英文药名: Comtan(Entacapone Tablets)
中文药名: 恩他卡朋片,珂丹
药品简介
恩他卡朋(entacapone,商品名Comtan,简称 Ent)是一个特异性外周儿茶酚胺-O-甲基转移酶抑制剂(COMTI),为Orion研制生产的一类新药。
美国食品和药物管理局(FDA)于1999年10月批准该药上市,用于帕金森病(PD)的辅助治疗。
恩他卡朋的化学名为:(E)-2-氰基-3-(3,4二羟基-5-硝基苯)-N,N二乙基丙烯胺。分子式为C14H15N3O5,相对分子质量为305.29。
适应症
本品可与左旋多巴/卡比多巴合用作为治疗原发性帕金森病的辅助用药。
用法用量
Ent临床上常与左旋多巴/卡比多巴合用治疗帕金森病,剂量范围为每日400~1600mg,直到出现最佳疗效。Ent的最大安全剂量为每日200mg。如患者的多巴胺能不良反应增加(如运动障碍,体位性低血压),则左旋多巴或Ent的剂量需要减少。如果需要中止Ent,应避免突然停药。对患有心血管病、精神病、肝脏疾病及接受儿茶酚胺类药物治疗的患者,应慎用Ent。
食物不影响本品的吸收。
任何疑问,请遵医嘱!
不良反应
口服Ent的不良反应报告率大于5%,包括运动障碍增加25%,恶心14%,呕吐4%,痉挛10%,腹泻10%,尿液变色10%,腹痛8%,头昏眼花8%,便秘6%,疲劳6%,幻觉4%,味觉改变1%,消化不良2%,肠胃胀气2%,胃类1%,口干3%。在中止Ent治疗时觉有精神方面的不良反应,如忧虑2%,嗜睡2%,激动1%。运动障碍是联合用药最常见的不良反应,可能是增加左旋多巴浓度的结果,这可通过减少左旋多巴的剂量来控制。胃肠道反应,尤其腹演和轻度的中枢神经系统影响在临床试验中非常常见。但程度轻,不影响治疗。在COMTI存在时,左旋多巴的中枢神经系统不良反应会加重。Ent不会产生严重的血液学、血液动力学不良反应(如血压、心律失常)或心电图变化,在左旋多巴试验期间,PD患者经常发生体位性低血压,所以对心脏病患者应监测电生理、血压和药物浓度。
注意事项
应避免突然停药,以免产生不良反应。肝功能障碍者,应调整药物剂量。FDA把本品定为孕妇危险C级。作者迄今为未见孕妇使用本品的报道。在动物研究中,大剂量的Ent可增加对眼睛的影响。由于在乳汗中发现Ent,建议哺乳女慎用本品。尚未建立Ent在儿童中使用的安全性。
药物相互作用
临床对照试验中,发现Ent与异丙肾上腺素、肾上腺素、去甲肾上腺素、多巴胺、多巴酚丁胺、α-甲基多巴等药物合用可引起心律失常,所以应慎用。患者应同时测定心率,密切监视患者的心律失常和其他心脏疾病变化。Ent应避免与非选择性MAO抑制剂合用,如苯乙肼,环苯丙胺,以免这些药物阻断内源性儿茶酚胺的代谢途径。但Ent可与司来吉兰这样的MAO-B抑制剂合用。
由于Ent主要由胆道排泄,应避免与利福平、红霉素、氯霉素、考来烯胺、氨苄西林、丙磺舒等药物合用。
Ent应慎与神经抑郁药合用,以免加重中枢神经的抑郁作用。下列药物与Ent合用可增加患者的镇静作用;抗焦虑药、止痛药、镇静催眠药、非选择性H1-受体阻滞剂(溴苯那敏、马来酸氯苯那敏、氯马斯汀、赛庚啶、右氯苯敏、苯海拉明、羟嗪、抗敏胺、吡苄明)、巴比妥类、氟哌啶类、乙醇、吩噻嗪类、氯氮平、马普替林、吗茚酮、匹莫齐特、利司培酮、曲唑酮、三环类抗抑郁药。Ent与左旋多巴、卡比多巴合用不影响其动力学。
包装规格:
·200mg*100 片(Novartis 生产)
·200mg*30 片(ORION PHARMA生产)
·200mg*50 片
Comtan is used in the treatment of Parkinson’s disease. This is a form of medication known as a catechol-o-methyltransferase (COMT) inhibitor used along with levodopa/carbidopa. There may be other conditions where Comtan 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.
Comtan 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. Take this medicine with each dose of levodopa/carbidopa. 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.
Comtan Cautions
First and foremost you should not take Comtan if you have experienced an allergic or other adverse reaction to it or any other ingredient that is used in the production of Comtan. If you are worried that you may have had an adverse reaction to Comtan 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 Comtan 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. Comtan can make you feel dizzy therefore you should wait until you know what effects it has on your body before you partake in the above activities. 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. Comtan 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 there is not enough research for us to know if Comtan is excreted in the breast milk and so general advice at this time is to not breast-feed while on this medication. Comtan may turn the urine a brown color, however this is normal. 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. You must let the laboratory know that you are on this medicine if you undergo any blood tests as Comtan may affect the results. If you become dizzy while on this medication you should sit or stand up slowly and then contact your doctor. You should also try to avoid drinking any alcohol while taking this medication.
Comtan Side Effects
As is the case with most drugs Comtan is not without its side effects. Some of the things that you may notice when taking this medication include: loss of muscle control, sweating, constipation, diarrhea, sleepiness, vomiting, nausea, lightheadedness, or dizziness. 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. Comtan 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 confusion, severe muscle rigidity, muscle pain, high fever, flu-like symptoms, forgetfulness, shortness of breath, hallucinations, itching, unusual fatigue, loss of appetite, or continuing nausea. 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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Comtan Active Ingredients
Entacapone