英文药名: Relafen(Nabumetone Tablets)
中文药名: 萘丁美酮,萘普酮,瑞力芬,萘布美通,纳布美通片
药品名称
【药物名称】瑞力芬,萘丁美酮 【性 状】萘丁美酮的化学名为4-(6-甲氧基-2-萘基)丁酮-2。分子式为C15H16O2,分子量为228.29。本品为白色椭圆形薄膜包衣片。 药理作用
萘丁美酮是一个非酸性非甾体抗炎药。 本品经胃肠道吸收,经肝脏迅速代谢成主要代谢物:6-甲氧基-2-萘乙酸(6MNA)而起解热、镇痛、抗炎作用。抗炎镇痛解热的作用于萘丁美酮的活性代谢产物抑制了炎症组织中的前列腺素合成有关。 胃粘膜影响小:本品是一种非酸性、非离子性前体药物,在吸收过程中对胃粘膜无明显的局部直接影响;同时本品对胃粘膜生理性环氧合酶的抑制作用较小。因此本品引起的胃肠粘膜糜烂和出血的发生率较低。 对出血和凝血无影响:本品对健康志愿者的血标本,在体外进行诱导的血小板聚集作用无影响。对出血时间、凝血试验均无显著改变。 药代动力学
本品口服后在十二指肠被吸收,经肝脏转化为主要活性代谢物6-甲氧基-2-萘乙酸(6-MNA)。口服萘丁美酮1 g后,约35%转化为6-MNA,50%转化为其它代谢物随后从尿中排泄。6-MNA的血浆蛋白结合率约为99%。体内分布广乏,易于扩散的滑膜组织、滑液、纤维囊组织和各种炎性渗出物中,它可进入乳汁和胎盘。6-MNA的消除半衰期在青年人约为24小时,在老年人约为30小时。6-MNA经肝脏转化为非活性产物,80%从尿中排泄,10%从粪便中排泄。 适 应 症
适用于骨关节炎和类风湿性关节炎,以及其他需抗炎治疗的类似症状。 用法用量
成人每次1 g,每日1次,睡前口服。对严重或持续症状,或急性加重期,可另增加500 mg-1 g,清晨给药。1日最大剂量为2 g,分2次服用。体重<50 kg者以500 mg/日起始,逐渐上调至有效剂量。 任何疑问,请遵医嘱! 用药须知
萘丁美酮片应完整吞咽,不应咀嚼。 不良反应
胃肠道:恶心、呕吐、消化不良、腹泻、腹痛、便秘、胃肠气胀、便潜血试验阳性、胃炎、口干和口腔炎约1-3%。上消化道出血约0.7%。用本品的病例中,溃疡发生率在短疗程(6周-6个月)组和在长疗程(8年)组分别为0.1%和0.95%。每日口服萘丁美酮2 g的腹泻发生率增加。 神经系统:表现有头痛、头晕、疲劳、耳鸣、多汗、失眠、多梦、嗜睡和紧张,发生率小于1.5%。 皮肤:皮疹和瘙痒约2.1%,水肿约1.1%。 少见或偶见的不良反应有 胃肠道:黄疸、食欲增加或减退、吞咽困难、肠胃炎、肝功能异常、黑便和肝衰竭。 神经系统:衰弱、兴奋、焦虑、多疑、抑郁、不适感、感觉异常、震颤和眩晕,视觉异常。 皮肤:大疱性皮疹、荨麻疹、光敏感、风疹、迟发型皮肤卟啉症、中毒性表皮坏死松解症、多形红斑、Stevens-Johnson综合征。 心血管:血管炎。 代谢:体重增加。 呼吸系统:呼吸困难、嗜红细胞增多性肺炎、过敏性肺炎、原发性肺炎。 泌尿生殖系统:蛋白尿、氮血症、高尿酸血症、间质性肾炎、肾病综合征、阴道出血和肾衰。 血液:血小板病。 过敏:过敏样反应、过敏症、血管神经性水肿。 罕见的不良反应有 胃肠道:胆红素尿、十二指肠炎、嗳气、胆结石、龈炎、舌炎、胰腺炎和直肠出血。 神经系统:恶梦,味觉异常。 皮肤:脱发。 心血管:心绞痛、心律失常、高血压、心肌梗塞、心悸、晕厥和血栓性静脉炎。 呼吸系统:哮喘和咳嗽。 泌尿生殖系统:排尿困难,血尿,阳痿和肾结石。 全身症状:发热、寒战。 血液:贫血、白细胞减少、粒细胞减少症。 代谢:血糖升高,低钾血症和体重减轻。 禁 忌 症
活动性消化性溃疡、严重肝损害(如肝硬化)、对萘丁美酮及其他非甾体抗炎药过敏者禁用。 注意事项
已确定为阿斯匹林过敏的患者用萘丁美酮可能有相似的反应。 肝功能一些参数的变化,尤其是碱性磷酸酯酶,在慢性炎症患者中经常能见到,没有萘丁美酮增强这些变化的证据。 有消化性溃疡病史的患者应定期检查。 萘丁美酮的代谢,尿是主要的代谢途径。在肾功能损伤的病人中(肌酸酐清除少于30 mL/分钟),应考虑减少剂量或禁用。 有心力衰竭、水肿或有高血压者应慎用本品。用餐中服用本品的吸收率可增加,应在餐后或晚间服药。 孕妇及哺乳期妇女用药
动物实验研究表明无潜在的致畸性。同其他化合物一样,足够高剂量给予动物可见母系毒性,记录胚胎指征(家兔研究中剂量为300 mg/kg)。大鼠高剂量研究(320 mg/kg)可推迟分娩,这被认为是由于抑制前列腺素合成的作用。萘丁美酮活性代谢物在哺乳动物的乳汁中可发现。用于孕妇的安全性没有被确定。萘丁美酮偏不推荐孕妇及哺乳期妇女使用。 儿童用药
萘丁美酮没有推荐儿童使用的临床资料。 老年患者用药
在老年病人中通常对很多药物血药浓度较高。老年人使用本品应该维持最低的有效剂量。在这个年龄组推荐剂量每日不超过1 g,一些患者服用0.5 g会得到令人满意的效果。 药物相互作用
萘丁美酮的主要循环代谢物有很高的蛋白结合力,患者在同时接受口服抗凝血剂,乙内酰脲类抗惊厥药或磺酰脲类降低血糖的药物治疗时,应检查这些药物过量的征兆。如果需要,可调整剂量。 自愿患者研究表明,氢氧化铝凝胶,对乙酰氨基酚、阿斯匹林对萘丁美酮的生物利用度无影响。但通常不主张同时用两种或多种非甾体抗炎药。 在健康自愿者中,本品与抗凝剂华法林之间无相互作用。但尚无在病人中合并使用这两种药物的资料。 药物过量
没有特殊的解毒药。过量出现中毒症状时,及时洗胃或催吐,给予60 mg以上活性炭口服,以吸附消化道内残存药物,并给予适当的对症和支持疗法。 包装规格: ·500mg*56片(MEDA 生产) ·500mg*100 片 ·750mg*100 片
Relafen (Nabumetone) is a prescription medication that has been licensed to treat several conditions related to pain, inflammation, swelling, or stiffness. Specific Relafen uses include the relief of: osteoarthritis symptoms and rheumatoid arthritis symptoms. It is also used to treat juvenile arthritis symptoms, mild to moderate pain, such as lower back pain, neck pain, or leg pain, fibromyalgia symptoms, gout symptoms, chronic fatigue syndrome symptoms, symptoms of systemic lupus erythematosus, pain or inflammation caused by other conditions.
MECHANISM OF ACTION Relafen and other NSAIDs (nonsteroidal anti-inflammatory drugs) work by inhibiting the action of certain hormones that cause inflammation and pain in the body. These hormones are called prostaglandins. By blocking the effects of prostaglandins, Relafen can help alleviate pain, inflammation, and joint swelling associated with different forms of arthritis.
DOSAGE FORM Tablets: 500 and 750 Mg.
DOSAGE AND ADMINISTRATION
The recommended starting dose is 1,000 mg taken as a single dose with or without food. Some patients may obtain more symptomatic relief from 1,500 mg to 2,000 mg per day. Relafen can be given in either a single or twice-daily dose. The lowest effective dose should be used for chronic treatment . Patients weighing under 50 kg may be less likely to require dosages beyond 1,000 mg; therefore, after observing the response to initial therapy, the dose should be adjusted to meet individual patients' requirements. What to do if a dose is missed? Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at your next regularly scheduled time. Do not take extra medicine to make up the missed dose.
What to do in case of over dose? Seek emergency medical attention if you think you have used too much of this medicine. Symptoms of a Relafen overdose may include nausea, vomiting, stomach pain, drowsiness, black or bloody stools, coughing up blood, shallow breathing, fainting, or coma.
Precautions
Before you buy Relafen generic, tell your doctor if you are allergic to any drugs, or if you have: A history of heart attack, stroke, or blood clot. heart disease, congestive heart failure, high blood pressure. a history of stomach ulcers or bleeding. liver or kidney disease. Asthma. polyps in your nose. a bleeding or blood clotting disorder. if you smoke. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Taking Relafen during the last 3 months of pregnancy may harm the unborn baby. It is not known whether Relafen passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not give this medicine to a child without the advice of a doctor. Contraindications
Relafen is contraindicated in patients with known hypersensitivity to nabumetone or its excipients. Relafen should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Relafen is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery. STORAGE Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F) in well-closed container; dispense in light-resistant container.
DRUG INTERACTIONS Before you buy Relafen generic online, tell your doctor if you are taking any of the following drugs:
A blood thinner such as warfarin. Lithium. Methotrexate. Diuretics such as furosemide. Steroids Aspirin or other NSAIDs (non-steroidal anti-inflammatory drugs) such as etodolac (Lodine), flurbiprofen (Ansaid), indomethacin (Indocin), ketoprofen (Orudis), ketorolac (Toradol), mefenamic acid (Ponstel), meloxicam (Mobic), naproxen (Aleve, Naprosyn), piroxicam (Feldene), and others. An ACE inhibitor such as benazepril (Lotensin), captopril (Capoten), fosinopril (Monopril), enalapril (Vasotec), lisinopril (Prinivil, Zestril), ramipril (Altace), and others. This list is not complete and there may be other drugs that can interact with Relafen. Do not start using a new medication without telling your doctor.
SIDE EFFECTS Stop taking Relafen and seek medical attention if you have any of these serious side effects:
Chest pain, weakness, shortness of breath, slurred speech, problems with vision or balance. Black, bloody, or tarry stools. Coughing up blood or vomit that looks like coffee grounds. Swelling or rapid weight gain. Urinating less than usual or not at all. Nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes). Fever, sore throat, and headache with a severe blistering, peeling, and red skin rash. Bruising, severe tingling, numbness, pain, muscle weakness. This is not a complete list of all the possible side effects of Relafen. Always talk to your doctor about all the side effects of this medication.
Disclaimer: This report on medication is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use. |