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48 Cards in this Set
- Front
- Back
What is the location of where asthma and bronchitis take place? |
The conducing zone of the bronchial tree |
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What does COPD stand for? |
Chronic Obstructive Pulmonary Disease |
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What are two examples of COPD? |
Emphysema Small airways disease |
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What happens when an allergic asthmatic inhales an antigen? |
Mast cells in airway sense allergen as they have IGE receptors (immunoglobulin receptors) Mast cells release histamines when the allergen is encountered |
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When mast cells release histamines in response to an allergen, what 4 things does this cause? |
Bronchoconstriction Oedema Mucus secretion Inflammation |
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What are the two main drugs used in the treatment of asthma? |
Bronchodilators Anti-inflammatory agents |
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What are two examples of bronchodilators? |
Beta 2-agonists Muscarinic antagonists |
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What are some examples of anti-inflammatory agents? |
Glucocorticosteroids Xanthines Cromones Leukotrienes Anti-IgE |
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What is an example of a short acting beta-2 agonist? |
Salbutamol |
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What is an example of a long acting beta 2 agonist? N.B long acting means they can be taken once or twice a day |
Salmeterol |
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Theophylline is a __________ used as a bronchodilator in asthma |
xanthine |
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What is the mechanism of action for beta-agonists in the treatment of asthma as COPD? |
Stimulate the beta-2 receptors on lung epithelium Increase in cAMP Activates protein kinase A Phosphorylates MLCK (myosin light chain kinase) Relaxation of airway smooth muscle |
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What do beta-2 adrenorecptor agonists inhibit? |
Mast cell degranulation |
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How are beta-2 adrenorecptor agonists administered? |
Via the inhaled route (metered dose inhaler, dry powder, nebuliser) N.B photo is of a nebuliser |
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What are some side effects of beta-2 adrenoceptor agonists? |
Tremor Increased heart rate Hypokalemia (low [K+]) |
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Muscarinic antagonists relieve the symptoms of asthma. What do they prevent? |
Prevent smooth muscle contraction Prevent mucus secretion induced by activation of parasympathetic nerves Bronchoconstriction |
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What are two examples of muscarinic antagonists? |
Ipratropium bromide (6hr) Tiotropium bromide (24hr) |
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What are some side effects of muscarinic antagonists? |
Dry mouth (no saliva ---> mouth ulcers ---> can't swallow) Urinary retention Constipation Acute angle glaucoma |
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Current anti-inflammatory therapy includes: a) Glucocorticosteroids b) Theophylline c) Leuokotrirene receptor antagonists d) Anti-IgEL Omalizumab e) Cromones For each of these, state how they are administered. |
a) inhaled and oral b) oral c) oral d) subcutaneous e) inhaled |
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How do glucocorticosteroids work in asthma? |
Steroids are lipophilic so can pass through membrane Steroid binds GR (glucocorticoid receptor) which is bound to a heat shock protein (HSP90) HSP90 transfers the glucocorticosteroid in its GR receptor to the nucleus of the cell. Once inside nucleus, HSP90 disassociates. The complex of the steroid in its receptor affects gene expression in the nucleus |
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The complex of a glucocorticosteroid in its receptors affect gene expression. Gene expression can either be enhanced or repressed. What are these terms known as? |
Trans-activation Trans-repression |
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What can glucocorticoids enhance the expression of (trans-activation)? |
Annexin Beta-2 adrenoceptors Mitogen kinase phosphatase |
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What can glucocorticoids repress the expression of (trans-repression)? |
Cytokines Chemokines Adhesion molecules Inflammatory enzymes (COX2, NOS) |
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What are some actions of glucocorticosteroids in asthma? |
Inhibition of leukotriene and cytokine synthesis/release Inhibit recruitment of inflammatory cells (T cell,s eosinophils, mast cells) Anti-oedema Increases beta-adrenorecptor function (enhances bronchodilator effect of beta-2 agonists) |
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What does ICS stand for? |
Inhaled corticosteroids |
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What are some roles of ICS in asthma therapy? |
Prevents infiltration and activation of inflammatory cells Reduces mucosal oedema (swelling of airway wall) Improves airflow and hence lung function Decreases airway hyper responsiveness Reduce symptoms (e.g bronchospasm) Reduce frequency and severity of exacerbations Improves quality of life |
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What are some side effects of glucocorticosteroids taken by inhaled routes (e.g fluticasone propionate) ? |
Oral candidiasis ( fungal infection) Hoarseness, cough, voice problems, |
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What are some side effects of glucocorticosteroids when taken by the oral route or prolonged high dose? |
Growth retardation Bruising Suppression of hypothalamic pituitary axis (a complex set of direct influences and feedback interactions among : the hypothalamus, the pituitary & adrenal glands) Osteoporosis Hypertension Weight gain Ocular hypertension (pressure in eyes higher than normal) |
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What are leukotriene antagonists and 5-LO inhibitors?? |
Anti-inflammatory drugs that inhibit pathways to leukotriene synthesis or prevent leukotriene binding to its receptor |
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5-lipoxygenase inhibitors are examples of anti-leukotriene drugs. Give an example. |
Zileuton |
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Leukotriene receptor antagonists are examples of anti-leukotriene drugs. Give an example. |
Montelukast |
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For each of these statements about anti-leukotriene drugs, state whether they are true or false. 1.Relativelyshort acting (need to be taken multiple times per day)
2. Greatestbenefit in mild asthma (combination with GCS) 3.Usefulfor aspirin sensitive and exercise induced asthma 4. Oralbioavailability ( the fraction of the orally administered drug that reaches the systemic circulation) |
1. False - they are relatively long acting (once per day) 2. False- greatest benefit in severe asthma 3. True 4. True |
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What are some side effects of anti-leukotriene drugs? (rare) |
Headache GI disturbance ( as blocks COX and 5-LO) |
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How do xanthines work? |
Inhibit PDE so the metabolism of cAMP is impaired so there is more smooth muscle relaxation |
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What are two examples of xanthines (2) ? |
Theophylline Caffeine |
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What is the therapeutic window for xanthines? |
Aprox 10-20 ug/mL |
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What are some side effects of xanthines? |
Nausea Vomiting Arrhythmias Hypokalemia ( low [K+] ) Hypotension (low bp) Seizures |
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Xanthines interact with numerous drugs which increase/decrease plasma levels. True or false. |
True |
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What promotes plasma clearance of xanthines? |
Smoking |
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What are cromones? |
Drugs that inhibit inflammation in a number of allergen-mediated diseases N.B they are often found in medications for hay fever |
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Complete this statement about cromones: Cromones reduce inflammatory cell ___________ and _____________ |
activation recruitment |
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What are more effective : cromones or glucocorticosteroids? |
Glucocorticosteroids |
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What is an example of a cromone? |
Sodium cromoglicate |
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What is omalizumab (xolair) ? |
First biological agent for treatment of asthma |
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How does Omalizumab (xolair) work? |
Binds to free IgE and prevents it building up in the body (N.B Immunoglobulin E (IgE) are antibodies produced by the immune system. If you have an allergy, your immune system overreacts to an allergen by producing antibodies called Immunoglobulin E (IgE)) |
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How must Omalizumab (xolair) be given? |
As a subcutaneous injection |
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Omalizumab (xolair) is very costly. Therefore when is it used? |
Therefore only used in moderate to severe asthmatics whose asthma is not controlled by glucocorticosteroids |
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What are immunoglobulins? |
Immunoglobulin E (IgE) are antibodies produced by the immune system. If you have an allergy, your immune system overreacts to an allergen by producing antibodies called Immunoglobulin E (IgE). These antibodies travel to cells that release chemicals, causing an allergic reaction. |