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Flashcards in 48. Asthma drugs Deck (87):
1

asthma mechanism

bronchial hyperresponsiveness causes reversible bronchoconstriction

2

asthma can be triggered by

1. viral URI
2. allergens
3.stress
4. exercise
5. tobacco

3

test asthma with

metacholine challenge

4

ASTHMA symptoms and clinical findings

1. cough
2. wheezing
3. tachypnea
4. dyspnea
5. hypoxemia
6. decreased inspiratory/expiratory ratio
7. pulsus paradoxous
8. mucus plugging

5

pulsus paradoxus - definition

decreased in amplitude of systolic BP by >10 during inspiration

6

inspiratory / expiratory ratio in asthma
and why

decreased
expiration is prolonged

7

asthma - histology

1. smooth muscle hypetrophy
2. Curschmann spirals
3. Charcot- Leyden crystals

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Curchmann spirals

shed epithelium forms whorlded mucus plugs ( IN ASTHMA)

9

Charcot - Leyden crystals

eosinophilic, hexagonal, double-pointed , needle -like crystal from breakdown of eosinophils in sputum ( IN ASTHMA)

10

asthma bronchoconstriction is mediated by

1. β2 agonists ( albuterol, salmeterol, formoterol)
2. corticosteroids ( flutivasone, budesonide )
3. Muscarinic antagonists ( ipratropium )
4. Antileukotrienes ( montelukast, zafirlukast, zileuton )
5. omalizumab
6. Methylxanthines ( theophylline)
7. Metacholine

11

asthma - β2 agonists drugs

1. albuterol
2. saleterol
3. formoterol

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albuterol mechanism of action

β2 agonist ---> relaxes bronchial smooth muscle

13

albuterol used in

during acute exacerbation

14

salmeterol mechanism of action

β2 agonist ---> relaxes bronchial smooth muscle

15

formoterol - mechanism of action

β2 agonist ---> relaxes bronchial smooth muscle

16

β2 agonist - mechanism of action

relaxes bronchial smooth muscle ( increases cAMP)

17

salmeterol side adverse effects

1. tremor
2. arrhythmia

18

formoterol side adverse effects

1. tremor
2. arrhythmia

19

corticosteroids drugs

1. fluticasone
2. budesonide

20

role of corticosteroids ( fluticosine, budesonide) in asthma therapy

1st line therapy for chronic asthma

21

role of corticosteroids ( fluticosine, budesonide) - mechanism of action

Inhibit the synthesis of virtuallly ALL CYTOKINES . Inactivate NF-kB , the transcription factor that induces production of TNF- α and other inflammatory agents

22

asthma - muscarinic antagonists drugs

1. ipratropium
2. tiotropium

23

asthma - muscarinic antagonists (ipratropium , tiotropium ) mechanism of action

competitively blocks muscarinic receptors, PREVENTING BRONCHOCONSTRICTION

24

lung - muscarininc antagonists ( ipratropium, tiotropium) - used in

1. asthma
2. COPD

25

asthma - muscarinic antagonists ( ipratropium, tiotropium) - except asthma is used in

COPD

26

asthma - ipratropium vs tiotropium according to action

tiotropium is long acting

27

metacholine mechanism of action

Muscarinic receptor M3 agonist ---> bronchoconstriction

28

metacholine - used in

used in bronchial challenge test to help diagnose asthma

29

asthma challenge test can also be with

histamine

30

omalizumab - mechanism of action

Monoclonal anti-IgE antibody. It binds mostly unbound serum IgE and blocks binding to FcεRI

31

omalizumab used in

allergic asthma resistan to inhaled steroids and long - acting β2- agonist

32

omalizumab binds mostly

unbound serum IgE

33

asthma- antileukotrienes drugs

montelukast
2. zafilukast
3. Zileuton

34

montelukast , zafikast machanism of action

block leukotriene receptor ( cys LT1)

35

Zileuton mechanism of action

5-lipoxygenase pathway inhibitor . Block conversion of arachnoid acid to leukotrienes

36

montelukast, zafirkast - clinical use

asthma ( espeially aspirin- induced asthma )

37

zileuton side effect

hepatotoxicity

38

methylxanthines - drugs

theophylline

39

theophylline is metabolized by

cytochrome - P450

40

theophylline block action of

adenosine

41

adenosine receptor antagonists

1. theophylline
2. caffeine

42

theophylline usage in asthmais limited because

narrow therapeutic index

43

theophylline adverse effects

1. cardiotoxicity
2. neurotoxicity

44

asthma related response to mediators ( leukotrienes, histamine etc) is divided to

early response --> bronchoconstriction --> symptoms
late response ---> inflammation --> bronchial hyperreactivity

45

late response in asthma ?
inhibitors of this response

inflammation
inhibited by steroids and antileukotrienes

46

early response in asthma ?
inhibitors of this response ?

brochoconstriction
inhibited by β- agonists , theophylline, muscarinic antagonists

47

cAMP in asthma therapy

it include brochodilation

48

adenosine in lungs

bronchoconstriction

49

ach in lungs

bronchoconstriction

50

asthma treatment for acute exaceberation

albuterol

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1st line therapy for chronic asthma

corticosteroids ( fluticasone, budenosonide )

52

aspirin - induced asthma
treatment

montelukast
zafirlukast

53

asthma drug with cardiotoxicity as a side effect

theophylline

54

asthma drug with hepatotoxicity as a side effect

zileuton

55

asthma drug with neurotoxicity as a side effect

theophylline

56

asthma drug with narrow therapeutic index

theophylline

57

allergic asthma resistant to inhaled steroids and lonf acting β- agonists

omalizumab

58

omalizumab binds mostly unbound serum IgE and blocks

binding to FcεRI

59

asthma 's symptoms vary over in time in their

1. occurence
2. frequency
3. intensity

60

causes of prolonged expiration

1. bronchoconstriction ( airway narrowing )
2. airway wall thickening
3. increased mucus

61

asthma full treatment

there is not fullt treatment , only contrro

62

bronchial hyperresponsiveness in asthma is due to

inflammation

63

think asthma as a diagnosis when

1. Recurrent epidodes of wheezing
2. COugh at night
3. Coughing or wheezing after exercise
4. Cough, wheezing, chest tightness after exposure to allergens or pollutans
5. COld " go down to chest : or take longer than 10 days

64

• Bronchoconstriction is mediated by which two processes?

Inflammation and parasympathetic tone (these are targets for therapy)

65

• What is the mechanism of action of albuterol?

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

66

• A typical patient with asthma takes a combination of drugs that targets which two pathways mediating bronchoconstriction?

Inflammation and parasympathetic tone

67

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

Relief in acute asthma exacerbations

68

• Salmeterol and formoterol are ____ (short/intermediate/long)-acting agents. What class of drugs are they?

Long; β2-agonist

69

• List two adverse effects that a patient may experience while taking salmeterol.

Tremor and arrhythmias

70

• Name two inhaled corticosteroids commonly used to treat asthma.

Fluticasone and budesonide

71

• What mechanism of inhaled corticosteroids makes them useful to treat asthma?

They inhibit the synthesis of virtually all cytokines

72

• Inhaled corticosteroids are useful in treating asthma by inactivating what transcription factor?

Nuclear factor κB

73

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

Tumor necrosis factor-α

74

• A patient has chronic asthma. What class of drugs is considered first-line therapy for this patient?

Inhaled corticosteroids

75

• Does ipratropium cause a competitive or a noncompetitive receptor blockade? Mechanism?

Competitive; prevents endogenous acetylcholine from inducing bronchoconstriction

76

• Ipratropium is used to treat chronic obstructive pulmonary disease, as is what other long-acting muscarinic antagonist?

Tiotropium

77

• Name two clinical indications for the use of ipratropium.

Asthma and chronic obstructive pulmonary disease

78

• Name three examples of antileukotriene drugs.

Zileuton, zafirlukast, and montelukast

79

• Zileuton is an inhibitor of what pathway? Toxicity?

The 5-lipoxygenase pathway that produces leukotrienes from arachidonic acid; it is hepatotoxic

80

• What medication is used for allergic asthma resistant to inhaled corticosteroids and β2-agonists? Its mechanism of action?

Omalizumab, a monoclonal anti-immunoglobulin E antibody that binds unbound immunoglobulin E and blocks FcεRI binding

81

• Theophylline likely causes ____ by inhibiting phosphodiesterase and increasing what molecule?

Bronchodilation; cAMP

82

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

Decreased bronchial tone (i.e., it causes bronchodilation)

83

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

Theophylline, a methylxanthine

84

• A patient wants to try theophylline but is worried about side effects. What two side effects do you counsel the patient on?

Cardiotoxicity and neurotoxicity

85

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

Adenosine

86

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

Bronchoconstriction (early) and inflammation (late)

87

• In asthma, the early response to the release of mediators is ____, whereas the late response to the release of mediators is ____.

Bronchoconstriction; inflammation