药品详情：
【利培酮片risperidone 简述】
利培酮片risperidone是一类精神科药品。
【利培酮片risperidone 适应症】
1．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、妄想、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，本品可继续发挥其临床疗效。
2．可用于治疗双相情感障碍的躁狂发作，其表现为情绪高涨、夸大或易激惹、自我评价过高、睡眠要求减少、语速加快、思维奔逸、注意力分散或判断力低下(包括紊乱或过激行为)。
【利培酮片risperidone 规格】
本品为片剂，每片含有效成份0.25mg/0.5mg/1mg/2mg/3mg/4mg五种规格，每瓶60片装。
【利培酮片risperidone 服用方法】
1．精神分裂症 由使用其它抗精神病药改用本品者：开始使用时，应渐停原先使用的抗精神病药。若病人原来使用的是长效抗精神病药，则可用本品治疗来替代下一疗程的用药。已用的抗帕金森氏综合征的药是否需要继续则应定期地进行重新评定。
成人：每日1次或每日2次。起始剂量1mg，在1周左右的时间内逐渐将剂量加大到每日2～4mg，第2周内可逐渐加量到每日4～6mg。此后，可维持此剂量不变，或根据个人情况进一步调整。一般情况下，最适剂量为每日2～6mg。每日剂量一般不超过10mg。
2．治疗双相情感障碍的躁狂发作 推荐起始剂量每日1次、每次1～2mg，剂量可根据个体需要进行调整。剂量增加的幅度为每日1～2mg，剂量增加至少隔日或间隔更多天数进行。大多数患者的理想剂量为每日2～6mg，在所有的对症治疗期间，应不断地对是否需要继续使用本品进行评价。 3.肝肾功能损害的患者 肾功能损害患者清除抗精神病药物的能力低于健康成人；肝功能损害患者血浆中游离利培酮的浓度有所增加。无论何种适应症，肾功能损害患者或肝功能损害患者的起始及维持剂量应减半，剂量调整应减缓。此类患者在使用本品时应慎重。
【利培酮片risperidone 注意事项】
1. 老年痴呆患者 1.1 总死亡率 对包括本品在内的几个非典型抗精神病药进行的17项对照试验汇总分析结果显示，非典型抗精神病药物组老年痴呆患者的死亡率较安慰剂组有所增加。在对此类人群用本品进行的安慰剂对照试验中，本品组和安慰剂组患者的死亡率分别为4.0%和3.1%。死亡患者的平均年龄为86岁（范围在67～100岁之间）。
1.2 与呋塞米合用 在对老年痴呆患者用本品进行的安慰剂对照研究中，利培酮与呋塞米合并用药患者的死亡率高于单独使用利培酮或呋塞米的患者，分别为7.3%（平均年龄89岁，范围75-97岁）、3.1%（平均年龄84岁，范围70-96岁）和4.1%（平均年龄80岁，范围67-90岁）。在4项临床试验中的2项观察到了合用呋塞米和本品的患者死亡率增加的现象。 尽管尚未找到明确的病理生理学机制来解释这一现象，并且患者的死亡原因也不相同，但对老年患者合并给利培酮和呋塞米时需谨慎评估风险利益。在服用利培酮并合用其它利尿剂的患者中，并未出现以上死亡率增加的现象。由于脱水是老年痴呆患者很重要的致死因素，所以应尽量避免脱水的发生。
2. 脑血管意外（CAE） 在对老年痴呆患者（平均年龄85岁，范围73-97岁）进行的安慰剂对照研究中，观察到利培酮组包括死亡在内的脑血管方面不良事件（脑血管意外和短暂性脑缺血发作）的发生率较安慰剂组高。
3. 对α受体的阻断活性 由于本品具有对α受体的阻断作用，可能会发生（体位性）低血压，尤其是在治疗初期的剂量调整阶段。对于已知患有心血管疾病的患者（如心衰、心肌梗塞、传导异常、脱水、血容量降低或脑血管疾病）应慎用本品，剂量应按推荐剂量逐渐增加（见用法用量），如发生血压过低现象，应考虑减少剂量。
4. 迟发性运动障碍/锥体外系症状（TD/EPS） 同其它所有具有多巴胺受体拮抗剂性质的药物相似，本品也可能引起迟发性运动障碍，其特征为有节律的非自主运动，主要见于舌及面部。有报告表明，锥体外系症状的发生是迟发性运动障碍发展的风险因素，而与其它传统抗精神病药物相比，本品较少引起锥体外系症状，因此与传统抗精神病药物相比，本品引发迟发性运动障碍的风险较低。如果出现迟发性运动障碍的症状，应考虑停用所有的抗精神病药。
5. 抗精神病药的恶性综合征（NMS） 已有报告指出，服用传统的抗精神病药可能会出现恶性综合征，其特征为高热、肌肉僵直、颤抖、意识障碍和血清肌酸磷酸激酶水平升高，还可能出现肌红蛋白尿症（横纹肌溶解症）和急性肾衰。此时应停用包括本品在内的所有抗精神病药物。 对于路易氏小体性痴呆或帕金森氏病患者，在处方抗精神病药（包括本品）时，应权衡利弊，这类药物可能增加恶性综合征的风险。同时以上人群对抗精神病药物的敏感度增加，除出现锥体外系症状外还会出现混乱、迟钝、体位不稳而经常跌倒。
6. 高血糖和糖尿病 在使用本品期间，已有高血糖、糖尿病及原有糖尿病加重的报告。精神分裂症固有的糖尿病高风险性及正常人群中糖尿病发病率的上升，使非典型抗精神病药物的使用与葡萄糖异常间的相关性评估变得复杂。在精神分裂患者中糖尿病的患者应监测高血糖和糖尿病症状。
7.体质增加 已有显著的体重增加的报告。使用本品时，应进行体重监测。
8. QT间期 与其它抗精神病药物一样，对有心律失常病史、先天性QT间期延长综合征的患者给予本品，及与已知会延长QT间期的药物合用时，应谨慎。
9. 其它 传统的抗精神病药会减低癫痫的发作阈值，故癫痫患者应慎用本品。 服用本品的患者应避免进食过多，因为本品可能引起体重增加。 对于老年患者、肝功能损害患者、肾功能损害患者或老年痴呆患者推荐的特殊剂量，参见[老年用药]和[用法用量]部分。 本品对需要警觉性的活动有所影响。因此，在了解到患者对本品的敏感性前，建议患者在治疗期间不应驾驶汽车或操作机器。 请置于儿童不易拿到处。
【利培酮片risperidone 不良反应】
感染：下呼吸道感染、感染、肠胃炎、皮下脓肿 血液和淋巴系统：嗜中性白血球减少症 精神病性障碍：抑郁 神经系统：感觉异常、惊厥 眼部：睑痉挛 耳部和迷路：眩晕 心脏：心动过缓 血管：高血压 胃肠道：牙痛、舌痉挛 皮肤及皮下组织：湿疹 骨骼肌、结缔组织和骨异常：臀痛 全身及给药部位：疼痛 研究：体重下降、γ-谷氨酸转移酶升高、肝酶水平升高 中毒和损伤：跌倒 上市后经验 上市后首次判定为利培酮不良反应的不良事件见表5。不良反应按自发报告率分类： 很常见≥1/10 常见≥1/100，且1/10 少见≥1/1000，且＜1/100 罕见≥1/10,000，且1/1000 非常罕见＜1/10,000，包括个别病例。 依据自发报告频率，以上不良反应按发生率分类列于表5。 a 包括血小板减少、血小板计数下降、血小板压积减少、血小板产物减少 b 包括血管神经性水肿、后天性C1酯酶缺乏、口缘水肿、眼睑浮肿、面部浮肿、遗传性血管水肿、喉水肿、喉气管水肿、眼-呼吸道综合征、口腔水肿、眶周水肿、小肠部血管性水肿、舌水肿 c 包括心电图校正后的QT间期延长、心电图QT间期异常、心电图QT间期延长、QT间期延长综合征、先天性QT间期延长综合征。
Risperidone
Risperidone, sold under the brand name Risperdal among others, is an antipsychotic.[2] It is used to treat schizophrenia, bipolar disorder, and irritability associated with autism.[2] It is taken either by mouth or by injection into a muscle.[2] The injectable version is long-acting and lasts for about two weeks.[3]
Common side effects include movement problems, sleepiness, dizziness, trouble seeing, constipation, and increased weight.[2][4] Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, and high blood sugar levels.[2][3] In older people with psychosis as a result of dementia, it may increase the risk of dying.[2] It is unclear if it is safe for use in pregnancy.[2] Risperidone is an atypical antipsychotic.[2] Its mechanism of action is not entirely clear, but is believed to be related to its action as a dopamine antagonist and serotonin antagonist.[2]
Study of risperidone began in the late 1980s and it was approved for sale in the United States in 1993.[2][5] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.[6] It is available as a generic medication.[3] The wholesale price in the developing world is between $US 0.01 and $US 0.60 per day as of 2014.[7] The cost for a typical month of medication in the United States is between $US 100-200 as of 2015.[3] In 2016, it was the 159th most prescribed medication in the United States, with more than 3 million prescriptions.[8]
Medical uses
Risperidone is mainly used for the treatment of schizophrenia, bipolar disorder, and irritability associated with autism.[9]
Schizophrenia
Risperidone is effective in treating the acute exacerbations of schizophrenia.[10][11] A 2013 study compared 15 antipsychotic drugs in treating schizophrenia. Risperidone was ranked fourth, 11% more effective than paliperidone (fifth), 20-23% more effective than haloperidol, quetiapine, and aripiprazole, and 36% less effective than clozapine (first).[10]
Studies evaluating the utility of risperidone by mouth for maintenance therapy have reached varying conclusions. A 2012 systematic review concluded that evidence is strong that risperidone is more effective than all first-generation antipsychotics other than haloperidol, but that evidence directly supporting its superiority to placebo is equivocal.[12] A 2011 review concluded that risperidone is more effective in relapse prevention than other first- and second-generation antipsychotics with the exception of olanzapine and clozapine.[13] A 2016 Cochrane review suggests that risperidone reduces the overall symptoms of schizophrenia, but firm conclusions are difficult to make due to very low-quality evidence. Data and information are scarce, poorly reported, and probably biased in favour of risperidone, with about half of the included trials developed by drug companies. The article raises concerns regarding the serious side effects of risperidone, such as parkinsonism.[14] A 2011 Cochrane review compared risperidone with other atypical antipsychotics such as olanzapine for schizophrenia:[15]
Long-acting injectable formulations of antipsychotic drugs provide improved compliance with therapy and reduce relapse rates relative to oral formulations.[16][17] The efficacy of risperidone long-acting injection appears to be similar to that of long acting injectable forms of first generation antipsychotics.[18]
Bipolar disorder
Second-generation antipsychotics, including risperidone, are effective in the treatment of manic symptoms in acute manic or mixed exacerbations of bipolar disorder.[19][20][21] In children and adolescents, risperidone may be more effective than lithium or divalproex, but has more metabolic side effects.[22] As maintenance therapy, long-acting injectable risperidone is effective for the prevention of manic episodes but not depressive episodes.[23] The long-acting injectable form of risperidone may be advantageous over long acting first generation antipsychotics, as it is better tolerated (fewer extrapyramidal effects) and because long acting injectable formulations of first generation antipsychotics may increase the risk of depression.[24]
Autism
Compared to placebo, risperidone treatment reduces certain problematic behaviors in autistic children, including aggression toward others, self-injury, temper tantrums, and rapid mood changes. The evidence for its efficacy appears to be greater than that for alternative pharmacological treatments.[25] Weight gain is an important adverse effect.[26][27] Some authors recommend limiting the use of risperidone and aripiprazole to those with the most challenging behavioral disturbances in order to minimize the risk of drug-induced adverse effects.[28] Evidence for the efficacy of risperidone in autistic adolescents and young adults is less persuasive.[29]
Other uses
Risperidone has shown promise in treating therapy-resistant obsessive–compulsive disorder, when serotonin reuptake inhibitors are not sufficient.[30]
Risperidone has not demonstrated a benefit in the treatment of eating disorders or personality disorders.[31]
While antipsychotic medications such as risperidone have a slight benefit in people with dementia, they have been linked to higher incidences of death and stroke.[31] Because of this increased risk of death, treatment of dementia-related psychosis with risperidone is not FDA approved.[32]
Adverse effects
Common side effects include movement problems, sleepiness, dizziness, trouble seeing, constipation, and increased weight.[2][4] Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, and high blood sugar levels.[2][3] In older people with psychosis as a result of dementia, it may increase the risk of dying.[2]
While atypical antipsychotics appear to have a lower rate of movement problems as compared to typical antipsychotics, risperidone has a high risk of movement problems among the atypicals.[33][34] Atypical antipsychotics however are associated with a greater amount of weight gain.[34]
Drug interactions
§ Carbamazepine and other enzyme inducers may reduce plasma levels of risperidone.[35] If a person is taking both carbamazepine and risperidone, the dose of risperidone will likely need to be increased. The new dose should not be more than twice the patient's original dose.[36]
§ CYP2D6 inhibitors, such as SSRI medications, may increase plasma levels of risperidone.[35]
§ Since risperidone can cause hypotension, its use should be monitored closely when a patient is also taking antihypertensive medicines to avoid severe low blood pressure.[36]
Discontinuation
The British National Formulary recommends a gradual withdrawal when discontinuing antipsychotic treatment to avoid acute withdrawal syndrome or rapid relapse.[37] Some have argued the additional somatic and psychiatric symptoms associated with dopaminergic super-sensitivity, including dyskinesia and acute psychosis, are common features of withdrawal in individuals treated with neuroleptics.[38][39][40][41] This has led some to suggest the withdrawal process might itself be schizomimetic, producing schizophrenia-like symptoms even in previously healthy patients, indicating a possible pharmacological origin of mental illness in a yet unknown percentage of patients currently and previously treated with antipsychotics. This question is unresolved, and remains a highly controversial issue among professionals in the medical and mental health communities, as well the public.[42]
Dementia
Older people with dementia-related psychosis are at a higher risk of death if they take risperidone compared to those who do not. Most deaths are related to heart problems or infections.[36]
注：药品如有新包装,以新包装为准。以上资讯来源于网络或由高等医药院校的学生志愿者翻译（如有错漏，请帮忙指正），仅供医护人员内部讨论，不作任何用药依据，具体用药指引，请咨询主治医师。
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