Drugs To Treat Asthma

Question 1

Relievers/bronchodilators drugs work on the/are

Answer 1

beta 2 adrenoceptors
Muscarinic acetylcholine receptors
(both are GPCR)

Leukotriene antagonists

Question 2

Preventer drugs work on the/are

Answer 2

Glucocorticoid steroids
Monoclonal antibodies
Leukotriene antagonists

Question 3

examples of Relievers/bronchodilators drugs (agonists)

Answer 3

Theophylline
Salbutamol
Terbutaline

Question 4

Why are drugs specific to beta 2 adrenoceptors preferred in fighting asthma

Answer 4

because beta 1 drugs or non selective beta adrenoceptor drugs don’t work in the lungs but in the heart and thus prevent from beta 2 selective drugs from binding. Since beta 1 selective drugs are mainly heart focused they don’t do any good for asthma

Question 5

examples of preventer drugs (agonists)

Answer 5

Salmeterol
Formoterol
Preventer because they work longer and thus can prevent attacks in their time of activity

Question 6

How do long acting drugs work

Answer 6

1. catechol end binds to exosite which allows the other end of molecule (e.g salmeterol) to activate beta 2 adrenoceptor multiple times.
2. It can dissolve into the membrane (lipophillic) and leak out to activate receptor

Question 7

mechanism after receptor being

Answer 7

step1: G-portein with Alpha S subunit is activated by GTP binding
step2: G-Protein activated adenylyl cyclase
step3: adenylyl cyclase convers ATP into cAMPs
step4: cAMP activated Protein kinase A (PKA)
step5: PKA reduced celluar Ca levels which relaxes smooth muscle + mast cells granulate less

Question 8

Unwanted effects of beta adrenoceptor agonists

Answer 8

1. Tremors
2. Tachycardia
3. Nervous tension
4. Hypokaleamia

Question 9

Three methods of inhalation

Answer 9

1. MDI
2. Spacer
3. nebulizer

Question 10

Name the three alkylxanthine drugs

Answer 10

caffeine
theophylline
aminophylline

Question 11

Problems with alkylxanthine drugs

Answer 11

theophylline especially has a small therapeutic window and can be toxic at relatively small doses
all these drugs are effected by patients liver status. if a patient can for some reason (smoking) metabolize lower doses, it can be toxic at lower doses

Question 12

Muscarinic acetylcholine receptors effect what part of the nervous system

Answer 12

parasymphatetic

Question 13

Muscarinic acetylcholine receptor agonists (bad for asthma)

Answer 13

Acetylcholine 
Methacholine 
Muscarine
Lower potency = nicotine 
(ALSO MICHAEL HAS A SMALL PENIS)

Question 14

Muscarinic acetylcholine receptor antagonists (good for asthma)

Answer 14

Tubocurarine
ipratropium
Tiotropium

Question 15

Why is activating Muscarinic acetylcholine receptor bad?

Answer 15

Because it causes the increase secretion of goblet cells and the constriction of smooth muscle (and thus airways). That is why we need Muscarinic acetylcholine receptor antagonists

Question 16

Why is atropine (a MAcR antagonist) not good for asthma?

Answer 16

Because it is lipid soluble and would diffuse away from the lungs. It would also cause unpleasant parasymphatic action

Question 17

Good MAcR antagonists are

Answer 17

Tiotropium
ipratropium
They reverse/reduce/stop the effect of MAcR agonist mentioned

Question 18

What receptors do alkylxanthine do and through what receptors ?

Answer 18

Adenosine receptors antagonists - adenosine is a bronchoconstrictor so inhibiting its action causes bronchodilation. It also stops phosphodiesterases from breaking down cAMP. cAMP is responsible for repressing inflammation and causes relaxation of smooth muscles around the airways