神经系统药理5抗精神病药 和 与抗抑郁药.ppt

* * * * * * * 阿米替林：伴失眠的抑郁症患者 氯丙咪嗪：强迫症的首选药 * biogenic amine：生物胺 Hyperpyrexia： * * 对5-HT再摄取的抑制作用选择性强，对其他递质和受体作用甚微。 对抑郁症的疗效与三环类的相当，但安全性高于三环类 * 20世纪90年代初开发研制的，同时抑制5-HT,NE；而对肾上腺素能受体，胆碱能受体，组胺受体无亲和力。 * Noradrenergic and specific serotonergic antidepressant NA和特异性5-HT能抗抑郁药：阻断突触前膜的a2受体，削弱递质释放的抑制作用，使释放增加； NA释放增加后，激活5-HT神经元的a1受体，减弱5-HT1的抑制作用，使5-HT释放进一步增加， 但特异性阻断突触后膜5-HT2A, 5-HT2C and 5-HT3 比SSRIs起效快，安全，耐受性好；适用于各种抑郁症 * * * * 高效价/低剂量：锥体外系作用明显 低效价/高剂量：锥体外系副作用较轻 * 1.黑质-纹状体通路：各种原因减弱该通路的DA功能，可导致帕金森病，反之，出现多动症（D1，D5，D2，D4） 2.调控情绪反应；3.参与认知、思想、感觉、理解和推理能力的调控；I型精神分裂症与这2个通路的DA功能亢进密切相关。(D2，D3，D4) 4.主要调控垂体激素分泌（D2） * 1）The first local anesthetic introduced into medical practice, cocaine, was isolated by Niemann in 1860 and introduced into practice by Koller in 1884 as a topical ophthalmic anesthetic. Despite the fact that its chronic use was associated with psychological dependence (addiction), cocaine was used clinically because it was the only local anesthetic drug available for 30 years. 2）In an attempt to improve the clinical properties of cocaine, Einhorn in 1905 synthesized procaine, which became the dominant local anesthetic for the next 50 years. 3）Subsequently, newer local anesthetics were introduced with the goal of reducing local tissue irritation, minimizing systemic cardiac and CNS toxicity, and achieving a faster onset and longer duration of action. Lidocaine, which is still a widely used local anesthetic, was synthesized in 1943 by L?fgren. 4）易合成，但降低毒性却很难 5）New research into the mechanisms of local anesthetic-induced cardiac and spinal toxicity and identification of alternative drug targets for spinal analgesia (eg, opioid receptors, a2 adrenoceptors, NMDA receptors, N-type calcium channels, and adenosine receptors) suggest that it may be possible to develop safer drugs in the future. 6）To extend the duration of local anesthetic action, a variety of novel delivery systems are in development (eg, polymers, liposomes, and suspensions). * Local anesthetics effectively and rev