Lecture #5 - Drugs for Asthma

Question 1

B2 agonists:

• Short acting
• long acting

MOA:

Adverse

Answer 1

Stimulate AC causing ↑ of cAMP resulting in bronchodilation

Inhibits release of mediators from mast cells

1. Skeletal muscle tremors
2. Tachycardia
3. Anxiety, restlessness, apprehension

Question 2

Theophylline

MOA

Adverse (3)

Answer 2

Inhibits cAMP phosphodiesterases causing ↑ of cAMP
Competitive antagonist at adenosine receptors

Adverse:

1. Narrow therapeutic window
2. Convulsions
   Tachycardia
3. Circulatory collapse

Question 3

Ipratropium

MOA

Adverse

Answer 3

Competitively blocks the muscarinic receptors in the airways

Adverse:
Minimal, if dosage is to high may cause atropine like effects

Question 4

Corticosteroids

MOA

Adverse

Answer 4

MOA:
Reduce the synthesis of arachidonic acid by phospholipase A2 which inhibits the release of leukotrienes and prostaglandins

Adverse:

1. Short term- increaesd energy, insomnia, hunger, agitation and mood alterations
2. Long term- osteoporosis, cataracts, myopathy, hypothalamic –pituitary adrenal axis suppression, depression

Question 5

Cromolyn

MOA

Adverse

Answer 5

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*

Question 6

Zafirlukast
Montelukast

MOA

Adverse

Answer 6

Antagonist at the LTD4 leukotriene receptor
The LTE4 receptor is also blocked

Headache
Nausea

Question 7

Zileuton

MOA

Adverse

Answer 7

Inhibits 5-lipooxygenase to decrease production of leukotrienes

Adverse:
Contraindicated in patients with hepatic disease

Question 8

Diphenhydramine

MOA

Adverse

Answer 8

MOA:
Blocks histamine H1 receptors

Adverse:
Marked sedation or agitation due to muscarinic receptor blockade

Question 9

Chlorpheniramine

MOA

Adverse

Answer 9

MOA:
Blocks histamine H1 receptors

Adverse:

Slight sedation or agitation due to muscarinic receptor blockade

Question 10

Fexofedine

MOA

Adverse

Answer 10

MOA:
Blocks histamine H1 receptors

2nd generation
- not many adverse

Question 11

Loratidine
(Claritin®)

MOA

Adverse

Answer 11

MOA:
Blocks histamine H1 receptors

Nausea, fatigue, headache

Question 12

Cetirizine
(Zyrtec®)

MOA

Adverse

Answer 12

MOA:
Blocks histamine H1 receptors and blocks histamine release

Adverse:
Sedation, fatigue and dry mouth

Question 13

Doxepin
(Sinequan®)

MOA

Adverse

Answer 13

MOA:
Blocks histamine H1 receptors

Chronic uticaria not responding to other H1 antagonists

Disorientation, confusion in non-depressed patients

Question 14

4 Short acting B - agonists

Answer 14

Metoproterenol
Bitolterol
Albuterol
Terbutaline

Question 15

3 Long acting Beta -2 Selective Agonists

Answer 15

1. Salmeterol
2. Formoterol
3. Vilanterol

Question 16

_____mostly for children under 2 years old since they cannot use the inhalation formulas

Answer 16

theophylline

Question 17

Which of the following are inhalation, oral and IV

beclomethasone
methylprednisolone
flunisolide
triamcinolone
prednisone

Answer 17

Inhalation administration:
Beclomethasone (Venceril®)
Flunisolide (Aerobid®)
Triamcinolone (Azmacort®)

Oral administration:
Prednisone (Meticorten®)

Intravenous administration:
- Methylprednisolone

Question 18

Corticosteroids:

MOA

Answer 18

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

Question 19

SE of Oral corticosteroids

Short term use

Long term use

Answer 19

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

Question 20

What are the two 1st generation glucocorticoid nasal sprays?

Three 2nd generation?

Answer 20

1. Beclomethasone
2. Flunisolide
3. Mometasone
4. Fluticasone
5. Ciclesonide

Question 21

Which nasal spray interacts with CYP3A4?

Answer 21

Fluticasone

Question 22

St. john’s wort decreases the effect of what 2 drugs?

Answer 22

1. Loratadine

2. Fexofenadine