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Pharmacology B > Lecture 10 - Drugs & Asthma/COPD > Flashcards

Lecture 10 - Drugs & Asthma/COPD Flashcards

1
Q

What is COPD?

A

slow progressive airway obstruction due to chronic inflammation

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2
Q

COPD is common in _____.

A

smokers

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3
Q

Other causes of COPD?

A

air pollution and occupational exposures

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4
Q

Symptoms of COPD?

A
  • cough
  • mucus hypersecretion
  • dyspnea (shortness of breath)
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5
Q

What does COPD include?

A
  • chronic bronchitis (inflammation of bronchi)

- emphysema (destruction of alveolar structure - airways collapse during expiration)

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6
Q

What is asthma?

A

chronic inflammatory disorder of the airways

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7
Q

What is asthma characterized by?

A

recurring episodes of hyper responsiveness to stimuli that causes bronchoconstriction

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8
Q

Symptoms of asthma?

A

recurring episodes of cough, wheezing, tight chest, dyspnea (shortness of breath)

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9
Q

What is asthma based on?

A

triggering stimuli characterized as extrinsic (allergenic) or intrinsic (non-allergenic)

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10
Q

extrinsic asthma = ?

A

allergenic

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11
Q

intrinsic asthma = ?

A

non-allergenic

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12
Q

Describe extrinsic asthma (allergenic)

A
  • External stimuli such as environmental allergens (dust, mold, pollen, dander, foods) trigger plasma cells to produce antigen specific IgE antibodies
  • Allergen & IgE binding to mast cells result in degranulation and release of inflammatory mediators
  • Allergens typically have some glycoproteins that immune cells recognize as an antigen, a harmful substance that induced immune cells to produce antibody (IgE) that specially recognize the antigen
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13
Q

Describe Intrinsic Asthma

A
  • Non-allergenic asthma
  • Symptoms triggered by non-allergenic factors (anxiety, stress, cold air, dry air, smoke, exercise, viruses)
  • The mechanisms initiating the asthma attack are not completely understood:
  • Abnormalities in the autonomic regulation of airway functions suggested to increase responsiveness.
  • The innate immune system involved, the role of adaptive immune system remains elusive.
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14
Q

What are the asthma symptoms amenable to drug therapy?

A
  • Excessive airway smooth muscle tone
  • Inflammation
  • Mucus plugging
  • Pulmonary edema
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15
Q

Asthma & COPD Drugs:

Drugs divided based on treatment strategies?

A

1) controllers

2) relievers

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16
Q

Asthma & COPD Drugs:

Drugs divided based on targets?

A

1) Airway muscle tone:
- Bronchodilators (Beta-adrenergic, methylxanthines, anticholinergics, leukotriene modifiers)

2) Inflammation:
- Anti-inflammatory agents (Corticosteroids, mast cell stabilizers, anti-IgE monoclonal-antibody, leukotriene modifiers)

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17
Q

What are bronchodilators?

A

Agents that interact with smooth muscle cells lining the airways (bronchiole) and relax smooth muscles

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18
Q

List some Beta-adrenergic bronchodilators

A
  • Albuterol/Salbutamol
  • Terbutaline
  • Salmeterol
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19
Q

List a Methylxanthine bronchodilator

A

-Theophylline

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20
Q

List some anticholinergic bronchodilators

A
  • Tiotropium

- Ipratropium

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21
Q

List some leukotriene modifier bronchodilators

A
  • Zileuton
  • Zafirlukast
  • Montelukast
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22
Q

Sympathetic nervous system causes ________

A

bronchodilation

running from tiger, need air to breath

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23
Q

Parasympathetic nervous system causes _______

A

bronchoconstriction

just relaxing to the max so you don’t need to breath too hard

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24
Q

What receptor causes bronchodilation?

A

B2 (sympathetic)

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25
Q

What receptor causes bronchoconstriction?

A

M3 (parasympathetic)

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26
Q

Ca2+ increase causes _______

A

bronchoconstriction

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27
Q

Ca2+ decrease causes _______

A

bronchodilation

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28
Q

Describe how bronchoconstriction happens

A

Activation of parasympathetic nervous system:

  • ACh binds to M3 receptors
  • Activation of Gq
  • PLC activation
  • Increased DAG and IP3 hydrolysis
  • increase of cytoplasmic Ca2+
  • Ca2+ calmodulin activates myosin via MLCK
  • myosin binds to actin –> actin slide past myosin
  • contraction (that occurs as long as Ca2+ is present)

*Adenosine also increases Ca2+ levels (PLC activation via A1 receptor)

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29
Q

Describe how bronchodilation happens

A
  • Activation of beta2 receptor, GPCR (NE, E)
  • Activation of Gs
  • AC activation
  • ATP converted into cAMP - PKA activation:
    1) promotion of SR Ca2+ pumps causes a decrease in cytoplasmic Ca2+
    2) inhibition of MLCK, enzyme activation myosin, prevents myosin binding to actin
  • dilation/relaxation
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30
Q

Albuterol/Salbutamol and Terbutaline are ____-acting

A

short

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31
Q

Salmeterol are ____-acting

A

long (12 hours)

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32
Q

MOA of B2 agonists

A

Stimulate AC thereby increasing the formation of cAMP which acts to relax the airway smooth muscle leading to bronchodilation

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33
Q

Route of admin of B2 agonists

A

Typically administered via inhalation:

  • Albuterol and Terbutaline available in tablet form
  • Terbutaline can also be administered SC
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34
Q

Indication of B2 agonists

A
  • Extensively used in the treatment of asthma
  • In inhaled form, Albuterol is the DOC for the treatment of acute attacks. For severe attacks, SC injection of Terbutaline or epinephrine may be required along with corticosteroids
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35
Q

What is the DOC for the treatment of acute asthma attacks?

A

Albuterol (inhaled form)

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36
Q

What is the DOC for the treatment of severe asthma attacks?

A

SC injection of Terbutaline or epinephrine may be required along with corticosteroids

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37
Q

We do we co-administer corticosteroids with anti-inflammatory drugs?

A

to prevent the development of desensitization and promote efficacy of B2 agonists

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38
Q

Adverse effects of B2 agonists?

A
  • B1 receptors on the heart may get stimulated causing tachycardia
  • skeletal muscle tremor
  • tolerance may develop with very frequent use
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39
Q

Drug interactions with B2 agonists?

A
  • Not effective on patient taking propranolol for HTN or other heart/circulatory conditions
  • Co-administration of long term B2 receptor agonists with corticosteroids prevents desensitization.
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40
Q

Theophylline is a _____

A

Methylxanthine

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41
Q

Proposed mechanism of Theophylline (Methylxanthine)?

A
  • Inhibits phosphodiesterase resulting in an increase in cAMP (cAMP acts to relax the airway)
  • Inhibit adenosine receptors; systemic & CNS effects
  • *Adenosine has been shown to cause the contraction os isolated bronchial smooth muscle and provoke the release of histamine from mast cells
  • Can stimulate the contractility of diaphragmatic muscles
42
Q

Route of admin of Theophylline?

A

Aerosol is the safest, other routes can adversely affect the heart & CNS.

43
Q

Indication of Theophylline?

A
  • Used as a second choice for the treatment of acute attacks. However, it has a narrow therapeutic window and pharmacokinetic slightly unpredictable (vary widely among similar patients) so it should be given under supervision
  • *Can be given to Pts on propranolol
  • COPD
  • May reverse the steroid insensitivity
44
Q

Adverse effects of Theophylline?

A

Common SE: headache, insomnia, tremors

Serious SE: anaphylactic shock, nausea & vomiting, stimulates heart, fever, seizures

Since it is metabolized by Cytochrome P450 enzymes, drug interactions may result in toxic concentrations

Caution: increased CV effects if given w B2 agonist

45
Q

Ipratropium is a ____ acting anticholinergic

A

short

46
Q

Tiotropium is a ____ acting anticholinergic

A

long

47
Q

MOA of anticholinergics (ipratropium and tiotropium)?

A
  • Blocks muscarinic receptors, preventing bronchial constriction and mucus secretion
  • No effect on inflammation
48
Q

Route of admin of anticholinergics (ipratropium and tiotropium)?

A

aerosol

49
Q

Indication of Ipratropium

A
  • For the treatment of COPD and chronic bronchitis
  • The treatment of acute asthma attacks in children, adults and those that are intolerant of B agonists
  • Ipratropium enhances the bronchodilation produced by B agonists. Therefore, this combination can be an effective treatment of severe asthma attacks.
50
Q

SE of ipratropium

A
  • Aerosol ipratropium is generally well tolerated, however, excessive use may cause atropine like effects (dry mouth, dilated pupils, tachycardia, stupor)
  • Caution with glaucoma (Increased IOP)
  • Caution in prostatic hypertrophy (urinary retention)
51
Q

Leukotrienes are products of ______ ____ metabolism

A

arachidonic acid

52
Q

Leukotrienes cause ??

A

bronchoconstriction, increased bronchial reactivity, mucosal edema and the secretion of mucus

53
Q

MOA of leukotriene modifiers?

A

1) drugs that inhibit the synthesis of leukotrienes

2) drugs that block the receptors that leukotrienes act upon

54
Q

How can NSAIDs induce asthma?

A

-they inhibit COX enzymes which means AA just goes to hydroperoxide and then to leukotrienes (slide 31)

55
Q

Zileuton is a ??

A

leukotriene synthesis inhibitor

56
Q

MOA of Zileuton

A

-inhibits 5-Lipoxygenase, which is the enzyme that catalyzes the formation of leukotrienes from arachidonic acid

57
Q

Route of administration of Zileuton

A

orally active drug, administered 4 times a day

58
Q

Indication of Zileuton

A
  • The treatment of persistent asthma in adults and ASA-induced asthma
  • Prevents exercise and antigen-induced bronchospasm
59
Q

SE of Zileuton

A

Liver enzyme levels should be checked periodically for possibly hepatotoxicity

60
Q

Drug interactions of Zileuton

A

Inhibits CYP450 which may interfere with the metabolism of other drugs (ex. theophylline, warfarin)

61
Q

List 3 Leukotriene Receptor blockers

A
  • Zafirlukast

- Montelukast

62
Q

MOA of Leukotriene Receptor blockers?

A
  • Selective reversible inhibitors of the cysteine leukotriene-1 (CysLT1) receptor, thereby preventing leukotriene induced bronchoconstriction and airway wall edema.
  • Prevents also chemotactic; infiltration of neutrophils and eosinophils
63
Q

Route of admin of Zafirlukast

A

-Orally active, administered twice daily

64
Q

Indication of Zafirlukast?

A
  • Used for the treatment of mild to moderate asthma
  • Less effective than corticosteroids
  • Should not be administered to children under 8.
65
Q

Adverse effects/drug interactions of Zafirlukast?

A
  • Headache, GI disturbance
  • Inhibits CYP450 which may interfere with the metabolism of other drugs (ex. theophylline, warfarin)
  • Liver enzyme levels should be checked periodically for possible hepatotoxicity
66
Q

Route of admin of Montelukast

A

orally active, administered once daily

67
Q

Indication of Montelukast

A
  • Modestly effective in the treatment of persistent asthma in children and adults.
  • Less effective than corticosteroids.
  • Should not be administered to children under 6 years of age.
68
Q

Drug interaction/Adverse effects of Montelukast

A
  • Inhibits CYP450 which may interfere with the metabolism of other drugs (ex. theophylline, warfarin)
  • Liver enzyme levels should be checked periodically for possible hepatotoxicity
69
Q

What do anti-inflammatory agents do?

A

Reduce inflammation, edema and mucus production

70
Q

How do anti-inflammatory agents help in asthma?

A

They counteract airway inflammation and reduce asthma attacks and COPD flares/progression

71
Q

List some corticosteroids

A
  • Beclometasone
  • Flunisolide
  • Fluticasone
  • Budesonide
  • Mometasone
  • Methylprednisolone
  • Prednisone
72
Q

List some mast cell blockers

A
  • cromolyn sodium

- nedocromil

73
Q

______ = steroid hormones produced in the adrenal cortex

A

Corticosteroids

74
Q

List 2 subtypes of Corticosteroids

A

Glucocorticoids

Mineralocorticoids

75
Q

What do glucocorticoids do?

A

regulate glucose metabolism

76
Q

What do mineralocorticoid do?

A

salt & water balance

77
Q

Corticosteroids are the _____ of anti-inflammatory process

A

King

78
Q

Corticosteroids:

Beclometasone, Flunisolide, Fluticasone, Budesonide, and Mometasone are all _________

A

inhaled

79
Q

Corticosteroids:

Methylprednisolone is given _____

A

IV

80
Q

Corticosteroids:

Prednisone is given ______

A

orally

81
Q

MOA of corticosteroids

A
  • blocks the release of arachidonic acid hence the production of leukotrienes
  • increase the sensitivity of beta adrenergic receptors and prevents their desensitization
  • prevents long term changes in airways structure & function
82
Q

Corticosteroids:

Route of admin

A

-Aerosol is the preferred mode of administration to limit systemic side effects, however severe exacerbations of asthma may require IV (methylpredisolone) or oral (prednisone)

83
Q

Corticosteroids:

Indication

A
  • Aerosol used in most moderate cases of asthma and COPD

- Corticosteroids are the first line of anti-inflammatory therapy for all ages

84
Q

Corticosteroids:

Adverse effects

A
  • Aerosol administration of corticosteroids is safe. They may cause oropharyngeal candidiasis (thrush) and hoarseness
  • Chronic use may result in the suppression of the adrenal glands and endogenous production of corticosteroids
  • Common and permanent: Osteoporosis and cataracts in adults and growth retardation in children
  • Common and reversible: edema, weight gain, psychological (mood swings, insomnia, anxiety) increased risk of infection, delayed wound healing, elevated BP, loss of glucose control in diabetics, glaucoma, and finally OMG muscle weakness
85
Q

How can the adverse effects of corticosteroids be reduced?

A

with alternate day therapy for oral medication and morning administration (because AA is highest in the morning)

86
Q

Who is cromolyn sodium approved for?

A

the treatment of asthma in all ages

87
Q

Who is Nedocromil approved for?

A

Approved for the treatment of asthma in patients 12 and older

88
Q

Mast cell blockers:

MOA

A
  • poorly understood
  • inhibits the release of inflammatory mediators from mast cells, possibly by blocking ion-channels required for degranulation
89
Q

Mast cell blockers:

Route of admin?

A

aerosol, administered 2-4 times/day

90
Q

Mast cell blockers:

Indication

A
  • For the treatment of mild-moderate asthma
  • Dose not reverse an ongoing broncho-constriction, BUT, regular use reduces bronchial hyper-reactivity and inhibits acute and chronic responses
  • Less potent than inhaled glucocorticoids in controlling asthma
  • Trial period of 4-6 weeks is required to determine its efficacy
  • Anti-inflammatory DOC for the treatment of allergenic asthma in children (>2-3 yrs old)
  • Also helpful to prevent exercise-induced asthma
91
Q

Mast cell blockers:

Adverse effects?

A
  • Generally well tolerated.
  • Can cause throat irritation, dryness, cough, nasal secretions and congestion, nausea

Serious adverse effects are rare:

  • Anaphylaxis, hives, low BP, tightness in chest
  • Less than 2% experience reversible dermatitis, myositis, or gastroenteritis
92
Q

Omalizumab (Anti-IgE Monoclonal antibody):

MOA

A

Selectively binds human free IgE and thus prevents IgE binding to cells and reduces IgE levels. Both acute and prolonged inflammatory responses reduced.

93
Q

Omalizumab (Anti-IgE Monoclonal antibody):

Indication?

A

Used for allergic asthma

94
Q

Omalizumab (Anti-IgE Monoclonal antibody):

Route of admin?

A

SC injections

95
Q

Omalizumab (Anti-IgE Monoclonal antibody):

Adverse effects?

A

may cause anaphylaxis in some patients

96
Q

Goals of therapy with asthma & COPD?

A

1) Maintain normal activity levels
2) Maintain near normal pulmonary function rates
3) Prevent troublesome symptoms - cough, breathlessness @ night or during exertion
4) Avoid adverse effects of medications
5) Avoid drug interactions

97
Q

What is the treatment for mild COPD?

A

Bronchodilators as needed

98
Q

What is the treatment for moderate COPD?

A

Bronchodilators and anti-inflammatory drugs

99
Q

What is the treatment for severe COPD?

A

antibiotics, bronchodilators and anti-inflammatory drugs and oxygen therapy

100
Q

Asthma = ______

A

reversible

101
Q

COPD = ______

A

irreversible

102
Q

see slide 57

A

alrighty

Pharmacology B (21 decks)

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