SM_180a: Pulmonary Pharmacology

Question 1

Describe the layout of the COPD GOLD guidelines diagram in terms of symptoms and exacerbations

Answer 1

• Right is more symptomatic while left is less symptomatic
• Upper is greater exacerbations while lower is less exacerbations

Group D has high symptom burden and many exacerbations

Question 2

Describe the GINA asthma guidelines diagram

Answer 2

• Step 1 to 5 (from better to worse controlled)
• Each step has a preferred controller choice and a reliever

Question 3

What are the short-acting beta-2 agonists?

Answer 3

• Albuterol
• Levalbuterol

Question 4

What are the long-acting beta-2 agonists?

Answer 4

• Oladaterol
• Formoterol
• Salmeterol
• Others

Question 5

Beta-2 agonists act at ______ and ______, causing ______, ______, and ______

Answer 5

Beta-2 agonists act at skeletal and smooth muscle, causing vasodilation, bronchodilation, and liver glycogenolysis

Question 6

Beta-2 agonists act by _____ to _____ cAMP

Answer 6

Beta-2 agonists act on GPCRs to activate adenylate cyclase to increase cAMP

Question 7

Short-acting beta-2 agonists are used as _____ medication because they start working in 5-10 minutes

Answer 7

Short-acting beta-2 agonists are used as rescue medication for COPD and asthma because they start working in 5-10 minutes

(last for 4-6 hours)

Question 8

Long-acting beta-2 agonists are used as ______ medications because they act for 24 hours

Answer 8

Long-acting beta-2 agonists are used as controller medications because they act for 24 hours

(used everyday regardless of presence/absence of symptoms)

Question 9

Long-acting beta-2 agonists are ____ line ____ therapy for COPD

Answer 9

Long-acting beta-2 agonists are first line controller therapy for COPD

Question 10

Long-acting beta-2 agonists are only used in asthma when ______

Answer 10

Long-acting beta-2 agonists are only used in asthma when inhaled corticosteroids do not work

Question 11

Long-acting beta-2 agonists are not used without inhaled corticosteroids in treatment of asthma because of _____

Answer 11

Long-acting beta-2 agonists are not used without inhaled corticosteroids in treatment of asthma because of risk of asthma exacerbations

(particularly in African Americans)

(ICS + LABA associated with better asthma control)

Question 12

Long-acting beta-2 agonists _____ beta blockade

Answer 12

Long-acting beta-2 agonists do not cause beta blockade

Question 13

What are the short-acting muscarinic receptor antagonists?

Answer 13

• Ipratropium

Question 14

What are the long-acting muscarinic receptor antagonists?

Answer 14

• Tiotropium
• Aclidinium
• Umeclidinium
• Glycopyrrolate

Question 15

Muscarinic receptor antagonists reversibly inhibit the effects of acetylcholine on the ______, preventing ______ and thereby leading to ______

Answer 15

Muscarinic receptor antagonists reversibly inhibit the effects of acetylcholine on the M3 muscarinic receptor, preventing release of calcium and thereby leading to vasodilation

Question 16

Long-acting muscarinic antagonists are used as ____ line _____ therapy for COPD

Answer 16

Long-acting muscarinic antagonists are used as first line controller therapy for COPD

(can then add on LABA)

Question 17

Long-acting muscarinic antagonists are used only for _____ in asthma

Answer 17

Long-acting muscarinic antagonists are used only for persistent symptoms after using LABA and ICS in asthma

(limited role)

Question 18

A common side effect of muscarinic receptor antagonists is _______

Answer 18

A common side effect of muscarinic receptor antagonists is inhaled muscarnic antagonist-induced anisocoria (dilation of pleural)

(part of anticholinergic toxidrome)

Question 19

If a Group B COPD patient has persistent symptoms after using a long-bronchodilator (LABA or LAMA), treat them with _____

Answer 19

If a Group B COPD patient has persistent symptoms after using a long-bronchodilator (LABA or LAMA), treat them with LAMA + LABA

(less exacerbations, longer time to first exacerbation, and less pneumonia_

Question 20

What are the inhaled corticosteroids?

Answer 20

• Budesonide
• Mometasone
• Fluticasone
• Beclamethasone
• Others

Question 21

Inhaled corticosteroids act by binding to the _______ receptor, limiting _______, _______, and _______

Answer 21

Inhaled corticosteroids act by binding to the glucocorticoid receptor, limiting inflammation in airway, mucus production, and airway edema

Question 22

Inhaled corticosterois are used in treatment of COPD when ______

Answer 22

Inhaled corticosterois are used in treatment of COPD when patient has ongoing symptoms despite LABA / LAMA

Question 23

Inhaled corticosteroids are _____ therapy for asthma

Answer 23

Inhaled corticosteroids are frontline therapy for asthma

(if symptoms continue, increase ICS dose or add LABA)

Question 24

Adverse effects of inhaled corticosteroids include ______ and ______

Answer 24

Adverse effects of inhaled corticosteroids include oral candidiasis and pneumonia

Question 25

What are the leukotriene antagonists?

Answer 25

• Montelukast
• Zafirlukast
• Pranlukast
• Zileuton

Question 26

Montelukast/zafirlukast/pranlukast limit activation of the _____ receptor

Answer 26

Montelukast/zafirlukast/pranlukast limit activation of the CysLT₁ receptor

Question 27

Zileuton works by ______

Answer 27

Zileuton works by inhibiting breakdown of arachidonic acid into leukotriene A₄

Question 28

_______ is the most commonly used leukotriene antagonist because of _____ and _____

Answer 28

Montelukast is the most commonly used leukotriene antagonist because of its minimal drug-drug interactions and favorable side-effect profile

(zafirlukast and zileuton have been associated with hepatic dysfunction)

Question 29

Leukotriene antagonists can be used as a ______ option in asthma

Answer 29

Leukotriene antagonists can be used as controller option in asthma

Question 30

Phosphodiesterase-4 inhibitors (Roflumilast) act by blocking ______ to ______

Answer 30

Phosphodiesterase-4 inhibitors (Roflumilast) act by blocking phosphodiesterase-4 to prevent breakdown of cAMP

Question 31

Phosphodiesterase-4 inhibitors (Roflumilast) are used in treatment of COPD when ______, ______, or ______

Answer 31

Phosphodiesterase-4 inhibitors (Roflumilast) are used in treatment of COPD when FEV₁ < 50%, chronic bronchitis, or Group D with frequent exacerbations

(reduce exacerbations in patients with GOLD D COPD)

Question 32

Main side effect of phosphodiesterase-4 inhibitors (Roflumilast) is _______

Answer 32

Main side effect of phosphodiesterase-4 inhibitors (Roflumilast) is GI side effects

Question 33

Theophylline is a _______

Answer 33

Theophylline is a methylxanthine (non-selective PDE inhibitor)

Question 34

Use of theophyilline is limited due to its _____ therapeutic window and ability to cause _____ and _____ at toxic levels

Answer 34

Use of theophyilline is limited due to its narrow therapeutic window and ability to cause fatal arrhythmias and seizures at toxic levels

Question 35

Theophylline is an additional treatment option for asthma when ______

Answer 35

Theophylline is an additional treatment option for asthma when patient is in Step 3-5 and ICS and LABA have not worked

Question 36

Leukotriene antagonists act on the ______ pathway to limit ______, ______, and ______

Answer 36

Leukotriene antagonists act on the arachidonic acid metabolism pathway to limit airway smooth muscle contraction, inflammation, and edema