Pharm and Delivery of Drugs for Airway Obstruction

Question 1

Lung function tests in

1. Asthma
2. COPD

Answer 1

1. FEV1 is reduced, but can eventually get to normal FVC (takes longer)
2. Reduced FEV1 and FVC

Question 2

Asthma definition

Answer 2

Chronic inflammatory disease of the conducting airways
Characterized by reversible airflow limitation and airways hyperreactivity
Symptoms: intermittent wheezing, coughing, SOB

Question 3

The airways close off because of what 3 things in asthma

Answer 3

Smooth muscle contraction
Inflammation
Edema

Question 4

Treatment for mild asthma

Answer 4

Short acting beta2 adrenergic receptor agonists
They are reliever medications taken when needed
Active for 1-4 hours

Question 5

Treatment for severe asthma

Answer 5

Long acting beta2 adrenergic receptor agonists
Prophylactic treatment that you take all the time
Active for 12 hours (taken 2X/day)

Question 6

Natural ligand for B2-adrenergic receptor

Answer 6

Epinephrine

Binds B1 and B2 though

Question 7

Example of a SABA and LABA and their molecular structure

Answer 7

SABA: salbutamol (addition of methyl groups allows selectivity due to higher affinity for beta2)
LABA: salmeterol (long lipophilic side chains embed in the cell membrane and inhibit degradation_

Question 8

2 cellular actions from the activation at a B2 adrenergic receptor

Answer 8

Binding causes the release of cAMP within the smooth muscle
Causes the removal of Ca and the uncoupling of actin-myosin filaments
Results in smooth muscle relaxation

Question 9

Common side effects of B2 agonists

Answer 9

Off target effects on B1 (agitation, tremor, tachycardia)

Long term LABA use can cause desensitization of the receptor

Question 10

LABAs should be prescribe with ___

Answer 10

A corticosteroid

To reduce inflammation and the dose of LABA required

Question 11

COPD definition

Answer 11

Chronic inflammatory lung disease with airflow limitation that is not reversible
Symptoms include SOB, cough, sputum production

Question 12

What happens to lung function if you stop smoking?

Answer 12

Lungs start to decline at the normal rate instead of the accelerated rate
However, lung function does not improve to what a non-smoker at that age would have

Question 13

What is the FEV1/FVC value where COPD is diagnosed?

Answer 13

Ratio less than 0.7

Question 14

3 possible COPD disease mechanisms

Answer 14

Protease/Anti-protease imbalance that leads to tissue destruction
Oxidant/Anti-oxidant imbalance that leads to cell death
Autoimmune response to degraded tissue fragments

Question 15

All smokers will get which part of COPD?

Answer 15

Chronic bronchitis
Excess production of mucus to get rid of the particles
Increased mucus doesn’t impair the airflow function though, so not all smokers get COPD

Question 16

GOLD Therapy for COPD stages

1. Mild
2. Moderate
3. Severe
4. Very severe

Answer 16

1. Flu vaccine, SABAs
2. Add LABAs and pulmonary rehabilitation
3. Add inhaled glucocorticoids if repeated exacerbations
4. Add long term oxygen if chronic resp failure, and consider surgical treatments

Question 17

Corticosteroids bind glucocorticoreceptor complex which then… (2)

Answer 17

Prevents translocation of inflammatory transcription factors from cytosol into nucleus (trans-repression)
Up-regulates anti-inflammatory proteins by binding to glucocorticoid response elements (trans-activation)

Question 18

Side effects of inhaled steroids

Answer 18

Oral infections
Hoarseness
Long term –> systemic effects (osteoporosis, obesity, fat redistribution, hyperglycemia)