SOLVED QUESTIONS AND FULL SOLUTION
UPDATED
◉ 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
- PD4 normally converts cAMP to AMP
- inhibition increases cAMP levels
- increased cAMP *reduces inflammation, mucus production, cough,
and increases bronchodilation*
◉ indications for roflumilast.
Answer: - management of obstructive pulmonary disease
,- more selective/targeted than theophylline
◉ considerations for roflumilast.
Answer: much more expensive than theophylline
◉ side effects of roflumilast.
Answer: - headaches
- dizziness
- insomnia
- decreased appetite
- nausea
- diarrhea
- weight loss
- back pain
- flu-like symptoms
◉ how is asthma classified?.
Answer: - persistent or intermittent
- mild, moderate, or severe
, ◉ what are the variables when examining degree of impairment
with asthma.
Answer: - frequency of symptoms
- nighttime awakenings
- SABA use
- normal activity
- lung function (FEV1 > 80%)
◉ goals of asthma therapy.
Answer: - symptoms < 2x per week
- nighttime awakenings < 2x per month
- SABA use < 2x per week
- normal activity not restricted
- lung function (FEV1) > 80%
◉ considerations for asthma treatment.
Answer: - age dependent
- follows a predictable stepwise pattern
- progression of medicines is pretty similar regardless of age
◉ how often do you evaluate asthma therapy?.
Answer: every 2-6 weeks until control is achieved