E2: Asthma and COPD

Question 1

What class of drugs are the most effective bronchodilators?

Answer 1

B2 agonists

Question 2

Aside from being a B2 agonists, what are the other MOAs of the B2 agonist class? (4)

Answer 2

Activate adenylate cyclase
Increase cAMP
Relax smooth muscles
Stabilize mast cells

Question 3

What is the first line tx for asthma?

Answer 3

Short acting beta agonists (SABA)

Question 4

What are the SABAs? (2)

Answer 4

Albuterol

Levalbuterol

Question 5

Why are SABAs used to stop an asthma attack in progress?

Answer 5

Fast-acting!

Last ~4-8 hours

Question 6

How are SABAs/LABAs administered?

Answer 6

Inhaled

Question 7

What are the long acting beta agonists? (3)

Answer 7

Salmeterol
Formoterol
Vilanterol

*Often combined w/ Fluticasone

Question 8

How long does it take for LABAs to start working? How long do they last? How does this effect the way they are used?

Answer 8

Take 20-30 minutes to start working
Last for ~12 hours

***Therefore not used as a rescue inhaler! Used prophlyactically!

Question 9

LABAs are very ______

Answer 9

bronchoselective

Question 10

When txing a pt with asthma, you should combine always combine a LABA with a _____.

Answer 10

Corticosteroid

Question 11

Name the 2 muscarinic antagonists.

Answer 11

Ipratroium (Atrovent)

Tiotropium (Spiriva)

Question 12

What are muscarinic antagonists used to tx?

Answer 12

COPD/Emphysema

Can also use if pt is intolerant to B2 agonists

Question 13

Are muscarinic antagonists absorbed systemically or do they remain locally? Why?

Answer 13

Local - NO SYSTEMIC ABSORPTION

-Quaternary ammonium causes meds to remain trapped in lungs

Question 14

Which of the 2 muscarinic antagonists is longer acting?

Answer 14

Tiotropium (taken once daily)

Question 15

What are the 2 MOAs of Theophylline?

Answer 15

1. Block adenosine receptors (which cause bronchoconstriction)
2. Increase cAMP (phosphodiesterase inhibitor)

Question 16

What are the adverse effects of the B2 agonists (SABA/LABA)?

Answer 16

Tachycardia
Nervous/dizzy
Tremor

*Usually short lived effects

Question 17

What does tolerance mean in regards to pts on B2 agonists? How can you prevent this?

Answer 17

Tolerance: down regulation of # of beta receptors

-Prevent with corticosteroids

Question 18

What is Theophylline used to tx?

Answer 18

COPD/emphysema not controlled by B2 agonists or muscarinic antagonists
*But rarely used due to adverse effects!

Question 19

What are 2 important pharmacokinetic components of Theophylline?

Answer 19

LOW therapeutic index!

Do not switch patients between brands once patient has started

Question 20

Name 4 drugs that increase clearance of Theophylline.

Answer 20

Phenytoin
Smoking
Rifampin
Oral contraceptives

Question 21

Name 2 drugs that decrease clearance of Theophylline.

Answer 21

Cimetidine

Erythromycin

Question 22

What are 4 adverse effects of Theophylline? (One of them is kind of a benefit)

Answer 22

Nervousness, insomnia
Arrhythmias
Weak diuretic
Decreased diaphragm fatigue/increases contraction

Question 23

What is usually the cause of fatalities associated with a Theophylline overdose?

Answer 23

Arrhythmias

Question 24

Name the 3 Inhaled Corticosteroids.

Answer 24

Fluticasone
Beclomethasone
Flunisolide

Question 25

Why are corticosteroids helpful in the tx of asthma? (2)

Answer 25

Decrease inflammation | Improve response to B2 agonists (therefore may decrease the requirement for B2 agonists)

Question 26

In what instances are oral steroids used?

Answer 26

Severe cases of asthma | Asthma exacerbation

Question 27

Are inhaled corticosteroids absorbed systemically?

Answer 27

NO! | Only oral steroids are

Question 28

What are 3 adverse effects of inhaled corticosteroids? How can you help reduce these effects?

Answer 28

Oropharyngeal candidiasis (thrush) Hoarseness Modest decrease in bone density (women) *Decrease effects with spacer

Question 29

Name the Leukotriene Inhibitor

Answer 29

Montelukast

Question 30

Leukotriene Inhibitors are used in conjunction with:

Answer 30

B2 agonists

Question 31

What are 2 benefits of Leukotriene Inhibitors (Montelukast)?

Answer 31

Decrease asthmatic response to exercise and cold air | Decrease need for corticosteroids

Question 32

What are the adverse effects of the Leukotriene Inhibitors? (6)

Answer 32

``` HA Abd pain URI Sore throat Sleepiness Psych issues ```

Question 33

What Leukotriene Inhibitor may decrease an asthmatic's rxn to ASA and NSAIDs

Answer 33

Zileuton

Question 34

MOA of Omalizumab

Answer 34

Monoclonal Abs to IgE (prevents binding of IgE to mast cells and basophils)

Question 35

When is Omalizumab used?

Answer 35

Asthmatics with reactivity to allergens that are not controlled with steroids

Question 36

How/when is Omalizumab administered?

Answer 36

Sub Q injection every 3-4 weeks

Question 37

What is the primary adverse effect of Omalizumab?

Answer 37

Potential serious allergic rxn

Question 38

MOA of Benralizumab

Answer 38

Monoclonal Ab targeting IL-5

Question 39

When is Benralizumab used?

Answer 39

Severe asthma with eosinophilic phenotype

Question 40

MOA of Cromolyn Sodium

Answer 40

Inhibits release of histamine from mast cells

Question 41

When is Cromolyn Sodium used?

Answer 41

Primarily used in CHILDREN with asthma

Question 42

How often is Cromolyn Sodium used?

Answer 42

Several times a day, chronically, and prophylactically

Question 43

What is the primary adverse effect of Cromolyn Sodium?

Answer 43

Bad taste