1、28 第二十八章 作用于呼吸系统的药物 ppt课件l掌握掌握 平喘药的概念、分类，沙丁胺醇、平喘药的概念、分类，沙丁胺醇、氨茶碱、色甘酸钠的药理作用、临床应氨茶碱、色甘酸钠的药理作用、临床应用、不良反应。用、不良反应。l熟悉熟悉 呼吸系统药物分类，异丙托溴铵、呼吸系统药物分类，异丙托溴铵、糖皮质激素的作用特点，平喘药的临床糖皮质激素的作用特点，平喘药的临床应用。可待因、右美沙芬、喷托维林等应用。可待因、右美沙芬、喷托维林等药理作用特点。药理作用特点。l了解了解 镇咳药和祛痰药的概念；苯佐那酯、镇咳药和祛痰药的概念；苯佐那酯、溴己新的药理作用及临床应用。溴己新的药理作用及临床应用。l Respi
2、ratory disease is a familiar,repetitious disease.l The common symptoms are:cough,sputum(痰痰);asthma(哮喘哮喘).呼吸系统炎症呼吸系统炎症病原生物感染病原生物感染过敏反应过敏反应痰痰咳咳喘喘支气管痉挛支气管痉挛antitussivesexpectorantsAntiasthmaticslI.Antiasthmaticsl Asthma pathologic features:lSoakage（浸润）浸润）of inflammatory cells,lcontraction of airway smo
3、oth muscle,lmucosal thickening from edema and cellular infiltration,lthe plug of mucus in the airway lumen.l responsiveness of the trachea and bronchi to various stimuli.lAsthmatic stimuli include:inhaled allergens(吸入性过敏原吸入性过敏原);drugs;non-specific stimuli such as cold air,exercise,stress,and polluti
4、on.lBronchial inflammatory mediators:LTs,PGs,TXA2,PAF lcell factors ILs,TNF-,GM-CSF.lClassifications of antiasthmatics .Bronchodilators 1.-R agonists;2.Theophylline;3.M-R antagonists;.Antiinflamatory drugs .Mast-cell stabilizers 一一.Bronchodilators 1.-R agonists adrenerling;Ephedrine;isoprenaline;sel
5、ective 2-R agonists Salbutamol;Terbutaline Clenbuterol Formoterol;Salmeterol lBasic actions (+)ACintracellular cAMP:brochodilation;release of inflammatory mediators;microvascular leakage;mucociliary（粘膜纤毛）粘膜纤毛）transport.l2 selective agonistsl first line drugs for asthma at present bronchodilation iso
6、prenaline,but cardiovascular effects;po.absorbed well,long duration;adverse reactions not common.l2.Theophyllines 氨茶碱氨茶碱 aminophylline,胆茶碱胆茶碱 choline theophylline relax the smooth muscles of the bronchi;po.chronic asthma iv.acute asthma lmechanism of action unclear,possibly include:1)Inhibit PDEintr
7、acellular cAMP;2)endogenic CAs release;3)Inhibit adenosine(腺苷腺苷)receptors;4)anti-inflammation inflammatory response eosinophils mediated by ILs.l【Adverse effects】nausea,vomiting,tremor(颤抖颤抖),insomnia(失眠失眠),tachycardia.concentrations 20 g/ml toxic effects may occur;Rapid iv.aminophylline sudden death
8、,(probably due to cardiac arrhythmias)3.M-receptor antagonists 异丙阿托品异丙阿托品 Ipratropine 氧托品氧托品 oxitropium 泰乌托品泰乌托品 tiotropium second-line drugs for asthma.aerosol inhalant（气雾吸入剂）气雾吸入剂）【characteristics】1.selective M-R cGMP bronchodilation；2.aerosol administration poorly absorbed；3.used for chronic bron
9、chitis (Ach-mediated bronchospasm 支气管痉挛支气管痉挛）.二二.Antiinflamatory drugs Corticosteroids The glucocorticoids（糖皮质激素）糖皮质激素）used in treatment of asthma include:二丙酸倍氯米松二丙酸倍氯米松 Beclomethasone；氟尼缩松氟尼缩松 Flunisolide；布地奈德布地奈德 Budesonide【Mechanisms of Action】1.Anti-inflammatory action；2.Anti-allergic reaction 3
10、.lipocortin1（脂皮素脂皮素1）PLA2 LTs and PGs.4.prevent 2R down-regulation.【Clinical uses】Inhalation(the most common way);Usually po.iv.reserved for:severe acute exacerbations of asthma,（严重的哮喘急剧发作）严重的哮喘急剧发作）severe status asthmaticus.（严重的哮喘持续状态严重的哮喘持续状态）三三.Mast-cell stabilizers 色甘酸钠色甘酸钠 Sodium cromoglicate l
11、stabilize antigen-sensitized mast cells Ca 2+influx;release of inflammatory mediators.lInhalation,slowly(after 2-3d)main used in preventing asthmatic attacks,other allergic diseases.四四.Others 1.5-lipoxygenase inhibitor 齐留通齐留通 zileuton 2.LT-recepter antagonists 扎鲁司特扎鲁司特 zafirlukast 孟鲁司特孟鲁司特 monteluka
12、st 3.Anti-IgE monoclonal antibodiesII.Antitussiveslinhibit the cough reflexCentral antitussivesCodeine;Pentoxyverine;Benproperine;Peripheral antitussives Benzonatate l 可待因可待因 Codeine (+)opioid receptor(morphine)analgesic actions,antitussive actions.used for irritative dry coughing.Addiction（成瘾性）成瘾性）
13、(long-term use)苯佐那酯苯佐那酯 benzonatate the derivative of tertracaine1.Local anesthetic effects l the pulmonary stretch reflex；（肺牵张反射）肺牵张反射）l sensory nervous terminals；2.used to prevent cough during bronchoscopy（支气管镜检查）支气管镜检查）.III.Expectorants 乙酰半胱氨酸乙酰半胱氨酸 N-acetylcysteine Mucolytics（粘痰溶解剂）粘痰溶解剂）break d
14、isulfide bonds of mucus sputum viscosity（粘性）粘性）.Use in chronic obstructive pneumopathia.（慢性阻塞性肺病）慢性阻塞性肺病）溴己新溴己新 Bromhexine l breaks the mucoitin（粘多糖）粘多糖）of the sputum；lused in the chronic bronchitis（支气管炎）支气管炎）,asthma and bronchiectasis（支气管扩张症）支气管扩张症）.l For each drug category of antiasthmatics,lgive examples,ldescribe their mechanisms of action and major clinical uses.
