drug treatment for asthma Flashcards
What are the two main ways for treatment of asthma?
bronchodilators (relievers)
anti-inflammatory agents (preventers)
What is the main bronchodilator?
β2-adrenoceptor agonists
What is the main anti-inflammatory agent?
glucocorticoids
What are the types of bronchodilators?
β2-adrenoceptor agonists
muscarinic receptor antagonists
What are the anti-inflammatory agents?
glucocorticoids
leukotriene receptor antagonists
antibody to IgE
antibody to interleukin-5
Why are β2-adrenoceptor agonist so useful?
fast acting + effective relievers
relax airway smooth muscle
reverse bronchoconstriction (excitatory mediators)
inhibit mediator release from mast cells
stimulate cilia beat frequency
What is a short acting β2 agonist?
salbutamol
What is an example of a long acting β2 agonist?
formoterol
What is the main problem with β2-adrenoceptor agonists?
can mask inflammatory activity (bronchodilation without reversal of inflammation)
What are some muscarinic antagonists used?
ipratropium
tiotropium
How is glucocorticoids used for asthma therapy?
used prophylactically
used in combination with β2 agonists
administered via inhalation (fluticasone)
administered orally (prednisolone)
What enzyme metabolise arachidonic acid (free)?
phospholipase A2
How does glucocorticoids inhibit pro-inflammatory response?
stimulate lipocortin synthesis = inhibition of phospholipase A2
inhibit cyclooxygenase activity
What occurs when phospholipase A2 is inhibited?
decrease in arachidonic acid
decreases synthesis of leukotrienes and prostaglandins
What happens when cyclooxygenase activity is inhibited?
decrease prostaglandin
decrease influx of inflammatory cells
decrease mediator released from eosinophils
increase β2-adrenoceptors
decrease microvascular permeability
What are some adverse effects of glucocorticoids?
oropharyngeal candidiasis
suppression of hypothalamic-pituitary adrenal axis
osteoporosis
What is ciclesonide?
it is a glucocorticoid prodrug
What is Ciclesonide converted to?
active metabolite M1 in the lung
What is an anti-inflammatory and bronchodilator combination?
glucocorticoid (fluticasone) + long acting β2-agonist (formoterol)
What are leukotriene receptor antagonists?
anti-inflammatory and bronchodilator drugs
How are leukotriene receptor antagonists adminisitered?
orally
Who is leukotriene receptor antagonists useful for?
elderly and young children
What symptom reliefs does leukotriene receptor antagonists provide?
bronchodilation
reduce glucocorticoid dose in adults
Why is antibody to IgE used in asthma therapy?
decrease glucocorticoid required
decrease incidence of asthma exacerbations
decrease hospitalisation
Why is antibodies to interleukin-5 useful?
prevents interleukin-5 from binding to receptors
reduces eosinophil production and survival
reduces eosinophil numbers and mediator release
Why is an example of antibody that binds to interleukin-5?
Reslizumab (Cinqair)
