Flashcards in Obstructive Lung Disease Deck (57):
Short acting B2 Agonist
Tx for acute asthma exacerbation
Long acting agents (2) for prophylaxis
Inhaled Corticosteroids (2)
Others: 'sone' & 'ide'
Beclomethasone, Mometasone, Ciclesonide
MOA of inhaled corticosteroids (i.e.: Fluticasone/Budesonide)
Inhibits cytokine synthesis; Inactivates NF-KB, transcription factor that induces production of TNF alpha and other inflammatory agents
1st line therapy for chronic asthma (2)
AE: oral thrush (2)
Muscarinic Antagonists (2)
MOA of muscarinic antagonists (i.e.: Tiotropium/Ipratroprium)
Competitively block muscarinic receptors, preventing bronchoconstriction T
Long acting muscarinic antagonists (2)
MOA of antileukotrienes (i.e.: Montelukast/Zafirlukast)
block leukotriene receptors (CysLT1)
5-lipoxygenase pathway inhibitor; blocks conversion of arachidonic acid to leukotrienes
Anti-IgE monoclonal antibody
MOA of Omalizumab
binds unbound serum IgE & blocks FCERI binding
Tx for allergic asthma w/ increased IgE levels
MOA of Theophylline
Blocks action of adenosine
Metabolized by cytochrome P-450
↑cAMP due to ↓cAMP hydrolysis
Methylxanthine w/ limited use bc of narrow TI
non-specific muscarinic receptor M3 agonist to diagnose asthma
MOA of Cromolyn
"mast cell stabilizer"
Inhibits mediator release from mast cells
sensory nerve effects (↓ cough, neuropeptide release)
Clinical Roles of B2 Agonism (2)
Acute relief: min tachyphylaxis
Bronchoprotection: known triggers (cold air/allergens); attenuates w/ repeated use
Drug w/o anti-inflammatory properties
Drug to avoid PO administration
Drugs (2) w/ concerns for tachyphylaxis & what they should NOT be administered w/o...
Long acting B2 agonists: Salmeterol/Formoterol
Should NOT be administered w/o inhaled steroids in asthma
AE of B2 adrenergic agonists
Tachycardia, tremor, nervousness
Not entirely selective
B2 receptors also found on heart
MOA of corticosteroids
Bind cytoplasmic receptor assoc w/ HSP 70, 90 and immunophilin (target of cyclosporine)
Translocation to nucleus, acts as transcription factor w/ widespread cellular effects
Modulate production of anti-inflammatory proteins modifying histones & their transcription
Effects of glucocorticoids
↓ lymphocytes & macrophages; ↓ cytokine release
↓ endothelial cell adhesion molecules (ICAM-1)
↓ prostaglandin & leukotriene C4
↓ fibroblast proliferation
AE of Glucocorticoids
Immunosuppression, Gastric Ulcers, Osteoporosis, Muscle Wasting, Cataracts
Do inhaled corticosteroids offer immediate bronchorelaxation?
What are the side effects of inhaled steroids & what can be done to avoid them?
Dysphonia (hoarseness), Thrush
Pneumonia (mild risk) in COPD patients
Rinse mouth, use spacer device
What are the short and long term effects of oral corticosteroids?
Short: VERY effective, preferred to increasing dose of inhaled steroid; initiate Tx early in exacerbation
Long: for asthma & COPD-associated w/ sig toxicity
Where are the anticholinergics or muscarinic receptors found?
Heart, CNS, GI, sweat glands, GU, eye
What are the anticholinergics w/ systemic & non-systemic effects?
Atropine: systemic effects
Ipratroprium bromide: 'quaternary ammonium' not systemically absorbed
Side effect of inhaled anticholinergic
Synergistic combination of muscarinic antagonist & B2 agonist
Effects of leukotrienes in asthma
Potent effectors of airway obstruction
In addition to inhaled corticosteroid, what is the other add-on controller agent in asthma?
Which leukotriene is good to add for allergic rhinitis?
Adenosine receptor antagonist that can mediate bronchospasm & Histone deacetylase modulator (HDAC)
AE of Theophylline within therapeutic range (a)? dose dependent toxicity (b)?
a) Nervousness, insomnia, dyspepsia
b) Nausea, emesis, tachyarrhythmias, seizures
What is the 3rd line agent in asthma?
What is the phosphodiesterase-4 isotope specific methylxanthine?
Roflumilast, w/ a better side effect profile than Theophylline although (-) GI effects & weight loss
What is the FDA approved methylxanthine for SEVERE copd?
Roflumilast, ↓ exacerbation rates but not for acute bronchorelaxation
Characteristics of mab's
highly specific, long T1/2, subQ admin, $
What is the drug used in Tx-resistant asthma?
What are anti IL-5 mab's? (2)
Role of lL-5
cytokine for growth, differentiation, recruitment, activation and survival; may impair response to helminth infection & zoster
What are the 2 drugs used as add-on Tx for severe disease w/ eosinophilic phenotype?
Mepolizumab & Reslizumab
What are adjunct Tx for asthma?
Vaccination vs. pneumococcus/influenza
Control allergic rhinitis
Describe the pyramid levels of Asthma Tx
Oral Steroids (long term)
Theophylline, Leukotriene modifiers, Tiotropium, Long acting B2 agonists
What are the advantages and limitations of inhaled corticosteroids?
↓ exacerbations but do NOT change FEV1 or parenchymal destruction
Uses of mast cell stabilizer
Prophylaxis of mild to moderate persistent asthma & exercise induced asthma
What is the effect of Theophylline on endogenous B2 adrenergic receptors?
Enhance activity of endogenous Beta2 adrenergic receptors
All of the following are asthma controller medications, which affect the underlying causes of the disease EXCEPT:
Inhaled muscarinic receptor antagonists
Leukotriene receptor antagonists
Mast cell stabilizers
Inhaled muscarinic receptor antagonists