Pharmacology of Asthma Flashcards
What are the 5 main asthma drugs?
- Salbutamol
- Fluticasone
- Mometasone
- Budesonide
- Montelukast
What is the primary mechanism of action of salbutamol?
Agonist at the β2 receptor on airway smooth muscle cells
Activation reduces Ca2+ entry and this prevents smooth muscle contraction
What is the drug target site for salbutamol?
Beta 2 (β2) adrenergic receptor
What are the main side effects of salbutamol?
Palpitations/ agitation
Tachycardia/ Arrythmias
Hypokalaemia (at higher doses)
What is some extra information about salbutamol?
Salbutamol is a short acting beta agonist (SABA)
It’s half life is 2.5 - 5hrs
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 can be exacerbated by coadministration with corticosteroids
What is the primary mechanism of action of fluticasone?
Very powerful drugs - multiple actions on many different cell types
Fluticasone directly reduces the number of inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells = reduces the number of cytokines they produce
What is the drug target site for fluticasone?
Glucocorticoid receptor
What are the main side effects of fluticasone?
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
What is some extra information about fluticasone?
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.
What is the primary mechanism of action of mometasone?
Very powerful drugs - multiple actions on many different cell types
Mometasone directly reduces the number of inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells = reduces the number of cytokines they produce
What is the drug target site for mometasone?
Glucocorticoid receptor
What are the main side effects of mometasone?
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
What is some extra information about mometasone?
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.
What is the primary mechanism of action of budesonide?
Very powerful drugs - multiple actions on many different cell types
Budesonide directly reduces the number of inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells = reduces the number of cytokines they produce
What is the drug target site for budesonide?
Glucocorticoid receptor