部分中文利培酮处方资料（仅供参考） 通用名：利培酮　　 商品名：维思通 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。 药代学特征 利培酮经口服后可被完全吸收，并在1-2小时内达到血药浓度峰值，其吸收不受食物影响。在体内，利培酮部分代谢成9-羟基-利培酮，后者与利培酮有相似的药理作用。本品在体内可迅速分布，利培酮的血浆蛋白结合率为88%，9-羟基-利培酮的血浆蛋白结合率 为77%。该药的消除半衰期为3小时左右，抗精神病有效成份的消除半衰期为24小时。大多数病人在1天内达到利培酮的稳态，经过4-5天达到9-羟基-利培酮的稳态。用药一周后，70%的药物经尿液排泄，14%的药物经粪便排泄，经尿排泄的部分中，35-45%为利培酮和9-羟基-利培酮，其余为非活性代谢物。老年患者和肾功能不全患者的利培酮血浆浓度较高，清除速度较慢。 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 。 儿童用药 对于15岁以下儿童目前尚缺乏足够的临床经验 。 老年患者用药 建议起始剂量为每日0.5mg或更低 ，根据个体需要，剂量逐渐加大到每2次，每次1-2mg。在获得更多的经验前，老年人加量过程中应慎重。 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。 生产厂家: Janssen Pharmaceutical Inc. RISPERDAL(risperidone) is used for the treatment of schizophrenia in adults and adolescents ages 13-17 years. RISPERDAL(risperidone) is used alone or in combination with other medicines (valproate or lithium) in adults for the short-term treatment of bipolar mania; or alone in adults, children and adolescents ages 10-17 years for the short-term treatment of bipolar mania. RISPERDAL(risperidone) is used for the treatment of irritability associated with autistic disorder in children and adolescents ages 5-16 years. IMPORTANT SAFETY INFORMATION FOR RISPERDAL Elderly Patients with dementia-related psychosis treated with atypical antipsychotic drugs are at an increased risk of death compared to placebo. RISPERDAL (risperidone) is not approved for the treatment of patients with dementia-related psychosis. The most common adverse reactions observed in all clinical trials with RISPERDAL occurring at a rate of at least 10% were somnolence, increased appetite, fatigue, rhinitis, upper respiratory tract infection, vomiting, coughing, urinary incontinence, increased saliva, constipation, fever, tremors, muscle stiffness, abdominal pain, anxiety, nausea, dizziness, dry mouth, rash, restlessness, and indigestion. Neuroleptic Malignant Syndrome (NMS) is a rare and potentially fatal side effect reported with RISPERDAL ® 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 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. RISPERDAL 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. The connection between prolactin levels and side effects is unknown. High blood sugar and diabetes have been reported with RISPERDAL 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 atthebeginning and throughout treatment. 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 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. Some people taking RISPERDAL ® 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 may be reduced or it may go away over time. 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. Some medications interact with RISPERDAL. Please inform your healthcare professional of any medications or supplements that you are taking. Avoid alcohol while taking RISPERDAL. Inform your healthcare professional if you are pregnant or if you are planning to get pregnant while taking RISPERDAL. Do not breast-feed if you are taking RISPERDAL. RISPERDAL may affect your driving ability; therefore, do not drive or operate machinery before talking to your healthcare professional. RISPERDAL may affect alertness and motor skills; use caution until the effect of RISPERDAL is known. --------------------------------------------------------------- 注：以下产品不同规格和不同价格，购买以咨询为准！ --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: RISPERDAL 2MG/TABLET 28 TABLETS/BOTTLE 原产地英文药品名: RISPERIDONE 原产地英文化合物名称: 4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-1-piperidyl]ethyl]-3-methyl-2,6-diazabicyclo[4.4.0]deca-1,3-dien-5-one 中文参考商品译名: 维思通 2毫克/片 28片/瓶 中文参考药品译名: 利培酮 生产厂家中文参考译名: ORTHO MCNEIL JANSSEN 生产厂家英文名: ORTHO MCNEIL JANSSEN --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: RISPERDAL 1MG/TABLET 60 TABLETS/BOTTLE 原产地英文药品名: RISPERIDONE 原产地英文化合物名称: 4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-1-piperidyl]ethyl]-3-methyl-2,6-diazabicyclo[4.4.0]deca-1,3-dien-5-one 中文参考商品译名: 维思通 1毫克/片 60片/瓶 中文参考药品译名: 利培酮 生产厂家中文参考译名: ORTHO MCNEIL JANSSEN 生产厂家英文名: ORTHO MCNEIL JANSSEN --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: RISPERDAL 1MG/TABLET 56 TABLETS/BOTTLE 原产地英文药品名: RISPERIDONE 原产地英文化合物名称: 4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-1-piperidyl]ethyl]-3-methyl-2,6diazabicyclo[4.4.0]deca-1,3-dien-5-one 中文参考商品译名: 维思通 1毫克/片 56片/瓶 中文参考药品译名: 利培酮 生产厂家中文参考译名: ORTHO MCNEIL JANSSEN 生产厂家英文名: ORTHO MCNEIL JANSSEN --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: RISPERDAL 1MG/TABLET 28TABLETS/BOTTLE 原产地英文药品名: RISPERIDONE 原产地英文化合物名称: 4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-1-piperidyl]ethyl]-3-methyl-2,6diazabicyclo[4.4.0]deca-1,3-dien-5-one 中文参考商品译名: 维思通 1毫克/片 28片/瓶 中文参考药品译名: 利培酮 生产厂家中文参考译名: ORTHO MCNEIL JANSSEN 生产厂家英文名: ORTHO MCNEIL JANSSEN --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: RISPERDAL 0.5MG/TABLET 28TABLETS/BOTTLE 原产地英文药品名: RISPERIDONE 原产地英文化合物名称: 4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-1-piperidyl]ethyl]-3-methyl-2,6diazabicyclo[4.4.0]deca-1,3-dien-5-one 中文参考商品译名: 维思通 0.5毫克/片 28片/瓶 中文参考药品译名: 利培酮 生产厂家中文参考译名: ORTHO MCNEIL JANSSEN 生产厂家英文名: ORTHO MCNEIL JANSSEN --------------------------------------------------------------- 产地国家: 欧洲共同体国家 原产地英文商品名: RISPERDAL 0.5MG/TABLET 56TABLETS/BOTTLE 原产地英文药品名: RISPERIDONE 原产地英文化合物名称: 4-[2-[4-(6-fluorobenzo[d]isoxazol-3-yl)-1-piperidyl]ethyl]-3-methyl-2,6diazabicyclo[4.4.0]deca-1,3-dien-5-one 中文参考商品译名: 维思通 0.5毫克/片 56片/瓶 中文参考药品译名: 利培酮 生产厂家中文参考译名: ORTHO MCNEIL JANSSEN 生产厂家英文名: ORTHO MCNEIL JANSSEN 该药品相关信息网址1: http://www.risperdal.com/risperdal/ 该药品相关信息网址2: http://en.wikipedia.org/wiki/Risperidone 该药品相关信息网址3: http://baike.baidu.com/view/666527.htm?fr=ala0_1