Figgitt D P, McClellan K J
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 2000 Oct;60(4):925-54. doi: 10.2165/00003495-200060040-00006.
Fluvoxamine is a potent and selective serotonin reuptake inhibitor (SSRI) that has little or no effect on other monoamine reuptake mechanisms. Relative to other SSRIs, fluvoxamine is a weak inhibitor of cytochrome P450 (CYP) 2D6, a moderate inhibitor of CYP2C19 and CYP3A4 and a potent inhibitor of CYP1A2. In randomised, double-blind trials. fluvoxamine 100 to 300 mg/day for 6 to 10 weeks significantly reduced symptoms of obsessive-compulsive disorder (OCD) compared with placebo. Response rates of 38 to 52% have been reported with fluvoxamine, compared with response rates of 0 to 18% with placebo. In patients with OCD, fluvoxamine had similar efficacy to that of clomipramine and, in smaller trials, the SSRIs paroxetine and citalopram and was significantly more effective than desipramine. Maintenance therapy with fluvoxamine may reduce the likelihood of relapses in up to 67% of patients with OCD. Fluvoxamine < or = 300 mg/day for 6 to 8 weeks was as effective as imipramine in patients with panic disorder, and significantly more effective than placebo. In addition, treatment with fluvoxamine < or = 300 mg/day for > or = 8 weeks improved symptoms of social phobia (social anxiety disorder), post-traumatic stress disorder (PTSD), pathological gambling, compulsive buying, trichotillomania, kleptomania, body dysmorphic disorder, eating disorders and autistic disorder. Large trials comparing the efficacy of fluvoxamine and other SSRIs in patients with anxiety disorders are warranted. Fluvoxamine is generally well tolerated; in postmarketing studies, nausea was the only adverse event occurring in >10% of patients with less commonly reported events including somnolence, asthenia, headache, dry mouth and insomnia. Fluvoxamine is associated with a low risk of suicidal behaviour, sexual dysfunction and withdrawal syndrome. Fewer anticholinergic or cardiovascular events are associated with fluvoxamine than tricyclic antidepressants. Although comparative data are lacking, the tolerability profile of fluvoxamine appears to be broadly similar to those of other SSRIs.
Fluvoxamine has demonstrated short term efficacy in the treatment of OCD, panic disorder, social phobia, PTSD and in a range of obsessive-compulsive spectrum disorders. The drug is as effective as clomipramine in patients with OCD but appears to have a better tolerability profile. On the basis of current treatment guidelines, fluvoxamine, like other SSRIs, is recommended as first-line treatment for a number of anxiety disorders. It appears to offer some pharmacokinetic advantages and a different drug interaction profile to the other SSRIs with a broadly similar spectrum of adverse events. However, direct comparisons are required to assess the relative efficacy and tolerability of the different agents of this drug class.
氟伏沙明是一种强效且选择性的5-羟色胺再摄取抑制剂(SSRI),对其他单胺再摄取机制几乎没有影响。相对于其他SSRI,氟伏沙明是细胞色素P450(CYP)2D6的弱抑制剂,CYP2C19和CYP3A4的中度抑制剂以及CYP1A2的强效抑制剂。在随机双盲试验中,与安慰剂相比,氟伏沙明100至300毫克/天,持续6至10周可显著减轻强迫症(OCD)症状。据报道,氟伏沙明的有效率为38%至52%,而安慰剂的有效率为0%至18%。在OCD患者中,氟伏沙明与氯米帕明疗效相似,在较小规模试验中,与SSRI帕罗西汀和西酞普兰疗效相似,且显著优于地昔帕明。用氟伏沙明维持治疗可使高达67%的OCD患者复发可能性降低。对于惊恐障碍患者,氟伏沙明≤300毫克/天,持续6至8周与丙咪嗪疗效相同,且显著优于安慰剂。此外,氟伏沙明≤300毫克/天,持续≥8周可改善社交恐惧症(社交焦虑症)、创伤后应激障碍(PTSD)、病态赌博、强迫性购物、拔毛癖、盗窃癖、躯体变形障碍、饮食失调和自闭症的症状。有必要进行大型试验比较氟伏沙明与其他SSRI在焦虑症患者中的疗效。氟伏沙明一般耐受性良好;在上市后研究中,恶心是唯一在超过10%患者中出现的不良事件,较少报告的事件包括嗜睡、乏力、头痛、口干和失眠。氟伏沙明与自杀行为、性功能障碍和戒断综合征风险较低相关。与三环类抗抑郁药相比,氟伏沙明引起的抗胆碱能或心血管事件较少。虽然缺乏比较数据,但氟伏沙明的耐受性特征似乎与其他SSRI大致相似。
氟伏沙明已证明在治疗OCD、惊恐障碍、社交恐惧症、PTSD以及一系列强迫谱系障碍方面具有短期疗效。该药物在OCD患者中与氯米帕明疗效相同,但耐受性似乎更好。根据当前治疗指南,氟伏沙明与其他SSRI一样,被推荐作为多种焦虑症的一线治疗药物。它似乎具有一些药代动力学优势,并且与其他SSRI具有不同的药物相互作用特征,不良事件谱大致相似。然而,需要进行直接比较以评估该药物类别中不同药物的相对疗效和耐受性。