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Year 2 - BRS > 1.10 - Pharmacology of asthma (core drugs) > Flashcards

1.10 - Pharmacology of asthma (core drugs) Flashcards

1
Q

What are the five classes of asthma drugs?

A
  • salbutamol (SABA)
  • fluticasone (ICS)
  • mometasone (ICS)
  • budesonide (ICS)
  • montelukast (LTRA)
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2
Q

What is the primary mechanism of action of salbutamol?

A
  • agonist at the beta 2 receptor on airway smooth muscle cells
  • activation reduces Ca2+ entry and this prevents smooth muscle contraction
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3
Q

What is the drug target of salbutamol?

A

Beta 2 adrenergic receptor on airway smooth muscle cells

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4
Q

What are the main side effects of salbutamol? (3)

A
  • palpitations/agitation
  • tachycardia/arrhythmias
  • hypokalaemia (at higher doses)
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5
Q

What is some extra information about salbutamol?

A
  • it is a short acting beta agonist (SABA) with a half life of 2.5-5 hours
  • beta 2 selectivity is not absolute so cardiac (beta 1) effects can be seen
  • hypokalaemia can be caused via an effect on sodium/potassium ATPase which can be exacerbated by also giving corticosteroids
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6
Q

What is the primary mechanism of action of fluticasone?

A
  • very powerful drugs with multiple actions on many different cell types
  • directly decreases inflammatory cells e.g:
    • eosinophils
    • monocytes
    • mast cells
    • macrophages
    • dendritic cells
  • reduces the number of these cells and also the number of cytokines they produce
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7
Q

What is the drug target of fluticasone?

A

Glucocorticoid receptor

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8
Q

What are the local side effects of fluticasone? (3)

A
  • sore throat
  • hoarse voice
  • opportunistic oral infections
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9
Q

What are the systemic side effects of fluticasone? (5 + many more)

A
  • growth retardation in children
  • hyperglycaemia
  • decreased bone mineral density
  • immunosuppression
  • effects on mood
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10
Q

What is some extra information about fluticasone?

A
  • it has greater affinity for the glucocorticoid receptor compared to cortisol
  • oral bioavailability <1% so any systemic delivery via the inhaled route is predominantly through the pulmonary vasculature
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11
Q

What is the primary mechanism of action of mometasone?

A
  • very powerful drugs with multiple actions on many different cell types
  • directly decreases inflammatory cells e.g:
    • eosinophils
    • monocytes
    • mast cells
    • macrophages
    • dendritic cells
  • reduces the number of these cells and also the number of cytokines they produce
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12
Q

What is the drug target of mometasone?

A

Glucocorticoid receptor

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13
Q

What are the local side effects of mometasone? (3)

A
  • sore throat
  • hoarse voice
  • opportunistic oral infections
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14
Q

What are the systemic side effects of mometasone? (5)

A
  • growth retardation in children
  • hyperglycaemia
  • decreased bone mineral density
  • immunosuppression
  • effects on mood
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15
Q

What is some extra information about mometasone?

A
  • greater affinity for the glucocorticoid receptor than cortisol
  • oral bioavailability <1% so systemic delivery via inhaled route is predominantly via pulmonary vasculature
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16
Q

What is the primary mechanism of action of budesonide?

A
  • very powerful drugs with multiple actions on many different cell types
  • directly decreases inflammatory cells e.g:
    • eosinophils
    • monocytes
    • mast cells
    • macrophages
    • dendritic cells
  • reduces the number of these cells and also the number of cytokines they produce
17
Q

What is the drug target of budesonide?

A

Glucocorticoid receptor

18
Q

What are the local side effects of budesonide? (2)

A
  • hoarse voice
  • opportunistic oral infections
19
Q

What are the systemic side effects of budesonide? (5)

A
  • growth retardation in children
  • hyperglycaemia
  • decreased bone mineral density
  • immunosuppression
  • effects on mood
20
Q

What is some extra information about budesonide?

A
  • oral bioavailability >10%, so inhaled budesonide will still result in some systemic absorption through the gastro-intestinal tract
  • less potent than fluticasone and mometasone
21
Q

What is the primary mechanism of action of montelukast?

A
  • antagonism of CysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells
  • this decreases eosinophil migration, bronchoconstriction and inflammation induced oedema
22
Q

What is the drug target for montelukast?

A

CysLT1 leukotriene receptor (on eosinophils, mast cells, airway smooth muscle cells)

23
Q

What are the mild side effects of montelukast? (4)

A
  • diarrhoea
  • fever
  • headaches
  • nausea or vomiting
24
Q

What are the serious side effects of montelukast? (2)

A
  • mood changes
  • anaphylaxis
25
Q

What is some extra information about montelukast?

A

For prophylaxis of exercise-induced bronchoconstriction, montelukast should be administered at least 2 hours before initiating exercise

26
Q

What are the short term and long term therapeutic objectives for a patient with asthma?

A
  • short term = relief (relieve symptoms of breathlessness and expiratory wheeze during the acute asthma attack)
  • long term = prevention (dampen/prevent the late phase of the asthma attack, reduce the risk of further asthma attacks, attempt to improve lung function)
27
Q

Why is the inhalation route preferred over the oral route for salbutamol?

A

Inhalation = local effects, oral = systemic effects
(Inhalation reaches lungs directly and avoids bloodstream, therefore also has lower doses and fewer side effects)

28
Q

Evidence suggests that only 20% of the inhaled dose of salbutamol (or any inhaled drug) penetrates deep enough into the lungs to be able to influence lung function (e.g. reduce breathlessness). What do you think happens to the other 80% of inhaled salbutamol?

A
  • loss 1 - exhaled
  • loss 2 - absorption from lungs (must remain in lung to produce an effect)
  • loss 3 - mucociliary clearance
  • loss 4 - some is swallowed
  • loss 5 - some will be absorbed across the mucous membrane in the oral cavity and pharynx

Year 2 - BRS (84 decks)

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