respi - drugs for asthma Flashcards
1st line bronchodilator in asthma
β2-adrenoceptor agonist
1st line anti-inflam in asthma
corticosteroid
name a SABA
salbutamol
name a fast-acting LABA
formoterol
name a slow-acting LABA
salmeterol
name an ultra-long-acting β2 agonist
indacterol
moa of β2 agonist
- bronchodilation
- mast cell stabilisation
- ↑ mucociliary clearance
- ↓ microvascular leakiness
adverse effect of β2 agonist
- downreg of β2 receptors → reduced efficacy of β2-agonist-induced bronchodilation when required to relieve acute asthma attack
- tremors and muscle cramps
- palpitations and tachycardia
- hypokalaemia/hyperglycaemia
moa of ipratropium bromide
- SAMA
- inhibit M3 receptor-mediated bronchoconstriction
- reverses vagal nerve-mediated bronchospasm and mucus secretion
- adjunct to β2 agonist
adverse effects of ipratropium bromide
- dry mouth
- urinary retention
- unpleasant taste
moa of theophylline
- inhibits phosphodiesterases (PDEs)
- blocks adenosine receptors
- ↑ adrenaline release from adrenal medulla
- stimulate CNS respi centres
- some anti-inflam effects (stabilise mast cells, ↓ microvascular leakiness)
adverse effects of theophylline
- narrow therapeutic window
- many DDIs
- GI: nausea, vomiting, abdominal discomfort, anorexia
- CNS: nervousness, tremors, anxiety, insomnia, seizures
- CVS: arrhythmias
eg of ICS used in asthma
budesonide, fluticasone
factors that determine which ICS is selected for
- high receptor binding affinity –> low dose req (less systemic effects)
- extensive 1st pass metab (less systemic effects)
- highly lipophilic –> can be taken up well into lungs
moa of ICS
- ↑ β2 adrenoceptors
- ↓ airway hyperresponsiveness →↓ freq of acute asthma exacerbations
- prevent airway wall remodelling
- prevent late rxn (nocturnal asthma)
adverse effects of ICS
- oropharyngeal candidiasis
- dysphonia (due to muscle wasting)
- cough/throat irritation
- adrenal suppression
- easy bruising
- posterior subcapsular cataracts
- osteoporosis
name 2 leukotriene pathway inhibitors and their targets
- motelukast (CysLT receptor antagonist)
- zileuton (5-LOX inhibitor)
advantage of montelukast over zileuton
montelukast is a weak bronchodilator (on top of anti-inflam effects)
uses of leukotriene pathway inhibitors
- prophylaxis and chronic treatment of asthma
- NSAID exacerbated asthma
- exercise-induced asthma
adverse effects of leukotriene pathway inhibitors
- Churg-Straus syndrome
- glucocorticoid withdrawal
- suicidal thinking and neuropsychiatric adverse effects
moa of cromoglicic acid
- mast cell stabiliser →↓ mast cell degranulation
- ↓ secretion of inflam mediators
- ↑ secretion of annexin A1→ inhibit prostaglandin and leukotriene prodn
- prevents antigen, cold, dry air and exercise-induced bronchospasm
adverse effect of cromoglicic acid
- throat and nasal irritation, dry mouth, cough
- unpleasant/bitter taste → affect compliance
moa of omalizumab
- anti-IgE Ab
- depletes free IgE in serum
- decreases FcεRI expression on mast cells
adverse effects of omalizumab
- small increase in risk of heart attack, TIA and blood clots
- potential for anaphylaxis
name 2 anti-IL5 signalling Ab
- reslizumab (IV)
- mepolizumab (SC)