! Used prophlyactically!
LABAs are very ______
bronchoselective
When txing a pt with asthma, you should combine always combine a LABA with a _____.
Corticosteroid
Name the 2 muscarinic antagonists.
Ipratroium (Atrovent)
Tiotropium (Spiriva)
What are muscarinic antagonists used to tx?
COPD/Emphysema
Can also use if pt is intolerant to B2 agonists
Are muscarinic antagonists absorbed systemically or do they remain locally? Why?
Local - NO SYSTEMIC ABSORPTION
-Quaternary ammonium causes meds to remain trapped in lungs
Which of the 2 muscarinic antagonists is longer acting?
Tiotropium (taken once daily)
What are the 2 MOAs of Theophylline?
- Block adenosine receptors (which cause bronchoconstriction)
- Increase cAMP (phosphodiesterase inhibitor)
What are the adverse effects of the B2 agonists (SABA/LABA)?
Tachycardia
Nervous/dizzy
Tremor
*Usually short lived effects
What does tolerance mean in regards to pts on B2 agonists? How can you prevent this?
Tolerance: down regulation of # of beta receptors
-Prevent with corticosteroids
What is Theophylline used to tx?
COPD/emphysema not controlled by B2 agonists or muscarinic antagonists
*But rarely used due to adverse effects!
What are 2 important pharmacokinetic components of Theophylline?
LOW therapeutic index!
Do not switch patients between brands once patient has started
Name 4 drugs that increase clearance of Theophylline.
Phenytoin
Smoking
Rifampin
Oral contraceptives
Name 2 drugs that decrease clearance of Theophylline.
Cimetidine
Erythromycin
What are 4 adverse effects of Theophylline? (One of them is kind of a benefit)
Nervousness, insomnia
Arrhythmias
Weak diuretic
Decreased diaphragm fatigue/increases contraction
What is usually the cause of fatalities associated with a Theophylline overdose?
Arrhythmias
Name the 3 Inhaled Corticosteroids.
Fluticasone
Beclomethasone
Flunisolide
Why are corticosteroids helpful in the tx of asthma? (2)
Decrease inflammation
Improve response to B2 agonists (therefore may decrease the requirement for B2 agonists)
In what instances are oral steroids used?
Severe cases of asthma
Asthma exacerbation
Are inhaled corticosteroids absorbed systemically?
NO!
Only oral steroids are
What are 3 adverse effects of inhaled corticosteroids? How can you help reduce these effects?
Oropharyngeal candidiasis (thrush)
Hoarseness
Modest decrease in bone density (women)
*Decrease effects with spacer
Name the Leukotriene Inhibitor
Montelukast
Leukotriene Inhibitors are used in conjunction with:
B2 agonists
What are 2 benefits of Leukotriene Inhibitors (Montelukast)?
Decrease asthmatic response to exercise and cold air
Decrease need for corticosteroids
What are the adverse effects of the Leukotriene Inhibitors? (6)
HA Abd pain URI Sore throat Sleepiness Psych issues
What Leukotriene Inhibitor may decrease an asthmatic’s rxn to ASA and NSAIDs
Zileuton
MOA of Omalizumab
Monoclonal Abs to IgE (prevents binding of IgE to mast cells and basophils)
When is Omalizumab used?
Asthmatics with reactivity to allergens that are not controlled with steroids
How/when is Omalizumab administered?
Sub Q injection every 3-4 weeks
What is the primary adverse effect of Omalizumab?
Potential serious allergic rxn
MOA of Benralizumab
Monoclonal Ab targeting IL-5
When is Benralizumab used?
Severe asthma with eosinophilic phenotype
MOA of Cromolyn Sodium
Inhibits release of histamine from mast cells
When is Cromolyn Sodium used?
Primarily used in CHILDREN with asthma
How often is Cromolyn Sodium used?
Several times a day, chronically, and prophylactically
What is the primary adverse effect of Cromolyn Sodium?
Bad taste
