HY pharm Flashcards
SABA
examples
albuterol
LABA
examples
salmeterol and formoterol
long-acting anti-muscarinics
examples
tiotropium
short-acting anti-muscarinics
examples
ipratropium
inhaled corticosteroids
examples
fluticasone, budesonide, dexamethasone
albuterol MOA
stim adenylate cyclase → incr cAMP (→ incr Ca2+ efflux → relax airway smc →) BRONCHODILATION.
black box warning of LABAs
use of LABAs (without concomitant inhaled steroids) may be associated with increased asthma and cardiac mortality when used without an anti-inflammatory in asthma
→ LABAs not to be used as monotherapy in asthma.
anticholinergics MOA
Atropine-like activity - block muscarinic (parasympathetic) receptors
anticholinergics are more effective in ______ due to _____
anticholinergics are more effective in COPD due to INCREASED MUSCARINIC TONE IN COPD
What feature of anticholinergics reduces systemic absorption?
Quaternary structure
anticholinergics AE
dry mouth, urinary retention (older men with prostatic hypertrophy)
Which drug both increases bronchodilation and decreases bronchoconstriction?
Theophylline
Theophylline MOA
- Phosphodiesterase inhibitor leading to incr cAMP due to decr cAMP hydrolysis (→ incr bronchodilation).
- Adenosine inhibitor (→ decr bronchoconstriction)
Theophylline AE
cardiotoxicity, neurotoxicity (seizures, tachyarrhythmia, nausea)
(caffeine AF)
Leukotriene antagonists MOA
- inhibit 5-lipooxygenase
2. block LT receptors
Zileuteon MOA
inhibit 5-lipooxygenase
Montelukast MOA
block LT receptors
Zafirlukast MOA
block LT receptors
_____ are effective in aspirin and exercise-induced bronchospasm
Leukotriene antagonists
Which leukotriene antagonist is characterized by hepatotoxicity?
Zileuton
Which ICS has high GC activity (inc potency, smaller dose req)?
dexmathasone
Inhaled corticosteroids MOA (general)
Principally anti-inflammatory agents (decr the numbers of lymphocytes, mast cells and eosinophils and their associated cytokines)
Inhaled corticosteroids MOA (specific)
Inactivate NF-κB, the tfac that induces production of TNF-α and other inflammatory agents.
Inhaled corticosteroids AE
oral –> thrush, dysphonia
systemic –> weight gain, hyperglycemia, cataracts, osteoporosis, less frequently adrenal suppression
1st line tx asthma
inhaled corticosteroids (fluticasone)
Roflumilast
PDE-4 inhibitor (increases cAMP)
Weak bronchodilator, effective for reducing COPD exacerbation
Mast cell stabilizers
Use
prophylactic for bronchospasm, NOT for acute bronchodilation
Mast cell stabilizers
examples
Cromolyn
Nedocromil
cromolyn
MOA and use
blocks histamine and leukotriene release from mast cells
Use in PEDS and EXERCISE-INDUCED
nedocromil
MOA
blocks release of inflammatory mediators from mast cells AND blocks release from other cells (eos, macrophages, platelets)
inhaled mucolytics
examples
N-acetylcysteine
N-acetylcysteine
MOA
liquifies mucus in chronic bronchopulmonary diseases (COPD, CF) by disrupting disulfide bonds
______ is also an antidote for acetaminophen OD
N-acetylcysteine
Antihistamines
MOA
reversible inhibitors of H-1 receptors
1st generation anti-histamines
examples
Diphenhydramine, dimenhydrinate, cholorpheniramine
“-en/ine”, “-en/-ate.”
1st generation anti-histamines
uses/AE
allergy, motion sickness, sleep aid
AE: MORE anticholinergic effects
2nd generation anti-histamines
examples
Loratadine, fexofenadine, desloratadine, cetirizine
“-adine.”
2nd generation anti-histamines
uses/AE
allergy
AE: LESS anticholinergic effect and LESS sedating
Antitussives
examples
Dextromethorphan
Benzonatate
Expectorant
examples
Guaifenesin
codeine MOA
opiate, mu receptor
antitussive
Dextromethorphan
MOA
non-opiate but binds mu
Antagonizes NMDA glutamate receptors
antitussive
which drug may cause serotonin syndrome if combined w/ other serotonergic agents?
Dextromethorphan (antitussive)
Anti-IgE monoclonal therapy
example
omalizumab
omalizumab
MOA/use
Anti-IgE monoclonal Ab
binds unbound serum IgE & blocks binding to FcεRI on mast cells
use: allergic asthma with incr IgE levels resistant to inhaled steroids/long-acting B-2 agonists
Which ILD does not improve with corticosteroids?
ASBESTOSIS
which drug is cryptogenic organizing pneumonia EXQUISITELY sensitive to?`
CORTICOSTEROIDS
tx for pulmonary arterial hypertension (PAH)
group 1 pulmonary HTN
-anticoagulants
-vasodilators (Ca chan blockers, prostacyclins)
-endothelin antagonists
-PDE-5 inhibitors (cGMP)
guanylate cyclase stimulant (cGMP)
PDE-5 inhibitors MOA in PAH
(inc cGMP to promote vasodilation; sildenafil [Viagra]
heparin MOA
anticoagulant
indirect thrombin inhibitor, binds anti-thrombin-3 and inactivates thrombin
avoid using ____ in CF
anticholinergics