部分中文PROXYM处方资料（仅供参考） Etodolac依托度酸 【分类】消炎镇痛药 【化学名】（±）-1,8-二乙基-1,3,4,9-四氢吡喃[3,4-b]吲哚-1-乙酸。 【药理毒理】 本品为非甾体抗炎药。具有抗炎、解热和镇痛作用。其作用机理可能是通过阻断环氧合酶的活性，从而抑制了前列腺素（PG）的合成。 【药代动力学】 据国外文献报导，口服给药吸收良好，没有明显的首过效应，全身生物利用度达80％或以上。每12小时给药在600mg以内时，血药浓度-时间曲线下面积与给药剂量成正比关系。99％以上的依托度酸与血浆蛋白结合，游离部分少于1％。单剂给药200～600mg，在80±30分钟内其平均血浆峰值浓度(Cmax)介于14±4～37±9μg/ml范围内。其平均血浆清除率为47(±16)ml/h/kg，消除半衰期(t1/2)为7.3(±4.0)小时。依托度酸经肝脏代谢，16%的给药剂量经粪便排泄。通常不根据体重决定给药剂量，但在推荐剂量下个体间血药浓度的差异显著，尤其在有胃肠道病变或服用影响GI吸收、蛋白结合率、损害肝肾功能的药物者。 【适应症】 用以缓解下列疾病的症状和体征。 　　 （1）骨关节炎（退行性关节病变） 　　 （2）类风湿关节炎 　　 （3）疼痛症状本品可用于以上疾病急性发作的治疗，也可用于以上疾病的长期治疗。 【用法用量】 遵医嘱，服用依托度酸的剂量应个体化，以保证最佳的疗效和耐受性。 　　 （1）止痛：急性疼痛的推荐剂量为200～400mg，每8小时一次，每日最大剂量不超过1.2g。体重在60公斤以下者，每日最大剂量不应超过20mg/公斤体重。临床观察发现，每间隔12小时给药一次，在一些病人中依托度酸仍有止痛作用。 　　 （2）慢性疾病：依托度酸治疗慢性疾病(如骨关节炎、类风湿关节炎)的推荐剂量为每日0.4～1.2g，分次口服，每日最大剂量不应超过1.2g，体重在60公斤以下者，每日最大剂量不应超过20mg/公斤体重。依托度酸剂量每日0.4g以下，分次口服，或每晚单剂量给药0.4g或0.6g，在一些病人中有一定的疗效。  　　 （3）老年人服用：依托度酸在老年人中的药代动力学与普通人群无显著性差异，因此在老年人中使用无需调整剂量，但应当小心。另外老年人对前列腺素抗体的作用较年轻人敏感，因此针对某一个体增加药物治疗剂量时更应谨慎。 【不良反应】 据国外资料报导，2629例关节炎病人在开放、双盲的临床验证中观察4～320周的结果以及世界范围内的大约6万病人在依托度酸上市后的监测结果，上市后的自发性报道也包含在其中。临床研究显示，依托度酸总的耐受性较好，大多数不良反应轻微而且短暂，以下所列的发生率≥1％的，可能与药物相关。 　　 发生率>1％：全身症状：腹痛、乏力、不适、寒战、发热。消化系统：便秘、腹泻、消化不良、腹胀、胃炎、黑便、恶心、呕吐。 神经系统：焦虑、抑郁、头晕皮肤及附属器：搔痒、皮疹。特殊感觉：视物模糊，耳鸣。 泌尿生殖系统：排泄困难、尿频。  　　 发生率＜1％全身症状：过敏反应、类过敏反应、胸痛、胸闷。心血管系统：充血性心力衰竭、面色潮红、高血压、心悸、晕厥、血管炎(包括坏死性和过敏性)。 　　 消化系统：厌食、口干、十二指肠炎、肝酶升高、结肠炎、嗳气、肝功能衰竭、肝炎(包括瘀胆性肝炎)、肠溃疡、黄疸(包括瘀胆)、胰腺炎、伴或不伴出血穿孔的消化性溃疡、口炎(包括溃疡性口炎)、口渴。 　　 血液及淋巴系统：粒细胞缺乏、贫血、出血时间延长、瘀斑、溶血性贫血、中性粒细胞缺乏、全血细胞减少、血小板减少。 代谢和营养：浮肿、尿素氮增高、既往已控制很好的糖尿病病人中血糖升高、血肌酐增高。 　　 神经系统：失眠、嗜睡。呼吸系统：哮喘。 皮肤及附属器：血管性水肿、皮肤血管炎所致紫癜、多形红斑、Steven-Johnson综合征、多汗、荨麻疹、水疱样皮疹。 特殊感觉：畏光、短暂性视觉障碍。  　　 泌尿生殖系统：肾小球肾炎、肾盂肾炎、肾功能衰竭、肾乳头状坏死。据报道以下症状与服用依托度酸同时出现，其发生率小于1％，但两者是否存在必然的联系尚不清楚，仅用于提醒医生注意。其中包括两者之间因果关系不明确者以及经因果关系分析后确定其与依托度酸无关，但由于情况严重，且发生率较偶然事件发生率为高者。 全身性表现： 感染、非自主性肌肉运动、肌肉痉挛、肌无力、肌肉疼痛、直肠－耻骨疼痛、皮下结节，第一掌指关节压痛。 心血管系统：心律失常(包括心动过速)、心血管意外、心肌梗死。  　　 消化系统：食欲改变、结肠炎(包括缺血性结肠炎)、伴或不伴贲门痉挛或狭窄的食管炎、呕血、便血。 　　 血液及淋巴系统：不典型淋巴细胞、红细胞压积下降、血色素下降、嗜酸细胞增多、白细胞减少。 代谢与营养：体重改变。 神经系统：意识混乱、手抖、头疼、注意力不能集中、多梦、感觉异常、烦躁。 　　 呼吸系统：支气管炎、支气管痉挛、气短、过度通气、咽炎、鼻炎、鼻窦炎、打喷嚏。 皮肤及附属器：脱发、脆甲、毛细血管脆性增加、斑丘疹、过敏、皮肤脱屑。 　　 特殊感觉：眼/鼻烧灼感、结膜炎、耳聋、耳痛、鼻衄、异食癖、眼后刺痛。 泌尿生殖系统：乳房压痛、膀胱炎、阳痿、血尿、间质性肾炎、白带增多、夜尿多、肾结石、子宫不规则出血、阴道出血。 【禁忌】 有下列情况的病人应禁用 　　 （1）活动期消化性溃疡或与应用另一种NSAIDs有关的胃肠道溃疡或出血史。 　　 （2）不同NSAIDs之间可能存在交叉反应，因此在阿司匹林或其他NSAIDs治疗期间出现哮喘、鼻炎、荨麻疹或其他过敏反应者。 　 （3）对本品过敏者。 【注意事项】 长期服用NSAIDs的患者随时都可能发生溃疡、出血、穿孔等严重的胃肠道副作用。虽然在治疗初期轻微的胃肠道不适如消化不良等很常见，但对于长期服用NSAIDs者，即使没有任何胃肠道不适症状，医生仍然应时刻警惕胃肠道溃疡和出血的危险。 临床观察发现NSAIDs治疗3～6个月，上消化道症状性溃疡、大出血及穿孔的发生率约为1％，治疗一年其发生率升至2％～4％。医生也应告知病人一旦发生严重胃肠道损害时应当采取的措施。现有的研究均证实所有服用NSAIDs的病人无一例外地面临着消化道溃疡和出血的危险，而严重的消化道溃疡病史以及吸烟、饮酒等因素可以增加其危险性。年老体弱者的耐受性较差，大多数致命性消化道并发症发生于此人群中。 在健康志愿者中的观察提示，依托度酸引起消化道微量出血的潜在危险性较其他常用的NSAIDs为小。然而在既往有上消化道疾病病史的患者中，应当谨慎用药，权衡风险与利益进行选择，并严密监测其不良反应。 肾脏作用：象其他NSAIDs一样，给小鼠长期喂食依托度酸可导致其肾髓质变性和肾乳头坏死。雄鼠服用依托度酸两年，其肾盂移行上皮细胞增生的发生率增加。现已收到一些报告，依托度酸可以导致人肾脏发生不良反应：如血尿、急性间质性肾炎、肾功能不全等等。因此有肾功能损害的病人服用依托度酸时应小心。 前列腺素对于维持正常肾血流灌注起作用，因此任何NSAIDs均可以剂量相关地抑制前列腺素的合成，减少肾血流，加速肾功能的损害。尤其肾功能不全、心衰、肝功能异常、服用利尿剂和老年病人的相对危险性更大。 通常需停用NSAIDs以使其肾功能恢复到治疗前状态。依托度酸代谢产物主要经肾脏排泄，肾衰病人中葡萄糖醛酸酯代谢产物累积的程度尚不清楚，但其肾脏不良反应很可能与这些代谢产物有关。 肝脏作用：一项或多项肝功能异常见于15％的病人，若继续用药，这些异常可以消失、维持不变，也可能继续进展。据报道在依托度酸治疗的病人中约1％出现谷丙转氨酶(ALT)或谷草转氨酶(AST)的明显升高(正常上限3倍或以上)。当病人出现肝功能异常的症状和/或体征或出现肝功能检查异常时，应仔细评估，以期发现肝功能严重损害的早期征象。尽管严重的肝损害少见，当肝功持续异常或恶化，临床症状或体征提示肝病进展或出现全身性症状时(如嗜酸细胞增多、皮疹等)，应当停用依托度酸。 由于其他原因引起的肝肾功能损害可以改善依托度酸的代谢。此类病人以及需长期治疗的病人，尤其是老年人应当严密监测其潜在的不良反应，并根据需要调整药物剂量。血液系统作用：服用依托度酸或其他NSAIDs的病人有时可出现贫血，其原因可能由于液体潴溜、胃肠道失血或对促红细胞生成素的作用不完全所致。 长期服用NSAIDs(包括依托度酸)者若出现贫血的症状或体征应查血色素和红细胞压积。任何抑制前列腺素合成的药物都可能在某种程度上影响血小板的功能。 服用依托度酸的病人也应密切监测此方面的不良反应。 水钠潴留和浮肿：一部分服用依托度酸的病人会出现液体潴留和浮肿。因此象其他NSAIDs一样，已有液体潴留、高血压和心衰者应小心应用。实验室检测：任何NSAIDs均可能随时引发严重的胃肠道溃疡和出血，因此长期用药者更应坚持随访，严密监视其有无溃疡或出血的症状和体征。依托度酸导致血尿酸水平轻度下降，临床观察发现关节炎病人服用依托度酸(600mg/日～1000mg/日)四周后其血尿酸水平下降1mg％～2mg％，但在随后治疗的一年中则保持稳定。 【妊娠及哺乳期妇女用药】 妊娠期妇女：依托度酸对孕妇的作用情况由于缺乏恰当的对照组，因此没有肯定的结论，但应当慎用，必须权衡药物对病人的益处和对胎儿的潜在危险。NSAIDs对人类分娩、动脉导管闭合等心血管系统有影响，因此妊娠晚期应避免使用。依托度酸对人类分娩的影响尚不清楚。哺乳期妇女：目前还未知依托度酸是否分泌到人乳中，由于很多药物均可以分泌到乳汁中，故哺乳期妇女用依托度酸应当谨慎。 【儿童用药】 依托度酸用于儿童的安全性和有效性均未被证实，因此不推荐使用。 【药物相互作用】 抗酸剂：同时服用抗酸剂对依托度酸的吸收没有明显的影响，然而抗酸剂可使依托度酸的峰值浓度下降15～20％，但不影响达峰时间。 阿司匹林：依托度酸与阿司匹林合用时，尽管对游离依托度酸的清除不发生改变，但其蛋白结合率下降。此种药物相互作用的临床意义尚不清楚，然而由于两者同用时潜在的不良反应增加，因此临床不推荐此用法。 华法令：依托度酸与华法令同时应用可以使华法令的蛋白结合率下降，但不影响游离华法令的清除及凝血酶原时间，因此两药合用无需调整任何一种药物的剂量。然而上市后的一些报道显示两药合用使凝血酶原时间延长，因此应当慎用。 苯妥英钠：依托度酸与苯妥英钠之间无明显的药代动力学相互作用。 优降糖：依托度酸与优降糖合用时，药代动力学与药效学均无明显改变。 利尿剂：在健康志愿者中，依托度酸与速尿、双氢克尿噻之间无明显的药代动力学相互作用，依托度酸也不会减弱利尿剂的利尿效果。然而在已服用利尿剂或患有心、肾、肝功能衰竭的患者，两药同用应当小心。 甲氨喋呤：依托度酸与甲氨喋呤之间无明显的药代动力学相互作用。 环孢素、地高辛和锂：依托度酸因抑制前列腺素的合成，使肾脏对这些药物的清除发生改变，药物浓度增高，毒性增加。与环孢素相关的肾毒性也会增加。因此已服用这些药物的病人再接受依托度酸或其他NSAIDs治疗时，应当密切监测药物可能出现的毒性，尤其是已有肾功能损害者。 蛋白结合：体外研究资料表明，布洛芬、醋氨芬、苯妥英、丙磺舒、吲哚美辛、氯磺丙脲、优降糖、萘普生、格列吡嗪、炎痛喜康均对游离依托度酸的比例无明显影响。 相反，保泰松使游离态浓度增加(约80％)，尽管未经体内试验证实是否保泰松改变依托度酸的清除，但临床不推荐合用。实验室检测的相互作用服用依托度酸的患者尿中会出现其酚类代谢产物，因此测定尿胆红素可以出现假阳性反应。用快速诊断学方法在一部分服用依托度酸的病人中发现其尿酮体出现假阳性反应。这一现象与其他临床情况无相关性，也与给药剂量无关。 【贮藏】 避光，密闭保存。 What is etodolac? Etodolac is a nonsteroidal anti-inflammatory drug (NSAIDs). It works by reducing hormones that cause inflammation and pain in the body. NSAIDs treat the symptoms of pain and inflammation. They do not treat the disease that causes those symptoms. Etodolac is used to treat pain or inflammation caused by arthritis or osteoarthritis. Etodolac may also be used for purposes other than those listed in this medication guide. -------------------------------------------------------- Important information about etodolac Etodolac can increase your risk of life-threatening heart or circulation problems, including heart attack or stroke. This risk will increase the longer you use etodolac. Do not use this medicine just before or after having heart bypass surgery (also called coronary artery bypass graft, or CABG). Seek emergency medical help if you have symptoms of heart or circulation problems, such as chest pain, weakness, shortness of breath, slurred speech, or problems with vision or balance. Etodolac can also increase your risk of serious effects on the stomach or intestines, including bleeding or perforation (forming of a hole). These conditions can be fatal and gastrointestinal effects can occur without warning at any time while you are taking etodolac. Older adults may have an even greater risk of these serious gastrointestinal side effects. Call your doctor at once if you have symptoms of bleeding in your stomach or intestines. This includes black, bloody, or tarry stools, or coughing up blood or vomit that looks like coffee grounds. Do not use any other over-the-counter cold, allergy, or pain medication without first asking your doctor or pharmacist. Many medicines available over the counter contain aspirin or other medicines similar to etodolac (such as ibuprofen, ketoprofen, or naproxen). If you take certain products together you may accidentally take too much of this type of medication. Read the label of any other medicine you are using to see if it contains aspirin, ibuprofen, ketoprofen, or naproxen. Do not drink alcohol while taking etodolac. Alcohol can increase the risk of stomach bleeding caused by etodolac. Avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds). Etodolac can make your skin more sensitive to sunlight and sunburn may result. -------------------------------------------------------- Before taking etodolac Taking an NSAID can increase your risk of life-threatening heart or circulation problems, including heart attack or stroke. This risk will increase the longer you use an NSAID. Do not use etodolac just before or after having heart bypass surgery (also called coronary artery bypass graft, or CABG). NSAIDs can also increase your risk of serious effects on the stomach or intestines, including bleeding or perforation (forming of a hole). These conditions can be fatal and gastrointestinal effects can occur without warning at any time while you are taking an NSAID. Older adults may have an even greater risk of these serious gastrointestinal side effects. Do not use this medication if you are allergic to etodolac, or if you have a history of allergic reaction to aspirin or other NSAIDs. Before taking etodolac, 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; or if you smoke. If you have any of these conditions, you may need a dose adjustment or special tests to safely take etodolac. FDA pregnancy category C. This medication may be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Taking etodolac during the last 3 months of pregnancy may harm the unborn baby. Do not take etodolac during pregnancy unless your doctor has told you to. It is not known whether etodolac 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 etodolac to a child younger than 6 years old without the advice of a doctor. -------------------------------------------------------- How should I take etodolac? Take etodolac exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label. Do not crush, chew, or break an extended-release tablet. Swallow the pill whole. It is specially made to release medicine slowly in the body. Breaking the pill would cause too much of the drug to be released at one time. It may take up to 2 weeks of using etodolac before your symptoms improve. For best results, keep using the medication as directed. Talk with your doctor if your symptoms do not improve. If you take etodolac for a long period of time, your doctor may want to check you on a regular basis to make sure etodolac is not causing harmful effects. Do not miss any scheduled visits to your doctor. etodolac can cause you to have unusual results with certain medical tests. Tell any doctor who treats you that you are using etodolac. Store etodolac at room temperature away from moisture and heat. -------------------------------------------------------- What happens if I miss a dose? 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 happens if I overdose? Seek emergency medical attention if you think you have used too much of this medicine. Overdose symptoms may include nausea, vomiting, stomach pain, drowsiness, black or bloody stools, coughing up blood, shallow breathing, fainting, or coma. -------------------------------------------------------- What should I avoid while taking etodolac? When using etodolac do not use any other over-the-counter cold, allergy, or pain medication without first asking your doctor or pharmacist. Many medicines available over the counter contain aspirin or other medicines similar to etodolac (such as ibuprofen, ketoprofen, or naproxen). If you take certain products together you may accidentally take too much of this type of medication. Read the label of any other medicine you are using to see if it contains aspirin, ibuprofen, ketoprofen, or naproxen. Do not drink alcohol while taking etodolac. Alcohol can increase the risk of stomach bleeding caused by etodolac. Avoid prolonged exposure to sunlight. Etodolac may increase the sensitivity of the skin to sunlight. Use a sunscreen and wear protective clothing when exposure to the sun is unavoidable. -------------------------------------------------------- Etodolac side effects Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking etodolac and seek medical attention or call your doctor at once 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; or fever, headache, neck stiffness, chills, increased sensitivity to light, purple spots on the skin, and/or seizure (convulsions). Less serious etodolac side effects may include: upset stomach, mild heartburn or stomach pain, diarrhea, constipation; bloating, gas; dizziness, headache, nervousness; skin itching or rash; sore throat, stuffy nose; blurred vision; or ringing in your ears. This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088. -------------------------------------------------------- What other drugs will affect etodolac? Tell your doctor if you are taking an antidepressant such as citalopram (Celexa), duloxetine (Cymbalta), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem, Symbyax), fluvoxamine (Luvox), paroxetine (Paxil), sertraline (Zoloft), or venlafaxine (Effexor). Taking any of these drugs with etodolac may cause you to bruise or bleed easily. Before taking etodolac, tell your doctor if you are taking any of the following drugs: a blood thinner such as warfarin (Coumadin); cyclosporine (Gengraf, Neoral, Sandimmune); digoxin (digitalis, Lanoxin); lithium (Eskalith, Lithobid); methotrexate (Rheumatrex, Trexall); a diuretic (water pills) such as furosemide (Lasix); steroids (prednisone and others); aspirin or other NSAIDs (non-steroidal anti-inflammatory drugs) such as diclofenac (Cataflam, Voltaren), flurbiprofen (Ansaid), indomethacin (Indocin), ketoprofen (Orudis), ketorolac (Toradol), mefenamic acid (Ponstel), meloxicam (Mobic), nabumetone (Relafen), naproxen (Aleve, Naprosyn), piroxicam (Feldene), and others; or 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 etodolac. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. -------------------------------------------------------- Where can I get more information? Your pharmacist can provide more information about etodolac. Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed. Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist. --------------------------------------------------------------- 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！ -------------------------------------------------------------- 原产地英文商品名: PROXYM 300mg/tab 100tabs/box 原产地英文药品名: etodolac 中文参考商品译名: PROXYM 300毫克/片 100片/盒 中文参考药品译名: 依托度酸 中文参考化合物名称: （±）-1,8-二乙基-1,3,4,9-四氢吡喃[3,4-b]吲哚-1-乙酸 生产厂家中文参考译名: EMCORE 生产厂家英文名: EMCORE --------------------------------------------------------------- 原产地英文商品名: PROXYM 200mg/tab 100tabs/box 原产地英文药品名: etodolac 中文参考商品译名: PROXYM 200毫克/片 100片/盒 中文参考药品译名: 依托度酸 中文参考化合物名称: （±）-1,8-二乙基-1,3,4,9-四氢吡喃[3,4-b]吲哚-1-乙酸 生产厂家中文参考译名: EMCORE 生产厂家英文名: EMCORE