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Drugs Affecting the Respiratory System

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Title: Drugs Affecting the Respiratory System


1
Drugs Affecting the Respiratory System
  • By
  • Caiying Ye
  • Department of Pharmacology, School of Basic
    Medicine, Peking Union Medical College

2
Introduction
  • Antiasthmatics ???
  • Antitussives ???
  • Expectorants ???

3
??
  • ?????????????????,?? ??????????
  • ????????,?????????
  • ?????????,?????.
  • ???????????????,?????,????,????????????

4
??? Antiasthmatic Drugs
5
Aasthma
  • A chronic inflammatory disease of the airways
  • Clinical feature bronchospasm, bronchial
    obstruction, dyspnea
  • Pathologic changeslymphocyte infiltration,
    mucosal oedema, vascular leakage, airway smooth
    muscle proliferation.
  • Cellular infiltration invovling mast cell and
    eosinophil triggers bronchial inflammation and
    allergic response in susceptible population.
  • Treatment principleinhibit airway inflammation
    and inflammatory mediators.

6
Classifications
  • ß2 adrenoceptor agonists
  • Methylxanthinesaminophiline ???
  • Muscarinic antagonists ipratropium bromide?????
  • Glucocorticosteroids beclomethasone
    dipropionate??????
  • Mast cell stablizers sodium cromoglicate????

7
Effect of antiathmatic drugs on intracellular
levels of cAMP
8
1. Adrenoceptor agonists
Nonselective Epinephrine ????(Adrenalin) Ephedirine ??? Isoprenaline ??????
ß2 agonist Salbutamol ????(albuterol ???) Terbutaline ????(Breathair) Clenbuterol ???? Formoterol ???? Bambuterol ????
9
1. Adrenoceptor agonists
  • ????
  • Activate ß2 receptor
  • activate adenylyl cyclase cAMP
  • Ca2 relax airway smooth muscle
  • Activate a receptor
  • cause vasoconstriction reduce
    edema
  • improve airflow
  • dilate the bronchus to relieve bronchospasm
  • Activate ß receptor on the membrane of mast cell
    inhibit release of allergic mediators
    prevent allergic asthma attack

10
  • ????
  • ????????,?????????????ß 2??????,????,??????,?????
  • ?????????????,???????????????

11
  • ???? adrenaline,epinephrine
  • ?????????
  • Stimulate a, ß1 ß 2 receptors
  • ß???????
  • a????????????,????,???????
  • ????ß1??,??????.
  • ???a?????,?????????,??????.
  • ????,??????,???????

12
  • ???ephedrine
  • ???????,?????,????,??,??4-6??
  • ???????????,?????
  •  
  • ??????isoprenaline (???)
  • ??????( Stimulate both ß1 ß 2 receptors )
  • ????,1 min??????,??1-2 hr
  • ?????????,?????

13
????salbutamol(???)
  • ??
  • ?ß 2??????ß1??,???????
  • ???????????,????
  • ???????????????????????????????

14
2. theophylline ??? aminophylline
???cholinophylline
  • Pharmacologic effects
  • Relaxes airway smooth muscle
  • Improves respiratory function
  • Positive inotropic effect

15
  • Mechanism of relaxing airway smooth muscle
  • ? Inhibits phosphodiesterases,leading to
    intracellular accumulation of cAMP and smooth
    muscle relaxation.
  • ?Stimulates endogenous epinephrine noradrenalin
    release, relaxing airway smooth muscle.
  • ?Blocks adenosine receptor, antagonizing
    bronchial constriction induced by endogenous
    adenosine.

16
  • Improves respiratory function
  • enhancing diaphragmatic contraction,?????????
    ,???????,????????
  • Positive inotropic effect???????,??????,?????????
    ,????????????????????,?????????

17
Therapeutic uses
  • Acute or chronic asthma,cardiac asthma(?????)
  • Chronic obstructive pulmonary disease(????????)
  • Cardiac edema renal edema (???????)

18
Adverse effects
  • Gastrointestinalnausea, vomiting
  • Cardiovascularpalpitation (??),arrhythmias(????),
    ??,????????????,???????

19
3. Muscarinic antagonists
  • ??M??()??????cGMP??,???????????,????????,????? 

parasympathetic neurons
M 1 and M3 receptors
Ach
Mucus gland secretion increases Airway smooth
muscle cell contracts
20
Muscarinic antagonists
  • ????? ipratropium bromide
  • ??
  • ????????????
  • ??????
  • ??????????

21
4. Glucocorticoids
  • The best established anti-inflammatory drugs for
    the treatment of asthma.
  • Glucocorticoids produce significant
    anti-inflammatory, immunodepressive and
    anti-shock effect, probably by attenuating
    prostaglandin and leukotriene synthesis,
    preventing release of inflammatory mediators and
    decreasing mucus production.
  • Glucocorticoids are usually reserved for patients
    with severe persistent asthma.
  • Inhaled glucocorticoids achieves a significant
    anti-inflammatory effect without causing systemic
    adverse effects.

22
?????? beclomethasone
  • (????????)
  • ?????????
  • ????,???????,????
  • ???,NOT for acute asthmatic attacks!
  • ???????oral fungal infections(??????)?

23
5. Mast Cell Stabilizer
  • Cromolyn Sodium ????
  • (Nasalcrom,Intal)
  • Ketotifen ???
  • Nedocromil Sodium ?????(Tilade)

24
Pharmacologic Effects and Mechanism
  • ????????,????????????(inhibits chloride channels
    and inhibits the release of histamine and other
    autacoids from mast cells)
  • ???????????????? (depress the exaggerated
    neuronal reflexes triggered by irritant receptors
    in the airways)

25
Pharmacologic Effects and Mechanism
  • ??????????????(bronchial hyperreactivity)
    ????????????????????????,????????????????

26
Therapeutic Uses
  • (1) ?????,???????
  • (2) ??????????
  • (3) ??????
  • (4) ???????????
  • (5) ???????

27
Adverse Effects
  • (1)?????????,??????
  • (2)??????,??,??,??,????

28
??? Expectorants
29
??? Expectorants
  • ???(expectorants)
  • ???????,?????????????,??,??????,???????????
    ???
  • ?????
  • ?????????,?????????????????

30
??? Expectorants
  • ???????????
  • ???????,????????
  • ? ??????????????

31
??? Expectorants
  • 1.???????
  • ammonium chloride ???
  • guaifenesine ???????
  • potassium iodide ???
  • ipecac syrup ????
  • ?????????????
  • 2.Mucolytics ?????
  • acetylcysteine ??????,???
  • bromhexine ???,???

32
Classification of Mucolytics
  • (1) ??????????????? ???????????
  • (2) ??????????????????,??????????????????????????
    ?
  • (3) ???
  • (4) ?????????

33
???ammonium chloride
  • ?????,?????,??????????,????,???
  • ?????????
  • ????????????????
  • ??????????????????????????

34
?????? Acetylcysteine (???)
  • ??????N-????,??????????????????,?????????????,????
    ????,?????
  • ?????????????????
  • ????????,???????,??????

35
?????? Acetylcysteine (???)
  • ?????,???????,????????,???????????????????
  • ??????(penicillin)?
  • ????(cephalosporin)?
  • ???(tetracycline)??,??????????

36
???(Antitussives)
37
???(antitussives)
  • ???????,?????????, ?????,??????
  • Two Basic Types of Cough
  • Productive Cough Non-Productive
    Cough
  • Congested cough Dry/Hacking
    cough
  • removes excessive self-feed
  • secretions
  • DONT USE USE
    ANTITISSIVES
  • ANTITUSSIVES

38
???(antitussives)
  • Central antitussives
  • Narcotic ???(Opioids ???)
  • codeine ???
  • Non-narcotic ????(Non-opioids ????)
  • dextromethorphan ????
  • pentoxyverine ????,???
  • Peripheral antitussives
  • benzonatate ????

39
??? codeine
  • Strongly effective cough suppressant, 1/4
    morphine
  • Use for dry cough
  • Produce constipation, nausea and respiratory
    depression (60 mg).
  • Addictive liability
  • Rarely recommended for children.
  • NOT for cough accompanied with excessive
    secretions.

40
Dextromethorphan ????
  • The most popular antitussives
  • Selectively depresses the cough center in the
    medulla
  • 1530 mg 815 mg codeine as an antitussive
  • Therapeutic effect dry cough
  • No respiratory depression, no euphoria and
    physical dependence
  • Adverse effects are mild and rare dizziness,
    drowsiness, nausea

41
??? pentoxyverine
  • Selectively depresses the cough center, 1/3
    codeineatropine-like effect local anesthetic
  • ?????????????????????????
  • Therapeutic effect dry coughgood for children
  • ??????

42
Peripheral Antitussives
  • ??? narcotine
  • ???? benzonatate
  • ???????????????????,??????????

43
Thanks!
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