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 of salbutamol?
Beta 2 (β2) adrenergic receptor
What are the main side effects of salbutamol?
- Palpitations/ agitation
- Tachycardia/ Arrythmias
- Hypokalaemia (at higher doses)
How long action is salbutamol?
a short acting beta agonist (SABA). It’s half life is 2.5-5hours
What is the selectivity of salbutamol to Beta 2 like?
Beta 2 selectivity is not absolute – as a result, cardiac (beta 1) effects can be seen
How commonly prescribed are these drugs in the West London area in 2020?
- Salbutamol: 12th
- Fluticasone: 72nd
- Mometasone: 62nd
- Budesonide: 71st
- Montelukast: 95th
How can hypokalaemia happen with salbutamol?
- caused via an effect on sodium/ potassium ATPase
- effect 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 decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells
- It reduces the number of these cells and also the number of cytokines they produce
What is the drug target of fluticasone?
Glucocorticoid receptor
What are the local side effects of fluticasone?
- Sore throat
- hoarse voice
- opportunistic oral infections
What are the systemic side effects of fluticasone?
- Growth retardation in children
- Hyperglycaemia
- Decreased bone mineral density
- Immunosuppression
- Effects on mood
(Many others)
What receptor does fluticasone have a greater affinity for?
Greater affinity for the glucocorticoid receptor compared to cortisol.
What is the oral bioavailability of fluticasone like?
- Oral bioavailability <1%
- Therefore, any systemic delivery via the inhaled route is predominantly through the pulmonary vasculature
What the primary mechanism of action mometasone?
- Very powerful drugs
- Multiple actions on many different cell types
- Mometasone directly decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells
- It reduces the number of these cells and also the number of cytokines they produce.
What is the drug target of mometasone?
Glucocorticoid receptor
What are the local side effects of mometasone?
- Sore throat
- hoarse voice
- opportunistic oral infections
What are the systemic side effects of mometasone?
- Growth retardation in children
- Hyperglycaemia
- Decreased bone mineral density
- Immunosuppression
- Effects on mood
(Many others)
What receptor does mometasone have a greater affinity for?
Greater affinity for the glucocorticoid receptor compared to cortisol
What is the oral bioavailability of mometasone like?
- 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 decreases inflammatory cells such as eosinophils, monocytes, mast cells, macrophages, and dendritic cells
- It reduces the number of these cells and also the number of cytokines they produce
What is the drug target of budesonide?
Glucocorticoid receptor
What are the local side effects of budesonide?
- Hoarse voice
2. opportunistic oral infections
What are the systemic side effects of budesonide?
- Growth retardation in children
- Hyperglycaemia
- Decreased bone mineral density
- Immunosuppression
- Effects on mood
(Many others)
What is the oral bioavailability of budesonide like?
- Oral bioavailability >10%
2. Therefore, inhaled budesonide will still result in some systemic absorption through the gastro-intestinal tract
