Respiratory Pharmacology Flashcards
What is asthma?
A chronic inflammatory airway disease of intermittent airway obstruction and hyper-reactivity of the small airways
Reversible both spontaneously and with drugs
What should you always check before stepping up or down asthma medications?
- Check adherence
- Check inhaler technique
- Eliminate trigger factors
Describe the stepwise approach to asthma management
How are steroids used in the management of asthma?
Inhaled corticosteroids are a regular preventer when relievers alone are not sufficient
Name 3 inhaled corticosteroids
- Beclometasone
- Budesonide
- Fluticasone
How do inhaled corticosteroids work do manage asthma?
- Pass through plasma membrane to activate cytoplasmic receptors and modify transcription in the nucleus
- Increase B2 receptors and decrease inflammatory mediators
- reduces mucosal inflammation, widens airways, reduces mucus
- reduces symptoms, exacerbations and prevent death
What are some of the side effects of using inhaled corticosteroids?
- Can cause local immunosuppresion → candidiasis, hoarse voice
- Pneumonia risk in COPD
- Very few ADRs if taken correctly
What is the bioavailability of inhaled corticosteroids? How is this modfied to improve this?
- Poor oral bioavailability
-
Lipophilic side chain added which causes:
- slow dissolution in aqueous bronchial fluid
- high affinity for glucocorticoid receptor
What are the 2 types of B2 agonist? When is each used respectively?
SABA (short acting) - for symptoms relief through reversal of bronchocontriction
LABA (long acting)- add on therapy to ICS and SABA
Name 2 fast acting, SABAs
- Salbutamol
- Terbutaline
Give an example of a fast acting LABA
Formoterol
Give an example of a slow acting LABA
Salmeterol (12 hr)
Vilanterol (24 hr)
How do B2 agonists work?
- Bind to GPCR Gs in airways smooth muscle
- alpha s stimulates adenylate cyclase
- increase in cAMP → increases PKA
- Causes airways smooth muscle relaxation and increases mucus clearance by action of cilia
What happens if B2 agonists are used too frequently?
Can build a tolerance - reduces effectiveness of asthma control
What are some of the side effects of B2 agonists?
- Adrenergic effects - tachycardia, palpitations, anxiety and tremor
- Suptraventricular Tachycardia (risk in COPD patients)
- increases HR
- decreases refractory period at AVN
- increases glycogenolysis (liver)
- increases renin (kidney)
- Muscle cramps