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5月18日，Ortho-McNeil-Janssen制药公司下属子公司Janssen宣布，美国食品药品管理局(FDA)已批准Risperdal Consta(利培酮)用于双相I型情感障碍的维持治疗。Risperdal Consta可单用或与锂或丙戊酸盐联合使用。Risperdal Consta是一种长效抗精神病药，于2003年首次获FDA批准用于治疗精神分裂症。
该药再获FDA批准，是基于两项应用该药长期治疗双相I型情感障碍的前瞻性、随机、双盲、安慰剂对照研究的结果。第一项研究的结果显示，在延迟任何情感发作的复发时间方面，Risperdal Consta单药治疗显著优于安慰剂。 第二项研究的结果显示，在使用锂或丙戊酸盐的基础上加用Risperdal Consta比加用安慰剂能更显著延迟复发时间。
一项临床研究显示，服用Risperdal Consta精神分裂症患者的最常见不良反应是头痛、帕金森综合征、头晕、静坐不能、疲劳、便秘、消化不良、镇静、体重增加、口干和四肢疼痛。另一项研究显示，服用Risperdal Consta的双相I型情感障碍患者的最常见不良反应是体重增加(单用)和震颤(与其他药物联用)。
服用抗精神病药的痴呆相关精神病老年患者的死亡风险比服用安慰剂的患者的死亡风险更高。Risperdal Consta未获批准用于治疗痴呆相关精神病。
Risperidone Consta是长效型利培酮，为通过先进技术将利培酮包封于生物降解聚合物制成的微球的混悬水溶液。给药方法是每2周肌肉注射1次。
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Information on RISPERDAL CONSTA |
RISPERDAL® CONSTA® (risperidone) is used for the treatment of schizophrenia and for the longer-term treatment of Bipolar I Disorder.
IMPORTANT SAFETY INFORMATION FOR RISPERDAL® CONSTA®
Elderly Patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death compared to placebo. RISPERDAL® CONSTA® (risperidone) is not approved for the treatment of patients with dementia-related psychosis. Neuroleptic Malignant Syndrome (NMS) is a rare and potentially fatal side effect reported with RISPERDAL® CONSTA® and similar medicines. Call your doctor immediately if the person being treated develops symptoms such as high fever; stiff muscles; shaking; confusion; sweating; changes in pulse, heart rate, or blood pressure; or muscle pain and weakness. Treatment should be stopped if the person being treated has NMS.
Tardive Dyskinesia (TD) is a serious, sometimes permanent side effect reported with RISPERDAL® CONSTA® and similar medications. TD includes uncontrollable movements of the face, tongue, and other parts of the 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 overall dose taken by the patient. This condition can develop after a brief period of therapy at low doses, although this is much less common. There is no known treatment for TD, but it may go away partially or completely if therapy is stopped.
High blood sugar and diabetes have been reported with RISPERDAL® CONSTA® and similar medications. If the person being treated has diabetes or risk factors such as being overweight or a family history of diabetes, blood sugar testing should be performed at the beginning and throughout treatment with RISPERDAL® CONSTA®. Complications of diabetes can be serious and even life threatening. If signs of high blood sugar or diabetes develop, such as being thirsty all the time, going to the bathroom a lot, or feeling weak or hungry, contact your doctor. RISPERDAL® CONSTA® and similar medications can raise the blood levels of a hormone known as prolactin, causing a condition known as hyperprolactinemia. Blood levels of prolactin remain elevated with continued use. Some side effects seen with these medications include the absence of a menstrual period; breasts producing milk; the development of breasts by males; and the inability to achieve an erection.
Some people taking RISPERDAL® CONSTA® may feel faint or lightheaded when they stand up or sit up too quickly. By standing up or sitting up slowly and following your healthcare professional's dosing instructions, this side effect can be reduced or it may go away over time.
Blood problems such as low numbers of white blood cells have been reported in patients taking risperidone and similar medications. In some cases it has been serious and life-threatening. Depending upon your medical condition, your doctor may choose to test your blood as you start therapy with RISPERDAL® CONSTA®.
RISPERDAL® CONSTA® may affect your alertness or driving ability; therefore, do not drive or operate machinery before talking to your healthcare professional.
RISPERDAL® CONSTA® 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.
Painful, long lasting erections have been reported with the use of RISPERDAL® CONSTA®. Call your doctor immediately if you think you are having this problem.
Extrapyramidal Symptoms (EPS) are usually persistent movement disorders or muscle disturbances, such as restlessness, tremors, and muscle stiffness. If you observe any of these symptoms, talk to your healthcare professional.
Inform your healthcare professional if you become pregnant or intend to become pregnant during therapy with RISPERDAL® CONSTA®. Caution should be exercised when administering RISPERDAL® CONSTA® to a nursing woman.
RISPERDAL® CONSTA® may make you more sensitive to heat. You may have trouble cooling off, or be more likely to become dehydrated, so take care when exercising or when doing things that make you warm.
Some medications interact with RISPERDAL® CONSTA®. Please inform your healthcare professional of any medications or supplements that you are taking. Avoid alcohol while on RISPERDAL® CONSTA®.
In a study of people taking RISPERDAL® CONSTA®, the most common side effects in the treatment of schizophrenia were headache, tremors, dizziness, restlessness, tiredness, constipation, indigestion, sleepiness, weight gain, pain in the limbs, and dry mouth.
In a study of people taking RISPERDAL® CONSTA®, the most common side effects in the treatment of bipolar disorder were weight gain (when used alone) and tremors (when used with lithium or valproate).
RISPERDAL CONSTA
药理学特征
本品为苯并异恶唑衍生物，是新一代的抗精神病药。其活性成份利培酮是一种具有独特性质的选择性单胺能拮抗剂，它与5—羟色胺能的5-HT2受体和多巴胺的D2受体有很高的亲和力。利培酮也能与肾上腺素能受体结合，并且以较低的亲和力与 H1—组胺能受体和α2-肾上腺素受体结合。利培酮不与胆碱能受体结合。利培酮是强有力的D2拮抗剂，可以改善精神分裂症的阳性症状，但它引起的运动功能抑制，以及强直性昏厥都要比经典的抗精神病药少。对中枢系统的5—羟色胺和多巴胺拮抗作用的平衡可以减少发生锥体外系副作用的可能，并将其治疗作用扩展到精神分裂症的阴性症状和情感症状。
作用与用途 用于治疗急性和慢性精神分裂症以及其它各种精神病性状态的明显的阳性症状(如幻觉 、幻想、思维紊乱、敌视 、怀疑 )和明显 的阴性症状(如反应迟钝、情绪淡漠及社交淡漠、少语)。也可减轻与精神分裂症有关的情感症状(如：抑郁、负罪感、焦虑)。对于急性期治疗有效的患者，在维持期治疗中，维思通可继续发挥其临床疗效。
不良反应 1.与服用本品有关的常见不良反应是：失眠、焦虑、头痛、头晕、口干。 2.较少见的不良反应有：嗜睡、疲劳、注意力下降、便秘、消化不良、恶心、呕吐、腹痛、视物模糊、阴茎异常勃起、勃起困难、射精无力、性淡漠、尿失禁、鼻炎、皮疹以及其它过敏反应。
3.可能引起锥体外系症状，如：肌紧张 、震颤、僵直、流涎、运动迟缓、静坐不能、急性肌张力障碍。通过降低剂量或给予抗帕金森氏综合征的药物可消除。
4.偶尔会出现(体位性)低血压、(反射性)心动过速或高血压的症状。
5.会出现体重增加、水肿和肝酶水平升高的现象。
6.偶尔会由于病人烦渴或抗利尿激素分泌失调(SIADH)引发水中毒。
7.会引起血浆中催乳素浓度的增加，其相关症状为：溢乳、男子女性型乳房、月经失调、闭经。
8.偶见迟发性运动障碍、恶性症状群、体温失调以及癫痫发作。
9.有轻度中性粒细胞和/或血小板计数下降的个例报导。
禁忌症 已知对本品过敏的患者禁用。
注意事项 1.患有心血管疾病(如心衰 、心肌梗塞 、传导异常、脱水、失血及脑血管病变)的人应慎用，从小剂量开始并应逐渐增加剂量(见用法用量)。
2.由于本品具有α受体阻断活性，因此在用药初期和加药速度过快时会发生(体位性)低血压，此时则应考虑减量。
3.同其它具有多巴胺受体拮抗剂性质的药物相似，引起迟发性运动障碍，其特征为有 节律的不随意运动，主要见于舌及面部。如果出现迟发性运动障碍，应停止服用所有的抗精神病药。
4.已有报道 指出 ，服用经典的抗精病药会出现恶性症状群，其特征为高热、肌肉僵直、颤抖、意识改变和肌酸磷酸激酶水平升高。此时应停用包括本品在内的所有抗精神药物。
5.患有帕金森氏综合征的病人应慎用本品，因为在理论上该药会引起此病的恶化。
6.经典的抗精神病药会降低癫痫的发作阈值，故患有癫痫的病人仍应慎用本品。
7.服用本品的患者应避免进食过多，以免发胖。
8.鉴于本品对中枢神经系统的作用，在与其它作用于中枢的药物同时服用时应慎重 。
9.本品对需要警觉性的活动有影响 。因此 ，在了解到患者对该药的敏感性前，建议患者不应驾驶汽车或操作机器 。孕妇及哺乳妇女用药 怀孕妇女服用本品是否安全尚不明确 。动物实验表明：利培酮对生殖无直接的毒性，也无致畸作用。尽管如此，除非益处明显大于可能的危险 ，怀孕妇女仍不应服用本品。
本品是否会经人体乳汁排出尚不清楚 ，动物实验表明 ，利培酮和9—羟基-利培酮会经动物乳汁排出 。因此，服用本品的妇女不应哺乳 。
药物相互作用 1.本品可拮抗左旋多巴及其它多巴胺促效剂的作用。
2.酰胺咪嗪及其它的肝酶诱导剂会降低本品活性成份的血浆浓度，一旦停止使用酰胺咪嗪或其它肝酶诱导剂，则应重新确定使用本品的剂量，必要时可减量。
3. 酚噻嗪 、三环抗抑郁药和一些β—阻断剂会增加本品的血药浓度，但不增加抗精神病活性成份的血药浓度。
4.当和其它高度蛋白结合的药物一起服用时，不存在有临床意义的血浆蛋白的相互置换。
药物过量 1.本品可拮抗左旋多巴及其它多巴胺促效剂的作用。
2.酰胺咪嗪及其它的肝酶诱导剂会降低本品活性成份的血浆浓度，一旦停止使用酰胺咪嗪或其它肝酶诱导剂，则应重新确定使用本品的剂量，必要时可减量。
3. 酚噻嗪 、三环抗抑郁药和一些β—阻断剂会增加本品的血药浓度，但不增加抗精神病活性成份的血药浓度。
4.当和其它高度蛋白结合的药物一起服用时，不存在有临床意义的血浆蛋白的相互置换。 | 
