08.18 - Pharmacotherapy of Asthma, COPD (Malik) - Questions Flashcards
Toxicities of Cromolyns
No systemic tox; Irritation of Trachea
Interaction between Glucocorticoids and B2-agonists
Glucocorticoids increase transcription of B2AR’s
Omalizumab
Anti-IgE mAb
Anti-cholinergics
Atropine, Ipratropium
Leukotriene Receptor Blockers
Monteleukast, Zafirlukast
Anti-IgE mAb
Omalizumab
Zileuton inhibits __ formation by blocking __-
Leukotriene formation, FLAP
Systemic effects of Ipratropium
No significant
2 Notable adverse effects of Monteleukast
Laryngitis/Pharyngitis; Viral infections
Main effect of Beta agonists
Incr levels of cAMP
Action of cAMP in B2 agonist effects
Stimulates EPAC –> Decr Prolifer; Stim PKA –> Inhibit MLCK –> Relaxation
Interaction between Zileuton and Theophylline
CYP1A2
2 ways in which Glucocorticoids decrease inflammatory gene translation
Decrease transcription thru CBP; Destabilize mRNA thru TTP
2 main actions of Cromolyn Sodium
Inhibit mast cell degranulation; Reduce bronchial hyperactivity
Beta-2-specific: Slow onset, long-acting
Salmeterol, Formoterol (use with steroids)
Glucocorticoid with best pharmacokinetics and -dynamics
Ciclesonide
When is Theophylline used?
Adjuvant to beta-2 agonist and anti-muscarinic
Theophylline serum levesl 5-10 can cause
nervousness and insomnia
Zafirlukast and Monteleukast specifically antagonize ___
LTD4 receptors
Ligand for beta2 receptors in lung
Epinephrine
AA is metabolized by __
5-LO
Which GC has lowest oropharyngeal candidiasis
Ciclosenide
Interaction between Anti-muscarinics and B2-agonist
Anti-muscarinics enhance b2-mediated bronchodilation
Leukotriene Synthesis Inhibitor
Zileuton
G protein that mediates good B2 agonist effects
Gs
Response to corticosteroids in Asthma vs COPD
Good in Asthma, Poor in COPD
T/F: Beta-adrinergic receptors in lungs can be de-sensitized
False, only in heart
2 notable adverse effects of prolonged Oral Corticosteroids
Glucose intolerance; Incr BP and weight
If you have to use beta-blocker in airway disease, use
beta1-selective
Adverse effects of Anti-muscarinics
Pupillary dilation and cycloplegia
LABA’s
Salmeterol, Formeterol (use with steroids)
3 notable features of Cushingoid Syndrome
Muscle weakness; Ruddy complexion; High BP
Where is highest density of beta2-adrenergic receptors
Lung
2 Notable adverse effects of Zafirlukast
Liver enzymes elevated; GIT disturbances
2 main actions of Theophylline
Inhibits PDE; Inhibits Adenosine
LABA’s are only used
In combo with inhaled steroids
Selectivity of Isoproterenol
B1 and B2
Notable adverse effect of Zileuton
Liver enzymes elevated
Selectivity of Ephedrine
B1 and B2 and some Alpha
AA is metabolized by 5-LO, but ___ is what is inhibited by Zileutin
FLAP
Why not use ACEi’s in airway disease
Increased levels of Bradykinin, which causes PGE2-mediated sensitization of nerve endings (cough)
What combined tx is indicated for COPD
Anti-muscarinic + beta2 agonist
3 Minor effects of Beta agonists
Inhibit mast cell degran; Inhibit microvascular perm; Promote mucociliary transport
LTB4 is a ___ chemoattractant
Neutrophil
GC action that suppresses TH2 cell cytokine synthesis
Competes with GATA-3, which is TF for IL-4, -5, and -13
2 Notable Adverse Effects of Omalizumab
Serious Allergic Reactions; CV complications
Methylxanthines
Aminophylline, Theophylline
3 main Adverse Effects of B2 agonists
Incr HR and Arrythmias; PaCO2 may decrease; CNS toxicities
G protein that mediates inflammatory B2 agonist effects
Gq