Respiratory Pharmacology Flashcards

1
Q

In asthma, inflammatory cells release what

A

mast cells
eosinophils
T helper 2 cells

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2
Q

what bronchospastic mediators are released in asthma

A

histamine
leukotriene D4
Prostaglandin D2

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3
Q

what test/challenge is used to diagnose asthma

A

Methacholine

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4
Q

what inflammatory cells are increased in COPD

A

neutrophils
macrophages
cytotoxic T-lymphocytes

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5
Q

COPD can cause

A

progressive fibrosis
emphysema
ariway narrowing
excessive mucus

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6
Q

what is a risk factor for COPD

A
  • smoking

- deficiency in alpha1-proteinase inhibitor

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7
Q

what is allergic rhinitis and what does it activate

A

nasal epithelium inflammation

- IgE mediated activation of mast cells, basophils

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8
Q

what are important mediators of inflammation that induce symptoms characteristic of allergic rhinitis

A

histamine
prostaglandins
leukotrienes

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9
Q

where do most of the drugs go if they are inhaled

A

80-90% swallowed

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10
Q

Name the drugs that are given orally

A

Corticosteroids
Adrenergic Agonists
Methylxanthine (theophylline)

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11
Q

MOA for adrenergic agnoists

A

stimulates B2-adrenergic receptors

  • increases cAMP
  • activates PKA
  • induces bronchial smooth muscle cell relaxation
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12
Q

when do short-acting B2-adrenergic receptor agonists work

A

quick relief during asthma attack

  • onset 1-5 minutes
  • duration of action 4-6 hrs
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13
Q

Name3 long acting B2-adrenergic receptor agonists LABA

A

Salmeterol
Formoterol
Indacaterol

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14
Q

which B2-adrenergic receptor agonist for long acting, acts the longest and is it usually used for

A

Indacaterol

COPD

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15
Q

Why does Salmeterol have a longer duration of action than albuterol

A

Salmeterol has lipophilic side chain

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16
Q

Name B2- selective SABA

A

Albuterol
Terburtaline
Pirbuterol
Metaproterenol

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17
Q

what are B2-selective agonists SABA used for

A

all types of asthma attakcs

- not as effective in COPD

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18
Q

How often is B2- receptor selective agonists SABA used

A
  • not to be used several times a day
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19
Q

when one overdoses on B2- receptor selective agonist SABA, what more is needed?

A

need for more anti-inflammatory therapy

corticosteroids and Leukotriene inhibitor

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20
Q

What can account for the diminshed activity (tolerance) of B2-receptor selective agnoist SABA

A

B2-recetpor downregulation

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21
Q

what are adverse effects of B2-receptor selective agonist SABA

A
Tremor
restlessness
tachycardia
hypokalemia 
- more with oral dose than inhalation
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22
Q

Name 2 non-selective SABA

A

Isoproterenol and Epinephrine

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23
Q

MOA for Isoproterenol

A

nonselective B-agonist and potent bronchodilator

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24
Q

MOA for epinephrine

A

non-selective alpha, beta agonist and potent bronchodilator

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25
Q

How is Isoproterenol administered and how is it given to

A

acute asthma attack

-inhaled and oral

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26
Q

What is the law in the US for Isoproterenol

A

inhalation or sublingual administration is no longer marketed in the US

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27
Q

when is epinephrine used and how is it administered

A

acute asthma attack

- inhaled or subcutaneously - emergency circumstances

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28
Q

Name B2- selective agonists LABA

A

Salmeterol
Formoterol
Indacaterol

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29
Q

what is B2- selective agonists LABA used for

A

control (prophylaxis therapy) persistent asthma

- effective for asthma and COPD

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30
Q

when should one not take Salmeterol, Formoterol and Indacaterol

A

for acute asthma attack

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31
Q

what do B2- selective agonists LABA need to be taken with

A

anti-infammatory therapy ( corticosteroids, leukotriene, inhibitors )

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32
Q

Indacaterol can be specifically be used for what

A

COPD

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33
Q

Adverse effects of Salmeterol, Formoterol, and Indacaterol? how can this be helped

A
  • airway tolerance to B2 agonists: potential problem

- Corticosteroids may prevent tolerance by increasing B2 receptor numbers within airway

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34
Q

Name 2 muscarinic antagonists

A

Ipratropium and Tiotropium

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35
Q

MOA of Ipratropium and Tiotropium

A
  • reduces ACH -stimulated cyclic GMP

- inhibits mucus secretion

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36
Q

what is a popular combination inhaler

A

Ipratropium and Albuterol

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37
Q

Ipratroprium can specially be used for what

A

nasal discharge from rhinorrhea

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38
Q

What are adverse effects of Muscarinic antagonists

A

unpleasant bitter taste
dryness of mouth
cause glaucoma if sprayed in eye

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39
Q

MOA for methylxanthines

A

bronchodilator and anti-inflammatory activity

40
Q

name a drug of Methylxanthines

A

Theophylline

41
Q

MOA of Theophylline

A
  • inhibits phosphodisterases
  • functions as adenosine-receptor antagonist
  • anti-inflammatory
  • promotes contraction of diaphragmatic muscles
42
Q

Theophylline is FDA-indicated for what

A

Asthma and COPD

43
Q

Theophhylline is used as an adjunct with what in chronic severe asthma that are not controlled by what drugs

A
  • inhaled corticosteroids

- solely with corticosteroids and B-receptor agonsits

44
Q

Caffeine (Methylxanthine) used to treat what

A

apnea in preterm infants

45
Q

what are routes of administration for Theophylline

A
  • intravenous
  • tablets
    Not inhaled
46
Q

What are adverse effects of theophylline

A

low therapeutic index

toxicity is dose dependant

47
Q

low level toxicity of theophylline causes

A

nausea
vomiting
headache
restlessness

48
Q

higher level toxicity of theophylline causes

A

cardiac arrhythmias and seizers

49
Q

what enzyme increases the clearance of Theophylline

A

CYP1A2

50
Q

Name corticosteroids

A

Beclomethasone
Triamicinolone acetate
Budesonide
Fluticasone propionate

51
Q

MOA for corticosteroids

A

anti-inflammatory agents

  • act through glucocorticoid receptor
  • increases B2 receptors
  • decreases cytokines
52
Q

What is a use for corticosteriods?

A

inhaled corticosteroids are front-line therapy for persistent asthma
- less effective in COPD (reserved for COPD)

53
Q

What are corticosteroid combination inhalers

A

Fluticasone/Salmeterol

Budesonide/formoterol

54
Q

how do synergistic interactions between corticosterids and B2-agonists occur

A

corticosteroids up-regulate B2 receptor expression

55
Q

nasal spray corticosteroid is used for what

A

allergic rihinits

56
Q

What are adverse effects of Corticosteroids

A

Dysphonia
cough
oropharyngeal candidiasis

57
Q

Leukotriene inhibitor is FDA indicated for what

A

asthma

not front-line therapy for asthma

58
Q

name 3 Leukotriene inhibitors

A

Zafirlukast and Montelukast

Zileuton

59
Q

MOA of Zafirlukast and Montelukast

A

Antagonize Leukotriene receptor (LT1)

  • blocks cysteinyl leukotrienes
  • inhibits bronchoconstriction and airway inflammation
60
Q

When are leukotriene inhibitors used

A

potential alternative to medium-dose inhaled corticosteroids ( if corticosteroids are not tolerated) for prophylaxis of mild persistent asthma

61
Q

what is Montelukast used for

A

allergic rhinitis

62
Q

what is MOA for Zileuton

A

inhibits 5-lipooxygenase, (rate-limiting enzyme in leukotriene biosynthesis)

63
Q

what is the dosing for Montelukast, Zafirlukast and Zileuton

A

Montelukast: once daily
Zafirlukast: twice daily
Zileuton: 4 times daily

64
Q

how are anti-leukotrienes administered

A

oral

65
Q

how are Montelukast, Zafirlukast and Zileuton metabolized

A

CYPs

66
Q

what are adverse effects of Anti-leukotrienes

A

hepatic toxicity

67
Q

drug interaction of Zafirlukast

A

Warfarin, causes headache

68
Q

which anti-leukotriene does not inhibit hepatic CYPs

A

Montelukast

69
Q

Name Mast cell stabilizers

A

Cromolyn and Nedocromil

70
Q

MOA for Cromolyn and Nedocromil

A

inhibit mast cell degranulation and histamine release

71
Q

Name an anti-IgE therapy

A

Omalizumab

72
Q

MOA for Omalizumab

A

humanized monoclonal antibody against IgE.

- inhibits IgE binding to Ige receptors on mast cells

73
Q

when are anti-IgE therapy used

A
  • not font line asthma therapy

- reserved for severe asthma not controlled by corticosteroids

74
Q

what is the dosing for Omalizumab

A

subcutaneous injection every 2-4 weeks

75
Q

adverse effect of anti-IgE therapy

A

anaphylaxis

76
Q

What is alpha-1 proteinase inhibitor FDA-indicated for

A

COPD patients with deficiency in alpha 1 proteinase inhibitor

77
Q

what are the effects of alpha-1 proteinase inhibitor?

A

inhibits the activity of elastase

-excess elastase destroys lung parenchyma

78
Q

name an opioid found in common cold medications

A

Hydrocodone and codeine

79
Q

MOA for hydrocodone and codeine

A

suppresses cough by direct central action in medulla

80
Q

what are opioids used for

A

high doses used for pain

lower doses used for antitussive effects

81
Q

adverse effects of Hydrocodone and codeine

A

respiratory depression
constipation
dysphoria

82
Q

what is Benzonatate used for and MOA

A
  • cough
  • peripheral action, targets cough receptors of vagal afferent fibers , located in respiratory passages, lungs and pleura
83
Q

adverse effect of Benzonatate

A

Dizziness

84
Q

what is Expectorant/Guaifenesin used for and adverse effect

A
  • cough

- emetic

85
Q

Name 2 Mucolytics that are used for cough

A

N-acetylcysteine

Dornase Alpha

86
Q

what is Dornase Alpha FDA-indicated for

A

adjunct for cystic fibrosis

87
Q

Antihistamines (H1-receptor blockers) are used for what

A

rhinitis

88
Q

what Antihistamines (H1-receptor blockers) is used as sleep aid (Tylenol PM)

A

Diphenhydramine

89
Q

what are adverse effects of Antihistamines (H1-receptor blockers)

A

caution with glaucoma and prostate hypertrophy

CNS effects

90
Q

what are adverse effects of second generation antihistamines

A

lack significant anticholinergic actions

penetrate poorly into the CNS

91
Q

what is Ipratropium used for

A

rhinitis

92
Q

Name adrenergic agonists that treat Rhinitis

A

Oxymetazoline
pseudoephedrine
phenylephrine

93
Q

MOA for oxymetazoline, pseudophedrine, and phenylephrine

A

Phanylephrine: selective alpha 1 receptor agonist
Oxymetazoline: alpha receptor ( alpha 1 and 2) agonist
Pseudoephedrine ( alpha and beta agonist)

94
Q

Adverse effect of adrenergic agonist

A

rebound nasal congestion
tachycardia
hypertension

95
Q

who should avoid Oxymetazoline, Pseudophedrine, and Phenylephrine

A

patients with uncontrolled hypertension or ischemic heart disease