Section IV. Respiratory systems
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1 Section IV Respiratory systems
2 Chapter 6 Drugs for treatment of respiratory diseases Antitussives Expectorants Antiasthmatic drugs
3 Normal structures of respiratory system
4 Sensory and motor nervous pathways
5 Various diseases of respiratory system Common symptoms: cough sputum wheezing
6 Drugs acting on respiratory system Cough antitussive drugs centrally acting peripherally acting Sputum expectorant drugs sputum-diluting drugs mucolytic drugs Asthma antiasthmatic drugs bronchodilators receptor agonists theophyllines muscarinic antagonists anti-inflammatory drugs glucocorticosteroids mediator release inhibitors
7 A. Antitussives Centrally acting Addictive drugs: codeine 可待因 Non-addictive drugs: dextromethorphan 右美沙芬 pentoxyverine 喷托维林 ( 咳必清 ) Peripherally acting benzonatate 苯佐那酯
8 Respiratory center Centrally acting antitussives Motor nerves Sensory nerves Peripherally acting antitussives
9 A. Antitussives Codeine 可待因 H3CO O N CH3 HO Other additive antitussives: Dihydrocodeine( 双氢可待因 ); Drotebanol( 羟蒂巴酚 ); Pholcodine( 福尔可定 )
10 A. Antitussives 1. Pharmacological effects suppression of cough (1/4 of morphine) analgesia (1/7~1/10 of morphine) 2. Clinical uses Cough without sputum 3. Adverse effects Respiratory depression (at larger doses) Addiction Contraindicated in patients with thick sputum
11 A. Antitussives Dextromethorphan 右美沙芬
12 A. Antitussives Dextromethorphan 右美沙芬 1. Pharmacological effects suppression of cough muscarinic and NMDA receptor antagonism 2. Clinical uses cough without sputum, upper respiratory infection, acute or chronic bronchitis 3. Adverse effects Atropine-like side effects
13 A. Antitussives Pentoxyverine 喷托维林 ( 咳必清 ) Suppression of cough Muscarinic antagonism and local anesthetic effects Uses and adverse effects are similar to dextromethorphan
14 A. Antitussives Benzonatate 苯佐那酯 ( 退嗽 ) Peripherally acting Blocking cough reflex Local anesthetic effects CNS depression Others: Noscapine ( 那可汀 ); moguisteine ( 莫吉司坦 )
15 B. Expectorants Sputum-diluting drugs Stimulating bronchial secretion Amonium chloride 氯化铵 Potassium iodide 碘化钾 Mucolytic drugs Bromhexine 溴己新 Ambroxol 氨溴索 Acetylcysteine 乙酰半胱氨酸 Methylcysteine 美司坦 Carbocisteine 羧甲司坦 Mesna 美司钠
16 B. Expectorants Hydration: Sputum dilution Mucolysis Mucous glycoprotein network
17 C. Antiasthmatic drugs Bronchial asthma: inflammation; bronchoconstriction; airway hyperresponsiveness
18 C. Antiasthmatic drugs Immunological and non-immunological stimuli Airway inflammation bronchoconstriction glucocorticosteroids 2 receptor agonists disodium cromoglycate theophylline leukotriene modifiers muscerinic antagonists Airway hyperresponsiveness Wheezing (asthmatic symptoms)
19 C. Antiasthmatic drugs Airway pathological changes in pathogenesis of bronchial asthma
20 C. Antiasthmatic drugs Airway pathological changes in pathogenesis of bronchial asthma
21 C. Antiasthmatic drugs Bronchodilators Receptor agonists Non-selective:adrenaline, isoprenaline 2 -selective: moderate-acting: salbutamol, terbutaline long-acting: salmeterol, formoterol Theophyllines: aminophylline Muscarinic antagonists: ipratropine Anti-inflammatory drugs Glucocorticosteroids: Systemic: hydrocortisone, dexamethasone Inhalation: beclomethasone, budesonide Inhibitors of mediator release: cromolyn sodium, nedocromil
22 Drugs used in the treatment of asthma - Classification in Grash Course: Respiratory system (2nd Edition) - Relievers - Bronchodilators 2 agonists short-acting: salbutamol, terbutaline long-acting: salmeterol, formoterol Anticholinergics (muscarinic antagonists): ipratropine Xantines (theophyllines): aminophylline Preventers - Anti-inflammatory drugs Glucocorticosteroids: Inhaled steroids: beclomethasone, budesonide, fluticasone oral steroids: hydrocortisone, prednisone, dexamethasone Leukotriene (LT) receptor antagonists (leukotriene modifiers): LT antagonists: montelukast ( 孟鲁司特 ), zafirlukast ( 扎鲁司特 ) 5-lipoxygenase inhibitors: zileuton ( 齐留通 ) Inhibitors of mediator release: cromolyn sodium, nedocromil
23 C. Antiasthmatic drugs Bronchial dilators 2 receptor selective agonists Salbuterol 沙丁胺醇 Terbutaline 特布他林
24 Salbuterol 沙丁胺醇 1. Pharmacological effects Relaxing bronchial smooth muscles 2. Clinical uses C. Antiasthmatic drugs Controlling asthmatic symptoms Given by inhalation, oral or injection 3. Adverse effects Skeletal muscle tremor Cardiac stimulation (larger doses) Dysfunction of metabolism (hypokalemia, etc.)
25 Selectivity of 2 agonists
26 Aerosol inhalation
27 定量手控 气雾器 Spacer used for aerosol inhalation
28 Spacer will aid patients to inhale the aerosolized drugs easier
29 C. Antiasthmatic drugs 2 receptor selective agonists: long-acting Formoterol 福莫特罗 Salmeterol 沙美特罗
30 C. Antiasthmatic drugs Theophyllines Aminophylline 氨茶碱 - O - H3C N N H CH2NH2.. 2H2O O N N CH2NH2 - CH3-2 Theophyllines: One type of xanthine derivatives ( 甲基黄嘌呤类衍生物 )
31 C. Antiasthmatic drugs 1. Pharmacological effects Inhibiting phosphodiesterase; Blocking adenosine receptors; Increasing catecholamine release; Immunomodulation; Increasing respiratory muscle contractility; CNS stimulation, diuretic, gastric acid secretion, etc.
32 C. Antiasthmatic drugs 2. Clinical uses Bronchial asthma (p.o., i.v.) Others: acute pulmonary edema, etc. 3. Adverse effects GI reactions CNS stimulation CVS reactions Acute intoxication ( i.v. injection too rapidly )
33 C. Antiasthmatic drugs Muscarinic antagonists Ipratropine 异丙托溴铵, 异丙托品 CH2 CH CH3 O (CH3)2CHNCH3 CH O C CH C6H5 CH2 CH CH3 CH2OH
34 C. Antiasthmatic drugs Glucocorticosteroids Systemic: hydrocortisone 氢化可的松 prednisone 泼尼松 dexamethasone 地塞米松 Inhaled: beclomethasone dipropionate 二丙酸倍氯米松 budesonide 布地奈德 triamcinolone acetonide 曲安奈德 fluticasone propionate 丙酸氟替卡松 flunisolide 氟尼缩松
35 C. Antiasthmatic drugs Beclomethasone dipropionate 二丙酸倍氯米松 CH2OCOC 2H5 HO C O OCOC 2H5 CH3 O Cl
36 C. Antiasthmatic drugs 1. Pharmacological effects Antiinflammation: inhibiting inflammatory cell activities, antibody production, mediator release 2. Clinical uses As first-line drugs, currently Controlling chronic symptoms Ineffective for acute symptoms 3. Adverse effects Local: oropharyngeal candidiasis-using spacer Systemic effects
37 C. Antiasthmatic drugs Inhibitors of mediator release Disodium cromoglycate 色甘酸二钠 ( cromolyn ) ( 色甘酸钠 ) NaOOC O O COONa O OCH2CHCH 2O OH O
38 C. Antiasthmatic drugs 1. Pharmacological effects Inhibiting mediator release from mast or other cells Inhibiting sensory neuropeptide release 2. Clinical uses Prevention of allergic asthma Acting slowly (2-4 weeks) 3. Adverse effects Oropharyngeal irritation
39 Cromolyn Inhibits mediator release from mast cells
40 C. Antiasthmatic drugs Other inhibitors of mediator release Nedocromil sodium 奈多罗米钠 Tranilast 曲尼司特 Ketotifen 酮替芬 (H 1 receptor antagonist)
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