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pharmacology and therapeutics > pharmacology of asthma > Flashcards

pharmacology of asthma Flashcards

1
Q

primary mechanism of action of salbutamol

A

agonist at b2 receptor on airway smooth muscle cells. activation reduces ca2+ entry preventing smooth muscle contractions

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2
Q

what is the target of salbutamol

A

beta 2 adrenergic receptor

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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

extra info on salbutamol

A

= short acting beta agonist
half like is 2.5-5 hrs
beta 2 selectivity is not absolute - cardiac (beta1) effects cen be seen

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5
Q

how is hypokalaemia a side effect of high dose salbutamol

A

caused via effect on sodium/potassium atpase. effect can be exacerbated by coadministration with corticosteroids

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6
Q

mechanism of fluticasone

A

very powerful drug!
multiple actions on multiple cells
directly decreases inflammatory cells e.g eosinophils, monocytes, macrophages and dendritic cells. reduces the number of these cells and number of cytokines they produce

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7
Q

target of fluticasone

A

glucocorticoid receptors

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8
Q

what are the local side effects of fluticasone

A

sore throat, hoarse voice, opportunistic oral infections

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9
Q

what are the systemic side effects of fluticasone

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

extra info on fluticasone

A

greater affinity for glucocorticoid receptor compared to cortisol
oral bioavailability <1%, therefore any systemic delivery via inhaled route is predominantly through pulmonary vasculature

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11
Q

what is mechanism of action of mometasone

A

very powerful drugs!
multiple actions on many different cells
directly decreases inflammatory cells e.g eosinophils, monocytes, mast cells, macrophages and dendritic cells. reduces number of these cells and number of cytokines they produce

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12
Q

what is the target of mometasone

A

glucocorticoid receptor

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13
Q

local side effects of mometasone

A

sore throat, hoarse voice, opportunistic oral infections

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14
Q

systemic side effects of mometasone

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

what is mechanism of action of budesonide

A

very powerful drug!
multiple action on different cell types. directly decreases inflammatory cells e.g eosinophils, monocytes, mast cells, macrophages and dendritic cells. reduces number of cells and also number of cytokines they produce

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16
Q

target of budesonide

A

glucocorticoid receptor

17
Q

local side effects of budesonide

A

hoarse voice

opportunistic oral infections

18
Q

systemic side effects of budesonide

A 
growth retardation in children
hyperglycaemia
decreased bone mineral density
immunosuppression
effects on mood
many others
19
Q

extra info on budesonide

A

oral bioavailability >10%
therefore inhaled budesonide will still result in some systemic absorption through gi tract
less potent than fluticasone and mometasone

20
Q

mechanism of action of montelukast

A

antagonism of cysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells.
decreases eosinophil migration, bronchoconstriction and inflammation induced oedema

21
Q

target of montelukast

A

cysLT1 leukotriene receptor

22
Q

mild side effects of montelukast

A

diarrhoea
fever
headaches
nausea/vomiting

23
Q

serious side effects of montelukast

A

mood changes

anaphylaxis

24
Q

extra info on montelukast regarding prophylaxis of exercise induced bronchoconstriction

A

should be administered at least 2 hrs before initiating exercise

25
Q

bnf guidelines for salbutamol use in children

A

by inhalation:
child - 100-200micrograms, upto 4 times a day for persistent symptoms
by mouth:
for child 1 month-1yr - 100 micrograms/kg 3-4 times a day
2-5yrs - 1-2mg 3-4 times a day

26
Q

what % of the inhaled dose of salbutamol penetrates deep enough into lungs to be able to influence lung function

A

20%

pharmacology and therapeutics (9 decks)

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