美国FDA批准了Janssen公司开发的棕榈酸帕利培酮(paliperidone palmitate)缓释悬浮液Invega Sustenna,用于一月1次肌肉内注射急性和维持治疗成人精神分裂症.

IMPORTANT SAFETY INFORMATION FOR INVEGA® SUSTENNA™

INVEGA® SUSTENNA™ (paliperidone palmitate) is used for the treatment of schizophrenia.

INVEGA® SUSTENNA™is not approved for the treatment of dementia-related psychosis in elderly patients. Elderly patients who were given oral antipsychotics like INVEGA® SUSTENNA™ in clinical studies for psychosis caused by dementia (memory problems) had a higher risk of death.

Neuroleptic Malignant Syndrome (NMS) is a rare, but serious side effect that could be fatal and has been reported with INVEGA® SUSTENNA™ and similar medicines. Call the doctor right away if you develop symptoms such as a high fever, rigid muscles, shaking, confusion, sweating more than usual, increased heart rate or blood pressure, or muscle pain or weakness. Treatment should be stopped if you are being treated for NMS.

Tardive Dyskinesia (TD) is a rare, but serious and sometimes permanent side effect reported with INVEGA® SUSTENNA™ and similar medicines. Call your doctor right away if you start to develop twitching or jerking movements that you cannot control in your face, tongue, or other parts of your body. The risk of developing TD and the chance that it will become permanent is thought to increase with the length of therapy and the total dose received. This condition can also develop after a short period of treatment at low doses but this is less common. There is no known treatment for TD but it may go away partially or completely if the medicine is stopped.

One risk of INVEGA® SUSTENNA™ is that it may change your heart rhythm. This effect is potentially serious. You should talk to your doctor about any current or past heart problems. Because these problems could mean you're having a heart rhythm abnormality, contact your doctor IMMEDIATELY if you feel faint or feel a change in the way that your heart beats (palpitations).

High blood sugar and diabetes have been reported with INVEGA® SUSTENNA™ and similar medicines. If you already have diabetes or have risk factors such as being overweight or a family history of diabetes, blood sugar testing should be done at the beginning and during the treatment. The complications of diabetes can be serious and even life-threatening. Call your doctor if you develop signs of high blood sugar or diabetes, such as being thirsty all the time, having to urinate or "pass urine" more often than usual, or feeling weak or hungry.

Weight gain has been observed with INVEGA® SUSTENNA™ and other atypical antipsychotic medications. If you notice that you are gaining weight, please notify your doctor.

Some people may feel faint, dizzy, or may pass out when they stand up or sit up suddenly. Be careful not to get up too quickly. It may help if you get up slowly and sit on the edge of the bed or chair for a few minutes before you stand up. These symptoms may decrease or go away after your body becomes used to the medicine.

INVEGA® SUSTENNA™ and similar medicines have been associated with decreases in the counts of white cells in circulating blood. If you have a history of low white blood cell counts or have unexplained fever or infection, then please contact your doctor right away.

INVEGA® SUSTENNA™ and similar medicines can raise the blood levels of a hormone called prolactin and blood levels of prolactin remain high with continued use. This may result in some side effects including missed menstrual periods, leakage of milk from the breasts, development of breasts in men, or problems with erection.

If you have a prolonged or painful erection lasting more than 4 hours, seek immediate medical help to avoid long-term injury.

Call your doctor right away if you start thinking about suicide or wanting to hurt yourself.

INVEGA® SUSTENNA™ can make some people feel dizzy, sleepy, or less alert. Until you know how you are going to respond to INVEGA® SUSTENNA™, be careful driving a car, operating machines, or doing things that require you to be alert.

This medicine may make you more sensitive to heat. You may have trouble cooling off or be more likely to become dehydrated. Be careful when you exercise or spend time doing things that make you warm.

Some medications interact with INVEGA® SUSTENNA™ Please inform your healthcare professional of any medications or supplements that you are taking.

INVEGA® SUSTENNA™ should be used cautiously in people with a seizure disorder, who have had seizures in the past, or who have conditions that increase their risk for seizures.

Inform your healthcare professional if you become pregnant or intend to become pregnant during therapy with INVEGA® SUSTENNA™.

Do not drink alcohol while you are taking INVEGA® SUSTENNA™.

In a study of people taking INVEGA® SUSTENNA™, common side effects in the treatment of schizophrenia were reactions at the injection site, sleepiness, dizziness, feeling of inner restlessness, and abnormal muscle movements, including tremor (shaking), shuffling, uncontrolled involuntary movements, and abnormal movements of the eyes.

This is not a complete list of all possible side effects. Ask your doctor or treatment team if you have any questions or want more information.

If you have any questions about INVEGA® SUSTENNA™ or your therapy, talk with your doctor.

每月应用一次的新型抗精神病药注射制剂已获准用于治疗精神分裂症

 
New once-monthly antipsychotic injection approved for schizophrenia

2009年7月31日，杨森制药公司宣布，美国食品药品管理局(FDA)已批准Invega Sustenna(棕榈酸帕潘立酮)缓释混悬剂用于成人精神分裂症的紧急救治和维持治疗。Invega Sustenna是一种可注射的长效非典型抗精神病药，每月一次用药。

参加Invega临床试验的临床研究员、辛辛那提州立大学医学院精神病学与神经系统科学教授Henry A. Nasrallah博士表示，“对药物治疗依从性差是治疗精神分裂症症状、推迟复发时间的单个最严重的制约因素之一。批准Invega Sustenna 每月一次用药不仅会为医护人员提供一种治疗选择，而且同时还可以作为监测患者药物治疗依从性有无间断的可靠手段，这可能有助于优化精神分裂症的临床治疗效果。”

FDA的这条批准令是基于4项急性症状控制研究和1项较长期的Invega Sustenna与安慰剂维持治疗比较研究的数据。紧急救治试验表明，Invega Sustenna在改善阳性和阴性症状量表(PANSS)总评分方面优于安慰剂，而在较长期的维持治疗研究中，与安慰剂对照相比，该药可显著推迟复发时间。

在临床试验中，最常见的不良事件(发生率≥5%且发作频率至少为安慰剂的2倍)为注射部位反应、嗜睡/镇静、眩晕、静坐不能以及锥体外系功能障碍。在接受Invega Sustenna治疗的患者中发生少但很严重的不良反应有抗精神病药恶性综合征和迟发型运动障碍。

市售的Invega Sustenna是以毫克计的棕榈酸帕潘立酮，包括39、78、117、156及234 mg这几种剂量强度规格。医学会议上提供的临床试验数据常以帕潘立酮的毫克当量报告。各个剂量的棕榈酸帕潘立酮均相当于一定剂量的帕潘立酮(39、 78、117、156及234 mg的棕榈酸帕潘立酮分别相当于25、50、 75、100及 150 mg的帕潘立酮)。预注满药品的注射器无需再作调整或冷藏。患者的初始治疗方案为三角肌内注射2次，中间间隔1w(第1d为234mg，第8d为156mg)，此后每月注射一次，选择三角肌或臀大肌注射均可。