药品信息:
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VRAYLAR(cariprazine 中文药名:卡比米嗪胶囊)-获美国FDA批准新药治疗精神分裂和双相躁郁症
近日,美国FDA批准Forest Laboratories和Actavis Pharma的Vraylar(cariprazine,卡利拉嗪)上市,治疗成人精神分裂症(Schizophrenia)和狂躁型抑郁症(bipolar disorder)。
cariprazine是一种口服、每日一次的非典型抗精神病药物。在美国,该药已于2015年获准以品牌名Vraylar上市销售,目前已获批的适应症包括: (1)用于双相I型情感障碍(狂躁型抑郁症)成人患者狂躁或混合发作的紧急治疗,推荐的给药剂量范围为3-6mg/天; (2)用于精神分裂症成人患者的治疗,推荐的给药剂量范围为1.5-6.0mg/天。在欧盟,该药以品牌名Reagila上市销售。
批准日期:2015年9月17日;公司:Allergan和Gedeon Richter plc
VRAYLAR(卡比米嗪 cariprazine)胶囊,供口服使用
美国初次批准:2015
作用机制
不知道卡比米嗪在精神分裂症和I型双相障碍的作用机制。但是,卡比米嗪的疗效可能被通过一个部分激动剂活性在中枢多巴胺D2和五羟色胺5-HT1A受体和在五羟色胺5-HT2A受体拮抗剂活性的组合介导。卡比米嗪形成两个主要代谢物,去甲基卡比米嗪(DCAR)和二去甲基卡比米嗪(DDCAR),在体外有受体结合图形与母体药物受体结合图形相似。
适应症和用途
VRAYLAR是一种非典型抗精神病药物适用为:
⑴精神分裂症的治疗
⑵ 双相Ⅰ型障碍相关躁狂或混合发作的急性治疗。
剂量和给药方法
⑴给予VRAYLAR 1天1次有或无食物
● 精神分裂症 开始剂量 1.5mg/day 推荐剂量 1.5mg至6mg/day
●双极性情感障碍 开始剂量 1.5mg/day 推荐剂量 3mg至6mg/day
⑵ 每天剂量6mg以上不提供显著获益但剂量相关不良反应的风险增加
剂型和规格
胶囊:1.5mg,3mg,4.5mg,和6mg
禁忌证
对VRAYLAR已知超敏性
警告和注意事项
⑴心血管不良反应在老年患者有痴呆-相关精神病:心血管不良反应的发生率增加(如,卒中,短暂性脑缺血发作)
⑵ 抗精神病药物恶性症候群:处理用立即终止和密切监视
⑶ 迟发性运动障碍:如适当终止
⑷ 晚发生不良反应:因为VRAYLAR的长半衰期,开始VRAYLAR后监视不良反应和患者反应共几周和随每次剂量变化。
⑸ 代谢变化:监视高血糖/糖尿病,血脂异常和体重增量
⑹ 体位性低血压:监视心率和血压和警告有已知心血管或心血管病患者,和脱水或晕厥风险
不良反应
最常见不良反应(发生率 ≥ 5%和至少安慰剂率两倍)是:
⑴ 精神分裂症:锥体外系症状和静坐不能
⑵双极性情感障碍:锥体外系症状,静坐不能,消化不良,呕吐,嗜睡,和躁动。
药物相互作用
⑴ 强CYP3A4抑制剂:减低VRAYLAR剂量一半。
⑵CYP3A4诱导剂:建议不与 VRAYLAR使用。
特殊人群中使用
妊娠:有第三个三个月暴露新生儿中可能致椎体外系和/或戒断症状。
精神分裂症新药Vraylar简介
Vraylar是口服的多巴胺D3/D2受体的部分激动剂,由匈牙利的Gedeon Richter制药公司研发。Gedeon Richter在2012年把Vraylar的美国和加拿大开发权转让给Forest Laboratories。 多巴胺全名4-(2-氨基乙基)-1,2-苯二酚,是由大脑分泌的一种小分子胺类化合物。多巴胺是一种神经传导物质,能帮助细胞传送脉冲而影响情绪。
VRAYLAR (cariprazine Chinese drug name: carbimethazine capsule) - approved by the US FDA for the treatment of schizophrenia and bipolar bipolar disorder
Recently, the US FDA approved the marketing of Vraylar (cariprazine) from Forest Laboratories and Actavis Pharma to treat adult schizophrenia and bipolar disorder.
cariprazine is an oral, once daily atypical antipsychotic. In the United States, the drug was approved for sale under the brand name Vraylar in 2015. The currently approved indications include: (1) for adult patients with bipolar I type affective disorder (manic depression) For emergency treatment of mixed episodes, the recommended dose range is 3-6 mg/day; (2) is used for the treatment of adult patients with schizophrenia, and the recommended dose range is 1.5-6.0 mg/day. In the European Union, the drug is marketed under the brand name Reagila.
Approval date: September 17, 2015; Company: Allergan and Gedeon Richter plc
VRAYLAR (carbomizin cariprazine) capsule for oral use
US initial approval: 2015
Action mechanism
Not aware of the mechanism of action of carbimethazine in schizophrenia and type I bipolar disorder. However, the efficacy of carbimethazine may be mediated through a partial agonist activity at the central dopamine D2 and serotonin 5-HT1A receptors and in a combination of serotonin 5-HT2A receptor antagonist activity. Carbivirazine forms two major metabolites, demethylcarbazine (DCAR) and didemethylcarbimethazine (DDCAR), and has a receptor binding pattern similar to the parent drug receptor binding pattern in vitro.
Indications and uses
VRAYLAR is an atypical antipsychotic drug for:
(1) Treatment of schizophrenia
(2) Bipolar I-type disorder associated with acute treatment of manic or mixed episodes.
Dose and method of administration
(1) Give VRAYLAR once a day with or without food
● Schizophrenia Starting dose 1.5mg/day Recommended dose 1.5mg to 6mg/day
●Bipolar affective disorder Starting dose 1.5mg/day Recommended dose 3mg to 6mg/day
(2) A daily dose of 6 mg or more does not provide significant benefit but an increased risk of dose-related adverse effects
Formulations and specifications
Capsules: 1.5mg, 3mg, 4.5mg, and 6mg
Contraindications
Known hypersensitivity to VRAYLAR
Warnings and Precautions
(1) Cardiovascular adverse reactions in elderly patients with dementia-related psychosis: increased incidence of cardiovascular adverse events (eg, stroke, transient ischemic attack)
(2) Antipsychotic Malignant Syndrome: Immediate termination and close surveillance for treatment
(3) Delayed dyskinesia: if properly terminated
(4) Adverse reactions occurred late: Because of the long half-life of VRAYLAR, adverse reactions and patient responses were monitored after VRAYLAR for several weeks and varied with each dose.
(5) Metabolic changes: monitoring hyperglycemia/diabetes, dyslipidemia and weight gain
(6) Orthostatic hypotension: monitoring heart rate and blood pressure and warnings for patients with known cardiovascular or cardiovascular disease, and risk of dehydration or syncope
Adverse reactions
The most common adverse reactions (incidence ≥ 5% and at least twice the placebo rate) are:
(1) Schizophrenia: extrapyramidal symptoms and meditation cannot be
(2) Bipolar affective disorder: extrapyramidal symptoms, sedation, indigestion, vomiting, lethargy, and agitation.
Drug interaction
(1) Strong CYP3A4 inhibitor: Reduces the VRAYLAR dose by half.
(2) CYP3A4 inducer: It is recommended not to be used with VRAYLAR.
Use in special people
Pregnant: There may be extra- vertebral and/or withdrawal symptoms in neonates exposed to the third trimester.
Introduction to Vraylar, a new drug for schizophrenia
Vraylar is a partial agonist of the oral dopamine D3/D2 receptor, developed by Gedeon Richter Pharmaceuticals of Hungary. Gedeon Richter transferred Vraylar's US and Canadian development rights to Forest Laboratories in 2012. The full name of dopamine 4-(2-aminoethyl)-1,2-benzenediol is a small molecule amine compound secreted by the brain. Dopamine is a neurotransmitter that helps cells transmit pulses and affect mood.
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