氨酚羥考酮.ppt

1、1,急慢性中重度疼痛口服藥物規(guī)范治療探討,南京軍區(qū)南京總醫(yī)院 麻醉科 徐建國(guó) 教授,2,背景資料,1,泰勒寧的藥理藥代基礎(chǔ) 2,泰勒寧的特點(diǎn) 3,國(guó)外中重度疼痛治療的概況 A,急性疼痛 B,慢性疼痛,3,參考一,泰勒寧的藥理藥代基礎(chǔ),4,羥 考 酮,OXYCODONEINN 阿片類藥物：可待因的衍生物,5,化 學(xué) 結(jié) 構(gòu),6,藥 效 學(xué),鎮(zhèn)痛（主要應(yīng)用） 鎮(zhèn)咳（次要應(yīng)用） 鎮(zhèn)靜 腸蠕動(dòng)減少（止瀉，便秘） 呼吸抑制（大劑量的毒性反應(yīng)）,7,鎮(zhèn) 痛 作 用 機(jī) 制,受體激動(dòng)劑，主要作用在脊髓 與曲馬多（雙重受體作用機(jī)制）不同 與嗎啡有協(xié)同作用，無交叉耐受現(xiàn)象 與噴他佐辛（部分激動(dòng)劑）不同；與噴他佐

2、辛有拮抗作用,8,激 動(dòng) 受 體 的 效 應(yīng),亞型 效 應(yīng) 痛 呼吸 心率 血壓 瞳孔 精神情緒 - - 欣快，成癮 鎮(zhèn)靜 ? 欣快 幻覺，譫妄 欣快,9,嗎啡，可待因，羥考酮止痛作用及成癮性比較,10,參考二,泰勒寧的特點(diǎn),11,膠囊： 鹽酸羥考酮 5mg 對(duì)乙酰氨基酚 500mg 片劑： 鹽酸羥考酮 5mg 對(duì)乙酰氨基酚 325mg,泰勒寧- 氨酚羥考酮,12,1 受體結(jié)合飽和度不同 羥考酮 用于中到重度疼痛 嗎 啡 用于重度疼痛 2 口服生物利用度不同 羥考酮 60%80% 嗎 啡 15%64% 3 副作用 羥考酮幾乎沒有致幻作用（hallucination） 其它副作用弱于嗎啡,羥考酮

3、與嗎啡的主要差別,13,泰勒寧（氨酚羥考酮）鎮(zhèn)痛機(jī)理,鹽酸羥考酮 中樞+外周 對(duì)乙酰氨基酚 中樞+外周,14,泰勒寧與臨床常用阿片類鎮(zhèn)痛藥比較,嗎啡，泰勒寧,度冷丁,度冷丁,嗎啡,泰勒寧,成癮性,鎮(zhèn)痛效果,曲馬多,曲馬多,15,羥考酮 1、口服10-15分鐘起效 2、鎮(zhèn)痛效果持續(xù)4-6小時(shí) 對(duì)乙酰氨基酚 1、口服起效15-30分鐘 2、鎮(zhèn)痛效果持續(xù)6-8小時(shí),泰勒寧氨酚羥考酮,16,主要副作用,不良反應(yīng)輕微，一般無嚴(yán)重不良反應(yīng) 頭暈、嗜 睡 便秘 胃部不適、惡心、嘔吐 肝臟損害,17,臨床應(yīng)用（FDA）,限成人用 關(guān)節(jié)痛：可與NSAID合用，效良 背痛（持續(xù)性）：效良 癌痛：中、重度痛，效佳

4、牙痛：效佳 神經(jīng)痛：效良 術(shù)后痛：效佳,18,臨床應(yīng)用（復(fù)方：羥考酮+對(duì)乙酰氨基酚）,骨關(guān)節(jié)炎：優(yōu)于單獨(dú)用NSAID 術(shù)后痛： 優(yōu)于單獨(dú)應(yīng)用羥考酮或?qū)σ阴０被?牙痛：優(yōu)于單獨(dú)應(yīng)用羥考酮或?qū)σ阴０被?術(shù)后痛：優(yōu)于單獨(dú)應(yīng)用羥考酮或?qū)σ阴０被?優(yōu)點(diǎn)：有10%的患者用可待因無效（不能轉(zhuǎn)化為嗎啡），用羥考酮有效,19,參考三,國(guó)外中重度疼痛治療的概況,20,慢性疼痛-癌痛,90 to 95 percent of all cancer pain can be well controlled using a special set of guidelines . - World Health Orga

5、nization committee on cancer pain (These guidelines separate pain into levels of intensity and suggest tailoring the strength and potency of prescribed pain-relieving medications to the intensity. Not all cancer pain requires strong narcotics. But strong pain requires strong medications,21,cancer pa

6、in guideline,moderate pain be treated with a combination of NSAIDs 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 (du

7、ragesic patches) or methadone in combination with an NSAID. The 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

8、and sedatives-are often useful in treating opioid-resistant pain. For whatever reason, they do relieve pain, although they are not usually labeled as pain relievers. NCCN GUIDELINE,22,American Pain Society Releases New Clinical Guideline For Treatment Of Arthritis Pain,Among the major recommendation

9、s 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 moder

10、ate 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 co

11、nsidered 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 as

12、 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 treatm

13、ent 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.,23,Acute Pain Management: Operative or Medical Procedures and Trauma. Clini

14、cal 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 patients pain medicine only as needed can result in prolonged delays becaus

15、e 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 relief from pain. Physicians need to develop pain control plans befor

16、e 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 1992, AHCPR released a clinical practice guideline .The guideline was developed by an 18-member private-sector p