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體位性低血壓和免疫抑制等 2. 連續(xù)多次給藥機(jī)體易產(chǎn)生耐受性和成癮性 ? 耐受性 藥物反復(fù)使用后,機(jī)體對(duì)藥物反應(yīng)強(qiáng)度遞減。安靜時(shí)易誘導(dǎo)入睡,但易喚醒。有鎮(zhèn)靜和欣快癥狀 (2) 鎮(zhèn)靜和欣快 — 激動(dòng)邊緣系統(tǒng)和藍(lán)斑核的阿片受體 消除疼痛引起的焦慮、緊張、恐懼,提高對(duì)疼痛的耐受力。對(duì)慢性鈍痛 急性銳痛 – 作用強(qiáng),選擇性高。 ? 阿片受體激動(dòng)劑:?jiǎn)岱龋?morphine) ? 阿片樣物質(zhì)與受體結(jié)合 抑制腺苷酸環(huán)化酶,神經(jīng)末梢遞質(zhì)釋放減少 (如P物質(zhì)) 阻斷神經(jīng)沖動(dòng)傳遞 鎮(zhèn)痛等效應(yīng)。 與痛覺(jué)的整合和感受有關(guān)的丘腦內(nèi)側(cè)、腦室和導(dǎo)水管周圍灰質(zhì)阿片受體密度高。 異喹啉類:罌粟堿,無(wú)鎮(zhèn)痛作用,有松弛平滑 肌、舒張血管的作用。選擇性的消除或緩解痛覺(jué),減輕由疼痛引起的緊張、焦慮等情緒。 receptor. Some actions are mediated through the δ and κ receptors. Morphine has actions in many systems, such as CNS, eye, respiratory, cardiovascular, gastrointestinal and genitourinary system. These actions are sometimes used for therapeutic purposes and sometimes considered as side effects. ? Codeine is used for suppressing of cough and pain. It is much less potent than morphine. ? Heroin is more lipid soluble than morphine, and , therefore, crosses the bloodbrain barrier rapidly, where it is hydrolyzed into morphine in the brain。第十八章 鎮(zhèn)痛藥 Analgesics 昆明醫(yī)學(xué)院藥理學(xué) 秦渝兵 In the central nervous system there are 181。, δ and κopioid receptors. Most of the actions of narcotic nalgesics are mediated by the opioid 181。 thus it is a predrug. ? Fentanyl is 80 times more potent than morphine but has a short duration of action. It is used by anesthesiologists. ? Methadone is a highly effective analgesic after oral administration and has a much longer duration of action than morphine. Opiates have therapeutic roles in pain relief, and they have antitussive and antidiarrheal acti