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18 Cards in this Set
- Front
- Back
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•List the transmitters utilised and the receptors activated at the various locationsof the autonomic nervous system•State the major classes of drugs used in the management of respiratory disease and describe their pharmacological mechanism of action§β-agonists§Anticholinergics(muscarinic receptor antagonists)§Methylxanthines§Corticosteroids§Leukotriene receptor antagonists•Discusstheir major adverse effects•Discussdifferent routes of administration and the main advantages and disadvantages ofeach |
Pre-synaptic ganglia - cholinergic Receptor: Nicotinic Neurotransmitter: Acetylcholine Post-synaptic ganglia SNS - Adrenergic axon to adrenoceptor Neurotransmitter: Noradrenaline Post-synaptic ganglia PSNS - cholinergic axon muscarinic receptor neurotransmitter: acetylcholine |
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Receptors and their locations beta1, beta2, beta3 |
beta1: heart, increased HR & force GI smooth muscle - relaxation beta2 : bronchi - relaxation beta3: adipose tissue - lipolysis |
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•State the major classes of drugs used in the management of respiratory disease and describe their pharmacological mechanism of action §β-agonists (Sympathetic NS) |
Mechanism: beta2-adrenoceptors G protein (Gs) - AC - ATP-cAMP --> PKA --> phosphorylation of MLCK (Myosin light chain kinase) - 1. Relaxation of smooth muscle BRONCHODILATION 2. Stabilise mast cells & inhibit mediator release 3. Enhanced mucociliary clearance and decrease vas. perm. |
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Examples/side effects/other info |
Examples - short acting salbutamol, terbutaline Long acting: salmeterol, formoterolSide effects: tremor, hypokalaemia, tachycardia, paradoxical hypoxaemia *Tolerance - down regulation with prolonged use |
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Muscarinic receptor antagonists (parasympathetic NS) |
Bronchodilator Inhibition of normal G protein mech Mech: G protein (Gq) GDP-GTP PIP2 converted to IP3 via PLC to produce IP3 (2nd mes. in signal transduction - stimulates Ca2+ release) and DAG (activates PKC for bronchial smooth muscle contraction) |
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Examples/side effects/other info |
Examples: Fast acting: ipratropium, oxitroprium Long acting: tiotroprium, glycopyrronium Side effects: blurred vision, dry mouth, paradoxical bronchoconstriction, urinary retention ** in Glaucoma (pressure build up in eye) patients - suppresses contraction, reduces drainage **Prostatic hypertrophy - difficult to squeeze urethra |
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Adenosine receptor antagonism Methylxanthines - mech of action |
cAMP --> AMP stimulated by PDE phosphodiesterase
Methylxanthines block enzyme therefore more cAMP available to produce PKA so more MLCK Pi that causes bronchodilation |
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Examples/side effects/other info |
IV infusion for acute M - aminophylline Oral for chronic management - aminophylline, theophylline Side effects: Hypoalkaemia (low K+ in blood) Tachycardia CNS stimulation - imsomnia (take in morning) GI disturbances **Not used in first line therapy. Narrowtherapeutic window Monitoring - Toxicityprofile Metabolisedvia CP450 Interactions |
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Picture of theophylline effects |
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Summary of bronchodilation drugs (picture) |
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Anti-inflammatory mediators (2 drugs) |
Corticosteroids Leukotriene receptor antagonists |
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Corticosteroids (mechanism) |
•Suppressionof inflammatorygenes §Cytokines§Inflammatoryenzymes §Adhesionmolecules •Inhibitionof prostaglandin synthesis •Inhibitionof leukotriene synthesis Phospholipids --> PLA2 X --> arachidonic acid Arachidonic acid --> Cyclo-oxygenase X --> Prostaglandins & Leukotrienes |
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Corticosteroids effects |
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Corticosteroids: Examples/side effects/other info |
Inhalation - beclomestasone, buclesonide, fluticasone IV - hydrocortisone Oral - prednisolone Side effects: oral candidiasis/thrush Dysphonia (hoarseness/difficulty in speaking) Prolonged high doses: Adrenal suppression Osteoporosis Reduction in glucose uptake and increased fat metabolism GI upset - dec. prostaglandins Cushing's syndrome Hypertension - decreased Na+ excretion by kidneys increases blood volume |
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Leukotriene receptor antagonists (Effects and mech) |
Effects: dec. bronchoconstriction
dec. vascular permeability dec. mucous secretion |
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Leukotriene receptor antagonists (examples/side effects/info) |
Examples: montelukast, zafirlukast Side effects: Headache, Gi upset, Hypersensitivity (low eosinophil recruitment), Dry mouth |
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Leukotriene Rcptr Antagonists |
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Other drugs Cromones Mucolytics |
Cromones •Sodiumcromoglicate, nedocromil sodium •Consideredto act as mast cell stabilizers•Maybe of value in asthma with an allergic basis and exercise-induced asthma Omalizumab (NICE): monoclonal antibody that binds toIgE |
