17. Respiratory pharmacology Flashcards
what is asthma?
Chronic inflammatory airway disease
intermittent airway obstruction and hyper-reactivity small airways
reversible both spontaneously and with drugs
a heterogeneous disease
What are the 3 cardinal features of asthma?
- Reversible airflow obstruction,
- airway hyperresponsiveness,
- and airway inflammation
aims of asthma control?
- Minimal symptoms during the day and night
- Minimal need for reliever medication
- No exacerbations
- No limitation of physical activity
- Normal lung function (FEV1 and/or PEF >80% predicted or best)
What should you check before stepping up/down?
- Adherence
- Inhaler technique
- Eliminate trigger factors
what are the steps in asthma management?
- low dose ICS + SABA
- add inhaled LABA
- consider increasing ICS to medium dose or adding LTRA, if no response to LABA consider stopping it
- refer to specialist care
Give examples of inhaled corticosteroids?
- beclometasone
- budesonide
- fluticasone
How do ICS work?
Pass through plasma membrane, activate cytoplasmic receptors, activated receptor then passes in to nucleus to modify transcription
What are the effects of ICS?
- Reduces mucosal inflammation, widens airways, reduces mucus
- Reduces symptoms, exacerbations and prevents death
What genes are activated/repressed by ICS?
Activation: ↑β2 receptors, Anti-inflammatory mediators, also inhibit release of arachidonic acid
Repression: Inflammatory mediators: interleukins, chemokines, cytokines
What are the adverse effects of ICS?
• Can cause a local immunosuppressive action - candidiasis, horse voice
warnings, contraindications of ICS?
Pneumonia risk possible in COPD at high doses
DDIs of ICS?
very few if taken correctly
What is the purpose of the lipophilic side chains added to ICS?
slow dissolution in aqueous bronchial fluid - difficult to enter systemic circulation
high affinity for glucocorticoid receptor
Is there an issue of ICS are absorbed orally?
No:
• Poor oral bioavailability
• if absorbed: Transported from stomach to liver by hepatic portal system
• Almost complete first pass metabolism
High doses have potential to cause systemic side effects
Give examples of SABA.
Salbutamol, Terbutaline (both fast acting)