PHAR232 - Pharmalogical tools in Asthma

Question 1

Allergic Asthma

Question 2

Asthma hypersensitivity reaction - KNOW

Question 3

KNOW ADENOSINE AND ASTHMA

Question 4

Increased adenosine in lungs associated with asthma

Question 5

Question 6

KNOW, LEARN AND DRAW OUT

Question 7

KNOW AND DRAW OUT

Question 8

Mast cell degranulation - KNOW AND LEARN

Question 9

Draw out

Question 10

Main goal o asthma drug management is…

Answer 10

to find an adjunct treatments to combine with BETA AGONISTS to provide synergistic benefit and delay need for glucocorticoids

OPEN UP THE AIRWAYS

Question 11

In asthma treatment do you want drugs to bronchodilate or constrict for ease of airflow?

Answer 11

dilate

Question 12

2 key areas that we are focusing on with asthma medication interventions

Answer 12

Bronchoconstriction
Mast cell destabilisation

Question 13

What are the 3 categories of drugs used to manage asthma?

Answer 13

• Symptom relievers (short-acting beta2 agonists - salbutamol e.g. ventalin)
• Symptom controllers (long-acting beta2 agonists - salmetrerol)
• Symptom controllers - methylxanthines (theophylline) preventative for physical activity (longer acting)
• Symptom preventers (inhaled corticosteroids)
  _ NSAIDS

Question 14

Are methylxanthines used by an enhaler?

Answer 14

no they are oral medications

Question 15

MUST KNOW AND WRITE OUT - BETA2 RECEPTOR AGONIST MECHANISM OF ACTION

Answer 15

Question 16

What do beta 2 receptors usually respond to?

Answer 16

Adrenaline (NE)

Question 17

If you are a beta-2 agonist what are the drugs mimicking?

Answer 17

Adrenaline

Question 18

Must know systemic side effects of Beta2 receptor agonists

Answer 18

= increases SNS
- Overuse of inhalers can cause issues

Question 19

Does caffeine bronchodilate or bronchoconstrict?

Answer 19

bronchodilate
= Used as an old remedy for asthma
= related to the adenosine inhibition

Question 20

Review diagram

Question 21

MUST KNOW - METHYLXANTHINES AS BRONCHODILATORS - DRAW OUT

Answer 21

Question 22

What do A1 adenosine receptors to if they are agonised?

Answer 22

Bronchoconstrict

Question 23

What is a key mechanism of action for methylxanthines (MXs) e.g. theophylline and aminophylline?

Answer 23

Adenosine A1 receptor ANTAGONISTS
= bronchodilate

Question 24

What 2 mechanisms of action do methylxanthines have as bronchodilators?

Answer 24

• Adenosine A1 receptor antagonists
• Block phosphodiesterase (PDE)

Question 25

MUST KNOW - DRAW OUT MECHANISM OF ACTION - BLOCK PHOSPHODIESTERASE (PDE)

Answer 25

Question 26

What do methylanthines mimic?

Answer 26

Caffiene

Question 27

What side effects does methylxanthines have? MUST KNOW

Answer 27

Acts like caffiene Increases SNS Because adosine Rs are everywhere Methylxanthines target them all

Question 28

DRAW THIS OUT - ADENOSINE RECEPTORS AS A TARGET IN ASTHMA

Answer 28

Question 29

OVERVIEW OF A2B Adenosine receptor antagonists

Answer 29

Question 30

MUST KNOW MECHANISM OF ACTION OF A2B ADENOSINE RECEPTORS AS DRUG TARGETS

Answer 30

- Avoids histamine and proinflammatory mediatiors = reduces bronchodilation

Question 31

MUST KNOW THIS QUESTION - WRITE IT OUT AND KNOW

Answer 31

- WHY CHOOSE GS OR GQ ? - Why choose GQ ? = increase in histamine in asthma - Research wants to bypass A2B receptors

Question 32

A1 adenosine receptors as drug targets in astha

Answer 32

KNOW AND DRAW OUT

Question 33

Do methylxanthines have lots of side effects?

Answer 33

yes

Question 34

Where in the body has lots of adenosine A1 receptors?

Answer 34

Brain, SA and SV node in the heart

Question 35

MECHANISM OF ACTION OF A1 ADENOSINE RECEPTORS. KNOW AND DRAW OUT!!!!

Answer 35

- Review why it decreases CA++?? Type of receptor?

Question 36

Other approaches to asthma

Answer 36

- targets bacterial ribosomes - Can still effect human cells even if targeting bacterial ribosomes