导读:褪黑索类似物阿戈美拉汀agomelatine,既是首个褪黑素受体激动剂,也是5-羟色胺2C(S-HTx)受体拮抗剂。动物试验与临床研究表明该药有抗抑郁、抗焦虑、调整睡眠节律及调节生物钟作用,同时其不良反应少,对性功能无不良影. 褪黑索类似物阿戈美拉汀agomelatine,既是首个褪黑素受体激动剂,也是5-羟色胺2C(S-HTx)受体拮抗剂。动物试验与临床研究表明该药有抗抑郁、抗焦虑、调整睡眠节律及调节生物钟作用,同时其不良反应少,对性功能无不良影响,也未见撤药反应. 作用机制 动物试验 临床疗效 2005年Olie进行的2项双盲安慰剂平行对照研究,MDD患者随机接受阿戈美拉汀一日25mg或安慰剂,2周后病情改善不明显者剂量增加至一日50mg,为期6周,结果表明,阿戈美拉汀疗效明显优于安慰剂,药物剂量增加至一日50mg者2周后获得类似疗效,并且耐受性良好. 对睡眠的影响 褪黑素对睡眠以及生物周期节律有调节作用,阿戈美拉汀是否也有类似的作用引起人们的关注,尤其是很多抑郁症患者均存在睡眠障碍。动物试验已证实阿戈美拉汀具有与褪黑素类似的调节睡眠的作用。一项针对门诊MDD患者的研究比较了阿戈美拉汀一日25--5Omg与文拉法辛一日75一15Dmg的疗效,结果显示,两者治疗抑郁疗效类似,但阿戈美拉汀在Leeds睡眠评估问卷(LSEQ)量表的2项评分(入睡和睡眠质量)上较文拉法辛改善明显,并且观察发现,这种对睡眠的改善作用在用药1周时即显现,且对白天的警觉性无影响。 另一项标签开放性研究评估了阿戈美拉汀对MDD患者睡眠结构的影响。15例HAMD评分≥20的门诊MDD患者服用阿戈美拉汀一日25mg,为期42日,在第7,14,42日分别进行睡眠多导研究。结果显示,治疗42日患者的睡眠效率、睡后醒转次数及SW5总量均有改善,SWS在开始的那个睡眠周期改善尤为显著。从第7日起,SWS在最开始的4个睡眠循环中减少,在14日以前,δ波的比例增加。REM潜伏期、总量及密度均未见改变。提示阿戈美拉汀增加睡眠的连续性与质量,使在睡眠周期循环中的分配及6波的强度正常化。安全性与耐受性 安全性与耐受性 抗抑郁药物对性功能的影响已引起相当的重视,TCA、SSRI、选择性5-HT及去甲肾上腺素再摄取抑制剂(SNRI)等均存在对性功能不同程度的影响,但阿戈美拉汀对性功能的影响较小。与文拉法辛相比,阿戈美拉汀组性功能的各项心理与躯体症状评定均优于文拉法辛。 Valdoxan (Agomelatine) How does Valdoxan (Agomelatine) work: Valdoxan (Agomelatine) is the first in a new class of antidepressants called melatonergic agonists. This novel approach to treating depression has many advantages over current treatments. Valdoxan not only works effectively as an antidepressant, it has been shown to improve sleep/wake cycles without causing daytime sleepiness. Additionally, it doesn?t appear to have the side effect of loss of sexual desire or problems with stopping the drug (discontinuation symptoms) that other antidepressants do. Valdoxan interacts with receptors for melatonin and with melatonin antagonist receptors. Scientists believe that the dual action may be responsible for the re-regulation of the sleep/wake cycle. One of the most exciting properties of Valdoxan is that it relieves depression as well as drugs like Effexor and Paxil, but it does not cause loss of sexual function or the discontinuation symptoms that are often associated with SSRI (serotonin specific reuptake inhibitors) antidepressants. Dosage & Administration: A dose of 25 mg of Valdoxan (Agomelatine) once daily in the hours before bed effectively treats major depressive disorders. Further studies showed that it works in adults of all ages and in elderly people. Another clinical trial showed that Valdoxan has a similar effectiveness to venlafaxine, which is commonly known as Effexor. Side Effects:
Precautions: Valdoxan (Agomelatine) should not be used in patients who have liver problems like cirrhosis or active liver disease. It should not be taken by patients who are taking medicines that would slow down the breakdown of Valdoxan such as fluvoxamine (trade name Luvox) and the antibiotic ciprofloxacin (trade name Cipro). It should also not be taken by patients with age related dementia. Further Information: In January 2009 Valdoxan was granted marketing approval in the European Union for treatment of adult patients with major depression. The drug has not yet attained approval from the U.S. Food and Drug Administration as of mid-2009. Valdoxan was developed by French pharmaceutical company Servier. In the United States, Novartis has exclusive rights to develop and market the drug. |
阿戈美拉汀口服片剂-是一种全新作用机制的抗抑郁药简介:
导读:褪黑索类似物阿戈美拉汀agomelatine,既是首个褪黑素受体激动剂,也是5-羟色胺2C(S-HTx)受体拮抗剂。动物试验与临床研究表明该药有抗抑郁、抗焦虑、调整睡眠节律及调节生物钟作用,同时其不良反应 ... 责任编辑:admin |
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