浙江大学医学院：《药理学 Pharmacology》课程教学资源（PPT课件）支气管扩张药 Bronchodilators

Bronchodilators (支气管扩张药) Huifang Tang(汤慧芳 Department of pharmacology Zhejiang university, school of Medicine tanghuifang@ziu.edu.cn

Bronchodilators (支气管扩张药) Huifang Tang (汤慧芳) Department of Pharmacology Zhejiang university, school of Medicine tanghuifang@zju.edu.cn

Drugs acting on respiratory system Cough antitussive drugs centrally acting peripherally acting Sputum expectorant drugs sputum-diluting drugs mucolytic drugs Asthma antiasthmatic drugs Bronchodilators β receptor agonists theophyllines muscarinic antagonists Anti-inflammatory drugs glucocorticosteroids mediator release inhibitors

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

Why asthma makes it hard to breathe Air enters the respiratory system from the nose and mouth and travels through the bronchial tubes. In a non-asthmatic person, In an asthmatic person, the the muscles around the muscles of the bronchial tubes bronchial tubes are relaxed tighten and thicken, and the and the tissue thin air passages become allowing for easy inflamed and mucus- filled, makir difficult for air to move A Inflamed bronchial tube of an asthmatic Normal bronchial tube

Antiasthmatic drugs Immunological and non-immunological stimuli Airway inflammation bronchoconstriction glucocorticosteroids B2receptor agonists Pheophyll Ine Di Isodium cromoglycate Muscerinic antagonists Leukotriene modifiers Airway hyperresponsiveness A Wheezing(asthmatic symptoms)

Antiasthmatic drugs Airway inflammation bronchoconstriction Airway hyperresponsiveness Immunological and non-immunological stimuli Wheezing (asthmatic symptoms) glucocorticosteroids Disodium cromoglycate Leukotriene modifiers 2 receptor agonists Theophylline Muscerinic antagonists

CNS Airway Vag afferent Vagal efferent Tissue response cells sory receptor (mast ce or eosinophi Mediators from whaled intan response c Mucosa … lonic fiber Transmitter(ACh) Postgang onic neuron L Smooth musce cells

Drugs used in asthma Bronchodilators Anti-inflammatory agents Leukotriene antagonists Beta Release Lipoxygenase Receptor agonists inhibitors inhibitors inhibitors Muscarinic Steroids Antibodies antagonists Slow anti-inflam- Methylxanthines matory drugs Drugs used in chroni nic obstructive pulmonary disease Bronchodilators Anti-inflammatory agents Antibiotics Steroids

Bronchodilators aβ Receptor agonists D Non-selective: adrenaline, isoprenaline 口β2- selective: D moderate-acting: salbutamol, terbutaline D long-acting: salmeterol, formoterol D Theophylines: aminophylline 0 Muscarinic antagonists: ipratropium bromide

Bronchodilators  Receptor agonists Non-selective：adrenaline, isoprenaline 2-selective: moderate-acting: salbutamol, terbutaline long-acting: salmeterol, formoterol Theophyllines: aminophylline Muscarinic antagonists: ipratropium bromide

ATP Bronchodilation A Beta agonists CAME Bronchial tone AMP Acetylcholine-+0--Adenosine Muscarinic antagonists Theophy lline Bronchoconstriction

1.阝β receptor agonists HO -CHCH2-NH2 NOREPINEPHRINE non-selectivity HO OH 去甲肾上腺素 HO CH-CH2NH EPINEPHRINE 肾上腺素 HO OH CHa CHCH2-NH ISOPROTERENOL HO OH 异丙肾上腺素 CH(CHak JOH2C ALBUTEROLOL H-CH2-NH o B2 receptor selective agonists HO HOH2C CH-CH2NHCH2 (CH)s-OCH2( CH2)3 SALMETEROL 沙丁胺醇 HO FORMOTEROL HCONH FCH2NHCH-CH2 OCH3 福莫特罗 HO

1.  receptor agonists 去甲肾上腺素 异丙肾上腺素 沙丁胺醇 福莫特罗 肾上腺素 non-selectivity 2 receptor selective agonists

Bag onist c—NH Iberiotoxn c membrane AC LeYI BAR ATP GIPG. Cyclic AMP tCa2-actvated K channel activation Methylxanthines PDE 4 PLC-IP Ca pathway activity ↑PKA ↑Na'a2 exchange 5AMP ↑NaCa2 ATPase +MLCK