Pharmacology of Asthma Flashcards
How does salbutamol work?
Agonist at the β2 receptor on airway smooth muscle cells. Activation reduces Ca2+ entry and this prevents smooth muscle contraction.
What is salbutamol’s drug target?
Beta 2 (β2) adrenergic receptor
What are the main side effects of salbutamol?
Palpitations/ agitation, Tachycardia/ Arrythmias, Hypokalaemia (at higher doses)
What are 2 facts about salbutamol?
Salbutamol is a short acting beta agonist (SABA). It’s half life is 2.5-5hours. 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 effect can be exacerbated by coadministration with corticosteroids.
How does fluticasone work?
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 fluticasone’s drug target?
Glucocorticoid receptor
What are 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 (Many others)
What are 2 facts 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.
How does mometasone work?
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 does mometasone act on?
Glucocorticoid receptor
What are 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 (Many others)
What are 2 facts 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.
How does budesonide work?
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 does budesonide act on?
Glucocorticoid receptor
What are the side effects of budesonide?
Local side effects: Hoarse voice, opportunistic oral infections
Systemic side effects: Growth retardation in children, Hyperglycaemia, Decreased bone mineral density, Immunosuppression, Effects on mood (Many others)
