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Pharmacology Yr 2 > Pharmacology of asthma > Flashcards

Pharmacology of asthma Flashcards

1
Q

What drugs are used to treat asthma?

A
  • Salbutamol
  • Fluticasone
  • Mometasone
  • Budesonide
  • Montelukast
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2
Q

What is the target of salbutamol?

A

Beta 2 (β2) adrenergic receptor

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3
Q

What is the primary mechanism of action for salbutamol?

A

Agonist at the β2 receptor on airway smooth muscle cells. Activation reduces Ca2+ entry and this prevents smooth muscle contraction.

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4
Q

What are the main side effects of salbutamol?

A

Palpitations/ agitation

Tachycardia/ Arrythmias

Hypokalaemia (at higher doses)



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5
Q

What type of beta agonist is salbutamol?

A

Short acting (half-life is 2.5 hours)

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6
Q

How does salbutamol cause hypokalaemia?

A

Hypokalaemia can be caused via an effect on sodium/ potassium ATPase. This effect can be exacerbated by coadministration with corticosteroids



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7
Q

What is the drug target of fluticasone?

A

Glucocorticoid receptor

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8
Q

What is the primary mechanism of action of fluticasone?

A

Fluticasone directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce.

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9
Q

What are the main side effects of fluticasone?

A

Local side effects:
Sore throat, hoarse voice, opportunistic oral infections

Systemic side effects:
Growth retardation in children
Hyperglycaemia
Decreased bone mineral density
Immunosuppression
Effects on mood
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10
Q

How is fluticasone administered?

A

Oral bioavailability <1%. Therefore, any systemic delivery via the inhaled route is predominantly through the pulmonary vasculature.

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11
Q

What is the drug target for mometasone?

A

Glucocorticoid receptor

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12
Q

What is the primary mechanism of action of mometasone?

A

Mometasone directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce.

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13
Q

What are the side effects of mometasone?

A

Local side effects:
Sore throat, hoarse voice, opportunistic oral infections


Systemic side effects:
Growth retardation in children
Hyperglycaemia
Decreased bone mineral density
Immunosuppression
Effects on mood



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14
Q

How is mometasone administered?

A

Oral bioavailability <1%. Therefore, any systemic delivery via the inhaled route is predominantly through the pulmonary vasculature

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15
Q

What is the drug target of budesonide?

A

Glucocorticoid receptor

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16
Q

What is the primary mechanism of action for budesonide?

A

Budesonide directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells. It reduces the number of these cells and also the number of cytokines they produce.

17
Q

What are the side effects of budesonide?

A

Local side effects:
Hoarse voice, opportunistic oral infections

Systemic side effects:
Growth retardation in children
Hyperglycaemia
Decreased bone mineral density
Immunosuppression
Effects on mood
18
Q

How is budesonide administered?

A

Oral bioavailability >10%. Therefore, inhaled budesonide will still result in some systemic absorption through the gastro-intestinal tract.
Less potent than fluticasone and mometasone

19
Q

What is the drug target of montelukast?

A

CysLT1 leukotriene receptor

20
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 decreases eosinophil migration, broncho-constriction and inflammation induced oedema

21
Q

What are the side effects of montelukast?

A 
Mild side effects:
Diarrhoea
Fever
Headaches
Nausea or vomiting

Serious side effects:
Mood changes
Anaphylaxis

22
Q

What is the half life of salbutamol?

A

It’s half life is 2.5-5hours.

23
Q

Does salbutamol have absolute selectivity?

A

No
- Cardiac (beta 1) effects can be seen

  • Hypokalaemia can be caused via an effect on sodium/ potassium ATPase. (Can be exacerbated by coadministration with corticosteroids)
24
Q

What is fluticasones affinity for the glucorticoid receptor like compared to cortisol?

A

Greater affinity

Also for mometasone

25
Q

What is the potency of budesonide compared to momentasone and fluticasone?

A

Less potent

26
Q

How can montelukast be used in regards to exercise?

A

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

Pharmacology Yr 2 (9 decks)

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