Bronchodilators

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  • Created by: LBCW0502
  • Created on: 15-02-19 19:09
Which conditions have symptoms which are reversible?
Asthma
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Which conditions have symptoms which are irreversible?
Emphysema, COPD, chronic bronchitis
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Asthma and bronchitis affect which areas in the lungs?
Trachea, bronchi and broncioles
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COPD affects which areas in the lungs?
Respiratory bronchioles. Alveolar ducts, alveoli sacs (small airways disease, emphysema)
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What are the characteristics of an asthmatic bronchiole?
Bronchoconstriction, mucus secretion, oedema, inflammation, hyper-responsiveness
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Which drugs are used in the pharmacological treatment of asthma? (1)
Bronchodilators (beta 2 agonists, muscarinic antagonists - indirect, used more in COPD). Anti-inflammatory agents (glucocorticosteroids, xanthines, cromones - sodium cromoglicate/nedocromil sodium
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Which drugs are used in the pharmacological treatment of asthma? (2)
Leukotriene antagonists e.g. montelukast, anti-IgE/omalizumab
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Give examples of short acting beta agonists
Salbutamol, levalbuterol, terbutaline, pirbuterol (antimuscarinics - ipratropium, oxitropium)
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Give examples of long acting beta agonists
Salmeterol, formoterol, vilanterol (antimuscarinic - tiotropium, aclidinium, methylxanthines - theophylline, doxophylline)
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Give examples of fixed combination treatments
Salbutamol + ipratropium. Budesonide + formoterol. Fluticasone + salmeterol. Mometasone + formoterol. Vilanterol + fluticasone
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What are the two major mechanisms which cause relaxation of airway smooth muscle?
Beta agonist binding to GCRP (cascade reaction to cause elevation of cAMP in cells). Anti-muscarinic blocks M3 receptors to prevent binding of ACh to cause smooth muscle relaxation (also inhibits mast cell degranulation)
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What are the onset of actions for: salbutamol, salmeterol, formoterol, indaceterol, vilanterol?
3-5 min. 20-30 min. 3-10 min. 3-10 min. 10 mins
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What are the duration of actions for: salbutamol, salmeterol, formoterol, indaceterol, vilanterol?
<6 h. < 12 h. <12 h. >24 h. 24 h.
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What are the onset of actions for the following anticholinergics: ipratropium, oxitropium, tiotropium, glycopyrronium, aclidnium?
30-45 mins. 30-45 mins. 30-60 mins. 5-15 mins. 30-60 mins
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What are the duration of actions for the following anticholinergics: ipratropium, oxitropium, tiotropium, glycopyrronium, aclidnium?
4-6 h. 6-8 h. 24 h. 24 h. >12 h
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Describe features of salbutamol (1)
Analogue of adrenaline (initially formed isoprenaline but this drug affected receptors in the heart/side effects). Salbutamol interacts with b2 receptors in airways without affecting the heart (agonist)
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Describe features of salbutamol (2)
Administered via inhaled route (MDI, DPI, nebuliser - reduce side effects). Other b2 agonists include formoterol (BD), salmeterol (BD), indacaterol (OD)
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Give examples of ultra-LABAs
Vilanterol, olodaterol, carmoterol, milveterol - OD dosing
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What are the side effects of beta 2 adrenoceptor agonists?
Tremor, increased HR, hypokalemia (can induce arrhythmias) - targeting beta receptors at extra pulmonary sites. (Anti-muscarinic effects)
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Muscarinic antagonists such as ipratropium bromide and tiotropium bromide are derived from what?
Atropine/scopolamine from the deadly nightshade plan (Atropa Belladonna)
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Describe features of muscarinic antagonist action
Prevents smooth muscle contraction and mucus secretion induced by activation of parasympathetic nerves. Bronchoconstriction inhibited by muscarinic antagonists (ipratropium bromide - 6 h, tiotropium bromide - 24 h). Mainly used in COPD
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What are the effects of muscarinic antagonists?
Dry mouth (less rare - urinary retention, constipation, acute angle glaucoma)
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Give examples of other muscarinic antagonists?
Glycopyrronium bromide (OD), aclidinium bromide (BD), umeclidinium bromide (OD)
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Describe the interaction between glycopyrronium and indacaterol
Additive interaction and synergistic interaction. Increase in observed relevant response (main side effect - dry mouth/anti-muscarinic effects - sympathetic responses due to parasympathetic stimulation being inhibited)
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What are the current treatments of symptoms?
Short acting beta-2 agonists (SABA - salbutamol, terbutaline, fenoterol). Long acting beta-2 agonists (LABA - asthma/COPD, salmeterol, formoterol, COPD, indacaterol). Theophylline (oral, prophylactic, not first line)
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Describe features of xanthines (1)
Inhibit PDE (metabolism of cAMP is impaired) e.g. theophylline, aminophylline. Therapeutic window 10-20 ug/mL. Side effects - nausea, vomiting, arrhythmias, hypokalaemia, hypotension, seizures
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Describe features of xanthines (2)
Numerous drug-drug interactions which increase/decrease plasma levels. Smoking promotes plasma clearance (chemical structures similar to caffeine)
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Describe the effect of smoking on cells in the body
Damage to alveolar macrophages and neutrophils. Protease inhibitors. Alveolar wall destruction (emphysema), mucus hypersecretion (chronic bronchitis)
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Card 2

Front

Which conditions have symptoms which are irreversible?

Back

Emphysema, COPD, chronic bronchitis

Card 3

Front

Asthma and bronchitis affect which areas in the lungs?

Back

Preview of the front of card 3

Card 4

Front

COPD affects which areas in the lungs?

Back

Preview of the front of card 4

Card 5

Front

What are the characteristics of an asthmatic bronchiole?

Back

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