抑郁症药物治疗的最新研究进展.pptVIP

* The mechanism of action of SSRIs is based on a selective inhibition on the re-uptake of serotonin. SSRIs differ within their class with regard to the affinity for other neuronal systems like the dopaminergic, muscarinic and histaminergic system. By inhibiting the re-uptake of serotonin the concentration in the synaptic cleft increases, consequently enhancing the increase of neurotransmission activity on all postsynaptic receptors. * The mechanism of action of SNRIs is most comparable to that of TCAs. They act mainly on the NA and 5HT system by re-uptake inhibition but there is little to no affinity for other neuronal systems like the dopaminergic, muscarinic and histaminergic system. By inhibiting the re-uptake of noradrenaline and serotonin the concentration in both synaptic clefts increases resulting in increasing neurotransmission activity, although this may only occur in higher doses. * References: - Pinder RM, J Clin Psychiatry 1997; 58(11): 501-508 - Den Boer Th., J Clin Psychiatry 1996; 57 (suppl 4): 19-25 米氮平通过阻断?2-肾上腺素能自身受体，提升去甲肾上腺素传递。此外，米氮平通过2种具有协同作用的机制提升5羟色胺能传递： 1. 增加去甲肾上腺素供量，刺激5羟色胺能细胞体上的?1-异质受体，从而增加5-HT 细胞点燃 2. 阻断 ?2-肾上腺素能异质受体。 米氮平特异性提升 5-HT1介导的传递，因为米氮平阻断 5-HT2 和 5-HT3 受体。 （ SNRI）文拉法新----选择性NA和5-HT重吸收抑制剂 （75mg/d=SSRI,75-150mg/d=SNRI,150mg/d=SNDRI） noradrenaline increase in neurotransmission re-uptake pump serotonin SNRI Ⅹ Ⅹ ↓ ↓ ↓ ↓ little to no affinity for other neuronal systems like the dopaminergic, muscarinic and histaminergic system 文拉法辛的特点 起效快，服用后2周内即见效。有明显的抗抑郁及抗焦虑作用。有速效剂和缓释剂两种。 推荐剂量:治疗剂量为75－300mg/d,一般为150－200mg/d,分2－3次服。缓释剂每粒75/150mg,有效剂量75-300mg/d，日服一次 适应症 主要为抑郁症、焦虑症及难治性抑郁症。 文拉法辛的特点 不良反应：发生与剂量有关，大剂量（200mg/d)血压可升高 常见不良反应：恶心、口干、出汗、乏力、焦虑、震颤、阳痿、射精障碍。 个别病人出现肝酶、血清胆固醇升高。 禁忌症 严重肝、肾疾病、高血压、癫痫患者慎用。 禁与MAOI和其他5-HT激活药联用。避免出现中枢5-HT综合症。 肾上腺素能和特异性5-HT能抗抑郁药Noradrenergic and Specific Serotonergic Antidepressants（NaSSA） 代表药物 米氮平 NaSSA米氮平 NA 细胞体 5-HT 细胞体 突触前 NA神经元 ?2-自调受体 突触前 5-HT神经元 突触后5-HT神经元 5-HT1 5-HT2a 5-HT3 突触后 NA 神经元 去甲肾上腺