Block V- Pulm Asthma Drugs Flashcards

1
Q

True or false - most of asthma is due to allergies

A

false - only 30%

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2
Q

What causes exacerbations of asthma?

A

decrease in expiratory airway, air is trapped or occluded

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3
Q

What factors cause immediate bronchospasm?

A

Histamine, PAF, leukotrienes (C4, D4)

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4
Q

What causes late bronchospasm?

A

mast cells, platelets, macrophages releasing chemotaxins and leuotrien B4, PAF

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5
Q

What are the major categories of anti asthmatic drugs?

A

bronchidilator drugs

anti inflammatory drugs

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6
Q

What is the mechanism of action of bronchodilator therapy?

A

beta-2 AR agonist

  • causes decrease in Ca and decreased contractility
  • hyper polarization of K
  • Medication of choice
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7
Q

What are some selective Beta-2 AR agonists?

A
  • Metaproterenol
  • Albuterol
  • Terbutaline
  • Bitolerol
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8
Q

Why is inhalation therapy of Beta-2 AR agonists preferred?

A
  • more bronchodilation
  • fewer AE
  • faster onset of action
  • lower doses for effects
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9
Q

What are the advantages of a compressor driven nebulizer?

A
  • consistent dose without coordination needed

- but are expensive and non portable and prone to bacterial contamination

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10
Q

Which B2 AR agonist can be injected subcutaneously?

A

Terbutaline

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11
Q

What is unique about the metabolism of bitolterol?

A

-prodrug that is activated by lung esterases to tertbutylnorepinephrine

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12
Q

Which drug is the standard of inhaled beta-2 agonists for bronchospasm in asthma?

A

albuterol

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13
Q

Which drug is the only beta-2 agonist that can be used by subcutaneous injection for emergency treatment of status asthmatics?

A

Terbutaline

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14
Q

Which drug has the quickest onset of action of ant beta-2 agonist for asthma when inhaled?

A

Metaproterenol

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15
Q

Which drug has a long duration of action (8hr) when inhaled?

A

Bitolterol

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16
Q

Which drug has the longest duration of action of any Beta2 agonist and should be used only for maintenance treatment?

A

Salmeterol

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17
Q

What are the adverse effects of beta-2 agonists?

A
  • Skeletal muscle tremor
  • Anxiety, restlessness, apprehension
  • Tachycardia
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18
Q

Give an example of a Methylxanthine

A
  • Theophylline (oral)

- Amionphylline (IV)

19
Q

What is the MOA of Theophylline?

A
  • Inhibits cAMP Phosphodiesterase, causing buildup of cAMP and Smooth Muscle Relaxation
  • Antagonism of adenosine receptors
  • interference with uptake and storage of Ca by SR in striated muscle, results in increase in cytoplasmic concentration of Ca ions (increase contraction of cardiac and skeletal muscle)
20
Q

What affects the mean half-life of theophylline?

A

cigarette smoking shortens it

21
Q

What is notable about Theophylline’s pharmacokinetics?

A

narrow therapeutic window

22
Q

What are adverse effects of Theophylline?

A
  • Agitation
  • Hyperreflexia
  • Fasiculations
  • Convulsions
  • Tachycardia
  • Arrhythmias
  • Circulatory collapse
  • elevated body temp
  • Urinary retention
23
Q

What is the MOA of Ipratropium bromide?

A

Muscarininc receptor antagonist

  • anticholinergic drug
  • aerosol
24
Q

What is the biochemical effect of Ipratropium bromide?

A
  • inhibits ACh released from airway vagal nerves
  • muscarinic receptor antagonist
  • RESULTS IN
  • decreased concentration of inositol triphosphate
  • decreased release of Ca from ER = relaxation of bronchial smooth muscle
25
Q

What are the clinical uses of Ipratropium bromide?

A
  • combo with beta-2 agonists in severe acute asthma or if primary therapies are not well tolerated
  • with coexisting chronic bronchitis or cough
  • DOC for chornic bronchitis and emphysema
26
Q

What are adverse effects of Ipratropium bromide?

A

-drying in the mouth post inhale

27
Q

How are adrenal corticosteroids used for asthma?

A
  • treats the chronic inflammation
  • decreased inflammation will increase airway diameter
  • reduced frequency and severity of chronic asthma attacks
28
Q

What are examples of corticosteroids used in asthma?

A
  • Beclomethasone (Inhale)
  • Flunisolide (Inhale)
  • Triamcinolone (Inhale)
  • Predinsone (oral)
  • Methylpredinsone (IV)
29
Q

What is the biochemical effect of corticosteroids?

A
  • increased lipomodulin
  • inhibits phospholibpase A2
  • supresses arachidonic acid
  • inhibits release of leukotrienes and prostaglandins
  • reduces leukocyte chemotaxis and smooth muscle contraction and airway mucus secretion
30
Q

What are the therapeutic uses of adrenal corticosteroids in asthma?

A

-first line prophylactic therapy for all cases of asthma

31
Q

What are adverse effects of corticosteroids?

A

Systemic

  • hyperglycemia
  • edema
  • rounding of facial contour
  • osteoporosis
  • cataracts
  • myopathy
  • HPA axis supression
  • psychological depression

Local

  • oropharyngeal candidiasis
  • Dysphonia
  • dryness of mouth and throat
  • coughing
32
Q

What is an example of combination therapy ?

A

Symbicort

  • mixture of glucocorticoid and long acting B-AR agonist
  • Butenoside and Formototerol Fumarate
33
Q

What is the clinical indication for Cromolyn sodium?

A

prevention of asthma attacks

  • used prior to a challenge such as exercise or cold air
  • wil not reverse asthmatic bronchospasm
  • Combination therapy for those who do not respond well to primary lines of treatment
34
Q

What is the mechanism of action of Cromolyn sodium?

A
  • inhibits degranulation of mast cells (prevents release of histamine and other mediators)
  • reduces transmembrane influx of Ca induced by IgE-antigen interaction
  • Inhibits recruitment of neutrophils and eosinophils (inhibits NCF)
  • Attenuates ability of PAF to cause airway hyperractivity
35
Q

What are adverse effects of Cromolyn sodium?

A

-hypersensitivity (rash)

36
Q

What is the mechanism of action of Zileuton?

A

Inhibits synthesis of leukotreines by blocking 5-lipoxygenase
inhibits actions of LTB4

37
Q

What is the mechanism of action of Zariflukast?

A

LT receptor antagonist

-blocks LTD4 action

38
Q

What is the mechanism of action of Montelukast?

A

LT receptor antagonist

-blocks LTD4 action

39
Q

What are the clinical indications of Zariflukast?

A
  • prevent asthmatic attacks in patients over age of 12
  • not a rescue medication
  • reduces the need for rescue medications
  • improves pulmonary function in mild to moderat asthma
  • effective in aspirin induced asthma
  • prevents cold air induced bronchoconstriction
40
Q

What are contraindications of Zariflukast?

A

breast feeding

41
Q

What are drug interactions of Zariflukast?

A

any CYP450 metabolized drug

  • warfarin
  • inhibits CYP450
42
Q

what are the clinical uses of Zileuton?

A
  • prevent exercise, cold air, and aspirin induced asthma

- reduces nocturnal symptoms

43
Q

What are the adverse effects of Zileuton?

A
  • inc. alanine transaminase
  • contraindicated with hepatic disease
  • Dyspepsia
44
Q

What is the mechanism of action of omalizumab?

A
  • monoclonal antibody

- forms a complex with circulating IgE to lower serum concentration levels and prevent IgE from biding to mast cells