Drugs Asthma

Question 1

What are SABAs used for?

Answer 1

Relief of acute symptoms (rescue)

Question 2

What are systemic steroids used for?

Answer 2

Controller meds for very severe asthma
Usually given IV if episode is so bad that they cannot inhale albuterol

There are alot of side effects that can occur with systemic steroids

Question 3

What kind of bronchodilator is Epinephrine?

Answer 3

Nonselective sympathomimetic bronchodilator

Question 4

Why is epinephrine very short acting?

Answer 4

It has a catechol on its ring. Fast COMT metabolism

Question 5

Why does epinephrine have so many drug reactions?

Answer 5

It is non selective so binds to alpha and beta receptors

tachycardia due to beta 1 activation

Question 6

What kind of bronchodilator is Isoproterenol?

Isuprel

Answer 6

Short acting non selective beta 1 and beta 2 agonist

not used for asthma but for cardiostim effects

Question 7

What do beta 2 selective agents do?

Answer 7

Relaxes bronchial smooth muscle to increase lumen size (raises cAMP - prevents contraction)
Stablizes mast cell (decrease mediator release)

Question 8

What is the gold standard beta agonist for asthma?

Answer 8

Albuterol

Ventolin
Proventil
Proair

Question 9

What is the difference between albuterol and levalbuterol (Xopenex)

Answer 9

Albuterol is a racemic mixture while levalbuterol is a pure R isomer

Levalbuterol does not have better results than albuterol

Question 10

What are the dosage forms available for levalbuterol?

Answer 10

Nebulized solution
Inhaler (Xopenex)

Question 11

What are the adverse effects of albuterol and levalbuterol?

Answer 11

Cardiovascular effects due to beta 1 activity but less prone with correct inhaler techniques

fine muscle tremor, anxiety, tachycardia

Question 12

Why is regular use of albuterol not reccomended?

Answer 12

It can cause tachyphylaxis (where the beta 2 receptors do not respond as well)

Question 13

What is terbutaline sulfate used for?

Beta 2 selective

Answer 13

Usually tocolysis if lungs of fetus is not developed
Status asthmaticus (emergency uses)

Question 14

What are the controller medications for asthma?

Answer 14

Anti-inflammatory medications
1. Inhaled glucocorticoids
2. Leukotriene receptor antagonists
3. Anti allergy agents

Long acting bronchodilators
1. LABAs
2. Ipratropium/tiotropium
3. Theophylline

Question 15

What is the preffered treatment for persistent asthma?

Answer 15

Inhaled corticosteroids (alone or in combination)

Prevents airway remodeling and improves lung function

Question 16

What is the mechanism of action for ics?

Answer 16

1. Suppress IL and cytokine production
2. Reduce eosinophil infiltration and activation
3. inhibits macrophages
4. inhibits release of chemical mediators

Question 17

How do steroids primarily exert their effects?

Answer 17

By binding to intracellular glucocorticoid receptors to regulat gene transcription within target cells

in the nucleus where the DNA is

Question 18

What are the available ICS products for asthma use?

Answer 18

1. Budesonide (Pulmicort)
2. Ciclesonide (Alvesco)
3. Beclomethasone dipropionate (Beclovent, Vanceril)
4. Mometasone (Asmanex Twisthaler)
5. Fluticasone

Question 19

How does Fluticasone work to overcome side effects?

Answer 19

Through fast metabolism in the liver to the inactive metabolite which has much greater affinity for the glucocorticoid receptor

FP-17B-carboxylic acid derivative

Question 20

How often should ICS be used for asthma

Answer 20

QD if mild persistent asthma
BID for moderate to severe persistent asthma

Question 21

Why are systemic steroids used for asthma?

Answer 21

In severe cases Prednisone or Prednisolone is used to help gain prompt control of disease

Much greater side effect profile - only use if chronic

Question 22

What are the main side effects to ICS?

Answer 22

1. Deposition in mouth or throat - fungal infections (must wash out after use)
2. Mild reversible increase of glucose, decrease of potassium, fluid retention, and hypertension

Question 23

What must you do when using systemic steroids?

Answer 23

TAPER

Cause Addisons

Question 24

Why and when are LABAs used for asthma?

Answer 24

In combo with ICS for long term symptom control

Nocturnal asthma symptoms

Question 25

What type of drug is Salmetrol?

Answer 25

LABA

Question 26

Why is salmeterol not suitable for use as a rescue inhaler?

Answer 26

Slow onset of action

NOT PRN

Question 27

What is the major advantage of Formoterol?

Answer 27

Bronchodilation occurs within minutes and has a prolonged duration of action

up to 12 hours - is a LABA

Question 28

What are ultra LABAs?

Answer 28

Longer acting LABAs
24 hour duration of action

usually used in COPD

Question 29

What Ultra LABAs are approved for use in asthma?

Answer 29

Breo elipta
Trelegy

Question 30

What are leukotrienes?

Answer 30

mediators released from mast cells, eosinophils, and basophils
target for asthma therapy

Question 31

What inflammatory effects do leukotrienes have?

Answer 31

Increase vascular permeability
Increase bronchiolar smooth muscle contration
Increase mucus secretion
Increase eosinophil and neutrophil migration

Question 32

What pathway produces leukotrienes?

Answer 32

Lipoxygenase Pathway

Question 33

What receptors for leukotrienes are present on mast cells, eosinophils, and endothelial cells?

Answer 33

CysLT1
CysLT2

Question 34

What kind of drug is Zileuton (Zyflo)?

Answer 34

5-lipoxygenase inhibitor

inhibits the ENZYME

Question 35

What kind of drugs are zafirlukast (Accolate) and montelukast (Singulair)?

Answer 35

Leukotriene** RECEPTOR** antagonists

inhibits CysLT1

Question 36

What black box warning does montelukast (Singulair) have?

Answer 36

Increased risk of serious neuropsychiatric events (suicide)

Question 37

What is omalizumab (Xolair) used for?

Answer 37

Treatment for management of atopy (increased IgE)