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USMLE® Step 1 > USMLE (S1) Respiratory > Respiratory - Pharmacology > Flashcards

Respiratory - Pharmacology Flashcards

1
Q

Are H1-blockers reversible or irreversible inhibitors?

A

Reversible

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2
Q

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

A
  1. To treat allergy
  2. To treat motion sickness
  3. As a sleep aid
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3
Q

List three toxicities of first-generation H1-blockers.

A
  1. Sedation
  2. Antimuscarinic
  3. Anti-α-adrenergic symptoms
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4
Q

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

A

Second-generation H1-blockers

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5
Q

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

A

Allergies

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6
Q

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

A

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

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7
Q

What are three first generation H1-blockers?

A

Diphenhydramine, dimenhydrinate, and chlorpheniramine

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8
Q

What are four second generation H1-blockers?

A

Loratadine, fexofenadine, cetirizine, and desloratadine

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9
Q

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

A

Nonspecific β-agonists and β2-agonists

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10
Q

What is the mechanism of action of isoproterenol?

A

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

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11
Q

What is the adverse effect of isoproterenol?

A

Tachycardia

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12
Q

Isoproterenol induces tachycardia through its agonism of what receptors?

A

β1-Adrenergic receptors

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13
Q

What is the mechanism of action of albuterol?

A

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

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14
Q

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

A

It is used for relief in acute asthma exacerbations

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15
Q

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

A

Long

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16
Q

List two adverse effects of salmeterol.

A
  1. Tremor
  2. Arrhythmia
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17
Q

What enzyme converts adenosine triphosphate to cAMP?

A

Adenylyl cyclase

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18
Q

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

Highlight the signaling pathway involved in cellular activation.

A

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.

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19
Q

Theophylline falls into which class of drugs?

A

Methylxanthines

caffeine is also a member of the class

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20
Q

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

A

Bronchodilation; cAMP

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21
Q

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

A

Decreased bronchial tone (ie, it causes bronchodilation)

22
Q

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

A

Theophylline

23
Q

List two types of toxicity that theophylline can cause.

A
  1. Cardiotoxicity
  2. Neurotoxicity
24
Q

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

A

Adenosine

25
Q

Ipratropium is an example of what class of drugs?

A

Muscarinic antagonists

26
Q

Does ipratropium cause a competitive or a noncompetitive receptor blockade?

A

Competitive

27
Q

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

A

Acetylcholine

28
Q

Cromolyn prevents what process from occurring?

A

The release of leukotrienes and histamine from mast cells

29
Q

How is cromolyn used in the treatment of asthma?

A

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

30
Q

Name two corticosteroids commonly used to treat asthma.

A
  1. Beclomethasone
  2. Prednisone
31
Q

What mechanisms of corticosteroids make them useful to treat asthma?

A

They inhibit the synthesis of almost all cytokines

32
Q

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

A

Nuclear factor κB

33
Q

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

A

Tumor necrosis factor-α

34
Q

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

A

Inhaled corticosteroids

35
Q

Name three examples of antileukotriene drugs.

A
  1. Zileuton
  2. Zafirlukast
  3. Montelukast
36
Q

Zileuton is an inhibitor of what pathway?

A

The 5-lipoxygenase pathway that produces leukotrienes from arachidonic acid

37
Q

What is the mechanism of action of montelukast?

A

Montelukast blocks leukotriene receptors.

38
Q

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

A

Immunoglobulin E; mast

39
Q

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

A

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

40
Q

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?

A

Cromolyn and steroids

41
Q

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

A

Bronchoconstriction (early) and inflammation (late)

42
Q

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

A

Bronchoconstriction; inflammation

43
Q

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

A

Steroids

44
Q

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

A

Cytochrome P450

45
Q

Name two clinical indications for the use of ipratropium.

A

Asthma and chronic obstructive pulmonary disease

46
Q

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

A

Aspirin-induced asthma

47
Q

Bronchoconstriction is mediated by which two processes?

A

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

48
Q

Guaifenesin is an expectorant. How does it work?

A

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

49
Q

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

A

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

50
Q

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

A

N-Acetylcysteine

51
Q

Bosentan is used primarily to treat what condition?

A

Pulmonary hypertension

52
Q

By what mechanism does bosentan decrease pulmonary vascular resistance?

A

By competitively antagonizing endothelin-1 receptors

USMLE (S1) Respiratory (4 decks)

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