| Abilify（阿立哌唑 Aripiprazole）是一种口服和注射的药物，已获FDA批准用于治疗精神分裂症。它是多巴胺部分激动剂和血清素拮抗剂。 批准日期：2002年11月 公司：大冢美国制药公司 ABILIFY（阿立哌唑[aripiprazole]）片 ABILIFY DISCMELT（阿立哌唑[aripiprazole]）口服崩解片 ABILIFY（阿立哌唑[aripiprazole]）口服液 ABILIFY（阿立哌唑[aripiprazole]）注射液仅用于肌肉注射 美国最初批准：2002年 警告： 患有与痴呆症有关的精神病患者和患有抗癫痫药物的自杀行为的老年人死亡率增加，请参阅完整的警告信息的完整预定信息。 •用抗精神病药物治疗的老年痴呆症相关精神病患者死亡风险增加。ABILIFY未被批准用于治疗痴呆相关精神病患者。 •儿童，青少年和服用抗抑郁药的年轻人的自杀思维和行为风险增加。监测恶化和自杀念头和行为的出现。 最近的重大变化 警告和注意事项，病态赌博和其他强迫行为：08/2016 警告和注意事项，瀑布：02/2017 作用机制 阿立哌唑在精神分裂症或双相躁狂症中的作用机制尚不清楚。 然而，阿立哌唑的功效可以通过D2和5-HT1A受体的部分激动剂活性和5-HT2A受体的拮抗剂活性的组合来介导。 对除D2,5-HT1A和5-HT2A以外的受体的作用可以解释阿立哌唑的一些其他临床效果（例如，用阿立哌唑观察到的直立性低血压可以通过其对肾上腺素能α1受体的拮抗剂活性来解释）。 适应症和用法 ABILIFY是一种非典型的抗精神病药物。口服制剂适用于： •精神分裂症。 •与双相I相关的躁狂和混合发作的急性治疗 •重度抑郁症的辅助治疗。 •与自闭症有关的烦躁不安。 •治疗抽动秽语障碍。 注射用于： •与精神分裂症或双相躁狂症相关的躁动。 剂量和给药 初始剂量 推荐剂量 最大剂量 精神分裂症-成年人 10-15毫克/天 10-15毫克/天 30毫克/天 精神分裂症-青少年 2毫克/天 10毫克/天 30毫克/天 双极躁狂症-成人：单药治疗 15毫克/天 15毫克/天 30毫克/天 双极性躁狂症 -成人：辅以锂或丙戊酸钠 10-15毫克/天 15毫克/天 30毫克/天 双相躁狂症 2毫克/天 10毫克/天 30毫克/天 -儿科患者： 单药治疗或作为锂或丙 戊酸钠的辅助治疗 严重抑郁症 2-5毫克/天 5-10毫克/天 15毫克/天 -成人与抗抑郁药有关 与自闭症相关的易怒 2毫克/天 5-10毫克/天 15毫克/天 -儿科患者 患者<50公斤 2毫克/天 5毫克/天 10毫克/天 抽动秽语 - 患者<50公斤 2毫克/天 10毫克/天 20毫克/天 与精神分裂症或 9.75mg/1.3mLIM注射 30mg /天IM注射 双相躁狂症相关的躁动 -成人 口服制剂：每日一次，不考虑进餐。 •IM注射：两次服药之间至少等待2小时。每日最大剂量30毫克。 •已知CYP2D6代谢不良者：常用剂量的一半。 剂量形式和强度 •片剂：2mg，5mg，10mg，15mg，20mg和30mg •口腔崩解片：10mg和15mg •口服溶液：1mg/mL •注射：9.75mg/1.3mL单剂量小瓶 禁忌症 •已知对ABILIFY过敏。 警告和注意事项 •老年痴呆患者的脑血管不良反应 相关精神病：脑血管不良反应发生率增加（例如中风，短暂性脑缺血发作，包括死亡）。 •神经性恶性综合症：立即停药并密切监测。 •迟发性运动障碍：如果临床适当，则停用。 •代谢变化：非典型抗精神病药物与代谢变化有关，包括高血糖/糖尿病，血脂异常和体重增加。 o高血糖/糖尿病：定期监测患有糖尿病并有患糖尿病风险的患者的血糖。 o血脂异常：在用非典型抗精神病药物治疗的患者中观察到不希望的脂质水平改变。 o体重增加：非典型抗精神病药使用时观察到体重增加。监控重量。 •病理性赌博和其他强迫行为：考虑减少剂量或停药 •直立性低血压：监测心率和血压，并警告患有已知心血管或脑血管疾病的患者，以及脱水或晕厥的风险。 •白细胞减少症，中性粒细胞减少症和粒细胞缺乏症：已报道抗精神病药包括ABILIFY。具有临床显着低白细胞计数（WBC）或药物诱导的白细胞减少/中性粒细胞减少症史的患者应在治疗的最初几个月内经常监测其全血细胞计数（CBC），并应考虑停止使用ABILIFY在没有其他致病因素的情况下，WBC临床显着下降的第一个迹象。 •癫痫发作/惊厥：对有癫痫病史或癫痫发作阈值降低的病人慎用。 •认知和运动损伤的可能性：操作机器时要小心。 •自杀：自杀未遂的可能性是精神分裂症和双相情感障碍所固有的。密切监督高危患者。 不良反应 常见的不良反应（发生率≥5％，至少是安慰剂的两倍）是： •成人精神分裂症患者：静坐不能 •精神分裂症患儿（13至17岁）：锥体外系障碍，嗜睡和震颤 •患有双相躁狂症的成人患者（单药治疗）：静坐不能，镇静，烦躁不安，震颤和锥体外系疾病 •患有双相躁狂症的成人患者（锂或丙戊酸钠辅助治疗）：静坐不能，失眠和锥体外系障碍 •患有双相躁狂症的儿科患者（10至17岁）：嗜睡，锥体外系障碍，疲劳，恶心，静坐不能，视力模糊，唾液分泌过多和头晕 •患有严重抑郁症的成年患者（抗抑郁治疗的辅助治疗）：静坐不安，烦躁不安，失眠，便秘，疲劳和视力模糊 •患有自闭症的儿科患者（6至17岁）：镇静，疲劳，呕吐，嗜睡，震颤，发热，流口水，食欲下降，唾液分泌过多，锥体外系障碍和嗜睡 •患有抽动秽语疾病的儿科患者（6至18岁）：镇静，嗜睡，恶心，头痛，鼻咽炎，疲劳，食欲增加 •伴有精神分裂症或双相性躁狂症的成人患者：恶心 要报告疑似不良反应，请致电1-800-721-5072联系Bristol-Myers Squibb或1-800-FDA-1088或WWW.FDA.GOV/MEDWATCH联系FDA。 药物相互作用 药物相互作用引起的剂量调整： ABILIFY的因素剂量调整 已知的CYP2D6差的代谢产物给予常用剂量的一半 已知的CYP2D6差的代谢产物和强的CYP3A4抑制剂给予常用剂量的四分之一 强CYP2D6或CYP3A4抑制剂给予常用剂量的一半 强CYP2D6和CYP3A4抑制剂给予常用剂量的四分之一 强CYP3A4诱导剂在1至2周内双倍常用剂量 用于特定人群 •怀孕：在妊娠晚期接触的新生儿中可能引起锥体外系和/或戒断症状。 •哺乳母亲：考虑到药物对母亲的重要性，停止使用药物或护理。 包装提供/存储和处理 提供 ABILIFY®（阿立哌唑）片剂的一面有标记，有表32中列出的强度和包装。 ABILIFYDISLCELT®（阿立哌唑）口服崩解片剂是圆形片剂，两侧都有标记。 ABILIFY DISCMELT有表33中列出的优势和包装。 ABILIFY®（阿立哌唑）口服液（1mg/mL）以儿童防护瓶供应，并配有校准口服剂量杯。 ABILIFY口服液如下： 150mL瓶NDC 59148-013-15 ABILIFY®（阿立哌唑）肌注用注射液可作为即用型9.75mg/1.3mL（7.5mg/mL）透明1型玻璃瓶使用，如下所示： 9.75mg/1.3mL单剂量小瓶NDC 59148-016-65 存储 片 储存在25°C（77°F）;允许的偏差在15°C至30°C（59°F至86°F）之间[见USP受控室温]。 口服液 ABILIFY OS 1MG/ML 150ML ARIPIPRAZOLE ER SQUIBB & SONS LLC 59148-0013-15 储存在25°C（77°F）;允许的偏差在15°C至30°C（59°F至86°F）之间[见USP受控室温]。打开瓶装的ABILIFY口服液可以使用6个月，但不能超过瓶子的有效期。瓶子及其内容应在失效日期后丢弃。 注射 储存在25ºC（77°F）;允许的偏差在15°C至30°C（59°F至86°F）之间[见USP受控室温]。存放在原始容器中避光。保留纸箱直至使用。 ----------------------------------------------------------------- 包装规格：（注：以下产品不同规格和不同价格，采购以咨询为准） ----------------------------------------------------------------- ABILIFY 10MG UD BP 10X10 ARIPIPRAZOLE ER SQUIBB & SONS LLC 59148-0008-35 ABILIFY DISCMELT TB 10MG 30 ARIPIPRAZOLE ER SQUIBB & SONS LLC 59148-0640-23 ABILIFY DISCMELT TB 15MG 30 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0641-23 ABILIFY OS 1MG/ML 150ML ARIPIPRAZOLE ER SQUIBB & SONS LLC 59148-0013-15 ABILIFY SDV 9.75MG/1.3ML 7.5MG ARIPIPRAZOLE ER SQUIBB & SONS LLC 59148-0016-65 ABILIFY TAB 5MG 30 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0007-13 ABILIFY TAB 5MG UD 10X10 ARIPIPRAZOLE ER SQUIBB & SONS LLC 59148-0007-35 ABILIFY TAB 10MG 30 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0008-13 ABILIFY TAB 15MG 30 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0009-13 ABILIFY TAB 15MG UD 10X10 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0009-35 ABILIFY TAB 20MG 30 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0010-13 ABILIFY TAB 20MG UD 10X10 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0010-35 ABILIFY TAB 2MG 30 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0006-13 ABILIFY TAB 30MG 30 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0011-13 ABILIFY TAB 30MG UD 10X10 ARIPIPRAZOLE OTSUKA AMERICA PHARM 59148-0011-35 --------------------------------------------------------------------- ABILIFY(aripiprazole)Tablets、Orally Disintegrating Tablets、Oral Solution、 Injection General Information INDICATIONS and IMPORTANT SAFETY INFORMATION for ABILIFY® (aripiprazole) INDICATIONS ABILIFY is indicated for: Treatment of Schizophrenia in adults and adolescents 13 to 17 years of age Acute treatment of manic or mixed episodes associated with Bipolar I Disorder as monotherapy and as an adjunct to lithium or valproate in adult and pediatric patients 10 to 17 years of age Maintenance treatment of Bipolar I Disorder, both as monotherapy and as an adjunct to lithium or valproate in adults Use as an adjunctive therapy to antidepressants in adults with Major Depressive Disorder who have had an inadequate response to antidepressant therapy Treatment of irritability associated with Autistic Disorder in pediatric patients 6 to 17 years of age Treatment of Tourette’s Disorder in pediatric patients 6 to 18 years of age Special Considerations for Pediatric Uses: Treatment for pediatric patients should be initiated only after a thorough diagnostic evaluation and careful consideration of the risks and benefits of treatment. Medication should be part of a treatment program that also includes psychological, educational, and social interventions IMPORTANT SAFETY INFORMATION WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk (1.6 to 1.7 times) of death compared to placebo (4.5% vs 2.6%, respectively). Although the causes of death were varied, most of the deaths appeared to be cardiovascular (e.g., heart failure, sudden death) or infectious (e.g., pneumonia) in nature. ABILIFY is not approved for the treatment of patients with dementia-related psychosis. WARNING: SUICIDAL THOUGHTS AND BEHAVIORS Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of Major Depressive Disorder (MDD) and other psychiatric disorders. Anyone considering the use of adjunctive ABILIFY or another antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increased risk of suicidality in adults beyond age 24. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber. ABILIFY is not approved for use in pediatric patients with depression. Contraindication–Known hypersensitivity reaction to ABILIFY. Reactions have ranged from pruritus/urticaria to anaphylaxis. Cerebrovascular Adverse Events, Including Stroke–Increased incidence of cerebrovascular adverse events (e.g. stroke, transient ischemic attack), including fatalities, have been reported in clinical trials of elderly patients with dementia-related psychosis treated with ABILIFY. Neuroleptic Malignant Syndrome (NMS) – A potentially fatal symptom complex sometimes referred to as NMS may occur with administration of antipsychotic drugs, including ABILIFY. Rare cases of NMS occurred during ABILIFY treatment. Signs and symptoms of NMS include hyperpyrexia, muscle rigidity, altered mental status, and evidence of autonomic instability (e.g., irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmia). Additional signs may include elevated creatinine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure. The management of NMS should include: 1) immediate discontinuation of antipsychotic drugs and other drugs not essential to concurrent therapy; 2) intensive symptomatic treatment and medical monitoring; and 3) treatment of any concomitant serious medical problems for which specific treatments are available. Tardive Dyskinesia (TD)–The risk of developing TD (a syndrome of abnormal, involuntary movements) and the potential for it to become irreversible are believed to increase as the duration of treatment and the total cumulative dose of antipsychotic increase. The syndrome can develop, although much less commonly, after relatively brief treatment periods at low doses. Prescribing should be consistent with the need to minimize TD. There is no known treatment for established TD, although the syndrome may remit, partially or completely, if antipsychotic treatment is withdrawn. Metabolic Changes–Atypical antipsychotic drugs have been associated with metabolic changes that include: Hyperglycemia/Diabetes Mellitus–Hyperglycemia, in some cases extreme and associated with ketoacidosis, coma, or death, has been reported in patients treated with atypical antipsychotics including ABILIFY. Patients with diabetes should be regularly monitored for worsening of glucose control; those with risk factors for diabetes should undergo baseline and periodic fasting blood glucose testing. Any patient treated with atypical antipsychotics should be monitored for symptoms of hyperglycemia including polydipsia, polyuria, polyphagia, and weakness. Patients who develop symptoms of hyperglycemia should also undergo fasting blood glucose testing. In some cases, hyperglycemia has resolved when the atypical antipsychotic was discontinued; however, some patients required continuation of anti-diabetic treatment despite discontinuation of the suspect drug. Dyslipidemia–Undesirable alterations in lipids have been observed in patients treated with atypical antipsychotics. Weight Gain–Weight gain has been observed with atypical antipsychotic use. Clinical monitoring of weight is recommended. When treating pediatric patients, weight gain should be monitored and assessed against that expected for normal growth. Pathological Gambling and Other Compulsive Behaviors – Intense urges, particularly for gambling, and the inability to control these urges have been reported while taking ABILIFY. Other compulsive urges (e.g., eating, sexual, or shopping) have been reported less frequently. Prescribers should ask patients or their caregivers specifically about, and closely monitor for, the development of new or intense compulsive urges. Consider dose reduction or stopping ABILIFY, if such urges develop. Orthostatic Hypotension–ABILIFY may cause orthostatic hypotension and should be used with caution in patients with known cardiovascular disease, cerebrovascular disease, or conditions which would predispose them to hypotension. Falls–Antipsychotics may cause somnolence, postural hypotension, motor and sensory instability, which may lead to falls causing fractures or other injuries. For patients with diseases, conditions, or medications that could exacerbate these effects, complete fall risk assessments when initiating treatment and recurrently during therapy. Leukopenia, Neutropenia, and Agranulocytosis – Leukopenia, neutropenia, and agranulocytosis have been reported. In patients with a history of clinically significant low white blood cell count (WBC)/absolute neutrophil count (ANC) or history of drug-induced leukopenia/neutropenia, perform a complete blood count (CBC) frequently during the first few months of therapy. Consider discontinuing ABILIFY at the first sign of a clinically significant decline in WBC in the absence of other causative factors. Monitor patients with clinically significant neutropenia for fever or other symptoms or signs of infection and treat promptly if such symptoms or signs occur. Discontinue ABILIFY in patients with severe neutropenia (ANC <1000/mm3) and follow their WBC counts until recovery. Seizures/Convulsions–ABILIFY should be used with caution in patients with a history of seizures or with conditions that lower the seizure threshold. Potential for Cognitive and Motor Impairment – ABILIFY may impair judgment, thinking, or motor skills. Instruct patients to avoid operating hazardous machinery, including automobiles, until they are certain ABILIFY does not affect them adversely. Body Temperature Regulation – Disruption of the body’s ability to reduce core body temperature has been attributed to antipsychotic agents. Advise patients regarding appropriate care in avoiding overheating and dehydration. Appropriate care is advised for patients who may exercise strenuously, may be exposed to extreme heat, receive concomitant medication with anticholinergic activity, or are subject to dehydration. Suicide–The possibility of a suicide attempt is inherent in psychotic illnesses, Bipolar Disorder, and Major Depressive Disorder. Close supervision of high-risk patients should accompany drug therapy. Prescriptions should be written for the smallest quantity consistent with good patient management in order to reduce the risk of overdose. Dysphagia–Esophageal dysmotility and aspiration have been associated with antipsychotic drug use, including ABILIFY; use caution in patients at risk for aspiration pneumonia. Aspiration pneumonia is a common cause of morbidity and mortality in elderly patients, in particular those with advanced Alzheimer’s dementia. Alcohol-Advise patients to avoid alcohol while taking ABILIFY. Concomitant Medication – Dosage adjustments are recommended in patients who are CYP2D6 poor metabolizers and in patients taking concomitant CYP3A4 inhibitors or CYP2D6 inhibitors or strong CYP3A4 inducers. When the coadministered drug is withdrawn from the combination therapy, ABILIFY dosage should then be adjusted to its original level. When the coadministered CYP3A4 inducer is withdrawn, ABILIFY dosage should be reduced to the original level over 1 to 2 weeks. For patients who are known CYP2D6 poor metabolizers, administer half of usual dose. For patients who are known CYP2D6 poor metabolizers taking concomitant strong CYP3A4 inhibitors (e.g., itraconazole, clarithromycin), administer a quarter of usual dose. For patients taking strong CYP2D6 (e.g., quinidine, fluoxetine, paroxetine) or CYP3A4 inhibitors (e.g., itraconazole, clarithromycin), administer half of usual dose. For patients taking strong CYP2D6 and CYP3A4 inhibitors, administer a quarter of usual dose. For patients taking strong CYP3A4 inducers (e.g., carbamazepine, rifampin), double usual dose over 1 to 2 weeks. Commonly observed adverse reactions: (≥5% incidence and at least twice the rate of placebo for ABILIFY vs placebo, respectively): Adult patients with Major Depressive Disorder (adjunctive treatment to antidepressant therapy): akathisia (25% vs 4%), restlessness (12% vs 2%), insomnia (8% vs 2%), constipation (5% vs 2%), fatigue (8% vs 4%), and blurred vision (6% vs 1%) Adult patients (monotherapy) with Bipolar Mania: akathisia (13% vs 4%), sedation (8% vs 3%), tremor (6% vs 3%), restlessness (6% vs 3%), and extrapyramidal disorder (5% vs 2%) Adult patients (adjunctive therapy with lithium or valproate) with Bipolar Mania: akathisia (19% vs 5%), insomnia (8% vs 4%), and extrapyramidal disorder (5% vs 1%) Pediatric patients (10 to 17 years) with Bipolar Mania: somnolence (23% vs 3%), extrapyramidal disorder (20% vs 3%), fatigue (11% vs 4%), nausea (11% vs 4%), akathisia (10% vs 2%), blurred vision (8% vs 0%), salivary hypersecretion (6% vs 0%), and dizziness (5% vs 1%) Adult patients with Schizophrenia: akathisia (8% vs 4%) Pediatric patients (13 to 17 years) with Schizophrenia: extrapyramidal disorder (17% vs 5%), somnolence (16% vs 6%), and tremor (7% vs 2%) Pediatric patients (6 to 17 years) with irritability associated with Autistic Disorder: sedation (21% vs 4%), fatigue (17% vs 2%), vomiting (14% vs 7%), somnolence (10% vs 4%), tremor (10% vs 0%), pyrexia (9% vs 1%), drooling (9% vs 0%), decreased appetite (7% vs 2%), salivary hypersecretion (6% vs 1%), extrapyramidal disorder (6% vs 0%), and lethargy (5% vs 0%) Pediatric patients (6 to 18 years) with Tourette’s Disorder: sedation (13% vs 6%), somnolence (13% vs 1%), nausea (11% vs 4%), headache (10% vs 3%), nasopharyngitis (9% vs 0%), fatigue (8% vs 0%), and increased appetite (7% vs 1%) Dystonia–Symptoms of dystonia may occur in susceptible individuals during the first days of treatment and at low doses. Pregnancy-Neonates exposed to antipsychotic drugs, including ABILIFY, during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms. These complications have varied in severity, from being self-limited to requiring intensive care and prolonged hospitalization. ABILIFY should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Nursing Mothers–ABILIFY is present in human breast milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother and any potential risks to the infant. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c040bd1d-45b7-49f2-93ea-aed7220b30ac |