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