celecoxib塞来昔布英文说明书
celecoxib塞来昔布英文说明书
celecoxib塞来昔布英文说明书Brand Names: USCeleBREXBrand Names: CanadaACCEL-Celecoxib;ACT Celecoxib;Apo-Celecoxib;Bio-Celecoxib;Celebrex;GD-Celecoxib;JAMP-Celecoxib;Mar-Celecoxib;Mint-Celecoxib;Mylan-Celecoxib;PMS-Celecoxib;Priva-Celecoxib;RAN-Celecoxib;Riva-Celecoxib;Sandoz-Celecoxib;Teva-CelecoxibWarningThis drug may raise the chance of heart and blood vessel side effects like heart attack and stroke. If these happen, they can be deadly. The risk of these side effects may be greater if you have heart disease or risks for heart disease.However, the risk may also be raised in people who do not have heart disease or risks for heart disease. The risk of these health problems can happen as soon as the first weeks of using this drug and may be greater with higher doses or with long-term use. Do not use this drug right before or after bypass heart surgery.This drug may raise the chance of very bad and sometimes deadly stomach or bowel side effects like ulcers or bleeding. The risk is greater in older people. The risk is also greater in people who have had stomach or bowel ulcers or bleeding before. These problems may occur without warning signs. Talk with the doctor.What is this drug used for?It is used to ease pain and swelling.It is used to treat arthritis.It is used to ease painful period (menstrual) cycles.It is used to treat ankylosing spondylitis.It may be given to you for other reasons. Talk with the doctor.What do I need to tell my doctor BEFORE I take this drug?If you have an allergy to celecoxib or any other part of this drug.If you have an allergy to aspirin or NSAIDs.If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash;hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.If you have a sulfa (sulfonamide) allergy, talk with your doctor.If you have any of these health problems: Kidney disease or liver disease.If you have GI (gastrointestinal) bleeding.If you are having trouble getting pregnant or you are having your fertility checked. ?If you are pregnant or may be pregnant. Do not take this drug if you are in the third trimester of pregnancy. You may also need to avoid this drug at other times duringpregnancy. Talk with your doctor to see when you need to avoid taking this drug during pregnancy.If you are taking any other NSAID.If you are taking a salicylate drug like aspirin.If you are taking pemetrexed.This is not a list of all drugs or health problems that interact with this drug.Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this drug with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.What are some things I need to know or do while I take this drug?Tell all of your health care providers that you take this drug. This includes your doctors, nurses, pharmacists, and dentists.Have your blood work checked if you are on this drug for a long time. Talk with your doctor.High blood pressure has happened with drugs like this one. Have your blood pressure checked as you have been told by your doctor.Talk with your doctor before you drink alcohol.If you smoke, talk with your doctor.If you have asthma, talk with your doctor. You may be more sensitive to this drug.Do not take more than what your doctor told you to take. Taking more than you are told may raise your chance of very bad side effects.Do not take this drug for longer than you were told by yourdoctor.You may bleed more easily. Be careful and avoid injury. Use a soft toothbrush and an electric razor.The chance of heart failure is raised with the use of drugs like this one. In people who already have heart failure, the chance of heart attack, having to go to thehospital for heart failure, and death is raised. Talk with the doctor.The chance of heart attack and heart-related death is raised in people taking drugs like this one after a recent heart attack. People taking drugs like this one aftera first heart attack were also more likely to die in the year after the heart attackcompared with people not taking drugs like this one. Talk with the doctor.If you are taking aspirin to help prevent a heart attack, talk with your doctor.This drug may affect how much of some other drugs are in your body. If you are taking other drugs, talk with your doctor. You may need to have your blood work checked more closely while taking this drug with your other drugs.Liver problems have happened with drugs like this one. Sometimes, this has been deadly. Call the doctor right away if your child has signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.If you are 65 or older, use this drug with care. You could have more side effects. ?Use with care in children. Talk with the doctor.NSAIDs like this drug may affect egg release (ovulation) in women. This may cause you to not be able to get pregnant. Thisgoes back to normal when this drug is stopped. Talk with your doctor.This drug may cause harm to the unborn baby if you take it while you are pregnant.If you are pregnant or you get pregnant while taking this drug, call your doctor right away.Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.What are some side effects that I need to call my doctor about right away?WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.Signs of bleeding like throwing up blood or throw up that looks like coffee grounds;coughing up blood; blood in the urine; black, red, or tarry stools; bleeding from the gums; vaginal bleeding that is not normal; bruises without a reason or that getbigger; or any bleeding that is very bad or that you cannot stop.Signs of kidney problems like unable to pass urine, change in how much urine is passed, blood in the urine, or a big weight gain.Signs of high potassium levels like a heartbeat that does not feel normal; feeling confused; feeling weak, lightheaded, or dizzy; feeling like passing out; numbness or tingling; or shortness of breath.Signs of high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.Shortness of breath, a big weight gain, or swelling in the arms or legs.Chest pain or pressure or a fast heartbeat.Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight.Feeling very tired or weak.Hearing loss.Ringing in ears.Low mood (depression).A very bad skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis) may happen. It can cause very bad health problems that may not go away, and sometimes death. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.What are some other side effects of this drug?All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:Headache.Belly pain or heartburn.Upset stomach or throwing up.Loose stools (diarrhea).Dizziness.Sore throat.Stuffy nose.Runny nose.Cough.These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects. ?You may report side effects to your national health agency.How is this drug best taken?Use this drug as ordered by your doctor. Read all information given to you. Follow all instructions closely.Take with or without food. Take with food if it causes an upset stomach.Take with a full glass of water.You may sprinkle contents of capsule on applesauce. Do not chew.What do I do if I miss a dose?Take a missed dose as soon as you think about it.If it is close to the time for your next dose, skip the missed dose and go back to your normal time.Do not take 2 doses at the same time or extra doses.How do I store and/or throw out this drug?Store at room temperature.Store in a dry place. Do not store in a bathroom.Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets. ?Check with your pharmacist about how to throw out unused drugs.General drug factsIf your symptoms or health problems do not get better or if they become worse, call your doctor.Do not share your drugs with others and do not take anyone else's drugs.Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.Some drugs may have another patient information leaflet. If you have any questions about this drug, please talk with your doctor, nurse, pharmacist, or other health care provider.If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.。
塞来昔布说明书
塞来昔布【药物名称】中文通用名称:塞来昔布英文通用名称:Celecoxib其他名称:塞来考昔、西乐葆、Celebrex。
【临床应用】1.用于缓解骨性关节炎的症状和体征。
2.用于缓解成人类风湿关节炎的症状和体征。
3.用于幼年型类风湿关节炎(国外资料)。
4.作为常规疗法(内镜监测、手术等)的辅助治疗,可减少家族性腺瘤息肉(FAP)患者腺瘤性结直肠息肉量。
5.用于强直性脊柱炎、原发性痛经、急性疼痛。
【药理】1.药效学本药是昔布类非甾体类抗炎药(NSAIDs),能特异性抑制环氧酶-2(COX-2)。
炎性因子可诱导COX-2生成,导致炎性前列腺素类物质的合成和聚集,尤其是前列腺素E2,从而引起局部炎症、水肿和疼痛。
而本药可通过抑制COX-2阻止炎性前列腺素类物质的产生,达到抗炎、镇痛及解热作用。
体外及体内试验表明,本药与基础表达的环氧酶-1(COX-1)的亲和力极弱,治疗剂量下不影响由COX-1激活的前列腺素类物质的合成,因此不干扰组织中与COX-1相关的正常生理过程,尤其是在胃、肠和肾等组织中。
2.药动学本药口服吸收迅速而完全,相对生物利用度约为99%(相对于口服混悬液),口服后约3小时达血药峰浓度。
食物可延缓其吸收。
药物吸收后广泛分布于全身各组织。
稳态分布容积约为400L,血浆蛋白结合率约为97%。
本药主要在肝脏经细胞色素P450 2C9(CYP 2C9)代谢,已证实血浆中有3种代谢产物(醇、相应的羧基酸和其葡糖苷酸结合物),代谢产物对COX-1、COX-2无抑制活性。
服用单剂放射性核素标记的药物后,57%从粪便排出,27%随尿液排泄,粪便及尿液中的绝大多数代谢产物为羧基酸(给药剂量的73%)。
少量葡糖苷酸从尿液排泄,仅有少于3%给药量的药物以原形从粪便及尿液中排泄。
多次给药无蓄积作用。
血液透析不能有效清除药物。
【注意事项】1.禁忌症 (1)对本药过敏者。
(2)对阿司匹林或其他NSAIDs过敏者(可诱发哮喘、荨麻疹或过敏反应,有严重甚至致死的过敏反应报道)。
塞来昔布(西乐葆)说明书
药品名称:通用名称:塞来昔布胶囊英文名称:Celebrex (Celecoxib Capsules)商品名称:西乐葆成份:塞来昔布适应症:在决定使用本品前,应仔细考虑本品和其他治疗选择的潜在利益和风险。
根据每例患者的治疗目标,在最短治疗时间内使用最低有效剂量(见【注意事项】-警告)。
1)用于缓解骨关节炎的症状和体征。
2)用于缓解成人类风湿关节炎的症状和体征。
3)用于治疗成人急性疼痛。
(见【临床试验】)4)作为常规疗法(如:内镜监测,手术)的一项辅助治疗,可减少家族性腺瘤息肉(FAP)患者的腺瘤性结直肠息肉的数目。
目前尚不清楚FAP患者腺瘤性结直肠息肉数目减少的临床益处。
停用本品后其治疗效果是否能维持还不明确。
尚无本品治疗FAP患者超过6个月的疗效和安全性的研究(见【临床试验】、【注意事项】-警告和注意事项)。
规格:(1)0.1g (2)0.2g用法用量:在决定使用本品前,应仔细考虑本品和其他治疗选择的潜在利益和风险。
根据每例患者的治疗目标,在最短治疗时间内使用最低有效剂量(见【注意事项】-警告)。
骨关节炎和类风湿关节炎,根据个体情况决定本品治疗的最低剂量。
进食的时间对此使用剂量没有影响。
骨关节炎:本品缓解骨关节炎的症状和体征推荐剂量为200mg,每日一次口服或1OOmg每日两次口服。
类风湿关节炎:本品缓解类风湿关节炎的症状和体征推荐剂量为1OOmg至200mg,每日两次。
急性疼痛:推荐剂量为第1天首剂400mg,必要时,可再服200mg;随后根据需要,每日两次,每次200mg。
家族性腺瘤息肉(FAP):FAP患者在接受本品治疗时,应继续其常规的治疗。
用于FAP患者减少腺瘤性结直肠息肉数目治疗时,推荐剂量为口服400mg (200mg胶囊两粒)每日两次,与食物同服。
特殊人群肝功能受损患者:中度肝功能损害患者(Child-Pugh II级)本品的每日推荐剂量应减少大约50%。
不建议严重肝功能受损患者使用本品(见[药代动力学]-特殊人群)。
塞来昔布(celecoxib)
塞来昔布(celecoxib)
佚名
【期刊名称】《中国合理用药探索》
【年(卷),期】2022(19)6
【摘要】(一)体内过程空腹给药吸收良好,血药浓度达峰时间为2~3小时,血浆蛋白结合率约为97%。
本药在组织中广泛分布,可通过血脑屏障。
在肝脏内经羟化、氧化和葡萄糖醛酸化进行代谢。
主要通过肝脏清除,少于1%的药物以原型从尿中排出。
(二)适应症①骨关节炎。
②类风湿关节炎。
③急性疼痛。
④强直性脊柱炎。
(三)禁
忌症①对塞来昔布过敏者。
【总页数】1页(P29-29)
【正文语种】中文
【中图分类】R59
【相关文献】
bination of fasudil and celecoxib promotes the recovery of injured spinal cord in rats better than celecoxib or fasudil alone
2.高效液相色谱法测
定塞来昔布胶囊中塞来昔布的含量3.塞来昔布(celecoxib)治疗疼痛及炎症的临床前期及临床研究结果4.塞来昔布(celecoxib)通过前列腺素E_2途径影响胆管癌
细胞株生长和凋亡5.Effect of celecoxib on improving depression:A systematic review and meta-analysis
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西乐葆
【西乐葆药品名称】商品名称:西乐葆通用名称:塞来昔布胶囊英文名称:Celecoxib Capsules汉语拼音:Sailaixibu Jiaonang【西乐葆成份】西乐葆主要成份为塞来昔布。
【西乐葆性状】本药为口服硬胶囊,除活性成分外,尚含有一水乳糖、十二烷基硫酸钠、聚乙烯吡咯烷酮、羟甲基纤维素钠和硬脂酸镁。
【西乐葆药理作用】塞来昔布是具有独特作用机制的新一代化合物,即特异性抑制环氧化酶-2。
炎症刺激可诱导环氧化酶-2(COX-2)生成,因而导致炎性前列腺素类物质的合成和聚积,尤其是前列腺素E2,可引起炎症、水肿和疼痛。
而塞来昔布可通过抑制环氧化酶-2阻止炎性前列腺素类物质的产生,达到抗炎、镇痛及退热作用。
体外及体内试验表明,塞来昔布与基础表达的环氧化酶-1(COX-1)的亲和力极弱,治疗剂量的塞来昔布不影响由COX-1激活的前列腺素类物质的合成。
因此不干扰组织中与COX-1相关的正常生理过程,尤其在胃、肠、血小板和肾等组织中。
临床资料有关COX-2特异性的生物学术语的定义目前已有统一标准,它包括需要证实无COX-1型不良反应的发生,尤其是无药物导致的胃、十二肠溃疡和严重的上消化道不良反应(出血、穿孔、幽门梗阻),并且没有COX-1抑制血小板聚集活性的降低。
基于上述标准,临床上西乐葆的特异性在对照临床试验中得到了证实,这些临床试验包括治疗时间长达6个月的对照临床试验,及总数超过3000病人年的进一步的开放临床试验。
西乐葆严重上消化道并发症(出血、穿孔、幽门梗阻)的发生率与安慰剂组相比无显著性差异,与其他非特异性COX抑制剂相比,其发生率减少约为8倍。
在5个随机双盲对照试验中,对4000多例患有骨关节炎及类风湿关节炎的患者用内窥镜检查,比较西乐葆与安慰剂组,以及非特异性COX-1/COX-2抑制剂组的溃疡发生率,结果表明,西乐葆的溃疡发生率与安慰剂组相比无显著差异,在50-400mg,一天2次用药的剂量范围内,溃疡发生率与西乐葆应用剂量无关,且比非特异性COX-2/COX-2抑制剂小3-4倍。
西乐葆(塞来昔布胶囊)
劲通(双氯芬酸钠气雾剂)【药品名称】商品名称:劲通通用名称:双氯芬酸钠气雾剂英文名称:Diclofenac Sodium Aerosol【成份】每克含双氯芬酸钠12.5毫克。
辅料为:月桂氮卓酮、乙醇、丙二醇、抛射剂。
【适应症】用于缓解肌肉、软组织和关节的轻至中度疼痛。
如缓解肌肉、软组织的扭伤、拉伤、挫伤、劳损、腰背部损伤引起的疼痛以及关节疼痛等。
也可用于骨关节炎的对症治疗。
【用法用量】外用,将药瓶直立喷于患部。
一次喷药时间不超过2秒钟(喷药约2克),一日3次,一日用药总量不超过12克。
【不良反应】1.偶可出现局部不良反应:过敏性或非过敏性皮炎如丘疹、皮肤发红、水肿、瘙痒、小水泡、大水泡或鳞屑等。
2.局部使用本品而导致全身不良反应的情况少见,若将其用于较大范围皮肤长期使用,则可能出现:一般性皮疹、过敏性反应(如哮喘发作、血管神经性水肿、光敏反应等)。
如发生这种情况,应咨询医师。
【禁忌】1 对其他非甾体抗炎药过敏者禁用。
2 对丙二醇过敏者禁用。
【注意事项】1.由于本品局部应用也可全身吸收,故应避免长期大面积使用。
2.肝、肾功能不全者以及孕妇、哺乳期妇女使用前请咨询医师或药师。
3.不得用于破损皮肤或感染性创口。
4.12岁以下儿童用量请咨询医师。
5.避免接触眼睛和其他黏膜(如口、鼻等)。
6.如使用本品7日,局部疼痛未缓解,请咨询医师或药师。
7.对本品过敏者禁用,过敏体质者慎用。
8.本品性状发生改变时禁止使用。
9【药物相互作用】如与其他药物同时使用可能会发生药物相互作用,详情请咨询医师或药师。
【药理作用】本品为前列腺素合成抑制剂,具有抗炎、镇痛作用。
局部应用。
其有效成份可穿透皮肤达到炎症区域,缓解急、慢性炎症反应,使炎性肿痛减轻、疼痛缓解。
【批准文号】国药准字H19991425【生产企业】企业名称:广东同德药业有限公司生产地址:广东省湛江市椹川大道西五路4号。
如何正确使用塞来昔布缓解疼痛
如何正确使用塞来昔布缓解疼痛如何正确使用塞来昔布缓解疼痛塞来昔布(Celecoxib)是一种用于缓解疼痛和减轻炎症的非甾体抗炎药(NSAIDs)。
它能够帮助控制关节炎、偏头痛、月经痛和其他类型的疼痛。
在正确使用塞来昔布之前,有几个关键因素需要注意。
下文将介绍一些使用塞来昔布缓解疼痛的正确方法。
1. 遵循医生的指导使用塞来昔布前,建议咨询医生或药剂师。
根据您的疼痛类型和个人情况,他们会为您提供适当的剂量和使用说明。
确保按照医生的指导服用,并且不要自行调整剂量或停止使用。
2. 了解副作用和风险塞来昔布使用过程中可能会出现一些副作用和风险。
常见的副作用包括胃肠道不适、头晕、恶心等。
严重的副作用可能涉及肝脏和心血管系统。
在开始使用塞来昔布之前,务必详细了解相关的副作用和风险,并密切关注身体的反应。
3. 适量使用塞来昔布的剂量应根据医生的建议和个人状况来确定。
通常情况下,起始剂量为200毫克,之后根据需要酌情加量。
最大每日剂量一般为400毫克。
请务必遵循医生的建议,不要超过推荐的剂量。
4. 饭后服用为减少胃肠道不适的风险,建议在饭后服用塞来昔布。
同时,避免与其他药物一起服用,以避免相互作用。
5. 持续使用塞来昔布并非即刻生效的药物,通常需要持续几周才能发挥最佳效果。
在服用期间,注意观察疼痛状况,并确保及时咨询医生,以便进行必要的调整。
6. 不适情况下停止使用如果在使用塞来昔布期间出现严重胃痛、呕吐、黑便、皮肤发红、呼吸困难等症状,应立即停止使用并立即就医。
这些可能是严重的副作用的迹象。
7. 注意与其他药物的相互作用在使用塞来昔布之前,要告知医生您正在使用的其他药物,包括处方药、非处方药和补充剂。
某些药物可能与塞来昔布发生相互作用,导致不良反应或减低药效。
总的来说,正确使用塞来昔布可以有效缓解疼痛。
关键在于遵循医生的指导,了解副作用和风险,并按照适当的剂量和时间饭后服用。
同时,应密切观察身体反应,如有不适及时就医。
塞来昔布(西乐葆)说明介绍模板之欧阳歌谷创编
欧阳歌谷(2021.02.01)通用名称:塞来昔布胶囊英文名称:Celebrex (Celecoxib Capsules)商品名称:西乐葆塞来昔布在决定使用本品前,应仔细考虑本品和其他治疗选择的潜在利益和风险。
根据每例患者的治疗目标,在最短治疗时间内使用最低有效剂量(见【注意事项】-警告)。
1)用于缓解骨关节炎的症状和体征。
2)用于缓解成人类风湿关节炎的症状和体征。
3)用于治疗成人急性疼痛。
(见【临床试验】)4)作为常规疗法(如:内镜监测,手术)的一项辅助治疗,可减少家族性腺瘤息肉(FAP)患者的腺瘤性结直肠息肉的数目。
目前尚不清楚FAP患者腺瘤性结直肠息肉数目减少的临床益处。
停用本品后其治疗效果是否能维持还不明确。
尚无本品治疗FAP患者超过6个月的疗效和安全性的研究(见【临床试验】、【注意事项】-警告和注意事项)。
(1)0.1g (2) 0.2g在决定使用本品前,应仔细考虑本品和其他治疗选择的潜在利益和风险。
根据每例患者的治疗目标,在最短治疗时间内使用最低有效剂量(见【注意事项】-警告)。
骨关节炎和类风湿关节炎,根据个体情况决定本品治疗的最低剂量。
进食的时间对此使用剂量没有影响。
骨关节炎:本品缓解骨关节炎的症状和体征推荐剂量为200mg,每日一次口服或1OOmg每日两次口服。
类风湿关节炎:本品缓解类风湿关节炎的症状和体征推荐剂量为1OOmg至200mg,每日两次。
急性疼痛:推荐剂量为第1天首剂400mg,必要时,可再服200mg;随后根据需要,每日两次,每次200mg。
家族性腺瘤息肉(FAP): FAP患者在接受本品治疗时,应继续其常规的治疗。
用于FAP患者减少腺瘤性结直肠息肉数目治疗时,推荐剂量为口服400mg (200mg胶囊两粒)每日两次,与食物同服。
特殊人群肝功能受损患者:中度肝功能损害患者(Child-Pugh II级)本品的每日推荐剂量应减少大约50%。
不建议严重肝功能受损患者使用本品(见[药代动力学]-特殊人群)。
塞来昔布胶囊说明书
心血管系统:高血压加重、心绞痛、冠状动脉病变、心肌梗死。
全身性:过敏加重、过敏反应、乏力、胸痛、囊肿、全身水肿、 面部水肿、疲劳、发热、面部潮红、
Version No: 20120111
第 4 页,共 21 页
感冒样症状、疼痛、周围疼痛。
免疫系统疾病:单纯性疱疹、带状疱疹、细菌感染、真菌感染、软组织感染、病毒感染、念珠菌病、 生殖系统念珠菌病、中耳炎。
2.3% 2.0% 5.0% 8.1%
皮肤
皮疹
2.2%
2.8% 3.8% 6.2% 1.0% 4.2%
7.7% 5.3% 12.2% 3.6% 6.0%
9.0% 9.3% 10.9% 4.1% 3.4%
9.0% 5.8% 12.8% 3.5% 6.7%
3.6% 1.1% 2.3%
2.2% 2.1% 3.0%
3.1%
恶心
6.8%
5.3%
呕吐
3.2%
2.1%
呼吸困难
2.8%
1.6%
Version No: 20120111
第 6 页,共 21 页
高血压
12.5%
9.8%
在长期腺瘤息肉预防研究中,塞来昔布治疗组以下不良反应的发生率在 0.1%~1%之间,高于安 慰剂组。同时,这些不良反应在上市前的关节炎对照研究中未被报道,或在上市前的关节炎对照研究 中的发生率较低。
骨关节炎和类风湿关节炎,根据个体情况决定塞来昔布治疗的最低剂量。进食的时间对此使用剂 量没有影响。
骨关节炎:塞来昔布缓解骨关节炎的症状和体征推荐剂量为 200mg,每日一次口服或 100mg 每日两次 口服。
类风湿关节炎:塞来昔布缓解类风湿关节炎的症状和体征推荐剂量为 100mg 至 200mg,每日两次。
塞来昔布
炎症刺激诱导环氧化酶-2生成,从而导 致炎性前列腺素类物质的合成和聚积,尤其是前 列腺素E2,可引起炎症、水肿和疼痛。而本药可 通过抑制环氧化酶-2阻止炎性前列腺素类物质的 产生,达到抗炎、镇痛及退热作用。
机理
合成路线
克莱森缩合反应
对甲基苯乙酮
三构效关系
代谢过程
塞来西布是具有独特作用机制的新一代解热 药理作用 镇痛抗炎药,能特异性抑制COX-2(环氧化酶2)。它与常见非甾体抗炎药(NSAIDS)的抗炎 活性相当,其苯磺酰胺结构对COX-2(环氧化 酶-2)受体有高选择性,而对COX-1(环氧化酶1)没有抑制作用,主要用于骨关节炎(OA)和 类风湿性关节炎(RA)。
经结构优化得到塞来昔布(celecoxib)和罗非昔布 (rofecoxib)。塞来昔布于1997年首次被合成,是第一 个上市的COX-2选择性抑制剂,由于其靶向性强、副作用小, 自 1999年正式上市以来,其在全球的推广速度相当惊 人。 至2008年celecoxib是美国第九大常用药品。2003年的销 售额就就达到26亿美元。但在该类药物上市后的短短5年中, 药物监测发现,该类药物有增大心血管事件的风险。
代谢主要发生在肝,由细胞色素 CYP2C9代谢,主要以无活性的代谢产物 形式从尿及粪便中排出,仅有约3%的药 物未经代谢直接排出。所以代谢产物对 COX-1、COX-2均没有显著的抑制活性
药物相应作用:
1.酶抑制剂如氟康唑等可能使本品的血药浓度升 高;反之,酶诱导剂如巴比土酸盐或利福平等可 能使本品的血药浓度降低。 2.被P450CYP2D6代谢的药物如恩卡尼可能与本 品存在潜在的药动学相互作用。 3.与非甾体消炎药存在药理学相互作用。本品合 用阿司匹林比单用本品更易引起胃肠道出血。 4.本品与锂存在药动学相互作用。 5.本品合用华法林可能引起出血。 6.抗酸剂(如铝剂和镁剂)能使塞来西布的吸收 降低10%,但并不影响其临床作用。
塞来昔布
测定方法 极谱催化氢波法 高效液相荧光法
高效液相-质谱联用法
高效液相电离子梯度捕获法 高效液相紫外法
高效液相色谱法
谢谢大家!
炎症刺激诱导环氧化酶-2生成,从而导 致炎性前列腺素类物质的合成和聚积,尤其是前 列腺素E2,可引起炎症、水肿和疼痛。而本药可 通过抑制环氧化酶-2阻止炎性前列腺素类物质的 产生,达到抗炎、镇痛及退热作用。
机理
合成路线
克莱森缩合反应
对甲基苯乙酮
三氟乙酸甲酯
(对肼基苯磺酰胺盐酸盐)源自构效关系代谢过程代谢主要发生在肝,由细胞色素 CYP2C9代谢,主要以无活性的代谢产物 形式从尿及粪便中排出,仅有约3%的药 物未经代谢直接排出。所以代谢产物对 COX-1、COX-2均没有显著的抑制活性
药物相应作用:
1.酶抑制剂如氟康唑等可能使本品的血药浓度升 高;反之,酶诱导剂如巴比土酸盐或利福平等可 能使本品的血药浓度降低。 2.被P450CYP2D6代谢的药物如恩卡尼可能与本 品存在潜在的药动学相互作用。 3.与非甾体消炎药存在药理学相互作用。本品合 用阿司匹林比单用本品更易引起胃肠道出血。 4.本品与锂存在药动学相互作用。 5.本品合用华法林可能引起出血。 6.抗酸剂(如铝剂和镁剂)能使塞来西布的吸收 降低10%,但并不影响其临床作用。
1 2 3 4 6 5 1 5 4 2
3.熔点158~163℃。
3
4-[-5-(4-甲基苯基)-3-(三氟甲基)-1 H-吡咯-1-基]苯磺酰胺
发展历程
根据对环氧合酶两个亚型的 研究,在90年代初发现了具有选择 性抑制COX-2的两个先导化合物Ns398和Dup697。
经结构优化得到塞来昔布(celecoxib)和罗非昔布 (rofecoxib)。塞来昔布于1997年首次被合成,是第一 个上市的COX-2选择性抑制剂,由于其靶向性强、副作用小, 自 1999年正式上市以来,其在全球的推广速度相当惊 人。 至2008年celecoxib是美国第九大常用药品。2003年的销 售额就就达到26亿美元。但在该类药物上市后的短短5年中, 药物监测发现,该类药物有增大心血管事件的风险。
塞来昔布(西乐葆)说明介绍模板之欧阳德创编
通用名称:塞来昔布胶囊英文名称:Celebrex (Celecoxib Capsules)商品名称:西乐葆塞来昔布在决定使用本品前,应仔细考虑本品和其他治疗选择的潜在利益和风险。
根据每例患者的治疗目标,在最短治疗时间内使用最低有效剂量(见【注意事项】-警告)。
1)用于缓解骨关节炎的症状和体征。
2)用于缓解成人类风湿关节炎的症状和体征。
3)用于治疗成人急性疼痛。
(见【临床试验】)4)作为常规疗法(如:内镜监测,手术)的一项辅助治疗,可减少家族性腺瘤息肉(FAP)患者的腺瘤性结直肠息肉的数目。
目前尚不清楚FAP患者腺瘤性结直肠息肉数目减少的临床益处。
停用本品后其治疗效果是否能维持还不明确。
尚无本品治疗FAP患者超过6个月的疗效和安全性的研究(见【临床试验】、【注意事项】-警告和注意事项)。
(1)0.1g (2) 0.2g在决定使用本品前,应仔细考虑本品和其他治疗选择的潜在利益和风险。
根据每例患者的治疗目标,在最短治疗时间内使用最低有效剂量(见【注意事项】-警告)。
骨关节炎和类风湿关节炎,根据个体情况决定本品治疗的最低剂量。
进食的时间对此使用剂量没有影响。
骨关节炎:本品缓解骨关节炎的症状和体征推荐剂量为200mg,每日一次口服或1OOmg每日两次口服。
类风湿关节炎:本品缓解类风湿关节炎的症状和体征推荐剂量为1OOmg至200mg,每日两次。
急性疼痛:推荐剂量为第1天首剂400mg,必要时,可再服200mg;随后根据需要,每日两次,每次200mg。
家族性腺瘤息肉(FAP): FAP患者在接受本品治疗时,应继续其常规的治疗。
用于FAP患者减少腺瘤性结直肠息肉数目治疗时,推荐剂量为口服400mg (200mg 胶囊两粒)每日两次,与食物同服。
特殊人群肝功能受损患者:中度肝功能损害患者(Child-Pugh II级)本品的每日推荐剂量应减少大约50%。
不建议严重肝功能受损患者使用本品(见[药代动力学]-特殊人群)。
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Brand Names: US∙CeleBREXBrand Names: Canada∙ACCEL-Celecoxib;∙ACT Celecoxib;∙Apo-Celecoxib;∙Bio-Celecoxib;∙Celebrex;∙GD-Celecoxib;∙JAMP-Celecoxib;∙Mar-Celecoxib;∙Mint-Celecoxib;∙Mylan-Celecoxib;∙PMS-Celecoxib;∙Priva-Celecoxib;∙RAN-Celecoxib;∙Riva-Celecoxib;∙Sandoz-Celecoxib;∙Teva-CelecoxibWarning∙This drug may raise the chance of heart and blood vessel side effects like heart attack and stroke. If these happen, they can be deadly. The risk of these side effects may be greater if you have heart disease or risks for heart disease.However, the risk may also be raised in people who do not have heart disease or risks for heart disease. The risk of these health problems can happen as soon as the first weeks of using this drug and may be greater with higher doses or with long-term use. Do not use this drug right before or after bypass heart surgery.∙This drug may raise the chance of very bad and sometimes deadly stomach or bowel side effects like ulcers or bleeding. The risk is greater in older people. The risk is also greater in people who have had stomach or bowel ulcers or bleeding before. These problems may occur without warning signs. Talk with the doctor.What is this drug used for?∙It is used to ease pain and swelling.∙It is used to treat arthritis.∙It is used to ease painful period (menstrual) cycles.∙It is used to treat ankylosing spondylitis.∙It may be given to you for other reasons. Talk with the doctor.What do I need to tell my doctor BEFORE I take this drug?∙If you have an allergy to celecoxib or any other part of this drug.∙If you have an allergy to aspirin or NSAIDs.∙If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash;hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.∙If you have a sulfa (sulfonamide) allergy, talk with your doctor.∙If you have any of these health problems: Kidney disease or liver disease.∙If you have GI (gastrointestinal) bleeding.∙If you are having trouble getting pregnant or you are having your fertility checked. ∙If you are pregnant or may be pregnant. Do not take this drug if you are in the third trimester of pregnancy. You may also need to avoid this drug at other times during pregnancy. Talk with your doctor to see when you need to avoid taking this drug during pregnancy.∙If you are taking any other NSAID.∙If you are taking a salicylate drug like aspirin.∙If you are taking pemetrexed.∙This is not a list of all drugs or health problems that interact with this drug.∙Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this drug with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.What are some things I need to know or do while I take this drug?∙Tell all of your health care providers that you take this drug. This includes your doctors, nurses, pharmacists, and dentists.∙Have your blood work checked if you are on this drug for a long time. Talk with your doctor.∙High blood pressure has happened with drugs like this one. Have your blood pressure checked as you have been told by your doctor.∙Talk with your doctor before you drink alcohol.∙If you smoke, talk with your doctor.∙If you have asthma, talk with your doctor. You may be more sensitive to this drug.∙Do not take more than what your doctor told you to take. Taking more than you are told may raise your chance of very bad side effects.∙Do not take this drug for longer than you were told by your doctor.∙You may bleed more easily. Be careful and avoid injury. Use a soft toothbrush and an electric razor.∙The chance of heart failure is raised with the use of drugs like this one. In people who already have heart failure, the chance of heart attack, having to go to thehospital for heart failure, and death is raised. Talk with the doctor.∙The chance of heart attack and heart-related death is raised in people taking drugs like this one after a recent heart attack. People taking drugs like this one aftera first heart attack were also more likely to die in the year after the heart attackcompared with people not taking drugs like this one. Talk with the doctor.∙If you are taking aspirin to help prevent a heart attack, talk with your doctor.∙This drug may affect how much of some other drugs are in your body. If you are taking other drugs, talk with your doctor. You may need to have your blood work checked more closely while taking this drug with your other drugs.∙Liver problems have happened with drugs like this one. Sometimes, this has been deadly. Call the doctor right away if your child has signs of liver problems like dark urine, feeling tired, not hungry, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.∙If you are 65 or older, use this drug with care. You could have more side effects. ∙Use with care in children. Talk with the doctor.∙NSAIDs like this drug may affect egg release (ovulation) in women. This may cause you to not be able to get pregnant. This goes back to normal when this drug is stopped. Talk with your doctor.∙This drug may cause harm to the unborn baby if you take it while you are pregnant.If you are pregnant or you get pregnant while taking this drug, call your doctor right away.∙Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.What are some side effects that I need to call my doctor about right away?∙WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:∙Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips,tongue, or throat.∙Signs of bleeding like throwing up blood or throw up that looks like coffee grounds;coughing up blood; blood in the urine; black, red, or tarry stools; bleeding from the gums; vaginal bleeding that is not normal; bruises without a reason or that getbigger; or any bleeding that is very bad or that you cannot stop.∙Signs of kidney problems like unable to pass urine, change in how much urine is passed, blood in the urine, or a big weight gain.∙Signs of high potassium levels like a heartbeat that does not feel normal; feeling confused; feeling weak, lightheaded, or dizzy; feeling like passing out; numbness or tingling; or shortness of breath.∙Signs of high blood pressure like very bad headache or dizziness, passing out, or change in eyesight.∙Shortness of breath, a big weight gain, or swelling in the arms or legs.∙Chest pain or pressure or a fast heartbeat.∙Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight.∙Feeling very tired or weak.∙Hearing loss.∙Ringing in ears.∙Low mood (depression).∙ A very bad skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis) may happen. It can cause very bad health problems that may not go away, and sometimes death. Get medical help right away if you have signs like red, swollen, blistered, or peeling skin (with or without fever); red or irritated eyes; or sores in your mouth, throat, nose, or eyes.What are some other side effects of this drug?∙All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:∙Headache.∙Belly pain or heartburn.∙Upset stomach or throwing up.∙Loose stools (diarrhea).∙Dizziness.∙Sore throat.∙Stuffy nose.∙Runny nose.∙Cough.∙These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects. ∙You may report side effects to your national health agency.How is this drug best taken?∙Use this drug as ordered by your doctor. Read all information given to you. Follow all instructions closely.∙Take with or without food. Take with food if it causes an upset stomach.∙Take with a full glass of water.∙You may sprinkle contents of capsule on applesauce. Do not chew.What do I do if I miss a dose?∙Take a missed dose as soon as you think about it.∙If it is close to the time for your next dose, skip the missed dose and go back to your normal time.∙Do not take 2 doses at the same time or extra doses.How do I store and/or throw out this drug?∙Store at room temperature.∙Store in a dry place. Do not store in a bathroom.∙Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets. ∙Check with your pharmacist about how to throw out unused drugs.General drug facts∙If your symptoms or health problems do not get better or if they become worse, call your doctor.∙Do not share your drugs with others and do not take anyone else's drugs.∙Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.∙Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.∙Some drugs may have another patient information leaflet. If you have any questions about this drug, please talk with your doctor, nurse, pharmacist, or other health care provider.∙If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.。