Drugs for Pulmonary Disorders Flashcards

1
Q

What is the main advantage of drug delivery by the respiratory system?

A
  • Rapid, efficient delivery
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2
Q

What is aerosol drug administration?

A
  • Suspension of liquid and fine solid particles
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3
Q

What is the advantage of aerosol drug administration?

A
  • Delivered to site of action with limited side effects
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4
Q

Can aerosolized drugs produce systemic effects?

A

Yes. If high enough dose is administered, it will reach systemic circulation

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5
Q

What are the 3 types of aerosolized drug administration?

A
  • Nebulizers
  • Dry Powder Inhaler
  • Metered dose inhalers
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6
Q

Which type of aerosolized drug administration converts a liquid to a fine mist?

A

Nebulizer

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7
Q

Which type of aerosolized drug administration is a propellant?

A

Metered dose inhaler

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8
Q

Which type of aerosoloized drug administration is a powder used for inhilation?

A

Dry Powder Inhaler

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9
Q

What are 3 common problems with aerosol drug administration?

A
  • Difficulty self-administering drug leads to incorrect dosage
  • Altered breathing patterns affect administration
  • Deposition of the drug into the oral mucosa
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10
Q

Which type of aerosol administration most negates incorrect dosing due to altered breathing patterns?

A
  • Nebulizer
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11
Q

What is a downside to a nebulizer?

A
  • Takes a long time to administer

- Cleaning after every session is time consuming

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12
Q

What is a common pulmonary chronic disease that affects millions worldwide?

A

Asthma

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13
Q

What are the 4 features of asthma?

A
  • Airway inflammation
  • Airway hyperresponsiveness
  • Bronchoconstriction
  • Hypersecretion of mucus
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14
Q

What is atopy?

A
  • Inherited predisposition to allergic diseases such as asthma, allergic rhinitis, or eczema
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15
Q

What condition does atopy underlie in almost all children, and most adults?

A
  • Asthma
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16
Q

What immunoglobin is typically elevated in patients with asthma?

A
  • Immunoglobin E (IgE)
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17
Q

What white blood cells are more common in inflamed airways than in normal airways?

A

Eosinophils

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18
Q

What glands hypertrophy in inflamed airways?

A

Mucus

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19
Q

Where does edema occur in inflamed airways?

A

Space between smooth muscles cells and epithelium

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20
Q

What are the 3 goals of therapy in reducing airway inflammation?

A
  • Terminate acute bronchial constriction
  • Reduce inflammation
  • Reduce hypersecretion of mucus
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21
Q

What is the distinguishing feature of COPD?

A
  • Airflow limitation is not reversible
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22
Q

What are 2 examples of COPD?

A
  • Chronic bronchitis

- Emphysema

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23
Q

What are the 4 treatment goals of COPD?

A
  • Reduce inflammation
  • Relieve bronchoconstriction
  • Reduce risk of/ treat infection
  • Control cough
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24
Q

What type of material is COPD usually related to?

A

Toxins such as:

  • Coal
  • Cigarette smoke
  • Etc…
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25
Q

What is a persistent risk due to chronic bronchitis? why?

A
  • Excessive secretions can lead to infection
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26
Q

What is the type of drug typically used to treat acute bronchoconstriction?

A
  • Beta-2 Adrenergic Agonists

- Stimulate B-2 receptors in the smooth muscle of the brochi and bronchioles

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27
Q

Describe the 4 step process by which B-2 agonists relax bronchioles.

A
  • B-2 receptor stimulation increases activity of enzyme adenylcyclase
  • Adenylcyclase increases production of intracellular cyclic AMP
  • Intracellular cyclic AMP activates protein kinase A
  • Protein kinase A inhibits phosphorlation of myosin, and lowers intracellular ionic calcium concentrations
  • Results in relaxation of smooth muscle of bronchioles
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28
Q

What drug stimulates both B-1 and B-2 receptors?

A

Epinephrine

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29
Q

What are the advantages of a B-2 selective agonist vs non-selective?

A
  • Limits cardiac effects

- Limits increase in heart rate

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30
Q

When may epinephrine be used to treat bronchoconstriction?

A
  • When it is in an acute phase to provide rapid therapeutic effect
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31
Q

What is a severe prolonged form of asthma that is unresponsive to standard drug treatment?

A
  • Status asthmaticus
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32
Q

What 3 conditions may epinephrine be used to treat?

A
  • Bronchiolitis
  • RSV
  • Status asthmaticus
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33
Q

What are the 4 classifications of Beta-2 Adrenergic Agonists in terms of duration of drug action?

A
  • Ultra-short acting (2 - 3 hours)
  • Short-acting (SABA) (3 - 6 hours)
  • Intermediate Acting (8 Hours)
  • Long-acting (LABA) (12 hours)
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34
Q

What are 2 ultra-short acting beta agonists?

A
  • Isuprel

- Bronkosol

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35
Q

What are 3 short-acting beta agonists?

A
  • Metaprel/ Aluprent
  • Brethine
  • Maxair
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36
Q

What are 3 intermediate-acting beta agonists?

A
  • Proventil
  • Xopenex
  • Tornalate
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37
Q

What are 2 long-acting beta agonists?

A
  • Serevent

- Foradil

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38
Q

What are 3 side-effects of high-dose inhalers?

A
  • Shaking
  • Nervousness
  • Tachycardia
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39
Q

Why will a B-2 agonist cause tachycardia?

A
  • Drugs are selective for B-2, but not exclusively

- Will bind to B-1 if B-2 are occupied

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40
Q

What is levalbuterol?

A
  • 60:40 R:S isomer of B-2 agonist

- May alleviate some side effects

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41
Q

What is Formoterol/ Foradil?

A
  • Highly selective Beta-2-agonist with a long duration of action
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42
Q

Why does Formoterol/ Foradil have such a long duration of action?

A
  • Formoterol is highly lipophilic when entering the plasma membrane in a “drug depot”
  • It is gradually released into its aqueous phase, which activates the B-2 receptors
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43
Q

What may occur if SABAs are overused?

A
  • Tolerance by desensitization of B-2 receptors
44
Q

How may tolerance to SABAs be reversed?

A

With inhaled corticosteroids

45
Q

What condition may result from SABA tolerance?

A

Status asthmaticus

46
Q

What receptors do inhaled anticholinergics act on?

A

Block muscarinic cholinergic receptors

47
Q

What is the 3-step mechanism of action of inhaled anticholinergics?

A
  • Decrease in the formation of cGMP
  • Decreases contractility of smooth muscle in the lung
  • Inhibits bronchoconstriction and mucus secretion
48
Q

Are inhaled anticholinergics used for acute occurances, or for control?

A

Control

49
Q

What condition are anticholinergics typically used for?

A
  • COPD
50
Q

What are 3 types of anti-cholinergics?

A
  • Ipratropium bromide/ Atrovent
  • Ipratropium + albuterol/ Combivent
  • Tiotropium/ Spiriva
51
Q

What are 6 side-effects of anti-cholinergics?

A
  • Dry mouth
  • Nervousness
  • GI upset
  • Headache
  • Worsening of narrow-angle glaucoma
  • Prostatic hypertrophy
52
Q

What is the difference between Atrovent and Spiriva?

A
  • Spiriva has a longer half-life due to slow disassociation rate from muscarinic receptors
53
Q

What are the primary actions of inhaled corticosteroids in the lungs?

A
  • Suppress inflamation in airways (limit hypertrophy of mucus cells, reduce edema, repair damaged epithelium)
  • Increase number and sensitivity of B-2 receptors (increase effectiveness of B-2 agonists)
54
Q

Are PO or IV administration of corticosteroids more effective for acute severe asthma attacks?

A

Act about the same

55
Q

How long does it take for systemic corticosteroids to take effect?

A

48 - 72 hours.

56
Q

Why should systemic corticosteroids be titrated down before discontinuing use?

A
  • Activate glucocortizoid receptors
  • These function through negative feedback
  • Body detects the change in cortisol levels, and slow production at the adrenal gland
  • If drug is not administered, there may be a severe drop in systemic cortisol
57
Q

Are long-term systemic or inhaled corticosteroids more associated with serious adverse effects?

A
  • Systemic
58
Q

What are 6 adverse effects of systemic corticosteroids?

A
  • Adrenal gland atrophy
  • Peptic ulcers
  • Hyperglycemia
  • Osteopenia & Osteoporosis
  • Aseptic necrosis of the hip
  • Immune suppresion
59
Q

What are 6 unpleasant side effects of systemic corticosteroids?

A
  • Moon face
  • Redistribution of weight
  • Thin skin
  • Acne
  • Fatigue
  • GI disturbance
60
Q

What are 5 inhaled corticosteroids?

A
  • Fluticasone (Flovent Diskus)
  • Budesonide (Pulmicort)
  • Triamcinolone (Azmacort)
  • Flunisolide (Aerobid)
  • Beclomethasone (Qvar, Beclovent)
61
Q

What are 2 oral corticosteroids?

A
  • Methyprednisolone (Depo-Medrol)

- Prednisone (Deltasone etc)

62
Q

What is usually paired with an inhaled corticosteroid?

A

Nasal spray

63
Q

Why is fluticasone proprionate/ Flovent have little bioavailability outside of the airway?

A
  • Rapidly inactivated by the liver (CYP450 3A4 pathway)

- The metabolite that is produced has limited affinity for the glucocorticoid receptor

64
Q

What are 2 examples of medications with a corticosteroid and bronchodilator component?

A
  • Fluticasone and salmeterol (Advair Diskus)

- Budesonide and formoterol (Symbicort)

65
Q

What is the advantage of combination agent aerosol medications?

A

Convenience

66
Q

What drug are methylxanthines chemically related to?

A

Caffeine

67
Q

What are 2 examples of methylxanthines?

A
  • Theophylline (Theo-Dur, etc)

- Aminophylline (Somophyllin)

68
Q

What 2 other pulmonary effects do methylxanthines have other than bronchodilation?

A
  • Inhibit pulmonary edema by decreasing vascular permeability
  • Increase ability of the cilia to clear mucus
69
Q

What 4 non-pulmonary effects do methylxanthines have?

A
  • Increase CO
  • Peripheral vasodilation
  • Mild diuretic effect
  • CNS stimulation
70
Q

Why are methylxanthines not often prescribed?

A

Narrow therapeutic index

71
Q

Why must methylxanthines serum levels be monitored regularly?

A
  • Narrow therapeutic index

- Normal caffinated drinks can raise levels easily

72
Q

What the mechanism of action of mast cell stabilizers?

A
  • Inhibit the release of histamine from mast cells
73
Q

In what stiuations are mast cell stabilizers used?

A
  • In prophylaxis to prevent acute asthma attacks
74
Q

How long is the half-life of mast cell stabilizers?

A

2.5 hours

75
Q

What are 2 mast cell stabilizers?

A
  • Cromolyn (Intal)

- Nedocromil (Tilade)

76
Q

What are Leukotriene?

A
  • Strong chemical mediators of bronchoconstriction, inflammation, and mucous secretion
77
Q

How are Leukotrienes formed?

A

By the lipoxygenase pathway of arachidonic acid metabolism in response to cellular injury

78
Q

What type of medication treats Luekotrienes?

A
  • Leukotriene modifiers
79
Q

What is the indication for Leukotriene modifiers?

A
  • Long-term treatment of asthma and allergies

- Acts on pathways related to long-term inflammation

80
Q

What are 3 Leukotriene Modifiers?

A
  • Zileuton (Zyflo)
  • Montelukast (Singulair)
  • Zafirlukast (Accolate)
81
Q

What is the mechanism of action of Zyflo?

A
  • Reduces formation of leukotrienes by blocking lipoxygenase
82
Q

What is the mechanism of action of Singulair and Accolate?

A
  • Block luekotriene receptors
83
Q

What is the mechanism of action of Omalizumab (Xolair)?

A
  • Binds to immunoglobulin E, preventing attachment to mast cells and basophils
  • Prevents release of pro-inflammatory and pro-allergic substances
84
Q

For whom is Xolair prescribed?

A
  • Severe, persistent asthma that can’t be controlled even with high doses of corticosteroids
85
Q

What is the meachanism of action of Mucolytics/ Expectorants?

A
  • Reduce viscosity of bronchial mucous and aid in its removal
86
Q

What is an OTC mucolytic?

A
  • Guaifenesin (Robitussin, etc…)
87
Q

What are 2 prescription examples of mucolytics/ expectorants?

A
  • Acetylcysteine (Mucomyst)

- Dornase Alfa-Recominant (Pulmozyme)

88
Q

What is the function of antitussives?

A
  • Dampen the cough reflex
89
Q

What are 2 examples of opoid antitussives?

A
  • Codeine

- Hydrocodone bitartrate (Hycodan)

90
Q

What are 2 examples of non-opoid antitussives?

A
  • Benzonatate (Tessalon)

- Dextromethorphan (Pediacare, etc…)

91
Q

What is the active ingredient in vicadin?

A
  • Hydrocodone bitartrate
92
Q

What is respiratory distress syndrome?

A
  • Condition where lungs are not producing surfactant
93
Q

In whom does respiratory distress syndrome most often occur?

A
  • Infants
94
Q

What is the function of surfactant?

A
  • Lines inner surface of alveoli allowing the lung to remain open during respiration
95
Q

What type of cell produces surfactant?

A

Type II/ Chief cells

96
Q

What are 2 drugs used to treat RDS?

A
  • Colfosceril (Exosurf)

- Ceractant (Survanta)

97
Q

What is Respiratory Syncytial Virus?

A
  • Virus affecting infants and young children
98
Q

How is respiratory syncytial virus treated?

A
  • RSV antibodies given during RSV season to reduce risk of infection
99
Q

What is anaphylaxis?

A

Severe, sometimes life-threatening allergic reaction to a variety of agents

100
Q

What are 3 classes of agents that may cause anaphylaxis?

A
  • Foods
  • Stinging insects
  • Medications
101
Q

What are some symptoms of anaphylaxis?

A
  • Itching
  • Can’t breath
  • Throat swells
  • Lungs constricted
  • Vascular permeability shift –> edema
102
Q

What is the pathophysiology of anaphylaxis?

A
  • IgE forms during the first exposure to the allergen
  • IgE attaches to mast cells and basophils
  • At the 2nd exposure, the mast cells and basophils release chemical mediators
103
Q

What 3 effects do the chemical mediators of anaphylaxis cause?

A
  • Smooth muscle constriction causing bronchospasm and cramping
  • Increased vascular permeability (50 % of vascular volume shifts to tissues)
  • Vasodilation
104
Q

Why may someone have a reaction to penicillin when they’ve never had it before?

A

May have been exposed to a chemically similar drug such as cephalosporin

105
Q

What type of hypersensibility are most allergic reactions?

A
  • Type 1
106
Q

What drug is used to treat anaphylaxis?

A
  • Epinephrine
107
Q

What are the 2 effects of epinephrine?

A
Alpha-agonist:
- Increased peripheral vascular resistance
- Reverse vascular permeability
Beta-agonist:
- Bronchodilation
- Positive ionotropic effect