英文药名: Mirapex ER(pramipexole tablets) 中文药名: 米拉帕（普拉克索盐酸盐缓释片） 生产厂家: Boehringer Ingelheim 药品名称 药品名：盐酸普拉克索片 英文名：Pramipexole Dihydrochloride Tablets 性状: 本品为白色片。 药理毒性 药理作用 普拉克索是一种非麦角类多巴胺激动剂。体外研究显示，普拉克索对D2受体的特异性较高并具有完全的内在活性，对D3受体的亲和力高于D2和D4受体。普拉克索与D3受体的这种结合作用与帕金森氏病的相关性不明确。普拉克索治疗帕金森氏病的确切机制尚不清楚，目前认为与激活纹状体的多巴胺受体有关。动物电生理试验显示，普拉克索可通过激活纹状体与黑质的多巴胺受体而影响纹状体神经元放电频率。 毒理研究 -遗传毒性 普拉克索Ames实验、HGRRT V79基因突变试验、CHO细胞染色体畸变试验、小鼠微核试验结果均为阴性。 -生殖毒性 生育力实验中，大鼠给予普拉克索2.5mg/kg/天（按mg/m2推算，相当于人最大推荐剂量（1.5mg,tid）的5.4倍），可见动情周期延长，着床率降低，这可能与普拉克索导致的血清催乳素水平降低有关（在大鼠早期妊娠中，胚胎的着床和维持需要催乳素，而家兔和人则不需要）。妊娠大鼠于致畸敏感期给予普拉克索1.5mg/kg天（按血浆AUC推算，相当于人最大推荐剂量时AUC的4.3倍），可总吸收胎发生率增加，这可能与普拉克索导致的血清催乳素水平降低有关。妊娠家兔于致畸敏感期给予普拉克索10mg/kg/天（血浆AUC为人给予最大推荐剂量时AUC的71倍），未见异常。妊娠大鼠围产期给予普拉克索0.5mg/kg/天（按mg/m2推算相当于人的最高临床推荐剂量）或更高剂量，子代大鼠出生后生长未受不良影响。 -致癌性 小鼠与大鼠掺食法分别给予普拉克索0.3、2、10mg/kg/天（按mg/m2推算，分别相当于人最大推荐剂量的0.3、2.2和11倍）或0.3、2、8mg/kg/天（按血浆AUC推算，分别相当于人最大推荐剂时AUC的0.3、2.5和12.5倍），未见肿瘤发生率增加。 药代动力学 普拉克索口服吸收迅速完全。绝对生物利用度高于90%，最大血浆浓度在服药后1-3小时之间出现。与食物一起服用不会降低普拉克索吸收的程度，但会降低其吸收速率。普拉克索显示出线性动力学特点，患者间血浆水平差异很小。在人体内，普拉克索的血浆蛋白结合度很低（小于20%），分布容积很大（400普拉克索在男性体内的代谢程度很低。 以原形从肾脏排泄是普拉克索的主要清除途径。14C标记的药物大约有90%是通过肾排泄的，粪便中的药物少于2%。普拉克索的总清除率大约为500ml/分钟，肾脏清除率大约为400ml/分钟。年轻人和老年人的普拉克索清除半衰期（t1/2）从8?12小时不等。 适应症 本品被用来治疗特发性帕金森病的体征和症状，单独（无左旋多巴）或与左旋多巴联用。例如，在疾病后期左旋多巴的疗效逐渐减弱或者出现变化和波动时（剂末现象或开关波动），需要应用本品。 用法用量 *初始治疗： 起始剂量为每日0.375mg，然后每5-7天增加一次剂量。如果患者可以耐受，应增加剂量以达到最大疗效。 如果需要进一步增加剂量，应该以周为单位，每周加量一次，每次日剂量增加0.75mg，每日最大剂量为4.5mg。 然而，应该注意的是，每日剂量高于1.5mg时，嗜睡发生率增加（见【不良反应】）。 *维持治疗： 个体剂量应该在每天0.375mg至4.5mg之间。在剂量逐渐增加的三项重要研究中，从每日剂量为1.5mg开始可以观察到药物疗效。作进一步剂量调整应根据临床反应和耐受性进行。在临床试验中有大约5%的患者每天服用剂量低于1.5mg。当计划减少左旋多巴治疗时，每天服用剂量大于1.5mg对晚期帕金森病患者可能是有效的。在本品加量和维持治疗阶段，建议根据患者的个体反应减少左旋多巴用量。治疗中止： 突然中止多巴胺能治疗会导致非神经阻断性恶性综合症发生。因此，应该以每天减少0.75mg的速度逐渐停止应用普拉克索，直到日剂量降至0.75mg。此后，应每天减少0.375mg（见【注意事项】）。 *肾功能损害患者的用药： 普拉克索的清除依靠肾功能。 对于初始治疗建议应用如下剂量方案： 肌酐清除率高于50ml/min的患者无需降低日剂量。 肌酐清除率介于20-50ml/min之间的患者，本品的初始日剂量应分两次服用，每次0.125mg，每日两次。 肌酐清除率低于20ml/min的患者，本品的日剂量应一次服用，从每天0.125mg开始。 如果在维持治疗阶段肾功能降低，则以与肌酐清除率下降相同的百分比降低本品的日剂量，例如，当肌酐清除率下降30%，则本品的日剂量也减少30%。如果肌酐清除率介于20-50ml/min之间，日剂量应分两次服用；如果肌酐清除率低于20ml/min，日剂量应一次服用。 *肝功能损害患者的用药： 对肝功能衰竭的患者可能不需要进行剂量调整，因为所吸收的药物中大约90%是通过肾脏排泄的。然而，肝功能不全对本品药代动力学的潜在影响还未被阐明。 任何疑问，请遵医嘱！ 不良反应 基于汇总的安慰剂对照试验，其中包括1351名服用本品的患者和1131名服用安慰剂的患者，分析显示两组都经常发生不良事件。88%服用本品的患者和83.6%服用安慰剂的患者至少报告过一起不良事件。当本品日剂量高于1.5mg（见【用法用量】）时嗜睡的发生率增加。与左旋多巴联用时最常见的不良反应是运动障碍。便秘、恶心和运动障碍往往随治疗进行逐渐消失。治疗初期可能发生低血压，尤其本品药量增加过快时。 下面是安慰剂对照试验中服用本品所发生的药物不良反应（数字为高于安慰剂的发生率）： *精神障碍：常见（1%-10%）：失眠、幻觉、精神错乱 *神经系统异常：常见（1%-10%）：眩晕、运动障碍、嗜睡 *血管异常：不常见（0.1-1%）：低血压 *胃肠道异常：常见（1%-10%）：恶心、便秘 *全身异常：常见（1%-10%）：外周水肿 本品与嗜睡有关，与偶发的白天过度嗜睡及突然睡眠发作也有关。 *本品可能与性欲异常有关（增加或降低）。 另见【注意事项】 禁忌 对普拉克索或产品中任何其它成份过敏者。 注意事项 当肾功能损害的患者服用本品时，建议参照【用法用量】减少剂量。幻觉为多巴胺能受体激动剂和左旋多巴治疗的副反应。应告知患者可能会发生幻觉（多为视觉上的）。对于晚期帕金森病，联合应用左旋多巴，可能会在本品的初始加量阶段发生运动障碍。如果发生上述副反应，应该减少左旋多巴用量。 本品与嗜睡和突然睡眠发作有关，尤其对于帕金森病患者。在日常活动中的突然睡眠发作，有时没有意识或预兆，但是这种情况很少被报导。必须告知患者这种副反应，建议其在应用本品治疗的过程中要谨慎驾驶车辆或操作机器。已经发生过嗜睡和/或突然睡眠发作副反应的患者，必须避免驾驶或操作机器，而且应该考虑降低剂量或终止治疗。由于可能的累加效应，当患者在服用普拉克索时应慎用其它镇静类药物或酒精（见【对驾驶和操作机器能力的影响】和【不良反应】）。 有精神障碍的患者，如果潜在的益处大于风险，应仅用多巴胺能受体激动剂进行治疗。 普拉克索应避免与抗精神病药物同时应用（见【药物相互作用】）。 应定期或在发生视觉异常时进行眼科检查。 应注意伴随严重心血管疾病的患者。由于多巴胺能治疗与体位性低血压发生有关，建议监测血压，尤其在治疗初期。 已报道突然终止多巴胺能治疗时会发生非神经阻断性恶性综合症的症状（见【用法用量】）。 孕妇和哺乳期妇女用药 普拉克索对人妊娠期和哺乳期的影响还未被研究。它对大鼠和家兔没有致畸作用，但是，其在母体毒性剂量下对大鼠胚胎有毒性（见毒理研究）。本品禁用于妊娠期，除非确实需要，例如，对胎儿潜在的益处大于风险时。由于本品抑制人催乳素的分泌，因此其抑制泌乳。本品是否可分泌到妇女乳汁中还未作研究。大鼠乳汁中药物相关的放射性强度高于血浆。由于缺乏人体数据，应尽可能不在哺乳期内应用本品。然而，如果其应用不可避免的话，应中止哺乳。 The FDA has approved Mirapex ER (pramipexole dihydrochloride extended-release tablets, from Boehringer-Ingelheim Pharmaceuticals) as a treatment for the signs and symptoms of early idiopathic Parkinson's disease. This approval was based on data from a single, randomized, double-blind, placebo-controlled, multicenter clinical trial, and from a second study evaluating an overnight switch from Mirapex (pramipexole dihydrochloride tablets) to Mirapex ER. Results from the first study demonstrated that patients treated with Mirapex ER experienced clinically significant symptom relief, as measured by the mean change from baseline in Unified Parkinson's Disease Rating Scale (UPDRS)* II+III score, compared with placebo. In the second study, data showed that 85% of patients who completed the trial were successfully switched from Mirapex to Mirapex ER. Mirapex ER is not indicated for the treatment of advanced Parkinson's disease or restless legs syndrome (RLS). ---------------------------------------------------------------------- Mirapex ER , Mirapexin Prolonged Release , Sifrol ( Pramipexole ) This medicine is a dopamine agonist used to treat the signs and symptoms of early Parkinson disease. It may also be used to treat other conditions as determined by your doctor. Before Using This Medicine: Some medicines or medical conditions may interact with this medicine. INFORM YOUR DOCTOR OR PHARMACIST of all prescription and over-the-counter medicine that you are taking. DO NOT TAKE THIS MEDICINE if you are also taking another medicine that has pramipexole in it. ADDITIONAL MONITORING OF YOUR DOSE OR CONDITION may be needed if you are taking cimetidine, levodopa, butyrophenones (eg, haloperidol), metoclopramide, phenothiazines (eg, chlorpromazine), or thioxanthenes (eg, thiothixene). DO NOT START OR STOP any medicine without doctor or pharmacist approval. Inform your doctor of any other medical conditions, including kidney problems, low blood pressure, lightheadedness when you sit or stand up, daytime sleepiness, allergies, pregnancy, or breast-feeding. Tell your doctor if you drink alcohol or have a history of compulsive behavior (eg, eating, gambling, shopping).Tell your if you have trouble controlling your muscles. USE OF THIS MEDICINE IS NOT RECOMMENDED if you have severe kidney problems or are on dialysis. Contact your doctor or pharmacist if you have any questions or concerns about using this medicine. How to Use This Medicine: Follow the directions for taking this medicine provided by your doctor. An extra patient leaflet is available with this medicine. Talk to your pharmacist if you have questions about this information. Take this medicine by mouth with or without food. THIS MEDICINE MAY BE TAKEN WITH FOOD if it upsets your stomach. SWALLOW WHOLE. Do not break, crush, or chew before swallowing. Your dose will be started low and gradually increased to achieve the best results. DO NOT CHANGE YOUR DOSE sooner than recommended. STORE THIS MEDICINE at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store away from heat, moisture, and light. Do not store in the bathroom. KEEP THIS MEDICINE out of the reach of children and away from pets. IF YOU MISS A DOSE of this medicine, skip the missed dose and go back to your regular dosing schedule. DO NOT take 2 doses at once. IF YOU MISS SEVERAL DOSES, contact your doctor before you start to take this medicine again. Cautions: DO NOT USE THIS MEDICINE IF you are allergic to any ingredient in this medicine. DO NOT EXCEED THE RECOMMENDED DOSE without checking with your doctor. DO NOT SUDDENLY STOP TAKING THIS MEDICINE without checking with your doctor. Severe side effects, including fever, mental or mood changes, and stiff muscles, may occur. THIS MEDICINE MAY CAUSE DROWSINESS OR DIZZINESS. These effects may be worse if you take it with alcohol or certain medicines. Use this medicine with caution. DO NOT DRIVE OR PERFORM OTHER POSSIBLY UNSAFE TASKS until you know how you react to it. DO NOT DRINK ALCOHOL while you are using this medicine. CHECK WITH YOUR DOCTOR before you use medicines that may cause drowsiness (eg, sleep aids, muscle relaxers) while you are using this medicine; it may add to their effects. Ask your pharmacist if you have questions about which medicines may cause drowsiness. THIS MEDICINE MAY CAUSE DIZZINESS, LIGHTHEADEDNESS, OR FAINTING; alcohol, hot weather, exercise, or fever may increase these effects. To prevent them, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of any of these effects. Some patients who take this medicine have reported SUDDENLY FALLING ASLEEP while performing daily activities (eg, driving, eating, conversing). Many patients reported drowsiness before falling asleep. However, some patients did not experience drowsiness and felt that they were alert immediately before suddenly falling asleep. USE CAUTION when driving, operating machinery, or performing other activities that could be dangerous. Inform your doctor if you experience unusual drowsiness or sleepiness while using this medicine. Some people have experienced new, unusual, or increased urges (eg, gambling, sexual urges) while using this medicine. Tell your doctor right away if you notice such effects. Patients with Parkinson disease may have an increased risk of developing a certain type of skin cancer (melanoma). IT IS NOT KNOWN IF THIS MEDICINE ALSO INCREASES THE RISK OF MELANOMA. You may need to have skin exams while you are using this medicine. Discuss any questions or concerns with your doctor. LAB TESTS, including blood pressure or skin checks, may be performed while you use this medicine. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments. BEFORE YOU HAVE ANY MEDICAL OR DENTAL TREATMENTS, EMERGENCY CARE, OR SURGERY, tell the doctor or dentist that you are taking this medicine. BEFORE YOU BEGIN TAKING ANY NEW MEDICINES, either prescription or over-the-counter, check with your doctor or pharmacist. USE THIS MEDICINE WITH CAUTION IN THE ELDERLY; they may be more sensitive to its effects, especially hallucinations. FOR WOMEN: IF YOU BECOME PREGNANT, contact your doctor. You will need to discuss the benefits and risks of using this medicine while you are pregnant. IT IS NOT KNOWN IF THIS MEDICINE IS FOUND in breast milk. DO NOT BREAST-FEED while taking this medicine. Possible Side Effects: SIDE EFFECTS that may occur while taking this medicine include constipation; cough; dizziness; drowsiness; dry mouth; muscle spasms; nausea; stomach pain or upset; tiredness; or vomiting. If they continue or are bothersome, check with your doctor. CONTACT YOUR DOCTOR IMMEDIATELY if you experience abnormal thinking; balance problems; change in behavior, mood, or emotions; chest pain; confusion; decreased sexual ability; difficulty walking; fainting; hallucinations; increased urination; memory loss; muscle pain, tenderness, or weakness; new or unusual skin growths; severe or persistent drowsiness or sleepiness; shortness of breath; sudden irresistible urge to sleep or suddenly falling asleep at unusual times; swelling of the arms or legs; trouble swallowing; unusual or intense urges (eg, gambling, sexual urges); unusual twitching or muscle movements; vision changes; or vivid dreams or daydreams. AN ALLERGIC REACTION to this medicine is unlikely, but seek immediate medical attention if it occurs. Symptoms of an allergic reaction include rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue. This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your healthcare provider. Call your doctor for medical advice about side effects. Overdose: IF OVERDOSE IS SUSPECTED, contact your local poison control center or emergency room immediately. Symptoms of overdose may include agitation; chest pain; confusion; decrease in blood pressure; difficulty moving; drowsiness; nausea; sedation; or vomiting. Additional Information: DO NOT SHARE THIS MEDICINE with others for whom it was not prescribed. DO NOT USE THIS MEDICINE for other health conditions. IF YOU WILL BE USING THIS MEDICINE FOR AN EXTENDED PERIOD OF TIME, be sure to obtain necessary refills before your supply runs out. CHECK WITH YOUR PHARMACIST about how to dispose of unused medicine. --------------------------------------------------------------- 注：以下产品不同规格和不同价格，购买时请以咨询为准！ --------------------------------------------------------------- 产地国家: 加拿大 原产地英文商品名: MIRAPEX ER TABLET SR 24H 3mg/tab 30tabs/bottle 原产地英文药品名: Pramipexole Dihydrochloride 中文参考商品译名: 米拉帕24小时缓释片 3毫克/片 30片/瓶 中文参考药品译名: 盐酸普拉克索 中文参考化合物名称: 盐酸普拉克索; S(-)-2-氨基-6-正丙氨基-4,5,6,7-四氢苯并噻唑二盐酸盐 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: MIRAPEX ER TABLET SR 24H 0.375mg/tab 7tabs/bottle 原产地英文药品名: PRAMIPEXOLE DIHYDROCHLORIDE 中文参考商品译名: 米拉帕24小时缓释片 0.375毫克/片 7片/瓶 中文参考药品译名: 盐酸普拉克索 中文参考化合物名称: 盐酸普拉克索; S(-)-2-氨基-6-正丙氨基-4,5,6,7-四氢苯并噻唑二盐酸盐 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: MIRAPEX ER TABLET SR 24H 0.375mg/tab 30tabs/bottle 原产地英文药品名: Pramipexole Dihydrochloride 中文参考商品译名: 米拉帕24小时缓释片 0.375毫克/片 30片/瓶 中文参考药品译名: 盐酸普拉克索 中文参考化合物名称: 盐酸普拉克索; S(-)-2-氨基-6-正丙氨基-4,5,6,7-四氢苯并噻唑二盐酸盐 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: MIRAPEX ER TABLET SR 24H 0.75mg/tab 7tabs/bottle 原产地英文药品名: Pramipexole Dihydrochloride 中文参考商品译名: 米拉帕24小时缓释片 0.75毫克/片 7片/瓶 中文参考药品译名: 盐酸普拉克索 中文参考化合物名称: 盐酸普拉克索; S(-)-2-氨基-6-正丙氨基-4,5,6,7-四氢苯并噻唑二盐酸盐 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: MIRAPEX ER TABLET SR 24H 1.5mg/tab 7tabs/bottle 原产地英文药品名: Pramipexole Dihydrochloride 中文参考商品译名: 米拉帕24小时缓释片 1.5毫克/片 7片/瓶 中文参考药品译名: 盐酸普拉克索 中文参考化合物名称: 盐酸普拉克索; S(-)-2-氨基-6-正丙氨基-4,5,6,7-四氢苯并噻唑二盐酸盐 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: MIRAPEX ER TABLET SR 24H 1.5mg/tab 30tabs/bottle 原产地英文药品名: Pramipexole Dihydrochloride 中文参考商品译名: 米拉帕24小时缓释片 1.5毫克/片 30片/瓶 中文参考药品译名: 盐酸普拉克索 中文参考化合物名称: 盐酸普拉克索; S(-)-2-氨基-6-正丙氨基-4,5,6,7-四氢苯并噻唑二盐酸盐 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM --------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: MIRAPEX ER TABLET SR 24H 0.75mg/tab 30tabs/bottle 原产地英文药品名: Pramipexole Dihydrochloride 中文参考商品译名: 米拉帕24小时缓释片 0.75毫克/片 30片/瓶 中文参考药品译名: 盐酸普拉克索 中文参考化合物名称: 盐酸普拉克索; S(-)-2-氨基-6-正丙氨基-4,5,6,7-四氢苯并噻唑二盐酸盐 生产厂家中文参考译名: 勃林格殷格翰 生产厂家英文名: BOEHRINGER INGELHEIM ------------------------------------------------------------------ 产地国家: 美国 原产地英文商品名: PRAMIPEXOLE DI-HCL(MIRAPEX GENERIC) 0.125mg/tab 63Tabs/bottle 原产地英文药品名: PRAMIPEXOLE DIHYDROCHLORIDE 中文参考商品译名: 盐酸普拉克索(米拉帕仿制药) 0.125毫克/片 63片/瓶 中文参考药品译名: 盐酸普拉克索 中文参考化合物名称: 一水合二盐酸（S）-2-氨基-4，5，6，7-四氢-6-丙胺-苯并噻唑=盐酸普拉克索一水合物 该药品相关信息网址1: http://www.mirapex.com/ 该药品相关信息网址2: http://www.drugs.com/mirapex.html 该药品相关信息网址3: http://www.rxlist.com/mirapex-drug.htm