Pharmacology - COPD Flashcards
describe the physio-pathological pathway of COPD
smoking
stimulation of resident alveolar macrophages
cytokine production
activation of neutrophils, CD8+ Tcells, increased macrophage numbers
release of matrix metalloproteinases
what 2 diseases was COPD historically split into?
chronic bronchitis
Emphysema
d: COPD
chronic obstructive pulmonary disease characterised by increased resistance to air flow during expiration
what needs to be blocked in order to prevent contraction of airway smooth muscle?
M3 receptors
where are M1 receptors found and function?
ganglia
facilitate fast neurotransmission mediated by ACh acting on nicotinic receptors (nAChR)
where are M2 receptors found and function?
postganglionic neurone terminals
act as inhibitory autoreceptors reducing release of ACh
where are M3 receptors found and function?
airway smooth muscle
mediate contraction to ACh (also present on mucus-secreting cells evoking increased secretion)
name the SAMA muscarinic receptor antagonists currently used?
ipratropium
name the LAMA muscarinic receptor antagonists currently used?
Tiotropium
Glycopyrronium
Aclidinium
Umeclidinium
what way are SAMAs and LAMAs administered?
inhalation
How do SAMAs work?(mechanism)
Reduce bronchospasm caused by irritant stimuli and also block ACh-mediated basal tone
Decrease mucus secretion
Have little effect on the progression of COPD, their effect is mainly palliative
Have few adverse effects
vago-vagal reflex
is ipratropium non-selective/selective against Ms?
non selective
Why are M3 selective blockers superior to Ipratropium?
Block of M3 (and M1) is desirable, but block of M2 is not because release of ACh from parasympathetic post-ganglionic neurones is increased by autoreceptor antagonism
name a PDE4 inhibitor which surpresses inflammation and emphysema
rofumilast
name 2 ultra LABAs
indacaterol
olodaterol
