respiratory pharmacology Flashcards
What do the post ganglionic fibres supply (sympathetic division) (2)
Sub mucosal glands
Smooth muscle of blood vessels
Where are parasympathetic preganglionic fibres found
brainstem
Where are cell bodies of parasympathetic post ganglionic fibres found
walls of the bronchi and bronchioles
What does stimulation of post ganglionic cholinergic fibres cause (2)
bronchial smooth muscle fibre contraction
Increased mucus secretion
What does stimulation of post ganglionic non-cholinergic fibres cause
bronchial smooth muscle relaxation
What does smooth muscle contraction result from
phosphorylation of regulatory music light chains in the presence of elevated intracellular calcium ions
What is required for smooth muscle relaxation
return of intracellular calcium ion concentration to a basal level
What are example of reliever medications (4)
short acting beta2 adrenoceptor agonists
Long acting beta2 adrenoceptor agonists
CystLTI receptor antagonists
Methylxanthines
What are examples of controller/prevent or medications (4)
glucocorticoids
Cromoglicate
Humanised monoclonal IgE antibodies
Methylxanthines
What are beta2 adrenoceptor agonists
physiological antagonists of all spasmogens
Salbutamol
shorting acting beta2 adrenoceptor agonists
Sale troll and formoterol
long acting beta2 adrenoceptor agonists
Montelukast and zafirlukast
CysLTI antagonists
Theophylline
Methylxanthine, combines bronchodilator and anti-inflammatory actions
Effects of methylxanthines (4)
inhibit mediator release from mast cells
Increase mucus clearance
Increase diaphragmatic contractility
Reduce fatigue
Describe glucocorticoids (3)
suppress inflammation
Do not alleviate early stage bronchospasm
Long term treatment
Which type of drug is effective against early bronchospasm
cysLTIs, in combination with other drugs
Effects of glucocorticoids (5)
decrease formation of TH2 cytokines
Apoptosis
Preventing immunoglobulin production
Prevent allergen-induced influx into lungs
Reduce number of mast cells
Describe cromones (4)
second-line drugs
Infrequently used
Prophylaxis of allergic asthma
No direct effect on bronchial smooth muscle
Where are M1 receptors found
Ganglia
Where are M2 receptors found
post-ganglionic neurone terminals
Where are M3 receptors found
airway smooth muscle
Action of M3 receptors
mediate contraction to ACh
Evoke increased secretion
Muscarinic receptor antagonists (4)
Antagonists of bronchoconstriction
Reduce bronchospasm
Block ACh mediated basal tone
Decrease mucus secretion
Ipratropium
short acting muscarinic antagonist
Triotropium and glycopyrronium
long acting muscarinic antagonists
Which medication is a non-selective blocker
Ipratropium
How are adverse effects of generalised parasympathetic blockage avoided
The quaternary ammonium group reduces systemic absorption and systemic exposure
What drugs are effective as a combination treatment for COPD and why
LABA and LAMA as they work by complementary mechanisms to cause smooth muscle relaxation
When is the LAMA/LABA combination likely to be most effective
When both drugs are deposited in the same location in the airways
What other drugs maybe be used in treatment of COPD (2)
glucocorticoids
PDE4 inhibitors
By what methods can drugs be transported across the nasal epithelium (4)
Transcellular diffusion
Paracellular diffusion
Carrier mediated transported
Vesicle mediate transport
What factors affect drug absorption in the respiratory tract (4)
physical barrier of the epithelium
Degradation by proteases
Particle clearance
Macrophage action
What are the targets of treatment for rhinitis (4)
Anti-inflammatory
Mediator-receptor blockade
Nasal blood flow
Anti-allergic
what drugs are used in the anti-inflammatory component of rhinitis treatment + what are the effects (3)
Glucocorticoids
Reduced vascular permeability
Reduced inflammatory cell recruitment and activation
Reduced cytokine and mediator release
How are glucocorticoids administered in treatment of rhinitis
intranasal spray - sometimes orally
What drugs are used in the mediator receptor blockade component of rhinitis treatment (3)
anti-histamines
Muscarinic receptor antagonists
CysLTi receptor antagonists
What does H1 receptor antagonists do
Reduce effects of mast cell derived histamine
In what types of allergic rhinitis are H1 receptor antagonists effective against
Perennial
Seasonal
Episodic
What symptom are H1 receptor antagonists not effective at reducing
congestion
What methods of administration are used for H1 receptor antagonists
oral
Intranasal
What are examples of H1 receptor antagonists
Loratidine
Fexodenadine
Certrizine
Describe anticholinergic drug action
Block acetylcholine receptors
What symptom do anti-cholinergic drugs effect
Only rhinorrhoea
How are anti-cholinergic drugs administered + what is an adverse effect
intranasal
Dryness of the nasal membrane
Describe the action of cystLTis
Reduce effects of cysLTs on nasal mucosa
What types of asthma can cysLTIs treat
Perennial and seasonal
How are cysLT inhibitors administered
orally
What is an example of a cysLT inhibitor
Montelukast
What medication is used to target nasal blood flow in treatment of rhinitis
Vasoconstrictors
describe action vasoconstrictors (3)
Mimic effect of noradrenaline
Cause vasoconstriction via activation of beta1 adrenoceptors
This decreases swelling in the vascular mucosa
What is an example of a vasoconstrictor used in treatment of rhinitis
Oxymetazoline
Why is long term use of vasoconstrictors not recommended
there can be a rebound increase in nasal congestion upon continuation due to desensitisation and down regulation
What medication can be used for anti-allergic component of rhinitis treatment
sodium chromoglicate