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1、Part 12Analgesics,Opioid analgesicsSynthetic opioid analgesicsOther analgesics,1,医疗事业,General Considerations,Pain (疼痛)： 躯体痛快痛，慢痛 内脏痛 情绪反应Analgesia (镇痛)： 选择性抑制疼痛感觉， 不影响意识和其他感觉,2,医疗事业,Pain Classification,Headache(migraine),Acute,Chronic,Pain,Nociceptive,Mixed,Neuropathic,Visceral,Diabetic neuropathy (
2、DN)Post-herpetic neuralgia (PHN)Radiculopathy (RADIC),Cancer painLow back pain,OsteoarthritisRheumatoid arthritisFibromyalgia,IBSPancreatitisBladder painNoncardiac chest painAbdominal pain syndrome,InjuryPostoperativeFlare,An adverse or unpleasant reactionplus the reactions evoked by it,3,医疗事业,4,医疗事
3、业,5,医疗事业,Pain generation and reactions,6,医疗事业,Stimulation and depolarization of sensory nerve endings,7,医疗事业,Pain: peripheral sensory reflex,8,医疗事业,Peripheral mechanisms of pain,9,医疗事业,Peripheral mechanisms of pain,10,医疗事业,Primary & secondary hyperalgesia,11,医疗事业,The perception of somatic pain,1
4、2,医疗事业,The perception and conduction of somatic pain,13,医疗事业,Conduction pathways of pain,14,医疗事业,Cortical locations of pain,15,医疗事业,The fMRI imaging of pain,16,医疗事业,Classification of analgesics：Opioid analgesics (centrally acting) opiates synthetic agentsAntipyretic, analgesic, and anti-inflammatory
5、 drugs (peripherally acting) aspirin, indomethacinOther drugs (for special types of pain) carbamazepine, atropine, nitroglycerin, etc.,General Considerations,17,医疗事业,Morphine 吗啡,Morphine 吗 啡,Heroin 海洛因,A. Opioid Analgesics,18,医疗事业,Opium,19,医疗事业,Morphine:Morphus, the Greek god of dreams,20,医疗事业,1. Ph
6、armacological effects(1) Mechanisms of actions Acting on central opioid receptors receptors receptors receptors,A. Opioid Analgesics,21,医疗事业,ATP,cAMP,Opioid Receptors and Endogenous Ligands,Endorphin,Enkephalin,Dynorphin,K+,a,b,g,a,b,g,=,22,医疗事业,23,医疗事业,Mechanisms of morphine actions,24,医疗事业,Periphe
7、ral mechanisms of morphine actions,25,医疗事业,Central mechanisms of morphine actions: Pain inhibitory system,26,医疗事业,(2) Central nervous system effectsA. Analgesia：maximal analgesic efficacy； relieving unpleasant sensation; euphonia and potential of dependenceB. Depression of respiration: reducing the
8、sensitivity of respiratory center to CO2C. Depression of cough reflexD. Other central effects: miosis, emesis,A. Opioid Analgesics,27,医疗事业,(3) Cardiovascular effectsA. Postural hypotension： Releasing histamine; depressing CVS centersB. Increase of intracranial pressures： Respiratory depression brain
9、 CO2 increase vasodilatation in the brain,A. Opioid Analgesics,28,医疗事业,(4) Effects on smooth musclesA. GI tract：Contispation: increasing resting tone of smooth muscles and sphincters, decreasing propulsive peristalsis and secretions; Biliary tract：Oddis sphincter contraction, increasing the pressure
10、 in the biliary tractB. Respiratory tract：bronchoconstrictionC. Urinary tract：increasing vesical sphincter tone urinary retentionD. Uterus,A. Opioid Analgesics,29,医疗事业,(5) Other effectsA. Immune depressionB. Endocrine effects,A. Opioid Analgesics,30,医疗事业,2. Clinical uses(1) Analgesia the pain of hig
11、h intensity and the pain of terminal illnessCautions: a) obscure the symptoms and the progress of the disease; b) dependence or addiction; c) biliary colic: combined with atropine d) not used for long-term if no clear indications,A. Opioid Analgesics,31,医疗事业,(2) Cardiac asthma (acute left ventricula
12、r failure) As an adjuvant treatment A. Vasodilatation: afterload B. Sedation: anxiety C. Respiratory depression: breathing slowly and deeply(3) Diarrhea Mixture containing opiate,A. Opioid Analgesics,32,医疗事业,3. Adverse effects(1) Side effects(2) Tolerance and dependence psychological and physic depe
13、ndence: addiction withdrawal syndromes or abstinance syndromes,A. Opioid Analgesics,33,医疗事业,(3) Acute intoxication coma, respiratory depression, hypotension, pinpoint pupils reversed by naloxone, an opioid receptor antagonist(4) Contraindications labor and lactation; bronchial asthma and cor pulmona
14、l; increased intracranial pressures; severe hepatic damage,A. Opioid Analgesics,34,医疗事业,35,医疗事业,Morphine toxicity can be reversed by opioid receptor antagonist (naloxone),36,医疗事业,Analgesia; central antitussive,Codeine 可待因,A. Opioid Analgesics,37,医疗事业,B. Synthetic Analgesics,Pethidine 哌替啶Dolantin 度冷丁
15、,38,医疗事业,Pethidine,Morphine,Structures of natural opioid (morphine) and synthetic analgesics (pethidine)哌啶环中的叔氮与叔氮相隔两个碳原子的季碳与季碳相连的苯环,39,医疗事业,B. Synthetic Analgesics,Pethidine1. Pharmacological effectsSimilar to morphine but ineffective for cough and diarrhea, and its metabolite normeperidine has cen
16、tral stimulant effects.2. Clinical uses analgesia; cardiac asthma; preanesthetic medication or artificial hibernation; 3. Adverse effects similar to morphine, convulsion (overdose),40,医疗事业,Fentanyl （芬太尼）high efficacycombined with droperidol: neuroleptanalgesiaMethadone （美沙酮）orally effectivelong-acti
17、ngalso used for displacement in heroin or morphine detoxication,B. Synthetic Analgesics,41,医疗事业,Pentazocine （喷他佐辛, 镇痛新） receptor agonist / receptor partial agonist;low-narcotic analgesic drugpsychotomimetic effects: anxiety, nightmare, hallucinationsTramadol （曲马朵） Relatively weak efficacy and depend
18、ence,B. Synthetic Analgesics,42,医疗事业,Summary of opioid receptor ligands,43,医疗事业,附： 阿片受体拮抗药,Naloxone （纳洛酮）Naltrexone （纳曲酮）Antidotes for acute intoxication of opioidsTreatment of shock and other diseases,Opioid receptor antagonists,44,医疗事业,Summary of opioid receptor ligands,45,医疗事业,Rotundine （l-tetrah
19、ydropalmatine, 罗通定）dl-Tetrahydropalmatine （延胡索乙素） chronic pain sedative effects no addiction,C. Other Analgesics,46,医疗事业,附：癌痛的镇痛治疗,WHO提出的目标： 2000年，使癌症病人不痛！,47,医疗事业,附：癌痛的镇痛治疗,三级镇痛阶梯治疗： 轻度：解热抗炎镇痛药 中度：加用或改用弱阿片药, 辅助治疗药 重度：强阿片药，加非阿片及辅助治疗药 应用原则： 尽可能口服用药 按时规则用药，剂量个体化 辅助措施,48,医疗事业,WHO Analgesic Ladder,49,医疗事业,