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1、China National Pharmaceutical Foreign Trade Corporation Sales Company急慢性中重度疼痛口服药物规范治疗探讨南京军区南京总医院南京军区南京总医院 麻醉科麻醉科 徐建国徐建国 教授教授1China National Pharmaceutical Foreign Trade Corporation Sales Company背景资料背景资料1,泰勒宁的药理药代基础2,泰勒宁的特点3,国外中重度疼痛治疗的概况 A,急性疼痛 B,慢性疼痛2China National Pharmaceutical Foreign Trade Corpo
2、ration Sales Company参考一参考一 泰勒宁的药理药代基础3China National Pharmaceutical Foreign Trade Corporation Sales Company羟 考 酮 OXYCODONEINN阿片类药物：可待因的衍生物阿片类药物：可待因的衍生物4China National Pharmaceutical Foreign Trade Corporation Sales Company化 学 结 构5China National Pharmaceutical Foreign Trade Corporation Sales Company药
3、效 学镇痛（主要应用）镇痛（主要应用）镇咳（次要应用）镇咳（次要应用）镇静镇静肠蠕动减少（止泻，便秘）肠蠕动减少（止泻，便秘）呼吸抑制（大剂量的毒性反应）呼吸抑制（大剂量的毒性反应）6China National Pharmaceutical Foreign Trade Corporation Sales Company镇 痛 作 用 机 制受体激动剂，主要作用在脊髓受体激动剂，主要作用在脊髓与曲马多（双重与曲马多（双重受体作用机制）不同受体作用机制）不同与吗啡有协同作用，无交叉耐受现象与吗啡有协同作用，无交叉耐受现象与与喷喷他他佐佐辛辛（部部分分激激动动剂剂）不不同同；与与喷喷他他佐佐辛有拮
4、抗作用辛有拮抗作用7China National Pharmaceutical Foreign Trade Corporation Sales Company激 动 受 体 的 效 应亚型亚型 效效 应应 痛痛 呼吸呼吸 心率心率 血压血压 瞳孔瞳孔 精神情绪精神情绪 - - - - 欣快，成瘾欣快，成瘾 镇静镇静 ? ? 欣快欣快 幻觉，谵妄幻觉，谵妄 欣快欣快8China National Pharmaceutical Foreign Trade Corporation Sales Company吗啡，可待因，羟考酮止痛作用及成瘾性比较吗啡吗啡可待因可待因羟考酮羟考酮止痛作用止痛作用11/
5、121/41成瘾性成瘾性强强弱于吗啡弱于吗啡最小最小9China National Pharmaceutical Foreign Trade Corporation Sales Company参考二参考二 泰勒宁的特点10China National Pharmaceutical Foreign Trade Corporation Sales Company 胶囊：胶囊： 盐酸羟考酮盐酸羟考酮 5mg 对乙酰氨基酚对乙酰氨基酚 500mg 片剂：片剂： 盐酸羟考酮盐酸羟考酮 5mg 对乙酰氨基酚对乙酰氨基酚 325mg泰勒宁泰勒宁- 氨酚羟考酮氨酚羟考酮11China National Pha
6、rmaceutical Foreign Trade Corporation Sales Company 1 受体结合饱和度不同受体结合饱和度不同 羟考酮羟考酮 用于中到重度疼痛用于中到重度疼痛 吗吗 啡啡 用于重度疼痛用于重度疼痛2 口服生物利用度不同口服生物利用度不同 羟考酮羟考酮 60%60%80%80% 吗吗 啡啡 15%15%64%64% 3 副作用副作用 羟考酮几乎没有致幻作用（羟考酮几乎没有致幻作用（hallucinationhallucination） 其它副作用弱于吗啡其它副作用弱于吗啡 羟考酮与吗啡的主要差别羟考酮与吗啡的主要差别12China National Pharma
7、ceutical Foreign Trade Corporation Sales Company泰勒宁（氨酚羟考酮）镇痛机理 盐酸羟考酮盐酸羟考酮 中枢中枢+外周外周 对乙酰氨基酚对乙酰氨基酚 中枢中枢+外周外周13China National Pharmaceutical Foreign Trade Corporation Sales Company泰勒宁与临床常用阿片类镇痛药比较吗啡，泰勒宁吗啡，泰勒宁度冷丁度冷丁度冷丁吗啡吗啡泰勒宁泰勒宁成瘾性成瘾性镇痛效果镇痛效果曲马多曲马多 曲马多曲马多14China National Pharmaceutical Foreign Trade Cor
8、poration Sales Company羟考酮羟考酮 1、口服、口服10-15分钟起效分钟起效 2、镇痛效果持续、镇痛效果持续4-6小时小时对乙酰氨基酚对乙酰氨基酚 1、口服起效、口服起效15-30分钟分钟 2、镇痛效果持续、镇痛效果持续6-8小时小时 泰勒宁泰勒宁氨酚羟考酮氨酚羟考酮15China National Pharmaceutical Foreign Trade Corporation Sales Company主要副作用不良反应轻微，一般无严重不良反应不良反应轻微，一般无严重不良反应头晕、嗜头晕、嗜 睡睡便秘便秘胃部不适、恶心、呕吐胃部不适、恶心、呕吐肝脏损害肝脏损害16Ch
9、ina National Pharmaceutical Foreign Trade Corporation Sales Company临床应用（FDA）限成人用限成人用关节痛：可关节痛：可与与NSAID合用，效良合用，效良背痛（持续性）：效良背痛（持续性）：效良癌痛：中、重度痛，效佳癌痛：中、重度痛，效佳牙痛：效佳牙痛：效佳神经痛：效良神经痛：效良术后痛：效佳术后痛：效佳17China National Pharmaceutical Foreign Trade Corporation Sales Company临床应用（复方：羟考酮+对乙酰氨基酚）骨关节炎：骨关节炎：优于单独用优于单独用NSA
10、ID术后痛：术后痛： 优于单独应用羟考酮或对乙酰氨基酚优于单独应用羟考酮或对乙酰氨基酚 牙痛：优于单独应用羟考酮或对乙酰氨基酚牙痛：优于单独应用羟考酮或对乙酰氨基酚 术后痛：优于单独应用羟考酮或对乙酰氨基酚术后痛：优于单独应用羟考酮或对乙酰氨基酚 优优点点：有有10%的的患患者者用用可可待待因因无无效效（不不能能转转化化为为吗吗啡啡），用用羟羟考考酮有效酮有效18China National Pharmaceutical Foreign Trade Corporation Sales Company参考三参考三 国外中重度疼痛治疗的概况19China National Pharmaceutic
11、al Foreign Trade Corporation Sales Company慢性疼痛慢性疼痛-癌痛癌痛 90 to 95 percent of all cancer pain can be well controlled using a special set of guidelines .- World Health Organization committee on cancer pain (These guidelines separate pain into levels of intensity and suggest tailoring the strength and p
12、otency of prescribed pain-relieving medications to the intensity. Not all cancer pain requires strong narcotics. But strong pain requires strong medications20China National Pharmaceutical Foreign Trade Corporation Sales Company cancer pain guidelinemoderate pain be treated with a combination of NSAI
13、Ds and weak narcotics such as codeine (Tylenol with codeine), hydrocodone (Vicodin or Lortab), Percocet, Percodan or propoxyphene (Darvon), and severe pain be treated with strong opioids such as morphine, Demerol, Dilaudid, fentanyl (duragesic patches) or methadone in combination with an NSAID. The
14、guidelines also suggest adding an adjuvant medication to these narcotic and nonnarcotic medications when appropriate. These medications-which include steroids, bone-forming, antidepressant and anticonvulsant medications, antihistamines and sedatives-are often useful in treating opioid-resistant pain
15、. For whatever reason, they do relieve pain, although they are not usually labeled as pain relievers.NCCN GUIDELINE 21China National Pharmaceutical Foreign Trade Corporation Sales CompanyAmerican Pain Society Releases New Clinical Guideline For Treatment Of Arthritis PainAmong the major recommendati
16、ons in the APS Arthritis Pain Management Guideline are: All treatment for arthritis should begin with a comprehensive assessment of pain and function For mild to moderate arthritis pain, acetaminophen is the drug of choice for its mild side effects, over-the-counter availability and low cost For mod
17、erate to severe pain from both osteoarthritis and rheumatoid arthritis, COX-2 non-steroidal anti-inflammatory drugs (NSAIDS), such as Celebrex and Vioxx, are the drugs of choice for their pain-relieving potency and absence of gastrointestinal side effects. Use of non-selective NSAIDs should only be
18、considered if the patient is non-responsive to acetaminophen and COX-2 drugs and is not at risk for NSAID-induced GI side effects. Due to the high cost of the COX-2 agents, some patients might benefit from taking non-specific NSAIDS and a medication to moderate GI distress. Opioid medications, such
19、as oxycodone and morphine, are recommended for treating severe arthritis pain for which COX-2 drugs and non-specific NSAIDs do not provide substantial relief. Unless there are medical contraindications, most people with arthritis, including the obese and elderly, should be referred for surgical trea
20、tment when drug therapy is ineffective and function is severely impaired to prevent minimal physical activity. It is advised that surgery be recommended before the onset of severe deformity and advanced muscular deterioration. 22China National Pharmaceutical Foreign Trade Corporation Sales CompanyAc
21、ute Pain Management: Operative or Medical Procedures and Trauma. Clinical Practice Guideline.Half of all patients given conventional therapy for their painmost of the 23 million surgical cases each yeardo not get adequate relief. These patients continue to feel moderate to severe pain. Giving patien
22、ts pain medicine only as needed can result in prolonged delays because patients may delay asking for help. Aggressive prevention of pain is better than treatment because, once established, pain is more difficult to suppress. Patients have a right to treatment that includes prevention of or adequate
23、relief from pain. Physicians need to develop pain control plans before surgery and inform the patient what to expect in terms of pain during and after surgery. Fears of postsurgical addiction to opioids are generally groundless. Patient-controlled medication via infusion pumps is safe In February 19
24、92, AHCPR released a clinical practice guideline .The guideline was developed by an 18-member private-sector panel of pain experts. The multidisciplinary panel reviewed the research literature on pain management to develop the scientific base for the guideline. (After analyzing the results of more than 7,000 published studies, the panel concluded the following)23
