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当前位置:药品说明书与价格首页 >> 精神心理 >> 新药推荐 >> FANAPT(iloperidone)-用于治疗精神分裂症

FANAPT(iloperidone)-用于治疗精神分裂症

2011-02-25 13:07:41  作者:新特药房  来源:中国新特药网天津分站  浏览次数:276  文字大小:【】【】【
简介: 美国FDA批准伊潘立酮片Fanapt(iloperidone)上市,用于治疗精神分裂症。本品获准上市标志着对许多现有药物治疗仅部分有效的精神分裂症患者是一新的机会,本品可更好地控制他们的症状。本品获准上市是基 ...

美国FDA批准伊潘立酮片Fanapt(iloperidone)上市,用于治疗精神分裂症。本品获准上市标志着对许多现有药物治疗仅部分有效的精神分裂症患者是一新的机会,本品可更好地控制他们的症状。
本品获准上市是基于伊潘立酮2项纳入3000多例患者的安慰剂对照的主动控制精神分裂症患者症状和安全性的Ⅲ期临床研究结果。伊潘立酮是混合型多巴胺D2/5-羟色胺5HT2A受体阻断剂,属非典型精神抑制药。
伊潘立酮高亲和性地结合于5-羟色胺5HT2A和多巴胺D2、D3受体(Ki值分别为5.6、6.3、7.1 nM)。
伊潘立酮对多巴胺D4和5-羟色胺5HT6、5HT7和去甲肾上腺素NEα1受体 中度亲和性(Ki值分别为25、43、22、36 nM),对5HT1A、多巴胺D1和组胺H1受体低亲和性(Ki值分别为168、216、473 nM),对胆碱能蕈毒碱受体无可检测的亲和性(Ki>1 000 nM)。
伊潘立酮通过对多巴胺D2、D3、5-羟色胺5HT1A 和去甲肾上腺素NEα1/α2c受体阻断发挥作用。伊潘立酮代谢物P88的亲和性通常≤母体化合物,而代谢物P95仅对5HT2A、NEα1A、NEα1B、NEα1D、NEα2C受体有亲和性(Ki值分别为3.91、4.7、2.7、4.7 nM)。            
 伊潘立酮治疗精神分裂症的疗效经过2项安慰剂对照短期(4周和6周)临床研究的评价。两项研究遴选的患者符合DSM-Ⅲ/Ⅳ标准,伊潘立酮每日12~24 mg控制精神分裂症症状显著优于安慰剂。伊潘立酮推荐剂量范围为12 ~24 mg/日.
本品剂量规格:1 mg、2 mg、4 mg、6 mg、8 mg、10 mg和12 mg/片。辅料:乳糖一水物,微晶纤维素,羟丙基甲基纤维素,交联聚乙烯吡洛烷酮,硬脂酸镁和微粉硅胶。

制造商:
诺华制药公司

药理分类:
抗精神病药物(哌啶- benzisoxazole非典型)

活性成分(补):
Iloperidone 1毫克,2毫克,4毫克,6毫克,8mg,10毫克,12mg;标签。
指示(补):
急性治疗精神分裂症。

药理作用:
Iloperidone是一种非典型的抗精神病药物,其疗效在治疗精神分裂症可能在多巴胺2型和3(D2和D3)和羟色胺2A型(5 - HT2A受体)受体在中枢神经系统由于它的对立。

临床试验:
两个安慰剂和积极的控制进行了临床试验,以评估在治疗精神分裂症的iloperidone疗效。一个6周的试验比较了两种剂​​量的iloperidone(12-16mg/day和20-24mg/day后滴定法),安慰剂和药物的主动控制范围。主要终点是从基线简明精神病评定量表(BPRS)在治疗(42天)年末总分数的变化。为iloperidone两种剂量范围均优于安慰剂。在第2周,有效控制精神科药物似乎优于iloperidone。这可能被解释为更快速滴定法,这对于该药物成为可能。

在为期4周的审讯后,滴定iloperidone 24mg/day安慰剂进行了比较和主动控制的药物还需要一个初始滴定阶段。主要疗效终点是在对阳性和阴性症状量表(PANSS)的总分在治疗基线(28天)结束的变化。在这项研究中,iloperidone明显优于安慰剂,也有类似的功效有效控制药物。

法律分类:
接收

成人:
≥18yrs:1天1毫克每天两次,两次第2天2毫克,每日4毫克每日两次,第3天,4天两次6毫克,每日8mg两次5天,每天10毫克两次,第6天,每天12mg,每日两次7;目标范围6 - 12mg,每天两次,最大24mg/day。降低剂量1 / 2或CYP3A4的伴随CYP2D6的强抑制剂。返滴定,如果治疗停止“3天。定期重新评估。

儿童:
“18yrs:不推荐。

警告/注意事项:
心动过缓,低血钾,低镁血症,先天性QT间期延长,最近的心肌梗塞,无偿性心力衰竭,心律失常:避免(对扭转性室速德pointes的/突然死亡的风险)。心或脑血管疾病。尤监测电解质。钾,镁+ +。肝功能不全:不推荐。糖尿病或(取得基线空腹血糖)的危险因素。监控血糖。历史乳腺癌或癫痫发作。体位性低血压。已存在的低白细胞计数或白血球低下/中性粒细胞减少的历史:在第一数个月的治疗央行监测;停止,如果白细胞下降。暴露在高温下。脱水。自杀倾向。写实际金额最小的接收。抗精神病药物恶性症候群监控。老年人(老年痴呆症有关的精神病不)。妊娠(Cat.C)。哺乳母亲:不推荐。

互动(补):
避免这种情况导致QT间期延长(如奎尼丁,胺碘酮,索他洛尔,普鲁卡因胺,氯丙嗪,甲硫达嗪,莫西沙星,美沙酮)等药物。抗高血压药物,会增强。注意用酒精,中枢神经系统抑制剂。 Potentiated由CYP2D6的(如氟西汀,帕罗西汀)或CYP3A4的(例如,克拉霉素,酮康唑)抑制剂。

不良反应(补):
头晕,口干,乏力,鼻塞,体位性低血压,嗜睡,心动过速,体重增加; QT间期延长(QTc的停止,如果> 500msec仍然存在),阴茎异常勃起,抗精神病药物恶性症候群,迟发性运动障碍,高血糖,吞咽困难。

如何提供:
制表- 60
滴定包- 8(2 × 1毫克,2 × 2毫克,2 × 4毫克,2 × 6毫克)

最后更新:
二〇一〇年十一月三十日

Manufacturer:

 

Novartis Pharmaceuticals Corp

Pharmacological Class:

Antipsychotic (piperidinyl-benzisoxazole atypical)

Active Ingredient(s):

Iloperidone 1mg, 2mg, 4mg, 6mg, 8mg, 10mg, 12mg; tabs.

The FDA has approved the atypical antipsychotic, Fanapt (iloperidone, from Vanda Pharmaceuticals), a mixed dopamine D2/serotonin 5HT2A receptor antagonist, for the acute treatment of schizophrenia in adult patients. This approval was based on data from two Phase III, placebo-controlled clinical studies comparing Fanapt to placebo and active control in more than 3,000 patients with schizophrenia. Fanapt was shown to be superior to placebo in controlling symptoms of schizophrenia based on the Positive and Negative Syndrome Scale (PANSS) total score and the Brief Psychiatric Rating Scale (BPRS) total score.

Fanapt is expected to be available later this year.

Indication(s):

Acute treatment of schizophrenia.

Pharmacology:

Iloperidone is an atypical antipsychotic agent whose efficacy in the treatment of schizophrenia may be due to its antagonism at dopamine types 2 and 3 (D2, D3) and serotonin type 2A (5-HT2A) receptors in the CNS.

Clinical Trials:

Two placebo- and active-controlled clinical trials were conducted to assess the efficacy of iloperidone in the treatment of schizophrenia. A 6-week trial compared two doses ranges for iloperidone (12–16mg/day and 20–24mg/day, after titration) to placebo and an active control drug. The primary endpoint was the change from baseline on the Brief Psychiatric Rating Scale (BPRS) total score at the end of treatment (day 42). Both dose ranges for iloperidone were superior to placebo. Within the first 2 weeks, the active control psychiatric drug appeared to be superior to iloperidone. This may be explained by the more rapid titration that was possible for that drug.

In a 4-week trial, iloperidone 24mg/day after titration was compared to placebo and an active control drug which also required an initial titration phase. The primary efficacy endpoint was the change in baseline on the Positive and Negative Syndrome Scale (PANSS) total score at the end of treatment (day 28). In this study, iloperidone was superior to placebo and had similar efficacy to the active control medication.

Legal Classification:

Rx

Adults:

≥18yrs: 1mg twice daily on day 1, 2mg twice daily on day 2, 4mg twice daily on day 3, 6mg twice daily on day 4, 8mg twice daily on day 5, 10mg twice daily on day 6, 12mg twice daily on day 7; target range 6–12mg twice daily; max 24mg/day. Reduce dose by 1/2 with concomitant strong inhibitors of CYP2D6 or CYP3A4. Retitrate if therapy suspended >3 days. Reassess periodically.

Children:

<18yrs: not recommended.

Warnings/Precautions:

Bradycardia, hypokalemia, hypomagnesemia, congenital QT prolongation, recent MI, uncompensated heart failure, arrhythmias: avoid (risk of torsades de pointes/sudden death). Cardio- or cerebrovascular disease. Monitor electrolytes esp. K+, Mg++. Hepatic impairment: not recommended. Diabetes or risk factors (obtain baseline fasting blood sugar). Monitor for hyperglycemia. History of breast cancer or seizures. Orthostatic hypotension. Pre-existing low WBC count or history of leukopenia/neutropenia: monitor CBC during 1st few months of therapy; discontinue if WBCs decline. Exposure to extreme heat. Dehydration. Suicidal tendencies. Write Rx for the smallest practical amount. Monitor for neuroleptic malignant syndrome. Elderly (not for dementia-related psychosis). Pregnancy (Cat.C). Nursing mothers: not recommended.

Interaction(s):

Avoid other drugs that cause QT prolongation (eg, quinidine, amiodarone, sotalol, procainamide, chlorpromazine, thioridazine, moxifloxacin, methadone). May potentiate antihypertensives. Caution with alcohol, CNS depressants. Potentiated by inhibitors of CYP2D6 (eg, fluoxetine, paroxetine) or CYP3A4 (eg, clarithromycin, ketoconazole).

Adverse Reaction(s):

Dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence, tachycardia, increased weight; QT prolongation (discontinue if QTc >500msec persists), priapism, neuroleptic malignant syndrome, tardive dyskinesia, hyperglycemia, dysphagia.

How Supplied:

Tabs—60
Titration pack—8 (2 x 1mg, 2 x 2mg, 2 x 4mg, 2 x 6mg)

Last Updated:

11/30/2010

责任编辑:admin


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