Stuff to remember from slides MP324

Question 1

Tralokinumab AND lebrikizumab are…

Answer 1

Anti IL-13 biologics - used for allergic asthma in specialist cases when eosinophils are involved.

Question 2

Dupilimab is…

Answer 2

A biologic licenced for severe inflammatory asthma - most commonly IL-4 but can be due to IL-13

Question 3

Mepolizumab is a…

Answer 3

Anti IL-5 antibody

Question 4

Omalizumab is a

Answer 4

Anti IgE antibody

Question 5

Effects of theophylline in asthma?

Answer 5

(i) smooth muscle relaxation.
(ii) inhibit anaphylactic release of mediators (mast cells).
(iii) suppress oedema.
(iv) central stimulation of ventilation

However lots of side effects- GI, seizures, palpitations monitoring dose

Question 6

How does desensitisation of Beta 2 agonists occur?

Answer 6

One factor in the short duration of action is desensitisation (loss in response to the agonist over time). This is typical for GPCRs and for Beta 2 agonists.

One key form of desensitisation is brought about by this mechanism:

Phosphorylation of the occupied receptor by a specific receptor kinase, termed a GRK. This enables the binding of beta-arrestin.

Subsequent Internalisation of the receptor (no receptor on the surface - it cannot be activated).