呼吸系统药理学医学教学课件

1、第1页，共45页。Drugs acting on respiratory systemCough antitussive drugs centrally acting peripherally actingSputum expectorant drugs sputum-diluting drugs mucolytic drugsAsthma antiasthmatic drugs bronchial dilators receptor agonists theophyllines muscarinic antagonists anti-inflammatory drugs glucocorti

2、costeroids mediator release inhibitors第2页，共45页。1. Antitussives第3页，共45页。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 苯佐那酯第4页，共45页。第5页，共45页。Codeine 可待因第6页，共45页。1. Pharmacological effects supression of co

3、ugh analgesia2. Clinical uses Cough without sputum3. Adverse effects Respiratory depression (at larger doses) Addiction Contraindicated in patients with thick sputum第7页，共45页。Dextromethorphan 右美沙芬第8页，共45页。1. Pharmacological effects supression of cough muscarinic and NMDA receptor antagonism2. Clinica

4、l uses Upper respiratory infection, cough without sputum3. Adverse effects Atropine-like side effects Contraindicated in patients with glaucoma, pregnancy ( 3 m), psychotic disorders, etc. 第9页，共45页。Pentoxyverine喷托维林(咳必清) 第10页，共45页。Pharmacological effectsSupression of coughMuscarinic antagonism and l

5、ocal anesthetic effectsUses and adverse effects are similar to dextromethorphan第11页，共45页。Benzonatate苯佐那酯第12页，共45页。Pharmacological effectsPeripherally actingBlocking cough reflex Local anesthetic effectsCNS depression第13页，共45页。2. Expectorants第14页，共45页。Sputum-diluting drugsStimulating bronchial secret

6、ion 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 美司钠第15页，共45页。3. Antiasthmatic drugs第16页，共45页。AsthmaAsthma is physiologically characterized by increased responsiveness of the trachea and bronchi

7、 to various stimuli and by widespread narrowing of the airways that changes in severity either spontaneously or as a result of therapy.Its pathologic features are contraction of airway smooth muscle, mucosal thickening from edema and cellular infiltration, and inspissation in the airway lumen of abn

8、ormally thick, viscid plugs of mucus.第17页，共45页。第18页，共45页。Symptom: dyspnea, wheezing, stridor, coughing, an inability for physical exertion. The cough may sometimes produce clear sputum. Between episodes, most patients feel well but can have mild symptoms and they may remain short of breath after exe

9、rcise for longer periods of time than the unaffected individual. Asthma第19页，共45页。第20页，共45页。inflammationbronchoconstrictionAirway hyperresponsiveness Immunological and non-immunological stimuliWheezing (asthmatic symptoms)glucocorticosteroidsdisodium cromoglycate 2 receptor agonistsTheophyllinemuscer

10、inic antagonists 第21页，共45页。 Receptor agonists Non-selective：adrenaline, isoprotererol 2-selective: moderate-acting: salbutamol, terbutaline long-acting: salmeterol, formoterolTheophyllines: aminophyllineMuscarinic antagonists: ipratropine 1. Bronchial dilators第22页，共45页。Glucocorticosteroids: Systemic

11、: hydrocortisone, dexamethasone Inhalation: beclomethasone, budesonideInhibitors of mediator release: cromolyn sodium, nedocromil2. Anti-inflammatory drugs第23页，共45页。Bronchial dilators 2 receptor selective agonistsSalbuterol沙丁胺醇Terbutaline特布他林第24页，共45页。1. Pharmacological effects Relaxing bronchial sm

12、ooth muscles2. Clinical uses Controlling asthmatic symptoms Given by inhalation, oral or injection3. Adverse effects Skeletal muscle tremor Cardiac stimulation (larger doses) Dysfunction of metabolism (hypokalemia, etc.)Salbuterol 沙丁胺醇第25页，共45页。Selectivity of 2 agonists第26页，共45页。Aerosol inhalationle

13、ss systemic toxicity第27页，共45页。Spacer used for aerosol inhalation定量手控气雾器第28页，共45页。Spacer will aid patients inhale the aerosolized drugs easier第29页，共45页。2 receptor selective agonistslong-actingSalmeterolFormoterol第30页，共45页。 Theophyllines AminophyllineBronchial dilators第31页，共45页。1. Pharmacological effe

14、ctsBronchus dilation Inhibiting phosphodiesterase; Blocking adenosine receptors; Increasing catecholamine release;Immunomodulation;Increasing respiratory muscle contractility;CNS stimulation, diuretic, gastric acid secretion, etc.Theophyllines第32页，共45页。2. Clinical uses Bronchial asthma (p.o., i.v.)

15、Others: acute pulmonary edema, etc.3. Adverse effects GI reactions CNS stimulation Acute toxication ( i.v. injection too rapidly ) tachycarida, arrhythmia, seizure, coma, deathTheophyllines 第33页，共45页。 Muscarinic antagonistsIpratropineBronchial dilators第34页，共45页。Relaxing bronchial smooth musclesNo ef

16、fect on sputum secretionReplaced with or combined with 2 receptor selective agonists第35页，共45页。 Systemic (adverse effect): hydrocortisone prednisone dexamethasone Inhalation: beclomethasone dipropionate budesonide triamcinolone acetonide fluticasone propionate flunisolideGlucocorticosteroids 第36页，共45

17、页。Beclomethasone dipropionate 第37页，共45页。1. Pharmacological effects (Antiinflammation)Inhibiting inflammatory cell activities, Antibody production, mediator release, Inhibit increased responsiveness of the trachea and bronchi 2. Clinical uses As first-line drugs, currently Controlling chronic symptom

18、s Ineffective for acute symptoms Beclomethasone dipropionate第38页，共45页。Adverse effects Local: oropharyngeal candidiasisusing spacer Systemic effects a) Hypercorticism-like syndrome: central obesity (moon face, buffalo hump, etc.); hypertension; glycosuria, hypokalemia; etc.b) Increasing susceptibilit

19、y to infectionsc) Ingestive system: peptic ulcers, etc.d) Cardiovascular system: hypertension, arteriosclerosise) Myopathy and osteoporosis: vertebral compression fractures, spontaneous fractures, especially in postmenopausal womenf) Adrenal suppression第39页，共45页。Inhibitors of mediator releaseDisodium cromoglycate ( cromolyn )第40页，共45页。1. Pharmacological effectsInhibiting mediator release from mast or other cellsInhibiting sensory neuropeptide release and non-specifical stimulus induced bronc