Jarema Marek, Dudek Dominika, Landowski Jerzy, Heitzman Janusz, Rabe-Jabłońska Jolanta, Rybakowski Janusz
III Klinika Psychiatryczna IPiN w Warszawie.
Psychiatr Pol. 2011 Jul-Aug;45(4):611-25.
The pharmacological properties and possible clinical use of trazodon in the treatment of depression are presented. Trazodon is the only antidepressant from the SARI (Serotonin Antagonists and Reuptake Inhibitors) group available in Poland. It has a wide pharmacodynamic profile (being an antagonist of 5-HT2A and 5-HT2C serotoninergic receptors, alpha1 and alpha2 adrenergic receptors as well as H1 histaminergic receptors, and in higher doses it blocks the SERT serotonine transporter) which explains its wide therapeutic spectrum ranging from symptomatic treatment, through the potentialization of other drugs activity, all the way to monotherapy of depressive syndromes. An especially complex action on the serotoninergic system results in the lack of unwanted side-effects during treatment with trazodon (e.g. sexual dysfunction, significant body weight gain), which may be present during the treatment with other drugs (selective serotonin reuptake inhibitors). It is metabolised by the CYP450 isoenzyme: mainly the 2D6 and 3A4. This requires its dose to be adjusted when administered simultaneously with other drugs influencing the activity of those isoenzymes. Trazodon CR is an orally administered controlled release form, which simplifies its dosage and reduces the risk of adverse effects. Usually doses of 75 to 600mg daily are used; in the elderly those doses should be lower. Trazodon turned out to be effective in the treatment of various depressive syndromes, amongst them depression with insomnia, with anxiety and unrest, as well as depression in the elderly. In the recommended dose spectrum, trazodon is well tolerated. Unwanted adverse effects of the drug appear rarely and they are: somnolence, dizziness, gastrointestinal dysfunctions, and dry mouth.
本文介绍了曲唑酮治疗抑郁症的药理特性及可能的临床应用。曲唑酮是波兰唯一可用的5-羟色胺拮抗剂和再摄取抑制剂（SARI）类抗抑郁药。它具有广泛的药效学特性（是5-HT2A和5-HT2C血清素能受体、α1和α2肾上腺素能受体以及H1组胺能受体的拮抗剂，高剂量时可阻断血清素转运体SERT），这解释了其广泛的治疗谱，从对症治疗、增强其他药物活性，到抑郁症综合征的单一疗法。对血清素能系统的特别复杂作用导致曲唑酮治疗期间不会出现不良副作用（如性功能障碍、显著体重增加），而其他药物（选择性血清素再摄取抑制剂）治疗期间可能会出现这些副作用。它由CYP450同工酶代谢：主要是2D6和3A4。与影响这些同工酶活性的其他药物同时给药时，需要调整其剂量。曲唑酮控释片（Trazodon CR）是一种口服控释剂型，简化了用药剂量并降低了不良反应风险。通常每日剂量为75至600毫克；老年人剂量应更低。曲唑酮已被证明对各种抑郁症综合征有效，包括伴有失眠、焦虑和不安的抑郁症以及老年抑郁症。在推荐剂量范围内，曲唑酮耐受性良好。该药物的不良副作用很少出现，包括嗜睡、头晕、胃肠功能紊乱和口干。
