Pharmacology - Pharmacological Asthma

Question 1

What are the two types of drugs used in treatment of asthma and examples?

Answer 1

Relievers e.g. SABAs, LABAs, CysLT1.

Controllers/Preventors e.g. Glucocorticoid, Cromoglicate. Slide 3

Question 2

What are examples of Beta2 - adrenoceptor agonists?

Answer 2

SABAs - Salbutamol (first line treatment for mild asthma)

LABAs - Salmeterol/formoterol (co-administered, not for acute relief). Slide 7

Question 3

What do cysteinyl leukotriene receptor antagonists do?

Answer 3

Act competitively at the CysLT1 receptor to block smooth muscle contraction, mucus secretion and oedema. Slide 8

Question 4

When should CysLT1 receptor antagonists be used and what are examples of them?

Answer 4

They are effective as an add on therapy in mild persistent, antigen induced and exercise induced asthma.
E.g. montelukast, zafirlukast. Slide 9

Question 5

What do methylxanthines do and what are examples of them?

Answer 5

They inhibit phophodiesterases that inactivate messengers which relax smooth muscle. They also inhibit mediator release from M cells and increase mucus clearance.
E.g. theophylline and aminophylline. Slide 10

Question 6

When should methylxanthines be used?

Answer 6

In combination with Beta2 adrenoceptor agonists and glucocorticoids. Slide 11

Question 7

What is the molecular mechanism of glucocorticoids?

Answer 7

Bind with GRalpha and becomes activated and bind to glucocorticoid response elements in a promoter region of a gene. This reduces the amount of inflammatory proteins produced. Slide 14

Question 8

In regards to inflammation of bronchial asthma what are the effects of glucocorticoids?

Answer 8

They prevent the production of IgE antibodies.
Reduces formation of TH2 cells.
Reduce number of mast cells and IgE receptor expression.
Prevent allergen-induced influx of eosinophils. Slide 16

Question 9

When should you use glucocorticoids in asthma?

Answer 9

Effective for long term treatment especially with a LABA. Should not be used for short term use as it does not alleviate bronchospasm. Slide 18

Question 10

What are the overall clinical use of glucocorticoids in asthma?

Answer 10

Prevent inflammation and resolve established inflammation. Slide 18

Question 11

What are cromones and what do they do?

Answer 11

Now second line treatment.

Have a weak anti-inflammatory effect and decrease the sensitivity of irritant receptors. Slide 20

Question 12

What do anti-inflammatory monoclonal antibodies do?

Answer 12

Specific e.g. omalizumab for IgE.
Binds to the antibody and prevent sit from stimulating a response from mast cells and reduces the expression of their receptors. Slide 21