英文药名: Seroquel XR(quetiapine fumarate extended-release tablets) 中文药名: 思瑞康（富马酸喹硫平缓释片） 生产厂家: 阿斯利康 药品介绍 批准日期：2013年4月 公司：AstraZeneca SEROQUELXR（富马酸喹硫平 quetiapine fumarate）缓释片，供口服使用 最初美国批准：1997年 警告： 增加死亡率与老年痴呆症相关精神病老年住院患者;自杀的念头和BEHAVIORSSee完整处方完整黑框警告信息。 死亡率增加老年痴呆相关精神病 •老年痴呆患者相关精神病用抗精神病药物治疗是在死亡的风险增加。思瑞康XR没有被批准用于治疗老年痴呆症相关的精神病。 自杀的想法和行为 •提高对儿童，青少年和年轻的成年人服用抗抑郁药自杀的想法和行为的风险 •监测恶化，自杀念头和行为出现 目前的主要变化 警告和注意事项，脑血管不良反应，包括中风，老年痴呆患者相关精神病  4/2013 作用机理 精神分裂症，双相型障碍和抑郁症（MDD）的治疗思瑞康XR的作用机理，是未知的。然而，其在精神分裂症的功效可以通过多巴胺型2（D2）和血清素2A型（5HT2A）拮抗作用的组合来介导的。活性代谢物，N- desalkyl喹硫平（norquetiapine），具有在D2的相似的活性，但在5HT2A受体更大的活性，比母体药物（喹硫平）。双相抑郁和MDD喹硫平疗效可部分由高亲和力和norquetiapine展品去甲肾上腺素转运有效的抑制效应来解释。 拮抗作用比多巴胺和血清素具有相似或更大的亲和力其它受体可能解释一些奎和norquetiapine的其他影响：在组胺H1受体的拮抗作用可以解释嗜睡，对立的肾上腺素α1B受体可以解释体位性低血压，和对立的毒蕈碱M1受体可以解释抗胆碱作用。 适应症和用法 SEROQUEL XR是用于治疗表示的非典型抗精神病药物： •精神分裂症 •I型双相障碍，躁狂或混合发作 •双相情感障碍，抑郁发作 •重性抑郁障碍，抗抑郁药辅助治疗 用法用量 •吞咽药片的整体，不要分裂，咀嚼或咬碎 •采取没有食物或便餐（约300卡路里） •管理每日一次，优选在晚上 •老年用药：在考虑中老年人的最初给药期间较低的起始剂量（50毫克/天），速度较慢滴定，并将仔细监测 •肝损伤：下起始剂量（50毫克/天）和较慢的滴定可能需要 迹象 初始剂量 推荐剂量 极量 Schizophrenia-成人 300毫克/天 400-800毫克/天 800毫克/天 精神分裂症青少年（13至17岁） 50mg /天 400-800毫克/天 800毫克/天 I型双相情感障碍躁狂或混合急性单一疗法或辅助锂或双丙戊酸钠，成年人 300毫克/天 400-800毫克/天 800毫克/天 I型双相情感障碍，躁狂急性单药治疗 - 儿童和青少年（10至17岁） 50mg /天 400-600毫克/天 600mg /天 双相情感障碍，抑郁发作，成人 50mg/天 300毫克/天 300毫克/天 重度抑郁症，辅助治疗与抗抑郁药，成人 50mg/天 150-300毫克/天 300毫克/天 剂型和规格 缓释片剂：50毫克，150毫克，200毫克，300毫克和400毫克。 禁忌症 已知过敏思瑞康XR或配方中的任何组件。 警告和注意事项 •脑血管不良反应：增加脑血管不良事件（例如，中风，短暂性脑缺血发作）发生率一直被视为老年患者与非典型抗精神病药物治疗老年痴呆症相关的精神病 •抗精神病药物恶性症候群（NMS）：用立即停止并密切监测管理。 •代谢变化：非典型抗精神病药物已经与代谢变化有关。这些代谢变化包括高血糖，血脂异常，以及体重增加。 高血糖和糖尿病：监测患者高血糖的症状，包括多饮，多尿，多食和无力。监测患者的血糖经常有糖尿病或处于糖尿病风险 血脂异常：不良的改变是在与非典型抗精神病药物治疗的患者中观察到。建议适当的临床监测，包括在开头空腹血脂检测，并周期性，在治疗过程中。 体重增加：增益体重已被观察到;重量的临床监测建议。 •迟发性运动障碍：如果停止临床适宜。 •低血压：患者慎用使用与已知的心血管或脑血管疾病。 •血压升高的儿童和青少年：监视之初血压，并定期在儿童和青少年在治疗过程中。 •白细胞减少，粒细胞减少及粒细胞缺乏症：在治疗的头几个月的患者预先存在低白细胞计数或白细胞减少/中性粒细胞减少史经常监测全血细胞计数和在WBC下降的第一个征兆停止思瑞康XR在没有其他致病因素。 •白内障：镜头变化的患者长期喹硫平治疗期间被观察到。开始治疗时，建议镜检查，并在长期治疗期间6个月的间隔。 不良反应 最常见的不良反应（发生率≥5％和安慰剂组的两倍） 成人：嗜睡，口干，便秘，头晕，食欲增加，消化不良，体重增加，疲劳，构音障碍，鼻塞。 儿童和青少年：嗜睡，头晕，乏力，食欲增加，恶心，呕吐，口干，心动过速，增加重量。 药物相互作用 •伴随使用强CYP3A4抑制剂：当具有较强的CYP3A4抑制剂合用减少喹硫平剂量六分之一（例如，酮康唑，利托那韦） •伴随使用CYP3A4强诱导剂：强效CYP3A4诱导与长期治疗联合使用（超过7-14天）时增加喹硫平剂量高达5倍（例如，苯妥英，利福平，圣约翰草） •CYP3A4强诱导剂中止：由5折以内CYP3A4诱导停药7-14天减少剂量喹硫平。 特殊人群中使用 •怀孕：有限的人力数据。根据动物实验数据，可能会对胎儿造成伤害。只有潜在效益合理的潜在风险，应使用喹硫平。 •哺乳母亲：请停止药物或哺乳，考虑到药物的考虑重视母亲的健康。 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] SEROQUEL XR TAB 200MG 60  QUETIAPINE FUMARATE     00310-0282-60       SEROQUEL XR TAB 200MG UD 100  QUETIAPINE FUMARATE     00310-0282-39    SEROQUEL XR TAB 300MG 60  QUETIAPINE FUMARATE     00310-0283-60        SEROQUEL XR TAB 300MG UD 100  QUETIAPINE FUMARATE     00310-0283-39    SEROQUEL XR TAB 400MG 60  QUETIAPINE FUMARATE     00310-0284-60  SEROQUEL XR TAB 400MG UD 100  QUETIAPINE FUMARATE     00310-0284-39    SEROQUEL XR TAB 50MG 60  QUETIAPINE FUMARATE     00310-0280-60       SEROQUEL XR TAB 50MG HUD 100  QUETIAPINE FUMARATE     00310-0280-39    SEROQUEL XR TAB 150MG 60  QUETIAPINE FUMARATE     00310-0281-60       SEROQUEL XR TAB 150MG HUD 100  QUETIAPINE FUMARATE     00310-0281-39  阿斯利康制药公司近日宣布其生产的Seroquel X（quetiapine fumarate）已获得美国FDA批准上市。Seroquel XR是用于双相Ⅰ型精神障碍抑郁发作、躁狂发作和混合发作的急性期治疗的缓释片，也可作为锂或双丙戊酸钠的辅助用药，用于双相精神障碍的维持治疗。 它是第一个获得FDA批准的、每日一次、用于双相精神障碍，治疗抑郁和躁狂期的急性期治疗药物。 研究者指出，事实上该类病人抑郁症状出现的次数要比躁狂症状多3倍，Seroquel XR获批准上市，每天使用一次，已证实其控制双相精神障碍病人的抑郁和躁狂症状的效果显著。 完整信息和用药指南附件：http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=473a3ac4-67f4-4782-baa9-7f9bdd8761f4 SEROQUEL XR(QUETIAPINE FUMARATE)TABLET EXTENDED RELEASE ORAL INDICATIONS AND USAGE SEROQUEL XR is indicated for the treatment of schizophrenia. The efficacy of SEROQUEL XR in schizophrenia was established in part, on the basis of extrapolation from the established effectiveness of SEROQUEL. In addition, the efficacy of SEROQUEL XR was demonstrated in 1 short-term (6-week) controlled trial of schizophrenic inpatients and outpatients [ see Clinical Studies ]. The effectiveness of SEROQUEL XR in long-term use, that is, for more than 6 weeks, has not been systematically evaluated in controlled trials. Therefore, the physician who elects to use SEROQUEL XR for extended periods should periodically re-evaluate the long-term usefulness of the drug for the individual patient [ See Dosage And Administration ]. DOSAGE AND ADMINISTRATION Usual Dose SEROQUEL XR should be administered once daily, preferably in the evening. The recommended initial dose is 300 mg/day. Patients should be titrated within a dose range of 400 – 800 mg/day depending on the response and tolerance of the individual patient [ see Clinical Studies ]. Dose increases can be made at intervals as short as 1 day and in increments of up to 300 mg/day. The safety of doses above 800 mg/day has not been evaluated in clinical trials. SEROQUEL XR tablets should be swallowed whole and not split, chewed or crushed. It is recommended that SEROQUEL XR be taken without food or with a light meal (approximately 300 calories) [ see Clinical Pharmacology ]. Dosing in Special Populations Consideration should be given to a slower rate of dose titration and a lower target dose in the elderly and in patients who are debilitated or who have a predisposition to hypotensive reactions [see Use in Specific Populations (8.5, 8.7) and Clinical Pharmacology ]. When indicated, dose escalation should be performed with caution in these patients. For those patients who require less than 200 mg per dose of SEROQUEL XR during the initial titration, use the immediate release formulation. Elderly patients should be started on SEROQUEL immediate release formulation 25 mg/day and the dose can be increased in increments of 25–50 mg/day depending on the response and tolerance of the individual patient. When an effective dose has been reached, the patient may be switched to SEROQUEL XR at an equivalent total daily dose [ see Switching Patients from SEROQUEL Tablets to SEROQUEL XR Tablets ]. Patients with hepatic impairment should be started on SEROQUEL immediate release formulation 25 mg/day. The dose can be increased daily in increments of 25–50 mg/day to an effective dose, depending on the clinical response and tolerance of the patient. When an effective dose has been reached, the patient may be switched to SEROQUEL XR at an equivalent total daily dose [ see Switching Patients from SEROQUEL Tablets to SEROQUEL XR Tablets ]. The elimination of quetiapine was enhanced in the presence of phenytoin. Higher maintenance doses of quetiapine may be required when it is coadministered with phenytoin and other enzyme inducers such as carbamazepine and phenobarbital [See Drug Interactions ]. Maintenance Treatment While there is no body of evidence available to specifically address how long the patient treated with SEROQUEL XR should remain on it, it is recommended that responding patients be continued on SEROQUEL XR, but at the lowest dose needed to maintain remission. Patients should be periodically reassessed to determine the need for maintenance treatment. Re-initiation of Treatment in Patients Previoulsy Discontinued Although there are no data to specifically address reinitiation of treatment, it is recommended that when restarting therapy of patients who have been off SEROQUEL XR for more than one week, the initial dosing schedule should be followed. When restarting patients who have been off SEROQUEL XR for less than one week, gradual dose escalation may not be required and the maintenance dose may be reinitiated. Switching patients from SEROQUEL tablets to SEROQUEL XR tablets Schizophrenic patients who are currently being treated with divided doses of SEROQUEL (immediate release formulation, eg. 2 to 3 times per day) may be switched to SEROQUEL XR at the equivalent total daily dose taken once daily. Individual dosage adjustments may be necessary. Switching from Antipsychotics There are no systematically collected data to specifically address switching patients with schizophrenia from other antipsychotics to SEROQUEL XR, or concerning concomitant administration with other antipsychotics. While immediate discontinuation of the previous antipsychotic treatment may be acceptable for some patients with schizophrenia, more gradual discontinuation may be most appropriate for others. In all cases, the period of overlapping antipsychotic administration should be minimized. When switching patients with schizophrenia from depot antipsychotics, if medically appropriate, initiate SEROQUEL XR therapy in place of the next scheduled injection. The need for continuing existing extrapyramidal syndrome medication should be reevaluated periodically. DOSAGE FORMS AND STRENGTHS 200 mg extended — release tablets 300 mg extended — release tablets 400 mg sustained — release tablets HOW SUPPLIED/STORAGE AND HANDLING 200 mg Tablets (NDC 0310-0282) yellow, film coated, capsule-shaped, biconvex, intagliated tablet with “SR 200” on one side and plain on the other are supplied in bottles of 60 tablets and 500 tablets and hospital unit dose packages of 100 tablets. 300 mg Tablets (NDC 0310-0283) pale yellow, film coated, capsule-shaped, biconvex, intagliated tablet with “SR 300” on one side and plain on the other are supplied in bottles of 60 tablets and 500 tablets and hospital unit dose packages of 100 tablets. 400 mg Tablets (NDC 0310-0284) white, film coated, capsule-shaped, biconvex, intagliated tablet with “SR 400” on one side and plain on the other are supplied in bottles of 60 tablets and 500 tablets and hospital unit dose packages of 100 tablets. Store SEROQUEL XR at 25ºC (77ºF); excursions permitted to 15-30ºC (59-86ºF) [See USP].