英文药名: Arthrotec(Misoprostol-Diclofenac Tablets)
中文药名: 米索前列醇，双氯芬酸片
生产厂家: Pfizer辉瑞
药品介绍
规格
双氯芬酸50毫克和米索前列醇200 微克
双氯芬酸75毫克和米索前列醇200微克
药理作用
1．药效学本药含双氯芬酸钠和米索前列醇，前者有抗炎、镇痛和解热作用，后者对胃和十二指肠黏膜有保护作用。双氯芬酸钠为苯乙酸>类非甾体类抗炎药，主要通过抑制环氧酶以阻断花生四烯酸合成前列腺素，也可抑制脂氧化酶以阻断花生四烯酸转化为白三烯，从而发挥抗炎作用。同其他抗炎药一样，双氯芬酸钠的最主要的不良反应为胃肠道不良反应和黏膜损伤，原因在于双氯芬酸钠抑制胃肠黏膜生理性环氧酶-1，导致对局部有保护作用的前列腺素合成减少。本药中的米索前列醇为合成的前列腺素E1类似物，具有抑制胃酸分泌、增加重碳酸盐和粘液含量以及增加胃黏膜血流量等作用。米索前列醇可预防或减少双氯芬酸钠对胃黏膜产生的不良影响，而不影响后者的抗炎、镇痛和解热作用。有研究表明，本药的疗效与双氯芬酸、吡罗昔康及萘普生相当，对胃、十二指肠黏膜的不良反应则较少。因此本药较适用于有消化性溃疡史(伴或不伴出血、穿孔)、有较严重慢性胃炎史、有使用非甾体类抗炎药引起胃肠不良反应史的关节炎患者，可防止胃肠黏膜损伤。
2．药动学本药单次或多次使用，双氯芬酸钠和米索前列醇之间不产生药动学的相互影响，药物生物效应与两种成分单独使用时相当：空腹口服双氯芬酸钠在胃肠道吸收完全。单剂口服50mg后，达峰时间为1?2小时，血药浓度峰值为1．5μg／ml。血浆蛋白结合率在90％以上，在肝、肾及血液中浓度高。药物进入关节滑膜液后，其清除速度比在血浆中慢，滑膜液药物浓度高于血浆浓度。双氯芬酸钠主要在肝内代谢，然后以葡萄糖醛酸或硫酸结合物的形式排出体外(其中2／3经肾排出，1／3经胆汁随粪便排出)。半衰期为1－2小时。尚未发现双氯芬酸钠的药动学与年龄相关。肾功能受损者，按常规剂量单次给药不会引起蓄积。双氯芬酸钠的药动学在肝功能不全者中无显著改变。米索前列醇口服吸收迅速，经去脂化后成为有活性的代谢物米索前列醇酸。该成分在血浆中易检出，达峰时间约为10分钟，与血浆蛋白结合率不足90％。口服米索前列醇，80％随尿排出，清除半衰期为30分钟。米索前列醇不影响动物肝脏的细胞色素P450酶系统。
适应症
用于骨性关节炎和类风湿关节炎，可改善其症状；米索前列醇用于预防非甾体类抗炎药诱发的胃及十二指肠溃疡。
注意事项
1，禁忌症
(1)对双氯芬酸钠、其他非甾体类抗炎药、前列腺素过敏者。
(2)活动性消化性溃疡、其他胃肠道出血患者。
(3)严重肾功能不全或肾功能进行性恶化者(肌酐清除率小于30ml／min)(国外资料)。
(4)严重肝功能不全者(国外资料)。
(5)孕妇。
2．慎用
(1心脏病患者。
(2)正使用锂剂的患者。
(3)凝血功能障碍或血友病患者(因本药抗血小板效应可能使病情恶化)(国外资料)。
(4)脱水者(使用本药有增加肾毒性的危险)(国外资料)。
(5)有高血压或其他易引起体液潴留疾病的患者(国外资料)。
(6)轻至中度肝、肾功能不全者。
(7)老年人。
3．药物对儿童的影响18岁以下儿童用药的安全性和有效性尚未确立。
4．药物对妊娠的影响本约有引起动脉导管早闭的报道，米索前列醇可引起子宫收缩、流产。孕妇禁用。服用本药期间应避免怀孕，如已受孕应立即停药。美国药品和食品管理局(PDA)对本药的妊娠安全性分级为X级。
5．药物对哺乳的影响尚不清楚本药是否进入乳汁，不推荐哺乳妇女使用。
6．用药前后及用药时应当检查或监测长期使用应监测肝肾功能、血细胞及血电解质。
不良反应
1．消化系统主要为胃肠道不良反应，表现为腹痛、腹泻、恶心、呕吐、消化不良、胃肠胀气、胃炎、便秘及嗳气。也可引起肝功能异常。
2．生殖系统可引起月经失调、白带增多，痛经、绝经后阴道出血等。
3．其他可引起头痛、头晕、皮疹、过敏反应及水肿等。
国外不良反应参考
1．血液有贫血的报道，但比单用双氯芬酸钠时少。单用双氯芬酸钠时可产生其他血液学不良反应，如抑制血小板聚集、中性粒细胞减少、血小板减少等。
2.心血管系统有引起体液潴留和水肿的报道。
3．中枢神经系统有引起头痛、头晕的报道，发生率与单用双氯芬酸钠时相似或略低。
4．胃肠道常见腹泻、腹痛、恶心、味觉障碍，消化不良和胃肠胀气。尚可引起消化性溃疡，但比单用双氯芬酸钠时少。
5．泌尿／生殖系统米索前列醇可引起月经间期出血、月经过多、痛经，绝经后阴道出血。此药造成的子宫收缩可危及妊娠。有滥用米索前列醇促宫颈成熟或诱导分娩导致子宫穿孔的报道。本药还可引起血清肌酸酐升高。
6．肝脏分别有7％和12％的患者出现天门冬氨酸氨基转移酶、丙氨酸氨基转移酶显著升高(氨基转移酶升高在骨性关节炎患者中比在类风湿关节炎患者中更常见)。血清胆红素升高不常见(少于1％)，但可出现碱性磷酸酶升高(10％)。罕见肝坏死、黄疸和致死性肝炎。本药引起肝功能异常的发生率与单用双氯芬酸钠时相似。
7．皮肤可出现皮疹(5％)。
8．其他部分患者(少于5％)自述有流感样症状。变应反应和过敏反应很少发生。
给药说明
1．国外资料建议本药不与其他非甾体类抗炎药合用。
2．与食物同服，勿咀嚼、咬碎药片。
3．本药过量可出现意识模糊、嗜睡、全身张力减低、震颤、惊厥、呼吸困难、发热、低血压及心动过缓等。
4．中毒解救：急性用药过量可洗胃、催吐以排出胃中药物，服用活性炭以减少药物吸收，也可导尿。
用法用量
成人
常规剂量 *口服给药一次1片，一日2-3次。
国外用法用量参考
成人 *常规剂量 *口服给药 国外的双氯芬酸钠米索前列醇有两种规格， Arthrotec(R)50片剂含50rug双氯芬酸钠和0．2mg米索前列醇， Arthrotec(R)75片剂含75mg双氯芬酸钠和0．2mg米索前列醇。米索前列醇的最大剂量不超过每日0．8mg。
1．强直性脊柱炎：使用Arthrotec(R)50，一次1片，一日2-4次。
2．骨性关节炎：推荐使用Arthrotec(R)50，一次1片，一日3次。对不能耐受此剂量的患者，建议用Arthrotec(R)75或Arthrotec(R)50，一次1片，一日2次，但预防溃疡的作用会降低。双氯芬酸钠的最大推荐剂量为一日150mg。
3．类风湿关节炎：推荐使用Arthrotec(R)50，一次1片，一日3-4次。对不能耐受此剂量的患者，建议用Arthrotec(R)75或Arthrotec(R)50， 一次1片，一日2次，但预防溃疡的作用会降低。双氯芬酸钠的最大推荐剂量为一日225mg。
4．肌腱炎，滑囊炎：使用Arthrotec(R)50，一次1片，一日2-3次。
*肾功能不全时剂量
轻至中度肾衰竭患者用药不需调整剂量，但必须严密监测肾功能。
*肝功能不坌肘剂量
轻至中度肝功能不全患者，如必需使用，不需调整剂量，但应密切随访。
*老年人剂量
老年人可能对本药的不良反应不耐受，应降低剂量，或使用最低有效剂量。
任何疑问，请遵医嘱！
贮藏：原包装贮存于不高于25℃的干燥处。
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包装规格：
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·200mcg/50mg*100 片(Pharmacia 生产)
·200mcg/50mg*120 片
·200mcg/75mg*90 片
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Arthrotec is used in the treatment of joint pain, stiffness and swelling that is caused by arthritis in those patients whom are at a high risk of developing ulcers. This is a form of medication known as a nonsteroidal anti-inflammatory agent (NSAID) in combination with a prostaglandin analog. There may be other conditions where Arthrotec is a good choice of medication for you and so do not be surprised if your doctor prescribes you this medication for another condition. However you can expect a full explanation for why he or she has done so.
Arthrotec Directions
As is the case with all drugs, it is vital that you carefully follow the instructions given to you by your doctor. In most cases this will be written on the label of the medicine bottle or box and you must read this information very carefully. If you do happen to have any questions about how to take this medicine then you should talk to your pharmacist, nurse or doctor and they will be happy to help you. You must not crush, break or chew this medicine and should instead swallow it whole with a glass of water. It is not important if you take this medicine with food or on an empty stomach, however you must not mix the medicine in with your food or with any liquid. You should take it with food if you find that it upsets your stomach. Where you keep the medicine is very important and in this case it must be stored at room temperature (77 degrees F) away from the sun and in the bottle or box provided or in an airtight container. You must take the medicine as directed by your doctor and if you can take it at the same time everyday i.e. at breakfast time, then that may help you to remember. It is very important that you take this medicine everyday as directed and do not miss a dose, even if you are feeling better. Failure to take your medicine as directed will likely result in the worsening of your symptoms. In the unfortunate scenario that you do forget to take a dose, you must take the missed dose as soon as you remember unless this is near the time of your next dose. In this case you should just forget about the missed dose and carry on with your normal schedule, as you must never take two doses of a single medication at the same time. If you have any concerns then you should contact your pharmacist, nurse or doctor for more information.
Arthrotec Cautions
First and foremost you should not take Arthrotec if you have experienced an allergic or other adverse reaction to it or any other ingredient that is used in the production of Arthrotec. If you are worried that you may have had an adverse reaction to Arthrotec in the past then you should discuss this with your doctor. Stopping a medicine suddenly will often result in a worsening of symptoms and side effects and in most cases your doctor will want you to come off a medicine slowly, a process known as tapering. There may be tests that are required by your doctor to check for side effects and/or monitor how effective the medicine is for you, however your doctor will talk to you about what is required. It is important to attend all laboratory and doctor appointments while you are taking Arthrotec and additional appointments may be necessary when a change to the dose is made and during the initial starting period. You should avoid performing tasks such as driving; operating heavy machinery or any other dangerous activities until you know what effects this medicine has on you. You should never change or alter the dose of any medication unless you have talked it through with your doctor. It is vital that you notify your doctor or pharmacist before you begin any new medication, even if it is only one brought over the counter. Arthrotec may have adverse effects on the fetus in pregnant women and so all women who may be thinking about getting pregnant should weigh up the pros and cons of taking this medicine during pregnancy with their doctor. Also Arthrotec is excreted in the breast milk and so general advice at this time is to not breast-feed while on this medication. However it is wise to consult your doctor and discuss all of the options with him or her. If you become pregnant at any time while on treatment with this medication then you must contact your doctor immediately. Diabetic patients must check their blood glucose levels regularly as Arthrotec can affect these levels and you must talk with your doctor before you attempt to alter any diabetic medications. It is important that before you undergo any dental work or surgery of any kind that you let the dentist or doctor know that you are taking this medication. Elderly taking this medicine should exercise caution, as they may be more sensitive to the effects of Arthrotec. Arthrotec increases your risk of developing serious bowel or stomach problems such as bleeding and ulceration. This risk is even higher if you are elderly, if you have a history of drinking and smoking, if you take blood-thinning medications such as warfarin, if you take this medicine for a long period of time, or if you are also taking corticosteroid medicines such as prednisone. Taking this medicine may also put you at a higher risk of obtaining serious blood vessel and heart problems. You must take this medicine as prescribed by your doctor, but at the lowest possible dose and for the shortest length of time possible.
Arthrotec Side Effects
As is the case with most drugs Arthrotec is not without its side effects. Some of the things that you may notice when taking this medication include: headache, dizziness, drowsiness, constipation, heartburn, gas, diarrhea, vomiting, or nausea. These may be minor and go away during the course of treatment, however if they do bother you then you must talk to your doctor. Arthrotec was prescribed to you, as your doctor believes that the benefits will outweigh the side effects and so it is usual to expect some symptoms. However these symptoms should not cause you major discomfort and if this is the case then please talk to your doctor. You must talk to your doctor as soon as possible if you experience any hoarseness, difficulty breathing or swallowing, swelling of the face, hands, tongue, throat, eyes, lips, feet or ankles, persistent or severe nausea or fatigue, fever, chills or sore throat, right sided tenderness, dark urine, yellowing of the eyes and skin, painful, peeling, blistered, swollen, reddened or itching skin, black tarry stools, vomit that looks like coffee grounds, persistent or severe stomach pain, change in urine output, unexplained weight gain over a short period of time, one sided weakness, slurred speech, numbness of an arm or leg, changes in vision, fainting, dizziness, sudden severe headache, sudden leg pain, sudden shortness of breath, crushing or sharp chest pain, hearing loss, weight loss, loss of appetite, unusual bruising or bleeding, or diarrhea that lasts for longer than one week. Fortunately it is uncommon for someone to have an allergic reaction to this medicine, however they do occur and if you notice severe dizziness, a rash, itching, trouble breathing or swelling then you must seek immediate medical attention. If you experience any symptoms that worry you, even if they are not listed above, then it is vital that you talk to your doctor, pharmacist or nurse about it.
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Arthrotec Active Ingredients