部份中文阿立哌唑处方资料（仅供参考） 药理作用 本品是多巴胺和5-羟色胺系统的稳定剂，是突触后多巴胺受体的阻滞剂，同时又是突触前自主受体的激动剂，与D2和D3受体的亲和力非常强。本品是D2受体的部分激动剂，在活体多巴胺功能亢进模型中显示出较强的阻滞作用，而在多巴胺功能低下的模型中则表现出较强激动作用；本品能够抑制多巴胺激动剂引起的垂体前叶催乳素的升高，这种抑制作用可以被氟哌啶醇完全阻滞，因此，本品作用特点不是阻断而是稳定多巴胺系统的作用。同时本品又是5-HT1A受体的部分激动剂和5-HT2A受体的阻滞剂。从而发挥抗精神分裂症的焦虑、抑郁、认知缺损和阴性症状。本品能透过血-脑屏障，而且与D2受体的结合随剂量的增加而增加。 药动学 本品口服生物利用度为87%，达峰时间为3～5h，血浆蛋白结合率大于99%。药物在肝脏经细胞色素P450CYP3A4和CYP2D6代谢，代谢途径包括脱氢和羟基化。其主要代谢产物脱氢阿立哌唑占药时曲线下面积(AUC)的40%，对多巴胺D2受体的亲和力与母体化合物相似，并可能具有药理活性。给药量的25%经肾排泄(其中原形药物少于1%)，另有约55%随粪便排出体外(原形药物占18%)。药物母体和脱氢阿立哌唑的半衰期分别为75h和94h，代谢减弱者半衰期可达146h。 适应证 用于治疗精神分裂症，对急性复发者、慢性患者及情感性精神分裂症有效。 禁忌证 对本品过敏者禁用，孕妇及12岁以下儿童不建议使用。 注意事项 1.本品可经哺乳大鼠的乳汁分泌。哺乳期妇女用药期间应暂停哺乳。 2.用药前后及用药时应检查或监测血常规、血压、心率(尤其是对心血管疾病患者)和空腹血糖。 3.进食时服用本品，母体化合物和脱氢阿立哌唑的血药浓度峰值及AUC均无显著改变，但达峰时间分别延迟3h和12h。 不良反应 本品不良反应少且轻，主要包括以下几方面。 1.心血管系统：可出现心率增加或心动过速，罕见QT间期延长。有出现直立性低血压的报道。 2.中枢神经系统：可出现头痛、头晕目眩、失眠、嗜睡、静坐不能等。每天30mg较低剂量更易引起嗜睡。另有研究表明，口服本品每天15mg或30mg，锥体外系不良反应的总发生率与对照组相似。 3.代谢/内分泌系统：可出现体重增加(发生率低于氟哌啶醇)和血清催乳素浓度升高。有报道，应用非典型精神抑制药可致高血糖，并可能导致酮症酸中毒、高渗性昏迷甚至死亡，但由于本品尚在试验阶段，因此尚不明确本品上市后是否有增加这种风险的可能。 4.胃肠道：可出现恶心(4%)、呕吐(5%)和便秘(2%)。 5.其他：有资料提示，治疗期间可能发生精神病药恶性综合征。 6.有以下情况者慎用： ①有自杀倾向者慎用。 ②老年精神病患者慎用。 ③精神病药恶性综合征者慎用。 ④可能出现迟发性运动障碍者慎用。 ⑤可能促使体温升高的疾病患者慎用。 ⑥糖尿病患者(血糖控制差)或血糖升高者慎用。 ⑦心血管病(如心肌梗死、缺血性心脏病、心力衰竭、传导异常)或脑血管病患者慎用。 ⑧易发生低血压(如脱水、血容量过低、降压药治疗)者慎用。 ⑨有患吸入性肺炎风险者慎用。 ⑩有癫痫发作史或癫痫发作阈降低(如阿尔茨海默病)者慎用。同时服用中枢神经系统抑制药(包括酒精)者慎用。 用法用量 口服：第1周，每天5mg，1次/d；第2周，增加为每天10mg，1次/d；用药2周后，可根据患者的疗效和耐受情况增加剂量为每次15mg，1次/d。每天最大剂量不应超过30mg。 药物相应作用 1.CYP2D6抑制剂(如氟西汀、帕罗西汀)可抑制本品的代谢，导致本品血药浓度升高。 2.酮康唑、奎尼丁分别抑制CYP3A4和CYP2D6介导的本品的代谢，均可使本品血药浓度升高。建议合用时本品剂量减半；停用酮康唑或奎尼丁后，本品需加量。 3.本品可能增强某些降压药的降压作用。 4.与卡马西平合用，可降低本品血药浓度。 エビリファイ錠３ｍｇ／エビリファイ錠６ｍｇ／エビリファイ錠１２ｍｇ／エビリファイ散１％ ・商品名： エビリファイ錠 ・英名： Otsuka Abilify Tablets ・一般名： アリピプラゾール錠 ・成分： Aripiprazole ・メーカー： 大塚製薬 (Otsuka) 包装 エビリファイ錠3mg：［PTP］100錠(10錠×10)、500錠(10錠×50) ［プラスチックボトル］500錠、1,000錠 エビリファイ錠6mg：［PTP］100錠(10錠×10)、500錠(10錠×50) ［プラスチックボトル］500錠、1,000錠 エビリファイ錠12mg：［PTP］100錠(10錠×10)、500錠(10錠×50) ［プラスチックボトル］500錠 エビリファイ散1％：［プラスチックボトル］100g、500g 製造販売元 大塚製薬株式会社 完整资料附件：http://www.info.pmda.go.jp/go/pack/1179045B1021_1_21/ The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse effects (risks) as well as efficacies (benefits). It is important to minimize adverse effects and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment. Brand name : ABILIFY Tablets 3mg 　Active ingredient: Aripiprazole 　Dosage form: blue tablet, diameter: 6 mm, thickness: 2.5 mm 　Print on wrapping: identification code-OG72, print on back of the sheet -エビリファイ錠3mg   6mg 12mg Effects of this medicine This medicine acts on receptors for dopamine, a neurotransmitter in the brain, to suppress symptoms such as hallucination and delusion and to stabilize unstable mental status. It also improves moods of lack of motivation and apathy, and symptoms such as unrestrained emotions and behaviors. It is usually used in the treatment of schizophrenia, for improvement of manic episodes associated with bipolar disorder and for depression/depressive state. Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines. If you have diabetes or if you or your family has a history of diabetes. If you have hepatic disorder, cardiovascular disease or hypotension. If you have a convulsive disease such as epilepsy, or a history thereof. If you have suicidal attempt or suicidal ideation. If you have a predisposition to organic brain disorder. If you have a highly impulsive comorbid disorder. •If you are pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is to be written by a healthcare professional> •For schizophrenia: In general, for adults, start with taking 2 to 4 tablets (6 to 12 mg of the active ingredient) daily, then take 2 to 8 tablets (6 to 24 mg of the active ingredient) daily at one time or in two divided doses as a maintenance dose. The dosage may be adjusted according to age and symptoms. However, the daily dose should not exceed 10 tablets (30 mg of the active ingredient). For improvement of manic episodes associated with bipolar disorder: In general, for adults, take 4 to 8 tablets (12 to 24 mg of the active ingredient) at one time, once daily. The starting dose is determined as 8 tablets (24 mg of the active ingredient), and the dosage may be adjusted according to age and symptoms. However, the daily dose should not exceed 10 tablets (30 mg of the active ingredient). For depression/depressive state (administration should be limited to patients who showed an inadequate response to existing antidepressant therapy.): In general, for adults, take one tablet (3 mg of the active ingredient) at one time, once daily. The dosage may be adjusted according to age and symptoms. The dose increase per day should be one tablet (3 mg of the active ingredient). However, the daily dose should not exceed 5 tablets (15 mg of the active ingredient). This preparation contains 3 mg of the active ingredient in a tablet. In any case, strictly follow the instructions. •If you miss a dose, take a dose as soon as you remember. However, if it is almost time for the next dose, skip the missed dose and follow your regular dosing schedule. You should never take two doses at one time. •If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist. •Do not stop taking this medicine unless your doctor instructs you to do so. Precautions while taking this medicine •This medicine may cause sleepiness; decreased attentiveness, concentration and reflex movements. Avoid operating dangerous machinery such as driving a car. •Alcohol may intensify the therapeutic effects of the medicine. Be careful when drinking alcohol. Possible adverse effects of this medicine The most commonly reported adverse reactions include insomnia, nervousness, akathisia (restlessness), tremor (trembling of limbs), anxiety, weight loss, muscle rigidity, loss of appetite, somnolence, hypokinesia (expressionless face), salivation (drooling), weight gain, nausea, vomiting, dystonia (muscle tone abnormalities) and constipation. If any of these symptoms occur, consult with your doctor or pharmacist. The symptoms described below are rarely seen as initial symptoms of the adverse effects indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •dry mouth, excessive intake of water, increased urine output [diabetic ketoacidosis, diabetic coma] •being silent without moving, muscle stiffness, sudden fever [neuroleptic malignant syndrome] •moving the tongue, putting the tongue out and pulling it back in, continual movement of the mouth appearing to chew something [tardive dyskinesia] •nausea, vomiting, constipation, intense abdominal pain [paralytic ileus] •weakness, muscle pain, reddish brown urine [rhabdomyolysis] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information •Keep out of the reach of children. Store away from direct sunlight, heat and humidity. •If there is remainder, this is to be discarded. Do not store it. Ask the pharmacy or medical institution about how to discard the remainder.