支气管痉挛【精品课件】.pptVIP

Drugs for Respiratory System GAO Fen-Fei Introduction Symptom of respiratory system: no sputum---antitussives Cough sputum --- expectorants Asthma ----- antiasthmatic drugs ANTITUSSIVES Classification: Central antitussives Dependent central antitussives Independent central antitussives Peripheral antitussives Dependent Central Antitussives Opioid alkaloids. Morphine is the most effective drug for the suppression of cough, but have addiction. Mechanism: suppressing of cough center Codeine Selectively suppress cough center in medulla oblongata(延髓). Potency: Suppression of cough: ≈1/10 of morphine Analgesia: ≈1/7 of morphine Respiratory depression, constipation, tolerance, dependence ＜ that of morphine Pharmacokinetics: Well absorbed from oral and injection. 10﹪ converted to morphine through demethyl. Clinical Uses: Dry cough Adverse Reactions: Respiratory suppression in high dose; Tolerance and physical dependence with frequently repeated administration; Suppress secretion of bronchial gland and movement of cilia. Independent Central Antitussives Stereoisomers of opioid molecules that are devoid of analgesic effects and addiction liability. Classification: -orphan(吗啡南类)-antitussives : dextromethorphan(右美沙芬) Amido(胺基)-antitussives: pentoxyverine(喷托维林;咳必清), clofedanol(氯苯达诺;敌退咳) piperidine(哌啶基)-antitussives: cloperastine(氯哌斯汀) morpholine(吗啉基)-antitussives: promolate(普罗吗酯), fominoben(福米诺苯); Others: eprazinone(依普拉酮), zipeprol(齐培丙醇). Dextromethorphan Dextrorotatory stereoisomers of a methylated derivative of levorphanol(羟甲左吗南). Clinical Use: Dry cough. Often + Antihistamine drug Pentoxyverine Suppression of cough: ≈1/3 of codeine. Direct suppression of cough center Atropine-like action and local anesthesia action. Cloperastine Derivative of diphenhydramine(苯海拉明). Suppression of cough center Blocking H1-receptor Peripheral Antitussives Inhibiting receptor, afferent nerve, efferent nerve of cough reflex arc → cough suppressio