Pharmacology, Chapter 20

Front 1

True or False
Reversal of edema and cellular infiltration requires sustained treatment with anti-inflammatory agents.

Back 1

True

Front 2

How is short-term control of asthma achieved?

Back 2

Beta-adrenoceptor stimulants

Front 3

How is long term control of asthma achieved? (4 ways)

Back 3

Inhaled corticosteroids
Leukotriene inhibitors
Mast cell stabilizers
Monoclonal antibodies

Front 4

Describe how an asthmatic attack occurs.

Back 4

1. Allergen induces IgE production.
2. IgE binds to mast cells in the airway mucosa.
3. Upon reexposure, degranulation occurs and histamine, leukotrienes, and prostaglandins are released.
4. This causes muscle contraction and vascular leakage.

Front 5

True or False
The asthmatic response is typically not followed by a second more sustained phase.

Back 5

False

Front 6

What mediators are responsible for the late phase?

Back 6

IL5, 9, and 13 (Cytokines)

Front 7

What is different from a person with asthma and a normal person?

Back 7

Exaggerated reactivity of airways.

Front 8

How do adrenoceptor agonists treat asthma?

Back 8

1. Relaxation of smooth muscle.
2. Inhibition of microvascular leakage.
3. Increase ciliary activity.

Front 9

What is the MOA of Beta agonists?

Back 9

They activate adenylyl cyclase via Gs and increase intracellular cAMP.

Front 10

How are adrenoceptor agonists best delivered, and what is their optimal size?

Back 10

Inhalation
2-5 micrometers

Front 11

Effective, rapid-acting bronchodilator used in the treatment of severe hypotension. Maximal bronchodilation is achieved in 15 minutes.

Back 11

Epinephrine

Front 12

Longer duration, more pronounced CNS effects, lower potency than epinephrine.

Back 12

Ephedrine.

Front 13

Potent bronchodilator that achieves maximal effect in 5 minutes. Duration of action 1-1.5 hours.

Back 13

Isoproterenol

Front 14

These drugs achieve maximal bronchodilation within 15-30 minutes and last 3-4 hours. They can be diluted with saline.

Back 14

B-2 selective drugs.

Front 15

The ___ isomer of these drugs may cause inflammation and was the reason for the development of levalbuterol.

Back 15

S
R is active

Front 16

This drug can be given subcutaneously and can be used for hypotensive emergency.

Back 16

Terbutaline

Front 17

These long-acting B-2 agonists interact with inhaled corticosteroids to improve asthma control but should not be used in treatment of acute bronchospasm.

Back 17

Salmeterol and formoterol.

Front 18

These drugs inhibit PDE4 resulting in higher concentrations of cAMP.

Back 18

Methylxanthine drugs

Front 19

What is the purpose of cAMP? (3)

Back 19

1. Stimulation of cardiac function
2. Relaxation of smooth muscle.
3. Reduction of the immune and inflammatory activity of specific cells.

Front 20

What are the 3 proposed MOAs of methylxanthines?

Back 20

Inhibition of PDE
Inhibition of cell-surface receptors for adenosine.
Enhancement of histone deacetylation

Front 21

How does histone deacetylation enhance asthma treatment?

Back 21

Acetylation is necessary for activation of inflammatory gene transcription. Deacetylases prevent this action.

Front 22

Which methylxanthine has its most marked affects on the CNS, causing cortical arousal and deferral of fatigue?

Back 22

Caffiene

Front 23

Which methylxanthine has its most marked affects on smooth muscle?

Back 23

Theophyline.

Front 24

What effects do methylxanthines have on the heart?

Back 24

Positive chronotropic and inotropic effects.

Front 25

Theophylline has a broad therapeutic window.

Back 25

False

Front 26

Theophylline impoves ____-term control of asthma.

Back 26

long

Front 27

A potent competitive inhibitor of acetylcholine at postganglionic muscarinic receptors. Used as a bronchodilator.

Back 27

Atropine

Front 28

A longer-acting selective antimuscarinic agent approved for the treatment of COPD that binds to M1, M2, and M3 receptors.

Back 28

Tiotropium

Front 29

This drug is slightly less effective than B-agonists but causes bronchodilation and partial inhibition of provoked bronchoconstriction. Used for patients intolerant of inhaled B-agonists agents.

Back 29

Ipratropium Bromide

Front 30

These drugs contract engorged vessels in the bronchial mucosa and inhibit the infiltration of ashmatic airways by lymphocytes, eosinophils, and mast cells.

Back 30

Corticosteroids

Front 31

When should you administer corticosteroids?

Back 31

Early in the morning after endogenous ACTH secretion has peaked.

Front 32

For prevention of nocturnal asthma, when should you administer corticosteroids?

Back 32

In the evening.

Front 33

Inhalation of high doses of these two drugs are used to wean patients from chronic prednisone therapy.

Back 33

Fluticasone and ciclesonide.

Front 34

What is a problem caused by inhaled corticosteroids? How can you prevent it?

Back 34

Oropharyngeal Candidiasis. Gargle with water and spit after each treatment.

Front 35

Prodrug cleaved by esterases in bronchial epithelial cells that when absorbed, is tightly bound to serum protein. Less toxic corticosteroid.

Back 35

Ciclesonide.

Front 36

True or False
Inhaled corticosteroids are curative.

Back 36

False

Front 37

Only value is when taken prophylactically. Effective in inhibiting both antigen and exercise induced asthma.

Back 37

Mast cell stabilizers.

Front 38

What is the MOA of mast cell stabilizers?

Back 38

Alters the function of delayed chloride channels in the cell membrane, inhibiting cell activation.

Front 39

Which leukotriene is a potent neutrophil chemoattractant?

Back 39

LTB4

Front 40

Which two leukotrienes cause bronchoconstriction, increased bronchial reactivity, mucosal edema, and mucus hypersecretion?

Back 40

LTC4 and LTD4.

Front 41

A 5-LOX inhibitor that can cause liver toxicity.

Back 41

Zileuton

Front 42

LTD4-receptor antagonist that improves asthma control and reduces the frequency of asthma exacerbations.

Back 42

Zafirlukast and montelukast.

Front 43

Explain how aspirin induced asthma attacks can occur with the use of leukotriene inhibitors.

Back 43

It shifts the arachidonic acid substrates to the LOX pathway.

Front 44

This drug inhibits the binding of IgE to mast cells but does not activate IgE already bound to these cells and thus does not provoke mast cell degranulation.

Back 44

Omalizumab

Front 45

Treats patients with severe disease characterized by frequent exacerbations, a high requirement for corticosteroid treatment, and poor pulmonary function.

Back 45

Omalizumab

Front 46

How should you treat a patient with occasional symptoms of asthma?

Back 46

An inhaled B2-receptor agonist prn.

Front 47

How should you treat a patient who requires rescue therapy more 2x/week, nocturnal symptoms more than 2x/month, or an FEV1<80%?

Back 47

1st: Low dose inhaled corticosteroid or treatment with a leukotriene blocker.
2nd: Mast cell stabilizers or leukotriene antagonists.

Front 48

How should you treat a patient with poorly controlled asthma despite regular treatment + inhaled corticosteroid?

Back 48

Theophylline.

Front 49

Which class of drugs inhibit the increase in mucus secretion caused by vagal stimulation?

Back 49

Muscarinic antagonists.

Front 50

How should you treat a patient with more severe asthma not controlled by an inhaled corticosteroid? (Most effective)

Back 50

Add a long-acting beta-2 agonists to corticosteroid.

Front 51

Characterized by airflow limitation that is not fully reversible with bronchodilator treatment.

Back 51

COPD

Front 52

Occurs in older patients, associated with neutrophilic inflammation, poorly responsive to high-dose inhaled corticosteroid therapy, associated with progressive, inexorable loss of pulmonary function over time?

Back 52

COPD

Front 53

COPD exacerbations involve _______ _______ of the lower airways.

Back 53

Bacterial infections

Front 54

How do you treat acute symptoms of COPD?

Back 54

Inhaled short acting B-agonist or an anticholinergic drug or the two in combo.

Front 55

How do you treat exertional dyspnea and limitation of activities due to COPD?

Back 55

Long-acting beta-agonist, or long acting anticholinergic.
(salmeterol or tiotropium)

Front 56

How do you treat severe airflow obstruction with future exacerbations due to COPD?

Back 56

Regular use of an inhaled corticosteroid or continuous nasal oxygen.