Respiratory - Pharmacology

Question 1

Are H₁-blockers reversible or irreversible inhibitors?

Answer 1

Reversible

Question 2

List three clinical uses of first-generation H₁-blockers.

Answer 2

2. To treat allergy
3. To treat motion sickness
4. As a sleep aid

Question 3

List three toxicities of first-generation H₁-blockers.

Answer 3

1. Sedation
2. Antimuscarinic
3. Anti-α-adrenergic symptoms

Question 4

Loratadine, fexofenadine, cetirizine, and desloratadine are examples of what class of drugs?

Answer 4

Second-generation H₁-blockers

Question 5

What is the clinical use of second-generation H₁-blockers?

Answer 5

Allergies

Question 6

What is the main difference between first- and second-generation H₁-blockers with regard to their toxicities?

Answer 6

Second-generation H₁-blockers are far less sedating because of decreased central nervous system entry

Question 7

What are three first generation H₁-blockers?

Answer 7

Diphenhydramine, dimenhydrinate, and chlorpheniramine

Question 8

What are four second generation H₁-blockers?

Answer 8

Loratadine, fexofenadine, cetirizine, and desloratadine

Question 9

What two types of β-agonists are used to treat asthma?

Answer 9

Nonspecific β-agonists and β₂-agonists

Question 10

What is the mechanism of action of isoproterenol?

Answer 10

It relaxes bronchial smooth muscle through agonism of β₂-adrenergic receptors

Question 11

What is the adverse effect of isoproterenol?

Answer 11

Tachycardia

Question 12

Isoproterenol induces tachycardia through its agonism of what receptors?

Answer 12

β₁-Adrenergic receptors

Question 13

What is the mechanism of action of albuterol?

Answer 13

Albuterol relaxes bronchial smooth muscle through its agonism of β₂-adrenergic receptors

Question 14

Is albuterol used as a controller medication or for relief of symptoms during exacerbations?

Answer 14

It is used for relief in acute asthma exacerbations

Question 15

Salmeterol is a _____ (short/intermediate/long) -acting agent.

Answer 15

Long

Question 16

List two adverse effects of salmeterol.

Answer 16

1. Tremor
2. Arrhythmia

Question 17

What enzyme converts adenosine triphosphate to cAMP?

Answer 17

Adenylyl cyclase

Question 18

Which enzyme is stimulated by β-receptor agonists, and what is the effect?

Highlight the signaling pathway involved in cellular activation.

Answer 18

Adenylyl cyclase; it increases the amount of cAMP.

β-receptor agonists activate adenylyl cyclase via G-protein receptors.

This leads to increased cAMP, which mediates effects like smooth muscle relaxation and increased heart rate.

Question 19

Theophylline falls into which class of drugs?

Answer 19

Methylxanthines

caffeine is also a member of the class

Question 20

Theophylline likely causes _____ by inhibiting phosphodiesterase and increasing what molecule?

Answer 20

Bronchodilation; cAMP

Question 21

What is the effect on bronchial smooth muscle of increased cAMP concentration?

Answer 21

Decreased bronchial tone (ie, it causes bronchodilation)

Question 22

The usage of what asthma drug is limited because of its narrow therapeutic index?

Answer 22

Theophylline

Question 23

List two types of toxicity that theophylline can cause.

Answer 23

1. Cardiotoxicity
2. Neurotoxicity

Question 24

In addition to inhibiting phosphodiesterase, theophylline also blocks endogenous _____ from inducing bronchoconstriction.

Answer 24

Adenosine

Question 25

Ipratropium is an example of what class of drugs?

Answer 25

Muscarinic antagonists

Question 26

Does ipratropium cause a competitive or a noncompetitive receptor blockade?

Answer 26

Competitive

Question 27

By competitively blocking muscarinic receptors, ipratropium prevents endogenous _____ from inducing bronchoconstriction.

Answer 27

Acetylcholine

Question 28

Cromolyn prevents what process from occurring?

Answer 28

The release of leukotrienes and histamine from mast cells

Question 29

How is cromolyn used in the treatment of asthma?

Answer 29

Cromolyn is most effective when used as prophylaxis and cannot be used for acute symptoms

Question 30

Name two corticosteroids commonly used to treat asthma.

Answer 30

1. Beclomethasone 2. Prednisone

Question 31

What mechanisms of corticosteroids make them useful to treat asthma?

Answer 31

They inhibit the synthesis of almost all cytokines

Question 32

Corticosteroids are useful in treating asthma by inactivating what transcription factor?

Answer 32

Nuclear factor κB

Question 33

Nuclear factor κB induces the production of inflammatory agents including _____ \_\_\_\_\_ \_\_\_\_.

Answer 33

Tumor necrosis factor-α

Question 34

What class of drugs is considered first-line therapy for chronic asthma?

Answer 34

Inhaled corticosteroids

Question 35

Name three examples of antileukotriene drugs.

Answer 35

1. Zileuton 2. Zafirlukast 3. Montelukast

Question 36

Zileuton is an inhibitor of what pathway?

Answer 36

The 5-lipoxygenase pathway that produces leukotrienes from arachidonic acid

Question 37

What is the mechanism of action of montelukast?

Answer 37

Montelukast blocks leukotriene receptors.

Question 38

In the pathogenesis of asthma, antigens bind to _____ on _____ cells.

Answer 38

Immunoglobulin E; mast

Question 39

In the pathogenesis of asthma, the binding of antigens to immunoglobulin E on mast cells results in what?

Answer 39

The release of mediators such as leukotrienes and histamine from mast cells

Question 40

In the treatment of asthma, what are two drug types that prevent the binding of antigens to immunoglobulin E on mast cells from resulting in the release of mediators?

Answer 40

Cromolyn and steroids

Question 41

In the pathogenesis of asthma, the release of mediators from mast cells results in what two responses?

Answer 41

Bronchoconstriction (early) and inflammation (late)

Question 42

In asthma, the early response to the release of mediators is primarily _____ whereas the late response to the release of mediators is primarily _____ .

Answer 42

Bronchoconstriction; inflammation

Question 43

In the treatment of asthma, what drug type prevents released mast cell mediators from inducing the late response of airway inflammation?

Answer 43

Steroids

Question 44

Theophylline is metabolized by what enzyme system, making drug interactions possible?

Answer 44

Cytochrome P450

Question 45

Name two clinical indications for the use of ipratropium.

Answer 45

Asthma and chronic obstructive pulmonary disease

Question 46

Zafirlukast and montelukast block leukotriene receptors and are especially useful in the treatment of which type of asthma?

Answer 46

Aspirin-induced asthma

Question 47

Bronchoconstriction is mediated by which two processes?

Answer 47

Inflammation and lack of sympathetic tone; these are targets for therapy

Question 48

Guaifenesin is an expectorant. How does it work?

Answer 48

It removes excess sputum in large doses, but it does not reduce the cough reflex

Question 49

N-Acetylcysteine is an expectorant. How does it work?

Answer 49

It is a mucolytic, which is used to dissolve mucus plugs (especially in patients with cystic fibrosis)

Question 50

Which mucolytic is also used as an antidote for acetaminophen overdose?

Answer 50

N-Acetylcysteine

Question 51

Bosentan is used primarily to treat what condition?

Answer 51

Pulmonary hypertension

Question 52

By what mechanism does bosentan decrease pulmonary vascular resistance?

Answer 52

By competitively antagonizing endothelin-1 receptors