《药理学教学课件：CNS drugs-4》由会员分享，可在线阅读，更多相关《药理学教学课件：CNS drugs-4（28页珍藏版）》请在金锄头文库上搜索。
1、1Chapter 17 Analgesics镇痛药镇痛药Liu YinghuaAssociate professorDepartment of pharmacology p10523Classifications according to the location： Somatic pain (躯体痛躯体痛) Visceral pain 内脏痛内脏痛 Algopsychalia 神经性痛神经性痛 What is pain?4Fast pain (sharp pain): 锐痛锐痛 Occurs immediately and disappeared after eliminating the
2、stimulation, with clear positioning.Dull pain: 钝痛钝痛 Positioning is not clear, long durationSomatic pain ：5Classification of AnalgesicsAnalgesics: on CNS .opioid receptor agonists .opioid receptor partial agonists .others6镇痛药镇痛药 analgesics受体亚型受体亚型镇痛镇痛呼吸抑制呼吸抑制瞳孔瞳孔胃肠运动胃肠运动行为精神行为精神身体依赖身体依赖脊髓以上脊髓以上缩小缩小减少
3、减少欣快欣快镇静镇静脊髓脊髓缩小缩小减少减少欣快欣快镇静镇静脊髓脊髓不安不安镇静镇静Morphine: derived from opium8A boy in the valleys of Hindu Kush mountain range9Morphine 吗啡吗啡 vChemical structure菲核菲核 N-甲基哌甲基哌啶环；啶环；环环A酚羟基；酚羟基；醇羟基；醇羟基；vPharmacokinetics：oral/IV/Inhalation；First pass effect;1/3 bound to plasma protein。甲基甲基-海洛因海洛因甲基甲基-可待因可待因纳纳洛
4、洛酮酮101)Analgesia in severe pain 阿片受体阿片受体 in 脊髓胶质区、丘脑内侧、脑脊髓胶质区、丘脑内侧、脑室及导水管周围灰质室及导水管周围灰质 2)Sedative and euphoria中脑边缘叶、蓝斑中脑边缘叶、蓝斑3)Respiratory depression呼吸中枢呼吸中枢MorphinePharmacological effectsv1.CNs：114)Anti-cough effectscough reflex(咳嗽中枢咳嗽中枢)5)Miosis 缩瞳缩瞳miosis (动眼副交感神经）动眼副交感神经）6)Vomit, body temperatu
5、re Emesis（vomit延髓催吐中枢）延髓催吐中枢）Change thermoregulation center7)Endocrine systemMorphinePharmacological effectsv1.CNs：12MorphinePharmacological effectsv2. Smooth muscle： Gastrointestinal tract: constipationBiliary tract: Oddis sphincter contraction Uterus: extend stage of laborBronchial smooth muscle:
6、contractionHistamine release13Morphine Pharmacological effectsv3.Cardiovascular： no effect on HR. dilate blood vessel, decrease peripheral resistance 释放组胺释放组胺(可被抗组胺药对抗可被抗组胺药对抗) 激激动动孤孤束束核核阿阿片片受受体体，抑抑制制交交感感中中枢枢(可被纳洛酮对抗可被纳洛酮对抗)。v4.Immunosupression(R):HIVExcitation conduction of pain in CNS SPPresynapse
7、PostsynapseGluMechanism of morphineSPPresynapsePostsynapse activate receptorReducing release of SP K+ 外流外流 Ca2+内流内流Endogenous opioid peptide16v与脑内阿片受体结合与脑内阿片受体结合, ,干扰或抑制痛干扰或抑制痛觉的传入和整合等过程。觉的传入和整合等过程。SPSPSPSPEEOpioid receptorEndogenous opioid peptidesSensory neuronsTo CNSEMorphine mechanism of action1
8、71.Analgesia：All kinds of pain 2.Cardiac asthma机制：机制： 扩扩张张血血管管，降降低低外外周周阻阻力力，减减少少心心脏脏前后负荷前后负荷镇静、消除恐惧镇静、消除恐惧 降低呼吸中枢对降低呼吸中枢对CO2 2的敏感性、缓的敏感性、缓 解急促浅表的呼吸。解急促浅表的呼吸。3. Adjuvant drug for anesthesia4. Anti-diarrhea （止泻）（止泻）Morphine Therapeutic uses18vNormal dose：sedation, constipation, nausea and vomiting, ur
9、inary retention, postural hypotension, respiratory depressionvTolerance and dependence： tolerance is due to p-glycoprotein physical dependence: withdrawal syndromeMorphine Adverse effects1920vAcute poisoning：coma pinpoint pupils respiratory depression hypotension (Respiratory paralysis is a major ca
10、use of death）vRescue：Artificial respiration,oxygen intake, Naloxone纳洛酮纳洛酮, Nikethamide.vContraindications：Childbirth and breastfeeding women；asthma, pulmonary heart disease；intracranial hypertension (抑制呼吸致抑制呼吸致CO2聚积引起聚积引起脑血管扩张使颅内压增高脑血管扩张使颅内压增高)Morphine Adverse effects21Codeine 可待因可待因.Less efficient
11、than morphine .Oral .potential for addiction; ;block the action of morphine，induce the withdrawal syndrome in addict; used to acute poisoning and respiratory depression by morphine.vnaltrexone纳曲酮：纳曲酮：similar with naloxone. Higher bioavailability and longer duration, only p.o.28要要 求求【掌握掌握】吗啡的药理作用、作用机制、吗啡的药理作用、作用机制、临床应用、个良反应、成瘾的危害性；临床应用、个良反应、成瘾的危害性；哌替啶的临床应用。哌替啶的临床应用。【熟悉熟悉】阿片受体亚型和特性；可待阿片受体亚型和特性；可待因和人工合成镇痛药美沙酮的作用、因和人工合成镇痛药美沙酮的作用、曲马多的临床应用及不良反应。阿片曲马多的临床应用及不良反应。阿片受体拮抗药：纳洛酮与纳屈酮。受体拮抗药：纳洛酮与纳屈酮。
