Pharm - asthma Flashcards
What are the 5 main drugs used for asthma
Salbutamol
FLuticasone
Mometasone
Budesonide
Montelukast
What is the drug target for salbutamol
Beta 2 (β2) adrenergic receptor
What is the drug target for fluticasone
Glucocorticoid receptor
What is the drug target for mometasone
Glucocorticoid receptor
What is the drug target for budesonide
Glucocorticoid receptor
What is the drug target for montelukast
CysLT1 leukotriene receptor
What is the primary mechanism of action for salbutamol
Agonist at the β2 receptor on airway smooth muscle cells. Activation reduces Ca2+ entry and this prevents smooth muscle contraction.
What is the primary mechanism of action for 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 primary mechanism of action for 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 primary mechanism of action for budesonide
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 primary mechanism of action for montelukast
Antagonism of CysLT1 leukotriene receptor on eosinophils, mast cells and airway smooth muscle cells decreases eosinophil migration, broncho-constriction and inflammation induced oedema
What are the side effects of salbutamol
Palpitations/ agitation
Tachycardia/ Arrythmias
Hypokalaemia (at higher doses)
What are the 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 the 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 the side effects of budesonide
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 the side effects of montelukast
Mild side effects:
Diarrhoea
Fever
Headaches
Nausea or vomiting
Serious side effects:
Mood changes
Anaphylaxis
What is the half life of salbutamol
2.5-5hours.
What else may be seen with salbutamol
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.
What happens if we give corticosteroids with salbutamol
Hypokalaemia can be caused via an effect on sodium/ potassium ATPase. This effect can be exacerbated by coadministration with corticosteroids
Extra information 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.
Extra information 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.
Extra information budesonide
Oral bioavailability >10%. Therefore, inhaled budesonide will still result in some systemic absorption through the gastro-intestinal tract.
Less potent than fluticasone and mometasone
Extra information montelukast
For prophylaxis of exercise-induced bronchoconstriction, montelukast should be administered at least 2 hours before initiating exercise.
What is the reliever therapy for children under 5
SABA for symptom relief as well as maintenance therapy
What is the mechanism for Montelukast - why might this be helfpul for NSAID-induced asthma
Montelukast is a leukotriene recpetor antagonist therefore in the lungs and smooth muslce we stop the cells from binding to leukotrienes which stop eosinophils depisiting their contents and causing inflammation
