Module 9: Pulmonary Pharmacology Flashcards

1
Q

asthma is characterized by

A

chronic inflammatory disease

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2
Q

asthma is characterized by increased sensitivity to

A

irritants and bronchoconstrictors

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3
Q

asthma may be caused by…

A

genetics or induced by exposure to environmental agents

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4
Q

what structure becomes hypersensitive in asthma

A

bronchial tree

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5
Q

severe cases of asthma can lead to

A

asphyxia

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6
Q

COPD includes which 2 symptoms

A

emphysema and chronic bronchitis

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7
Q

emphysema is characterized by (2)

A
  • Damage to alveoli and small bronchioles
  • Limits ability to oxygenate blood
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8
Q

emphysema is a disease of

A

lung tissue damage

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9
Q

chronic bronchitis is a ____________ disorder

A

an inflammatory disorder

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10
Q

chronic bronchitis characteristics (2)

A
  • Increases mucous production and coughing
  • Inflammation of bronchioles leads to decreased oxygenation
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11
Q

COPD damage is considered

A

irreversible

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12
Q

tx of COPD (vague)

A

control symptoms and limit further damage

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13
Q

β-2 selective agonists stimulate

A

β-2 adrenergic receptors in bronchioles

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14
Q

how do β-2 selective agonists cause bronchodilation

A

via β2 G-protein receptor

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15
Q

what does the β-2 G-protein receptor do

A
  • Stimulates Ca-activated K channel
  • hyperpolarizes & decreases Ca entry
  • thus leads to muscle relaxation

↑cAMP = ↓Ca = smooth muscle relaxation

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16
Q

mainstay of asthma and COPD therapy

A

β-2 selective agonists

esp when combined with inhaled steriods

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17
Q

long acting β-2 adrenergic agonists are linked to

A

increased asthma deaths

  • should only be used in combo with inhaled steroids *

Formoterol
Arformoterol
Salmeterol

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18
Q

Long-acting β2 adrenergic agonists act at what two sites on receptor?

A

normal site and another that binds irreversibly.

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19
Q

high lipid solubility of β-2 selective agonists leads to

A

prolonged tissue action

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20
Q

short acting β-2 inhalational agents (4)

A

Levalbuterol (Xopenex)

Albuterol (Proventil HFA)

Metaproterenol

Pirbuterol (Maxair) (D/C’ed due to CFC propellant)

LAMP- turn the lamp on and off = short acting

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21
Q

long acting β-2 selective agonists

A
  1. Formoterol (Foradil) (racemic)
  2. Arformoterol (Brovana) (enantiopure)
  3. Salmeterol (Serevent)
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22
Q

albuterol + ipratropium is an (anticholinergic/antimuscarinic)

A

antimuscarinic

(Anticholinergics categories: antimuscarinics, which block muscarinic receptors, and antinicotinics, which block nicotinic receptors)

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23
Q

Albuterol + Ipratropium (Combivent) is useful for

A

COPD and in some asthma cases

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24
Q

tissue drying effects of albuterol + ipratropium may aggravate

A

coughing and some asthma

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25
Q

COPD patients have an ↑ risk of adverse cardiovascular effects with

A

Albuterol + Ipratropium (Combivent)

26
Q

contraindicated in narrow angle glaucoma

A

Albuterol + Ipratropium (Combivent)

27
Q

Long-acting β2 adrenergic agonists with Corticosteroid (3)

A
  • Salmeterol/Fluticasone (Advair)
  • Formoterol/Mometasone (Dulera)
  • Formoterol/Budesonide (Symbicort)
28
Q

inhaled steroids (5)

A
  • Ciclesonide (Alvesco)
  • Mometasone (Nasonex)
  • Budesonide (Rhinocort)
  • Fluticasone (Flovent HFA)
  • Beclomethasone (QNASL)
29
Q

inhaled steroids are typically better than

A

systemic steroids

fewer side effects

30
Q

systemic steroids (4)

A
  • Methylprednisone (Solu-medrol)
  • Prednisolone (Orapred)
  • Prednisone (Rayos)
  • Hydrocortisone (Solu-cortef)
31
Q

steroid moa

A

Bind to intracellular steroid receptors that form dimers and are transported into cell nucleus and regulate transcription, decreasing inflammatory protein synthesis.

32
Q

what kind of drug is theophylline

A

methylxanthines

Theophylline: 1,3-dimethylxanthine

33
Q

theophylline is structurally similar to (2)

A

caffeine and theobromine

34
Q

theophylline is found naturally in

A

cocoa beans, trace in tea

35
Q

aminophylline is …

A

2 theophylline molecules with a 1,2-ethanediamine coupler for increased duration.

36
Q

theophylline acts as a ____________ by ____________

A

bronchodilator by inhibiting phosphodiesterase (non-selective) leading to an increase in intracellular cAMP.

37
Q

what does theophylline do to intracellular cAMP

A

increases it

38
Q

theophylline also acts as an agonist for

A

several adenosine receptors and triggers some catecholamine release from adrenals.

39
Q

roflumilast class

A

Newer selective PDE4 inhibitor

40
Q

where is PDE4 found in greater amounts

A

in airway smooth muscle and epithelial cells

41
Q

which has less side effects and why: theophylline or roflumilast

A

roflumilast because theophylline is NON selective

42
Q

leukotriene receptor antagonists (2)

A

Zafirlukast (Accolate)

Montelukast (Singulair)

43
Q

zileuton class

A

5-lipoxygenase inhibitor

44
Q

zileuton mechanism of action

A

leukotriene inhibitor:
* Inhibits the production of the leukotrienes from arachidonic acid
* antagonizes 5-lipoxygenase

Not the same as leukotriene receptor antagonists!

45
Q

zileuton affects on coagulation

A

May inhibit warfarin metabolism due to metabolic competition

May thus increase prothrombin time

46
Q

up to 2% of patients taking zileuton may demonstrate…

A

↑ liver enzymes

Cease use if liver enzyme levels increase over 3 X normal

47
Q

zileuton is contraindicated in patients with

A

Contraindicated in patients with active liver disease

48
Q

sodium cromolyn prevents…

A

mast cell degranulation

49
Q

sodium cromolyn blocks …(4)

A

histamine, leukotriene, prostaglandin and cytokine release

50
Q

mechanism of action of sodium cromolyn

A

Acts as an anti-inflammatory agent, not a bronchodilator

Blocks IgE trigger molecules on mast cells from being activated

51
Q

T/F sodium cromolyn blocks the binding of IgE

A

FALSE

it just blocks the response

52
Q

mechanism of action of sodium cromolyn may be by blocking ____________ entry into the cell

A

calcium

53
Q

what is sodium cromolyn used for

A

Asthma and prevent bronchospasms due to irritants

54
Q

side effects of sodium cromolyn (3)

A

allergy, arrhythmias and polycythemia (both rare)

55
Q

omalizumab is a

A

monoclonal antibody

56
Q

omalizumab mechanism of action

A
  • Binds to human IgE in blood and on surface of B lymphocytes
  • but not to IgE receptor on mast cells and basophils
57
Q

omalizumab binding to IgE in blood decreases

A

IgE presence on mast calls

58
Q

Since large percentage of asthmatics have high IgE levels, omalizumab lowers…(2)

A

asthmatic reactions

other hypersensitivity reactions

59
Q

uses of omalizumab (2)

A

Severe asthma that does not respond to steroids

Chronic spontaneous urticaria that does not respond to antihistamines

60
Q

side effects of omalizumab

A

anaphylaxis (0.2%), stroke, heart disease, cancer?