Pinder R M, Brogden R N, Speight T M, Avery G S
Drugs. 1977 Mar;13(3):161-218. doi: 10.2165/00003495-197713030-00001.
Doxepin is closely related in structure and general pharmacological properties to other tricyclic antidepressant drugs such as amitriptyline and imipramine. It combines antidepressant activity with a sedative effect and in this respect resembles amitriptyline, with which it shares a similar profile of clinical action. The mood elevating effect of doxepin appears to be similar to that of amitriptyline but is probably less marked than that of imipramine and in some studies has been slower to take effect than imipramine. At dosages which have achieved a similar overall response rate, doxepin tends to cause fewer or less troublesome side-effects than imipramine, amitriptyline or amitriptyline-prephenazine. The more marked sedative properties of doxepin make it more useful than imipramine in depressed patients with sleep distrubances and in depression associated with anxiety. The benzodiazepines remain the drugs of choice in anxiety states. but when anxiety is accompained by significant depression, doxepin is more effective than chlordiazepoxide or diazepam. Doxepin is usually well tolerated, and in particular by the elderly and those with cardiovascular disease. Side-effects are similar in nature to those of other tricyclic antidepressants, with dry mouth, drowsiness and constipation being the most common. Postural hypotension is uncommon. Although doxepin appears to cause fewer cardiovascular side-effects in usual therapeutic doses, it has an intrinsic cardiotoxicity on overdosage similar to other tricyclics.
多塞平在结构和一般药理特性上与其他三环类抗抑郁药如阿米替林和丙咪嗪密切相关。它兼具抗抑郁活性和镇静作用,在这方面类似于阿米替林,临床作用也与之相似。多塞平的情绪提升作用似乎与阿米替林相似,但可能不如丙咪嗪明显,且在一些研究中起效比丙咪嗪慢。在达到相似总体有效率的剂量下,多塞平引起的副作用往往比丙咪嗪、阿米替林或阿密替林 - 奋乃静少或轻。多塞平更显著的镇静特性使其在伴有睡眠障碍的抑郁症患者以及与焦虑相关的抑郁症患者中比丙咪嗪更有用。苯二氮䓬类药物仍是焦虑症的首选药物,但当焦虑伴有明显抑郁时,多塞平比氯氮䓬或地西泮更有效。多塞平通常耐受性良好,尤其是老年人和患有心血管疾病的人。副作用本质上与其他三环类抗抑郁药相似,最常见的是口干、嗜睡和便秘。体位性低血压不常见。虽然多塞平在常规治疗剂量下似乎引起较少的心血管副作用,但过量服用时与其他三环类药物一样具有内在的心脏毒性。