Asthma

Question 1

Drugs

Answer 1

Salbutamol
Fluticasone
Mometasone
Budesonide
Montelukast

Question 2

Salbutamol action

Answer 2

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

Question 3

Salbutamol target

Answer 3

Beta 2 (β2) adrenergic receptor

Question 4

Salbutamol side effects

Answer 4

Palpitations/ agitation
Tachycardia/ Arrythmias
Hypokalaemia (at higher doses)

Question 5

Salbutamol other

Answer 5

Salbutamol is a short acting beta agonist (SABA). It’s half life is 2.5-5hours.

Beta 2 selectivity is not absolute – as a result, cardiac (beta 1) effects can be seen.
Hypokalaemia can be caused via an effect on sodium/ potassium ATPase. This effect can be exacerbated by coadministration with corticosteroids

In 2020, salbutamol was the 12th most commonly prescribed drug in the West London area

Question 6

Fluticasone action

Answer 6

Very powerful drugs. Multiple actions on many different cell types. 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.

Question 7

Fluticasone target

Answer 7

Glucocorticoid receptor

Question 8

Fluticasone side effects

Answer 8

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
(Many others)

Question 9

Fluticasone other

Answer 9

Greater affinity for the glucocorticoid receptor compared to cortisol.

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

In 2020, fluticasone was the 72nd most commonly prescribed drug in the West London area

Question 10

Mometasone action

Answer 10

Very powerful drugs. Multiple actions on many different cell types. 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.

Question 11

Mometasone target

Answer 11

Glucocorticoid receptor

Question 12

Mometasone side effects

Answer 12

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
(Many others)

Question 13

Mometasone other

Answer 13

Greater affinity for the glucocorticoid receptor compared to cortisol.

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

In 2020, mometasone was the 62nd most commonly prescribed drug in the West London area

Question 14

Budesonide action

Answer 14

Very powerful drugs. Multiple actions on many different cell types. 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.

Question 15

Budesonide target

Answer 15

Glucocorticoid receptor

Question 16

Budesonide side effects

Answer 16

Local side effects:
Hoarse voice, opportunistic oral infections

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

Question 17

Budesonide other

Answer 17

Oral bioavailability >10%. Therefore, inhaled budesonide will still result in some systemic absorption through the gastro-intestinal tract.

Less potent than fluticasone and mometasone

In 2020, budesonide was the 71st most commonly prescribed drug in the West London area

Question 18

Montelukast action

Answer 18

Antagonism of CysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells decreases eosinophil migration, broncho-constriction and inflammation induced oedema

Question 19

Montelukast target

Answer 19

CysLT1 leukotriene receptor

Question 20

Montelukast side effects

Answer 20

Mild side effects:
Diarrhoea
Fever
Headaches
Nausea or vomiting

Serious side effects:
Mood changes
Anaphylaxis

Question 21

Montelukast other

Answer 21

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

In 2020, montelukast was the 95th most commonly prescribed drug in the West London area