Lecture #5 - Drugs for Asthma Flashcards
B2 agonists:
- Short acting
- long acting
MOA:
Adverse
Stimulate AC causing ↑ of cAMP resulting in bronchodilation
Inhibits release of mediators from mast cells
- Skeletal muscle tremors
- Tachycardia
- Anxiety, restlessness, apprehension
Theophylline
MOA
Adverse (3)
Inhibits cAMP phosphodiesterases causing ↑ of cAMP
Competitive antagonist at adenosine receptors
Adverse:
- Narrow therapeutic window
- Convulsions
Tachycardia - Circulatory collapse
Ipratropium
MOA
Adverse
Competitively blocks the muscarinic receptors in the airways
Adverse:
Minimal, if dosage is to high may cause atropine like effects
Corticosteroids
MOA
Adverse
MOA:
Reduce the synthesis of arachidonic acid by phospholipase A2 which inhibits the release of leukotrienes and prostaglandins
Adverse:
- Short term- increaesd energy, insomnia, hunger, agitation and mood alterations
- Long term- osteoporosis, cataracts, myopathy, hypothalamic –pituitary adrenal axis suppression, depression
Cromolyn
MOA
Adverse
MOA:
Decrease in the release of mediators such as histamine and leukotrienes
Adverse:
Occasional coughing
Can be used to prevent symptoms before exposure to a trigger
Less effective then steroids
Must be used 3-4 times/day*
Zafirlukast
Montelukast
MOA
Adverse
Antagonist at the LTD4 leukotriene receptor
The LTE4 receptor is also blocked
Headache
Nausea
Zileuton
MOA
Adverse
Inhibits 5-lipooxygenase to decrease production of leukotrienes
Adverse:
Contraindicated in patients with hepatic disease
Diphenhydramine
MOA
Adverse
MOA:
Blocks histamine H1 receptors
Adverse:
Marked sedation or agitation due to muscarinic receptor blockade
Chlorpheniramine
MOA
Adverse
MOA:
Blocks histamine H1 receptors
Adverse:
Slight sedation or agitation due to muscarinic receptor blockade
Fexofedine
MOA
Adverse
MOA:
Blocks histamine H1 receptors
2nd generation
- not many adverse
Loratidine
(Claritin®)
MOA
Adverse
MOA:
Blocks histamine H1 receptors
Nausea, fatigue, headache
Cetirizine
(Zyrtec®)
MOA
Adverse
MOA:
Blocks histamine H1 receptors and blocks histamine release
Adverse:
Sedation, fatigue and dry mouth
Doxepin
(Sinequan®)
MOA
Adverse
MOA:
Blocks histamine H1 receptors
Chronic uticaria not responding to other H1 antagonists
Disorientation, confusion in non-depressed patients
4 Short acting B - agonists
Metoproterenol
Bitolterol
Albuterol
Terbutaline
3 Long acting Beta -2 Selective Agonists
- Salmeterol
- Formoterol
- Vilanterol
_____mostly for children under 2 years old since they cannot use the inhalation formulas
theophylline
Which of the following are inhalation, oral and IV
beclomethasone methylprednisolone flunisolide triamcinolone prednisone
Inhalation administration:
Beclomethasone (Venceril®)
Flunisolide (Aerobid®)
Triamcinolone (Azmacort®)
Oral administration:
Prednisone (Meticorten®)
Intravenous administration:
- Methylprednisolone
Corticosteroids:
MOA
Reduce the synthesis of arachidonic acid by inhibiting phospholipase A2 activity
Thereby inhibiting the synthesis and release of leukotrienes and prostaglandins
prevent bronchoconstriction from occurring
SE of Oral corticosteroids
Short term use
Long term use
Side effects with short-term use: increased energy, insomnia, hunger, agitation and mood alteration
Side effects with long-term use:
osteoporosis, cataracts, myopathy, hypothalamic-pituitary-adrenal axis suppression, depression
What are the two 1st generation glucocorticoid nasal sprays?
Three 2nd generation?
- Beclomethasone
- Flunisolide
- Mometasone
- Fluticasone
- Ciclesonide
Which nasal spray interacts with CYP3A4?
Fluticasone
St. john’s wort decreases the effect of what 2 drugs?
- Loratadine
2. Fexofenadine
