asthma Flashcards

1
Q

What is the drug target of salbutamol?

A

Beta 2 adrenergic receptor on airway smooth muscle cells

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2
Q

What is the primary mechanism of action of salbutamol?

A
  • Agonist at beta 2 receptor on airway smooth muscle cells
  • Activation reduces Ca2+ entry preventing smooth muscle contraction
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3
Q

What are the main side effects of salbutamol?

A
  • Palpitations/agitation
  • Tachycardia/arrythmias
  • Hypokalaemia (at higher doses)
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4
Q

Explain the selectivity for beta 2 from salbutamol

A

Beta 2 selectivity is not absolute so cardiac (beta 1) effects can be seen

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5
Q

What’s the half-life of salbutamol like?

A

It’s a short acting beta agonist (SABA) with a half life of 2.5-5 hours

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6
Q

What side effect can be seen via effect on Na+/K+ ATPase?

A

Hypokalaemia; can be exacerbated by also giving corticosteroids

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7
Q

What is the primary mechanism of action of fluticasone?

A
  • V powerful drugs that do loads
  • Directly decreases inflammatory cells:
    • Eosinophils
    • Monocytes/macrophages
    • Mast cells
    • Dendritic cells
  • Also reduces number of these cells and the cytokines they produce
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8
Q

What is the drug target of fluticasone?

A

Glucocorticoid receptor

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9
Q

What are the main local side effects of fluticasone?

A
  • Sore throat
  • Hoarse voice
  • Opportunistic oral infections
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10
Q

What are the main systemic side effects of fluticasone?

A

Loads more than this

  • Growth retardation in children
  • Hyperglycaemia
  • Decreased bone mineral density
  • Immunosuppression
  • Effects on mood
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11
Q

Compare fluticasone to cortisol in terms of glucocorticoid receptor affinity

A

It has a greater affinity for glucocorticoid receptor than cortisol

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12
Q

What is the oral bioavailability of fluticasone?

A

Oral bioavailability <1% so any systemic delivery via inhaled route is done through pulmonary vasculature

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13
Q

What is the primary mechanism of action of mometasone?

A
  • V powerful drugs that do loads
  • Directly decreases inflammatory cells:
    • Eosinophils
    • Monocytes/macrophages
    • Mast cells
    • Dendritic cells
  • Also reduces number of cytokines they produce
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14
Q

What is the drug target of mometasone?

A

Glucocorticoid receptor

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15
Q

What are the main local side effects of mometasone?

A
  • Sore throat
  • Hoarse voice
  • Opportunistic oral infections
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16
Q

What are the main systemic side effects of mometasone?

A

Loads more than this

  • Growth retardation in children
  • Hyperglycaemia
  • Decreased bone mineral density
  • Immunosuppression
  • Effects on mood
17
Q

Compare mometasone’s affinity for glucocorticoid receptor to cortisol

A

Greater affinity than cortisol

18
Q

What’s the oral bioavailability of mometasone like?

A

Oral bioavailability <1% so any systemic delivery via inhaled route is done through pulmonary vasculature

19
Q

What is budesonide primary mechanism of action?

A
  • V powerful drugs that do loads
  • Directly decreases inflammatory cells:
    • Eosinophils
    • Monocytes/ macrophages
    • Mast cells
    • Dendritic cells
  • Also reduces number of cytokines they produce
20
Q

What is the drug target of budesonide?

A

Glucocorticoid receptor

21
Q

What are the main local side effects of budesonide?

A
  • Hoarse voice
  • Opportunistic oral infections
22
Q

What are the main systemic side effects of budesonide?

A

Loads more than this

  • Growth retardation in children
  • Hyperglycaemia
  • Decreased bone mineral density
  • Immunosuppression
  • Effects on mood
23
Q

Compare the potency of budesonide to fluticasone and mometasone

A

Less potent than fluticasone and mometasone

24
Q

What’s the oral bioavailability of budesonide like?

A

Oral bioavailability 10% so inhaled budesonide will still result in some systemic absorption through GI tract

25
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
26
Q

What is the drug target of montelukast?

A

CysLT1 leukotriene receptor

27
Q

What are the main mild side effects of montelukast?

A
  • Diarrhoea
  • Fever
  • Headaches
  • Nausea or vomiting
28
Q

What are the serious side effects of montelukast?

A
  • Mood changes
  • Anaphylaxis
29
Q

How long before exercise should montelukast be administered?

A

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