MW L3 Asthma treatment 1

Question 1

3 main therapeutic targets for asthma

Answer 1

Bronchoconstriction
Inflammation
Allergy

Question 2

3 drug types targeting β-adrenoreceptors

Answer 2

Salbutamol
Long acting β2 agonists
Adrenaline (emergencies)

Question 3

2 e.g. of long acting β2 agonists

Answer 3

formoterol and salmeterol

Question 4

Do β agonists produce anti-inflammatory effect?

Answer 4

No - limited evidence

Question 5

How do we make sure we get a selective response with β agonists?

Answer 5

Using inhalation to get more in the lungs and less in the periphary

Question 6

Name a non-selective β agonist

Answer 6

Isoprenaline

Question 7

Duration of β agonist action correlates with….

Answer 7

lipophilicity
-more lipophilic = longer acting, slower onset
(forms a depot in the lipid membrane and leaches out to interact with receptor)

Question 8

How does β2 agonism cause bronchodilation?

Answer 8

β is Gas coupled - converts ATP to cAMP
This activates PKA
1. Opens K channels
2. Inactivates MLCK
3. Calcium sequestration

Question 9

Other than β agonism what is another bronchodilating drug class? (2)

Answer 9

Phosphodiesterase (PDE) inhibitors

Muscarinic antagonists

Question 10

How do PDE inhibitors cause bronchodilation?

Answer 10

Inhibit PDE which usually breaks down cAMP.
Leads to increased cAMP
This activates PKA
1. Opens K channels
2. Inactivates MLCK
3. Calcium sequestration

Question 11

e.g. of PDE inhibitor

Answer 11

Theophylline

Question 12

Problems with PDE inhibitors

Answer 12

narrow therapeutic window

PDE inhibition in the brain causes nausea, dizziness

Question 13

Muscarinic antagonists e.g.

Answer 13

Hyoscine - historic use, often with opioids.