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Flashcards in Respiratory - Pharmacology Deck (52):
1

Are H1-blockers reversible or irreversible inhibitors?

Reversible

2

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

To treat allergy and motion sickness and as a sleep aid

3

List three toxicities of first-generation H1-blockers.

Sedation, antimuscarinic, and anti-α-adrenergic symptoms

4

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

Second-generation H1-blockers

5

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

Allergies

6

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

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

7

What are three first generation H1-blockers?

Diphenhydramine, dimenhydrinate, and chlorpheniramine

8

What are four second generation H1-blockers?

Loratadine, fexofenadine, cetirizine, and desloratadine

9

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

Nonspecific β-agonists and β2-agonists

10

What is the mechanism of action of isoproterenol?

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

11

What is the adverse effect of isoproterenol?

Tachycardia

12

Isoproterenol induces tachycardia through its agonism of what receptors?

β1-Adrenergic receptors

13

What is the mechanism of action of albuterol?

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

14

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

It is used for relief in acute asthma exacerbations

15

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

Long

16

List two adverse effects of salmeterol.

Tremor and arrhythmia

17

What enzyme converts adenosine triphosphate to cAMP?

Adenylyl cyclase

18

What enzyme is inhibited by β-receptor agonists? What is the effect?

Adenylyl cyclase; it increases the amount of cAMP

19

Theophylline falls into which class of drugs?

Methylxanthines; caffeine is also a member of the class

20

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

Bronchodilation; cAMP

21

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

Decreased bronchial tone (ie, it causes bronchodilation)

22

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

Theophylline

23

List two types of toxicity that theophylline can cause.

Cardiotoxicity and neurotoxicity

24

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

Adenosine

25

Ipratropium is an example of what class of drugs?

Muscarinic antagonists

26

Does ipratropium cause a competitive or a noncompetitive receptor blockade?

Competitive

27

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

Acetylcholine

28

Cromolyn prevents what process from occurring?

The release of leukotrienes and histamine from mast cells

29

How is cromolyn used in the treatment of asthma?

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

30

Name two corticosteroids commonly used to treat asthma.

Beclomethasone, prednisone

31

What mechanisms of corticosteroids make them useful to treat asthma?

They inhibit the synthesis of almost all cytokines

32

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

Nuclear factor κB

33

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

Tumor necrosis factor-α

34

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

Inhaled corticosteroids

35

Name three examples of antileukotriene drugs.

Zileuton, zafirlukast, montelukast

36

Zileuton is an inhibitor of what pathway?

The 5-lipoxygenase pathway that produces leukotrienes from arachidonic acid

37

What is the mechanism of action of montelukast?

Montelukast blocks leukotriene receptors.

38

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

Immunoglobulin E; mast

39

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

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

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?

Cromolyn and steroids

41

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

Bronchoconstriction (early) and inflammation (late)

42

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

Bronchoconstriction; inflammation

43

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

Steroids

44

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

Cytochrome P450

45

Name two clinical indications for the use of ipratropium.

Asthma and chronic obstructive pulmonary disease

46

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

Aspirin-induced asthma

47

Bronchoconstriction is mediated by which two processes?

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

48

Guaifenesin is an expectorant. How does it work?

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

49

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

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

50

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

N-Acetylcysteine

51

Bosentan is used primarily to treat what condition?

Pulmonary hypertension

52

By what mechanism does bosentan decrease pulmonary vascular resistance?

By competitively antagonizing endothelin-1 receptors

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