【商品名】思瑞康 Seroquel
【英文名】Quetiapine fumarate
【性状】
25毫克片剂：圆形，桃红色； 100毫克片剂：圆形，黄色.；200毫克片剂：圆形，白色。

【药效学特征】
喹硫平是一种不典型抗精神病药物，对多种神经递质受体有相互作用。在脑中，喹硫平对五羟色胺(5HT2)受体具有高度亲和力，且大于对脑中多巴胺D1和多巴胺D2受体的亲和力。喹硫平对组织胺受体和肾上脉腺素能∝1受体同样有高亲和力，对肾上腺素能∝2受体亲和力低，但对胆碱能毒蕈碱样受体或苯二氮卓受体基本没有亲和力。喹硫平对抗精神病药物活性测定如条件回避反射呈阳性结果。

【不良反应】
喹硫平短期对照试验中所报告的最常见和最显著的不良事件为：困倦（17.5%），头晕（10%），便秘（9%），体位性低血压（7%），口干（7%），以及肝酶异常（6%）。
与其它具有α1肾上腺素能阻断作用的抗精神病药物一样，喹硫平片可能导致直立性低血压（伴有头晕），心悸，某些病人会有晕厥；这些事件易发生于开始的剂量增加期。
偶有报道服用喹硫平片的病人出现癫痫，但其发生率并不高于安慰剂组。
与其它抗精神病药物一样，用喹硫平片治疗的病人罕见有神经阻滞剂恶性综合征。
与其它抗精神病药物一样，服用喹硫平片会伴有白细胞计数改变，在临床对照试验中所报告的发生率为1.6%。偶尔有嗜酸性粒细胞增加的报道。
在服用喹硫平片的某些病人曾观察到出现无症状的血清转氨酶（ALT，AST）或 ψ－GT水平增高。这种增高通常在继续喹硫平片治疗过程中恢复。在喹硫平片治疗过程中曾观察到有非空腹状态下血清甘油三酯和总胆固醇水平轻微升高现象。
喹硫平片治疗可伴有轻微的与剂量有关的甲状腺激素水平下降，尤其是总T4和游离T4。几乎所有的病人在停用喹硫平后其对总T4和游离T4的影响可以恢复.

【药代学特征】
喹硫平口服后吸收良好，代谢完全。人类血浆中主要的代谢产物不具有明显的药理学活性。
进食对喹硫平的生物利用度无明显影响。喹硫平的小分队半衰期大约为7小时。83%的喹硫平与血浆蛋白结合。
临床试验证实，每日两次给药时喹硫平是有效的。正电子发射断层摄影术(PET)研究资料进一步证实，该药对5HT2和D2受体的占据作用在给药后可持续12小时。喹硫平的药代动力学是线性的，男女无差别。
老年愉喹硫平的平均清除率较18-65岁成年人低30-50%。严重肾损害(肌酐清除率低于30ml/min/1.73m2)和肝损害(稳定性酒精性肝硬化)的患者，喹硫平的平均血浆清除率可下降约25%，但个体清除率值都在正常人群范围之内。
喹硫平代谢较完全，服用放射性标记的喹硫平后尿或粪便中原型化合物仅占未改变的药物相关物质的5%以下。大约73%的放射性活性物从尿中排出，21%从粪便中排出。
离体研究证实喹硫平的主要代谢酶为细胞色素P450酶系统的CYP3A4。
喹硫平及其几种代谢产物是细胞色素P450酶1A2,2C9，2C19,2D6和3A4的弱抑制剂，但只在高于300-450毫克/日的人类有效剂量范围的10-50倍的深度时才出现。根据这些离体研究结果，喹硫平与其它药物合用时不易导致具有临床意义的与细胞色素P450酶相关的药物抑制作用。
【适应症】
“思瑞康”用于治疗精神分裂症。

【服用方法】
“思瑞康”应每日两次给药，饭前饭后均可。
成人 ：前4天治疗期的日总剂量为50毫克(第一日)，100毫克(第二日)，200毫克(第三日)和300毫克(第四日)。从第四日以后，将近剂量逐渐增加到有效剂量范围，一般为300－450毫克/日。可根据病人的临床反应和耐受性将剂量在150－750毫克/日之间调整。
肾脏和肝脏损害 ：口服喹硫平后的清除率在肾脏和肝脏损伤的病人中下降约25%。喹硫平在脏用词不当中代谢广泛，因此就在慎用于肝脏损害的患者。有肾脏或肝脏损害的病人，“思瑞康：的开始剂量应为25毫克/日。随后每日增加剂量，幅度为25－50毫克，直到有效剂量。

【禁忌症】
“思瑞康”禁用于对该产品的任何成分过敏的病人。

【注意事项】
心血管疾病
“思瑞康”可能会导致直立性低血压，尤其是在最初的加药期;在老年患者中上述现象较年轻患者多见。在临床试验中，使用喹硫平不伴发持久性QTc间期的延长。但与其它抗精神病药一样，如果效喹硫平与其它已知会延长QTc间期的药物合用时就在当谨慎，尤其是用于老年人时。
“思瑞康”应慎用于已知有心血管疾病、脑血管疾病或其它有低血压倾向的病人。
抽搐
在临床对照试验中，服用“思瑞康”的病人的抽搐发生率与服用安慰剂的病人无区别。与其它抗精神病药物一样，当用于治疗有抽搐病史的患者时应予以注意。
神经阻滞剂恶性综合征
抗精神病药物治疗会伴发神经阻滞剂恶性综合征。临床表现包手高热、精神状态改变、肌肉强直、植物神经功能紊乱以及肌酸磷酸激酶活性增加。若出现此种情况，应停用“思瑞康”并给予适当的治疗。
迟发性运动障碍
与其它抗精神病药物一样，长期服用“思瑞康”治疗也有导致迟发性运动障碍的可能性。如果出现迟发性运动障碍的体征和症状，应考虑减少“思瑞康”剂量或停用。
由于“思瑞康”可能会导致困倦。因此对操纵危险机器包括开车的病人应予提醒。

【孕妇及哺乳】
妇女用药
“思瑞康”用于人类妊娠时的疗效和安全性尚未肯定(对动物的生殖毒性资料见临床前案例性资料一节的生殖研究部分)。因此，只有在获益大于潜在危险的情况下“思瑞康”才能用于妊娠中的患者。
喹硫平在人类乳汁中的排泄情况尚不清楚。哺乳妇女若服用喹硫平应劝其在服药期间中断哺乳。
儿童用药
“思瑞康”用于儿童和青少年的安全性和有效性尚未进行评价。
老年患者用药
与其它抗精神病药物一样，“思瑞康”用于老年人也应慎彼一时，尤其在开始用药时。老年人的起始剂量应为25毫克/日。每日增加剂量，幅度为25－50毫克，直到有效剂量。有效剂量可能较一般年轻病人低。

【药物相互作用】
由于喹硫平主要具有中枢神经系统作用，“思瑞康”在与其它作用于中枢的药物或酒精合用时应当谨慎。
“思瑞康”与锂合用不会影响锂的药代动力学。
喹硫平不会诱导与安替比林代谢有关的肝脏酶系统。“思瑞康”和苯妥英(一种微粒体酶诱导剂)合用可增加喹硫平的清除率。如果效喹硫平与苯妥英或其它肝酶诱导剂(如卡马西平、巴比妥类、利福平)合用，为保持抗精神病症状的效果，应增加“思瑞康”的剂量。如果停用苯妥曲并换用一种非诱导剂(如丙戊酸钠)，则“思瑞康”的剂量需要减少。合用抗精神病药物利培酮或氟哌啶醇不会显著改变喹硫平的药代动力学。但“思瑞康”与硫利达嗪合用时会增加喹硫平的清除率。
与抗抑郁药丙米嗪(一种已知的CYP2D6抑制剂)或氟西汀(一种已知的CYP3A4和CYP2D6抑制剂)合用不会显著改变喹硫平的药代动力学。
在细胞色素酶P450中，介导喹硫平代谢的主要酶类为CYP3A4。与西咪替丁(CIMETIDINE)或氟西汀(两种药物都是已知的P450酶抑制剂)合用不会改变喹硫平的药代动力学。但是“思瑞康”与CYP3A4的强抑制剂[如全身应用的酮康只唑(KETOCONAZOLE)或红霉素]合用需谨慎。

【药物过量】
在临床试验中，对于“思瑞康”过量的经验不多。有人曾服用过10克“思瑞康”，未致死，而且病人完全恢复，无后遗症。
一般情况下，所报告的症状和体征是该药的已知药理学作用的增加，即困倦和镇静，心悸和低血压。
喹硫平无特异性解毒剂。遇到严重中毒的病人，应考虑多种药物介入的可能性，并建议采取积极的监护措施，包括开辟良好的气道，保证适当的氧气供应和呼吸，并且监测和维持心血管系统功能。
应采取严密的医疗监护和监测，直到病人恢复。

【储藏】
应贮存于30℃以下

【原产地英文商品名】SEROQUEL XR 24H 150mg/tab 60tabs/bottle
【原产地英文药品名】QUETIAPINE FUMARATE
【中文参考商品译名】
以下产品是不同规格和不同的价格，购买时请以电话咨询为准
思瑞康XR 24小时缓释片 300毫克/片 60片/瓶
思瑞康XR 24小时缓释片 300毫克/片 60片/瓶
思瑞康XR 24小时缓释片 400毫克/片 30片/瓶
思瑞康XR 24小时缓释片 200毫克/片 60片/瓶
思瑞康XR 24小时缓释片 300毫克/片 60片/瓶
思瑞康XR 24小时缓释片 50毫克/片 60片/瓶
思瑞康XR 24小时缓释片 50毫克/片 60片/瓶
思瑞康XR 24小时缓释片 150毫克/片 60片/瓶
思瑞康XR 24小时缓释片 150毫克/片 60片/瓶
思瑞康XR 24小时缓释片 200毫克/片 60片/瓶
【中文参考药品译名】富马酸喹硫平
【生产厂家中文参考译名】阿斯利康
【生产厂家英文名】ASTRAZENECA

Seroquel

Generic Name: quetiapine (kwe TYE a peen)
Brand Names: Seroquel, Seroquel XR

What is Seroquel?
Seroquel (quetiapine) is an antipsychotic medication. It works by changing the actions of chemicals in the brain.

Seroquel is used to treat schizophrenia in adults and children who are at least 13 years old. It is used to treat bipolar disorder (manic depression) in adults and children who are at least 10 years old.

Seroquel is also used together with antidepressant medications to treat major depressive disorder in adults.

Extended-release quetiapine (Seroquel XR) is for use only in adults and should not be given to anyone younger than 18 years old.

Seroquel may also be used for other purposes not listed in this medication guide.

Important information about Seroquel
Seroquel is not for use in psychotic conditions related to dementia. Seroquel may cause heart failure, sudden death, or pneumonia in older adults with dementia-related conditions. Stop using Seroquel and call your doctor at once if you have the following symptoms: very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, uncontrolled muscle movements, feeling light-headed, blurred vision, eye pain, increased thirst and urination, excessive hunger, fruity breath odor, weakness, nausea and vomiting.

You may have thoughts about suicide when you first start taking an antidepressant, especially if you are younger than 24 years old. Your doctor will need to check you at regular visits for at least the first 12 weeks of treatment.

Call your doctor at once if you have any new or worsening symptoms such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself.

Before taking Seroquel
Seroquel is not for use in psychotic conditions related to dementia. Seroquel may cause heart failure, sudden death, or pneumonia in older adults with dementia-related conditions.

If you have any of these other conditions, you may need a dose adjustment or special tests to safely take Seroquel:
liver or kidney disease;
heart disease, high blood pressure, heart rhythm problems;
a history of heart attack or stroke;
a history of low white blood cell (WBC) counts;
a thyroid disorder;
seizures or epilepsy;
cataracts;
high cholesterol or triglycerides;
a personal or family history of diabetes; or
trouble swallowing.

You may have thoughts about suicide when you first start taking an antidepressant such as Seroquel, especially if you are younger than 24 years old. Tell your doctor if you have worsening symptoms of depression or suicidal thoughts during the first several weeks of treatment, or whenever your dose is changed.

Your family or other caregivers should also be alert to changes in your mood or symptoms. Your doctor will need to check you at regular visits for at least the first 12 weeks of treatment.

FDA pregnancy category C. It is not known whether Seroquel will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using Seroquel. It is not known whether quetiapine passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are taking this medication. Do not give Seroquel to a child without a doctor's advice. Extended-release quetiapine (Seroquel XR) is for use only in adults and should not be given to anyone younger than 18 years old.

How should I take Seroquel?
Take Seroquel exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Your doctor may occasionally change your Seroquel dose to make sure you get the best results.

Take this medicine with a full glass of water. You may take Seroquel with or without food. Do not crush, chew, or break an extended-release tablet. Swallow the pill whole. Breaking the pill may cause too much of the drug to be released at one time.

To be sure Seroquel is not causing harmful effects, your blood cells, blood pressure, and vision may need to be tested often. Visit your doctor regularly.

Seroquel may cause you to have high blood sugar (hyperglycemia). Talk to your doctor if you have any signs of hyperglycemia such as increased thirst or urination, excessive hunger, or weakness. If you are diabetic, check your blood sugar levels on a regular basis while you are taking Seroquel.

Store Seroquel at room temperature away from moisture and heat.

What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include extreme drowsiness, fast heart rate, feeling light-headed, or fainting.

What should I avoid while taking Seroquel?
Seroquel may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Avoid becoming overheated or dehydrated during exercise and in hot weather. You may be more prone to heat stroke.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Avoid drinking alcohol. It can increase certain side effects of Seroquel.

Seroquel side effects
Get emergency medical help if you have any of these signs of an allergic reaction to Seroquel: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have any new or worsening symptoms while taking Seroquel, such as: mood or behavior changes, anxiety, panic attacks, trouble sleeping, or if you feel impulsive, irritable, agitated, hostile, aggressive, restless, hyperactive (mentally or physically), more depressed, or have thoughts about suicide or hurting yourself.

Stop using Seroquel and call your doctor at once if you have a serious side effect such as:
very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors;
feeling like you might pass out;
jerky muscle movements you cannot control, trouble swallowing, problems with speech;
blurred vision, eye pain, or seeing halos around lights;
increased thirst and urination, excessive hunger, fruity breath odor, weakness, nausea and vomiting;
fever, chills, body aches, flu symptoms; or
white patches or sores inside your mouth or on your lips.

Less serious Seroquel side effects may include:
dizziness, drowsiness, tired feeling;
dry mouth, sore throat;
nausea, vomiting;
stomach pain, upset stomach, constipation;
increased appetite;
breast swelling or discharge;
missed menstrual periods; or
weight gain.

This is not a complete list of Seroquel side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect Seroquel?
Before using Seroquel, tell your doctor if you regularly use other medicines that make you sleepy (such as cold or allergy medicine, sedatives, narcotic pain medicine, sleeping pills, muscle relaxers, and medicine for seizures, depression, or anxiety). They can add to sleepiness caused by Seroquel.

Tell your doctor about all other medicines you use, especially:
cimetidine (Tagamet);
lorazepam (Ativan);
steroids (prednisone and others);
an antibiotic such as erythromycin (E-Mycin, E.E.S, Ery-Tab), rifabutin (Mycobutin) or rifampin (Rifadin, Rimactane, Rifater);
an antifungal medication such as fluconazole (Diflucan), ketoconazole (Extina, Ketozole, Nizoral, Xolegal), or itraconazole (Sporanox);
HIV medicines such as fosamprenavir (Lexiva), indinavir (Crixivan), lopinavir/ritonavir (Kaletra), ritonavir (Norvir), saquinavir (Invirase), and others;
medicine for depression or mental illness, such as fluoxetine (Prozac), haloperidol (Haldol), imipramine (Tofranil), risperidone (Risperdal), or thioridazine (Mellaril);
a medication to treat high blood pressure or a heart condition;
medications to treat Parkinson's disease; or
seizure medication such as carbamazepine (Tegretol), divalproex (Depakote), phenobarbital (Luminal, Solfoton), phenytoin (Dilantin), or valproate (Depakene).

This list is not complete and other drugs may interact with Seroquel. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?
Your pharmacist can provide more information about Seroquel.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Seroquel only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.