Drugs for Asthma Flashcards
salbutamol is use as a controller (true/false)
false, it is a reliever
list the a/e of mast cell stabilizer
- unpleasant taste
- cough
- nasal/throat irritation
- dry mouth
which class of bronchodilator is first line treatment of asthma
b2 agonist
briefly explain the MOA of anti-IgE monoclonal antibody
- deplete level of free IgE in serum
- decrease expression of FcεRI on mast cell (basophils)
what is the route & frequency of reslizumab
IV q4 weeks
list 1 drug example of mast cell stabiliser + explain the MOA
- cromogrilic acid
- decrease mast cell degranulation induced by IgE mediated FcεRI crosslinking
- decrease inflammatory mediators secretion by eosinophils, neutrophils & macrophages
- control cl- channel to inhibit cellular activation
- increase annexin a1 secretion to inhibit PG & leukotrine production
what is the MOA of muscarinic receptor antagonist
- inhibit m3 receptors, reducing bronchoconstriction
- reverse vagal nerve, reducing bronchospasm & mucus secretion
for patient with aspirin induced asthma, which pharmacological class should be prescribed to him?
a) leukotriene pathway inhibitors
b) muscarinic receptor antagonist
3) mast cell stabiliser
4) anti-igE monoclonal antibodies
leukotriene pathway inhibitor eg. montelukast
what are some limitations of anti-IgE monoclonal antibody
- expensive
- small risk of MI, TIA, blood clots
- potential for anaphylaxis
which interleukin is contributed to eosinophilic asthma?
IL4, IL13, IL5
why is leukotriene pathway inhibitors helpful in NSAIDS exacerbated respiratory disease
A) NSAIDS activate endogenous cortisol release to trigger Cushing’s syndrome
B) antagonist at cysteinyl leukotriene receptors suppress prostaglandin synthesis
C) inhibition of COX leads to arachidonic acid overflow to the 5-LOX pathway
C
what is the route & frequency of anti-IgE monoclonal antibody
SC q2-4 weeks
what is the 3 criteria for selection of ICS
- high receptor binding affinity (very low dose required)
- extensive first pass metabolism (lesser systemic a/e)
- highly lipophilicity (easier absorption)
what is the 3 type of asthma, which is the most common?
- allergic asthma (more common) - type 1 inflammation IgE mediated
- eosinophilic asthma - type 2 inflammation cell mediated
- mix asthma
what is the route for mast cell stabilizer (eg. cromogrilic acid) administration
inhalation & intranasal
what is a soft steroid? + give 1 drug example
A) it can be administered oral to produce few side effects
B) it can cause adrenal suppression
C) it require esterase activation and so has less side effect
ciclesonide
C) soft steroid is a pro drug that require esterase activation in the lung, therefore bypassing systemic a/e
what are the a/e of b2 agonist, which is the most common & severe
- tremors (common) & muscle cramp
- palpitation & tachycardia
- hypokalaemia & hyperglycaemia
- flushing (peripheral vasodilation)
- b2 adrenoceptor downregulation (if LABA is use alone, it increase the risk of asthma related death)
pt read online that a single drug, omalizumab, can be use to control allergic asthma. is omalizumab suitable?
A) no, it only works for eosinophilic asthma
B) yes, it can effectively control allergic asthma injected every 2-4 weeks subq
C) no, it increase the risk of TIA
D) yes, but pt require to learn to self-administer daily injections
C
- using omalizumab alone is not very effective
- risk of MI, TIA & blood clots
- potential for anaphylaxis
which of the following is belongs to the muscarinic receptor antagonist class
1. budesonide
2. cetirizine
3. ipratropium bromide
4. promethazine
ipratropium bromide (SAMA)
what are the administration route for magnesium sulphate
- IV
- nebulizer (efficacy is controversial)
what is the route of theophylline
- oral-ER
- IV
list some examples that trigger allergic asthma
- cold air
- dust mites
- pets
- smoke
- exercise
- pollen
what is the 3 symptoms of asthma
- cough
- wheezing
- SOB
what is the MOA of ICS
- does not directly relax airway smooth muscle
- possible prevention of airway wall remodelling
- decrease risk of asthma death
- decrease airway hyper-responsiveness in 4-6wks
- decrease freq of asthma exacerbation
- decrease need for b2 agonist
what does muscarinic antagonist block
acetylcholine to induce bronchodilation
what is the role of PDE
it convert cAMP to AMP, by inhibiting PDE, it increase cAMP, resulting in increase bronchodilation
what is the onset & duration of action for formoterol
onset 2-3min
duration 12hrs
what are the efficacy of cromogrilic acid
- single dose therapy before antigen-challenge, cold/dry air, or exercised to prevent bronchospasm
- reduce bronchial hyper-reactivity in 4 weeks
- inter-individual variability
what is the 2 other use of montelukast
as drug have a weak bronchodilator effect, it can be use
- as an adjunct therapy for mild-moderate asthma
- not to use alone as a reliever to rescue asthma attack
what is the 2 use of ICS
- first line prophylactic treatment of asthma
- prevention of nocturnal asthma
which of the following is not a steroid but can be an effective anti-inflammatory for mild asthma?
A) zileuton
B) fluticasone
C) theophylline
D) montelukast
A & D
leukotriene pathway inhibitors is an anti-inflammatory drug that can be use to treat mild-moderate asthma
formoterol have a slow onset and long duration of action (true/false)
false, formoterol (LABA) have a fast onset of 2-3min, with duration of 12hrs
what are the use & efficacy of muscarinic receptor antagonist
- adjunct therapy for b2 agonist & ICS
- for patient intolerant to b2 agonist
salmeterol is use as a controller (true/false)
true
long term therapy of fluticasone helps to improve adrenal function (true/false)
false, long term therapy of fluticasone can lead to adrenal suppression
can ICS be given during an acute asthma attack
yes (through IV), however must be given early as onset of action is slow
list 2 drug example of leukotriene pathway inhibitor
- montelukast (cysLT receptor antagonist)
- zileuton (5LOX inhibitor)
patient present w recurrent episodes of bruising & throat infection, which of the following drugs could cause these a/e
1. zileuton
2. budesonide
3. formoterol
4. ipratropium bromide
budesonide (ICS)
list one drug example of an anti-IgE monoclonal antibody, which pt is indicated?
drug: omalizumab
indication: pt w severe allergic asthma & elevated IgE level
what are the a/e of ICS
- cataract
- easy bruising
- oropharyngeal candidiasis
- muscle wasted (enfeebled voice; dysphonia, thin arms/legs)
- osteoporosis
- buffalo hump
- increase abdominal fats
what are the a/e of methylxanthine
CNS eg. tremors, insomnia, seizure
GI disturbance eg. diarrhoea, anorexia, nausea/vomiting
CVS: arrhythmia
why does ICS have rare systemic a/e
drug is taken through inhalation, which has limited absorption in the systemic circulation, hence less systemic a/e
pt complain of urinary retention, which of the drug is responsible for the a/e
A) montelukast
B) ipratropium bromide
C) formoterol
D) budesonide
B
- a/e of ipratropium includes unpleasant taste, dry mouth & urinary retention
can methylxanthine be use as an anti-inflammatory drug?
no, even though it have some anti-inflammatory effect on mast cell & T cells, & decrease micovascular leakiness
patient on methylxanthine (eg. theophylline) asked if he is able to drink coffee, what will be your health education
advice patient to avoid coffee, tea or chocolate as it increase the risk of drug toxicity due to the narrow therapeutic window of methylxanthine (eg. theophylline)
what is the use for mast cell stabilizer drug
- prophylactic control of asthma (inhalation route only)
- prophylactic control of allergic rhinitis & allergic conjunctivitis
which interleukin is contributed to allergic asthma?
IL4 & IL13
what is the administration route for anti-IL4/IL5 signalling monoclonal antibodies
intravenous
pt forgot where he put his SABA reliever inhaler and so uses his LABA controller instead, will LABA controller help?
A) no, onset of action of LABA is too slow
B) no, LABA are not bronchodilators, they are use to control ongoing inflammatory disease
C) yes, prescription of a SABA is not necessary if the pt has a LABA
D) yes, but only if the LABA is a formeterol
D
- formoterol have a fast onset of 2-3min and last for 12hrs
what is the indication & MOA of magnesium sulphate
indication: adjunct therapy for severe acute asthma
MOA:
- relax airway smooth muscle
- modulate release of histamine & acetylcholine
- has anti-inflammatory effect
list 2 drug from muscarinic receptor antagonist, what is the onset & duration of action for each?
- ipratropium bromide (SAMA, 5-30min onset, 6-8hrs duration)
- tiotropium bromide (LAMA, 30min onset, 24hrs duration)
explain why LABA should not be given alone to treat asthma
long term therapy of LABA can cause the downregulation of b2 adrenoceptor & increase the risk of asthma related death, it should be combined with ICS to counter the effect
list 3 drug example of ICS
- budesonide
- fluticasone
- ciclesonide
what is an additional advantage of montelukast but not zileuton
A) montelukast has fewer a/e
B) montelukast is a bronchodilator (although a weak one)
C) montelukast is more effective in NSAID exacerbated respiratory disease
B
- it is one third as effective as salbutamol
what is the MOA of b2 agonist
it mimic the action endogenous adrenaline at b2 adrenoceptors site, resulting in
- airway smooth muscle relaxation (bronchodilation)
- mast cell stabilisation
- decrease microvascular leakiness
- increase mucociliary clearance
give 1 drug example from the pharmacological class of methylxanthine, what is the MOA of it?
- theophylline
- inhibit PDE
- block adenosine receptor
- increase release of adrenaline from adrenal medulla
- CNS stimulant action on respiration
what are the 3 indication of leukotriene pathway inhibitor
- prophylaxis/chronic treatment of asthma
- nsaids/aspirin induced asthma
- exercised induced asthma
what are some limitations & a/e of an anti-IL4/IL5 signalling monoclonal antibodies drug
limitations: expensive, potential for anaphylaxis
a/e: oropharyngeal pain
montelukast have a strong bronchodilator effect (true/false)
false, it have a weak bronchodilator effect and therefore should not be given alone to rescue asthma attack
it is 1/3 as effective as salbutamol
claus-straug syndrome is associated to which class of drug? how to avoid it?
leukotriene pathway inhibitor
titrate the dosage of ICS slowly before discontinuing
give 1 drug example of anti-IL4/IL5 signalling monoclonal antibodies, and which patient is indicated
drug: reslizumab
indication: severe & persistent eosinophilic asthma in pt ≥18 y/o
list 3 a/e of muscarinic receptor antagonist
limited systemic a/e as drug is taken via inhalation
1. unpleasant taste
2. dry mouth
3. urinary retention (esp in elderly)
what are the use & efficacy of methylxanthine
- IV administration for severe acute asthma
- less effective bronchodilator than b2 agonist
