QUESTIONS WITH CORRECT SOLUTIONS
GRADED A+
◉ "-terol" mechanism of action. Answer: - beta 2 agonist
- epinephrine and "-terols"
◉ Short acting beta agonist (SABA) indications. Answer: quick relief
during asthma (or similar) exacerbation
◉ long acting beta agonist (LABA) indications. Answer: - long term
control of asthma
- must be combined with glucocorticoids
◉ side effects of -terols. Answer: - tachycardia is most common
- activation of the sympathetic nervous system (cross over of beta 2
agonists to beta 1 receptors)
◉ types of bronchodilators. Answer: - beta agonists (-terols)
- muscarinic antagonists
,◉ pulmonary muscarinic antagonist prototypes and route. Answer: -
ipratropium
- tiotropium
- both inhaled
◉ pulmonary muscarinic antagonist mechanism of action. Answer:
antagonize muscarinic receptors in the lungs causing:
- drying of respiratory secretions (a significant component of
bronchitis)
- permits the sympathetic nervous system (β2) to dominate
resulting in bronchodilation (especially useful in COPD)
◉ leukotriene modifiers for asthma prototype drug. Answer: -
montelukast (singulair)
◉ Montelukast mechanism of action. Answer: - inhibits leukotrienes,
a single mediator of inflammation
- leukotrienes trigger bronchospasm and inflammation
◉ indications and route for montelukast. Answer: - oral
- second line therapy as an adjunct for glucocorticoids
- NOT for acute attacks
,◉ montelukast side effects. Answer: neuropsychiatric problems:
- anxiety
- agitation
- aggression
- suicidal thoughts
◉ cromolyn mechanism of action. Answer: - blocks mast cells, thus
- inhibits the release of inflammatory mediators
◉ cromolyn indications and route. Answer: - inhaled
- regular use can reduce the frequency of chronic asthma attacks
- *used prophylactically for exercise-induced asthma*
◉ phosphodiesterase inhibitor prototypes. Answer: - theophylline
(methylxanthines)
- roflumilast
◉ theophylline mechanism of action. Answer: non selectively
inhibits phosphodiesterase
, ◉ indications for theophylline. Answer: - management of obstructive
pulmonary disease (especially COPD)
◉ considerations for theophylline. Answer: - lots of drug
interactions (including coffee)
- induction/inhibition of CYP hepatic enzymes
- *variable half life* makes dosing problematic
- thus is rarely used
◉ theophylline drug levels. Answer: < 20 mcg/mL = therapeutic, no
side effects
20 - 25 mcg/mL = GI (n/v/d) and CNS (stimulation) side effects
> 25 mcg/mL = dysrhythmias, convulsions, death
◉ what is the normal half life for theophylline and what causes
variability in this number?. Answer: - average is 8 hours
- half (4 hours) in smokers and youngins
- double (16 hours) in adults with heart/liver/kidney disease
◉ Roflumilast mechanism of action. Answer: - selective
phosphodiesterase type 4 (PD4) inhibitor