Drugs used in pulmonary diseases

1. Drugs used in pulmonary diseases LING ZHU

2. Coughing wheezing sputum (phlegm) inflammation

3. Drugs used in pulmonary diseases Antitussives 镇咳药 Expectorants 祛痰药 Antiasthmatic drugs 平喘药

4. Anti-asthmatic drugs 平喘药 PÍng chuǎn yào

5. Asthma is a chronic inflammatory disorder of the airways General characteristics: increased tracheobronchial responsiveness to many stimuli ↓ physiological air passage narrowing ↓ this is called airway inflammation, or bronchoconstriction ↓ paroxysmal dyspnea, coughing, wheezing, chest tightness asthma attack

6. Allergic asthma

7. Stimulation-induced asthma

8. Basic pharmacology stabilized membrane--cromolyn Antigenen muscle contraction vascular leakage Hyper-secretion edema Histamine SRS-A 5-HT muscle vascular mucus gland mast cells Trachea Bronchi Ach airway narrowing inflammation M-R antagonist exercises irritants dyspnea, coughing wheezing, chest tightness Theophylline Sympathomimetic agents Corticosteroids Leukotriene inhibitors

9. Treatment of Asthma

10. Relievers are medications used on an as-needed basis that act quickly to reverse broncho-constriction and relieve its symptoms. Controllers are medications taken daily on a long-term basis to keep asthma under clinical control chiefly through their antiinflammatory effects. Agents for asthma

11. Reliever Rapid-acting β2-agonists. Systemic glucocorticosteroids Theophylline M-R antagonist Controller Long-acting β2-agonists Glucocorticosteroids Sablized membrane—cromolyn Leukotriene modifiers Lower dose of theophylline Anti-IgE Agents for asthma

12. Theophylline 茶 碱

13. Theophylline 茶碱 Commonly used • Theophylline---茶碱 • Aminophylline----氨茶碱 • Cholinophylline---胆茶碱 • Diprophylline-----二羟丙茶碱 • 优喘平（优特舒、舒弗美）茶碱缓释片

14. Actions of theophylline • smooth muscle relaxation • high concentrations : phosphodiesterase inhibition ↓ intracellular cAMP↑ ↓ cardiac stimulation smooth muscle relaxation positive chronotropic

15. mechanisms of theophylline • inhibition of adenosine cell surface receptors modulators of adenylyl cyclase activity isolated airway smooth muscle Adenosine contraction histamine release from lung cells • Promote releaseing of Adr

16. Actions of theophylline 2. Anti-inflammatory action: • low-dose theophylline: inhibit late response to antigenic challenge 3. Increase contraction of muscle

17. +

18. Cardiovascular Effects • Direct positive chronotropic • Direct enhanced myocardial contractility • Low doses: increased catecholamine release • High doses: enhanced calcium influx

19. Renal Effects: Weak diuretics-- not therapeuticly important • Increased glomerular filtration • Reduced tubular sodium reabsorption

20. Multiple effects

21. theophylline: Clinical Use • Effective bronchodilator • Relieves airway obstruction in acute asthma • Decreases frequency and severity of symptoms in chronic asthma • Used in therapy for COPD

22. Theophylline • Therapeutic/toxic effects: related to plasma concentration • 5-20 mg/L ---improvement pulmonary function • > 20 mg/L—nausea, vomiting, headache, anxiety, anorexia • > 40 mg/L—seizures, arrhythmias

23. Sympathomimetic drugs 拟肾上腺素药

24. sympathomimetic drugs

26. Muscarinic Antagonists

27. Muscarinic Antagonists Mechanism of Action: • M- R: • Contraction of airway smooth muscle • Increased mucous secretion

28. Clinical Use— Antimuscarinic Drugs • Effective bronchodilators • Antimuscarinic drugs are only capable of preventing the cholinergic-mediated bronchospasm • Preferred route of administration (enhanced organ selectivity): inhalation • Antimuscarinic with limited systemic adverse effects: ipratropium bromide

29. Muscarinic Antagonists • Ipratropium bromide 异丙托溴胺、异丙托品 • Oxitropium 氧托溴胺、氧托品 • Isopropylscopolamine 异丙东莨菪碱 • Tiotropium 噻托溴胺、泰乌托品 可必特气雾剂： 异丙托品 + 沙丁胺醇

30. Sodium Cromoglycate 色甘酸钠sè gān suān nà

31. Cromoglycate 色甘酸 ----action • Inhibit: antigen- induced asthma • exercise- induced asthma • Reduce bronchial hyper-activity • No direct effect on airway smooth muscle tone • Will not reverse asthmatic bronchospasm 色甘酸钠（sodium cromoglicate，intal 咽泰）

32. Mechanism of Action • Alters function of calcium → inhibits cell activation Airway nerves------cough Mast cells -------degranulation Eosinophils---------inflammatory

33. Cromoglycate ------------ Pharmacokinetics • Poorly absorbed • administered by microfine powder inhalation or aerosol -------- may cause throat irritation

34. Clinical Use 1. Pre-treatment for asthma: • blocks bronchoconstriction antigen inhalation aspirin-induced blocks environmental agents • Reduces • bronchodilators medication requirements • symptomatic severity

35. Clinical Use 2. Reducing symptoms allergic rhinitis

36. Cromoglycate ◆Adverse/Side effects: --------minor and localized throat irritation cough mouth dryness wheezing chest tightness

37. Corticosteroids Corticosteroid effects: • Anti-inflammatory action • Diminish bronchial reactivity • Increase airway diameter • Reduced frequency of asthma attacks

38. Mechanisms of action: corticosteroids • Primary: anti-inflammatory action------ Inhibition of cytokine production • Secondary: enhancement of beta-receptor agonist effects

39. Clinical Use: Corticosteroids • Inhaled glucocorticosteroids are the most effective controller medications currently available • Systemic glucocorticosteroids are important in the treatment of severe acute exacerbations

40. Leukotriene modifiers

41. Leukotriene Pathway Inhibitors Zeleuton arachidonic acid eosinophils, 5-lipoxygenasemacrophages, mast cells basophils Leukotriene LTB4--chemattractant LTD4--bronchoconstriction LTC4 mucosal edema mucus hypersecretion bronchial reactivity↑ Zafirlukast Montelukast

42. Other drug groups • Calcium channel blockers • Nitric oxide donors • Potassium channel activators • Anti-IgE monoclonal antibodies

44. Antitussives 镇咳药

45. Antitussives

46. Expectorants 祛痰药

47. Expectorants