FDA批准酮咯酸氨丁三醇鼻用制剂用于短期疼痛治疗 5月17日，Roxro药业公司宣布，FDA已批准该公司生产的酮咯酸氨丁三醇（ketorolac tromethamine）鼻内制剂（商品名为Sprix鼻喷剂）用于中重度疼痛的短期治疗。该产品在非住院患者中可使用达到5天。 ROXRO制药公司近日宣布，FDA批准该公司的SPRIX（酮咯酸氨丁三醇）喷鼻剂用于需要阿片类药物进行镇痛的急性中度和中重度疼痛短期治疗（最多5天）。SPRIX是处方药酮咯酸鼻腔给药剂型，酮咯酸属于非甾体类抗炎药，SPRIX旨在为急性中度和中重度疼痛门诊患者提供一种方便、有效和快速作用的镇痛选择。非麻醉剂注射镇痛药酮咯酸氨丁三醇用于中重度疼痛，目前在美国医院经常使用。SPRIX获批为急性疼痛门诊患者提供一种替代常用的阿片类处方药的非麻醉剂和易于使用的选择。 “FDA批准SPRIX为医师治疗中度和中重度疼痛患者提供了一项重要工具。在患者和医生对越来越多使用麻醉剂表示担忧之时，这尤为重要。”ROXRO公司首席行政官Roberto Rosenkranz表示。 酮咯酸氨丁三醇鼻用制剂（SPRIX喷鼻剂） 2010年5月17日，位于美国加州Menlo Park 的Roxro制药公司今天宣布，美国食品药品监督管理局（FDA）已批准酮咯酸氨丁三醇（ketorolac tromethamine）的鼻内制剂（Sprix喷鼻剂）用于需要阿片类镇痛药进行控制的中度至中重度疼痛的短期治疗。 该制剂在非住院患者中可用于治疗达到5天。该公司称，酮咯酸是一种非甾体抗炎药（NSAID），在医院内常被作为一种肌内（IM）注射剂用于中重度疼痛的短期治疗。而这次批准的新制剂可通过鼻内给予，并通过鼻粘膜吸收，可与肌内注射剂同样快地达到峰浓度。伊利诺斯州芝加哥市的Rush大学医学中心矫形外科麻醉学部主任Askomur Buvanendran表示，该新产品“可满足用于急救疼痛控制的新的非类阿片、非注射的需要，因为该药在提供有效控制中度至中重度疼痛的同时，还可使发生滥用以及与麻醉性止痛剂相关的副作用的可能性降至最低。这种方便使用的喷鼻剂还能提供院外的疼痛治疗。” 该公司在声明中提到，这种新制剂已在伴有中度至中重度疼痛的患者中进行过单独给药和与吗啡联用的研究。该药的申请材料中包括来自14项共纳入超过1000名受试者的临床试验，以及4项成人对照性、有效性研究，在这些研究中均满足主要的研究终点。2项分别纳入超过300名进行选择性腹部或矫形外科手术患者的3期试验显示，与安慰剂组患者相比，使用Sprix后48h内疼痛强度的总评分显著降低，且差异有统计学意义。另外，接受了酮咯酸鼻内制剂的患者还显示与安慰剂组相比，其48h内吗啡的用量减少了26%~36%。 另外，同其他酮咯酸制剂一样，使用这种鼻内制剂的总持续时间应尽可地缩短，不超过5天。 其他风险和禁忌症如下： 1、酮咯酸可引起消化性溃疡、胃肠道出血和/或致命性胃或肠穿孔。鼻内用酮咯酸禁用于伴有消化性溃疡病或胃肠道出血史的患者； 2、鼻内用酮咯酸可抑制血小板功能，故应禁用于伴有疑似或确诊的脑血管出血、出血素质、未完全止血或出血风险较高的患者； 3、NSAID可能引起致命性严重心血管事件、心肌梗塞和中风的风险增加，该新闻发布稿提到。这种风险可能会随着用药持续时间的延长而增加，并且在伴有心血管病或心血管风险因素的患者中较高。这种酮咯酸鼻内制剂禁用于冠状动脉旁路移植血管（CABG）手术的围手术期疼痛的治疗。 4、鼻内用酮咯酸禁用于伴有晚期肾损害和具有因体液消耗而导致肾衰竭风险的患者；另外，该产品禁用于已知对阿司匹林、酮咯酸或其他NSAID、EDTA过敏或有过敏反应史的患者，以及既往曾进行过大手术的患者或分娩期间。不应与丙磺舒或己酮可可碱同时使用。 轻度、短暂性鼻部不适是该鼻内制剂最常见的不良反应。Roxro药业公司的首席执行官（CEO）Roberto Rosenkranz在该公司的声明中表示，“现已批准的酮咯酸的注射剂型已被医生们很好地接受用于院内治疗，因此我们相信，这种更为方便的剂型将会很快被使用。” 处方信息摘要 SPRIX®（酮咯酸氨丁三醇 ketorolac tromethamine）鼻腔喷雾剂 最初美国批准：1989年 警告： USE，消化道出血，心血管和肾脏风险的局限性 请参阅完整的黑框警告的完整处方信息。 使用限制-使用SPRIX和其他酮咯酸制剂的总持续时间不得超过5天。 胃肠（GI）风险酮咯酸可引起消化性溃疡，胃肠道出血，和/或胃或肠道，这可能是致命的穿孔。SPRIX是消化性溃疡病或胃肠道出血的历史禁忌。 出血风险-SPRIX抑制血小板功能及患者的疑似或确诊的脑血管出血，出血素质，不完全止血或出血的高风险是禁忌。 心血管（CV）风险的NSAID可导致严重的CV血栓事件，心肌梗塞和中风，它可以是致命的危险性增加。这种风险可能会随使用时间增加。患者心血管疾病或危险因素的心血管疾病可能会面临更大的风险。SPRIX禁忌用于冠状动脉旁路移植术（CABG）的设置处​​理的围手术期疼痛。 肾的风险-SPRIX是治疗晚期肾功能损害和禁忌的患者在肾功能衰竭的风险因血容量不足。 作用机理 SPRIX包含酮咯酸缓血酸胺，非类固醇抗炎药（NSAID）。酮咯酸是抑制酶环氧合酶（COX），花生四烯酸级联的早期分量，导致前列腺素，血栓烷，和前列环素的合成减少止痛剂。 酮咯酸不结合到阿片受体亚型（μ，κ，三角洲），但酮咯酸氨丁三醇的IM30毫克的剂量已经证明，与吗啡6毫克和12毫克所得之间的总的镇痛作用。酮咯酸具有无镇静或抗焦虑性能，并具有对肠能动性没有影响. 适应症和用法 SPRIX在成人患者表明为中度至中重度疼痛的短期（最多5天）的管理，需要在该阿片样物质的水平镇痛。 用法用量 对于成年患者<65岁：31.5毫克（一个15.75毫克喷雾每个鼻孔）每6至8小时。每日最大剂量是126毫克。 患者≥65岁，肾功能受损的患者，和患者小于50公斤（110磅）：15.75毫克（一个15.75毫克喷雾仅在一个鼻孔）每6至8小时。每日最大剂量是63毫克。 SPRIX尚未被证明是安全和有效的儿科患者。 SPRIX鼻喷剂应在24小时的取第一剂量，即使瓶子仍含一些药物中被丢弃。 剂型和规格 喷鼻剂： 每100微升酮咯酸氨丁三醇15.75mg喷雾。每个1.7克瓶含有8喷雾剂。 禁忌症 已知过敏酮咯酸，阿司匹林，其他NSAID，或EDTA。 使用患者的活动性消化性溃疡病，最近的胃肠道出血或穿孔，或消化性溃疡或胃肠道出血的历史。 服用阿司匹林或其它NSAID后使用患者哮喘，荨麻疹​​，或其它过敏型反应的历史。 使用任何重大手术前预防性镇痛。 期间冠状动脉旁路移植术（CABG）的设置围手术期使用。 使用在晚期肾脏疾病或患者的肾功能衰竭的风险因血容量不足。 使用分娩和分娩。 使用患者疑似或确诊的脑血管出血，出血性素质，不完全止血，而以出血的高危人群。 警告和注意事项 SPRIX不应该与IM/IV或口服酮咯酸，阿司匹林，或其它NSAID同时使用。 酮咯酸可引起严重的胃肠道不良反应包括出血，溃疡及穿孔。SPRIX应谨慎处方的患者溃疡病或胃肠道出血的病史。老年患者是在严重胃肠道事件的风险更大。 NSAIDs的影响血小板凝集，并可能导致出血并发症。SPRIX应慎用谁有凝血功能障碍或正在治疗的影响止血患者。不要在患者对他们来说，止血是非常关键的使用SPRIX。 酮咯酸可引起肾脏损害。SPRIX不应该在晚期肾脏疾病或患者的肾功能衰竭的风险因血容量不足使用，并应谨慎服用利尿剂或ACE抑制剂的患者使用。 在患者有无服用阿司匹林或NSAIDs的过敏史，可能会发生过敏性反应。SPRIX应立即在患者的过敏反应停药。 严重的和潜在致命的心血管血栓性事件，心肌梗塞和中风可以用NSAID治疗发生。 体液潴留和水肿已在服用NSAIDs的患者中观察到。SPRIX应谨慎患者心脏代偿或类似条件下使用。 的NSAIDs可导致严重的皮肤病的不良反应，如剥脱性皮炎，Stevens-Johnson综合征，和中毒性表皮坏死松解症，它可以是致命的。SPRIX应立即在患者的皮肤反应停止。 在怀孕期间，使用超过妊娠30周SPRIX可引起动脉导管过早关闭，导致胎儿造成伤害。 不良反应 最常见的不良反应（发生率> 2％）与SPRIX处理并在出现速度的患者至少两次安慰剂是鼻部不适，尿量rhinalgia，增加流泪，咽喉刺激，少尿，皮疹，心动过缓，减少，增加ALT和/或AST，高血压和鼻炎。 药物相互作用 与抗凝血剂联合使用可能会增加严重胃肠出血的风险。 完整处方资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=09a80ee7-274a-4f96-8b42-480436896050 ------------------------------------------------------- 【原产地英文商品名】SPRIX NASAL SPRAY PF 15.75mg/spray 8sprays/bottle 5bottles/box 12boxes/case 【原产地英文药品名】KETOROLAC TROMETHAMINE 中文参考商品译名】 注：以下产品不同的规格和不同的价格，采购以咨询咨询为准！ ※SPRIX PF喷鼻剂 15.75毫克/喷 8喷/瓶 5瓶/盒 ※SPRIX PF喷鼻剂 15.75毫克/喷 8喷/瓶 5瓶/盒 12盒/箱 【中文参考药品译名】酮咯酸氨丁三醇 【生产厂家中文参考译名】ROXRO PHARMA INC 【生产厂家英文名】ROXRO PHARMA INC The U.S. Food and Drug Administration (FDA) has approved SPRIX TM (ketorolac tromethamine) Nasal Spray, for the short-term (up to 5 days) management of acute moderate to moderately severe pain that requires analgesia at the opioid level. SPRIX is a prescription intranasal formulation of the analgesic ketorolac, a non-steroidal anti-inflammatory drug (NSAID),designed to provide ambulatory patients with a convenient, potent, and fast-acting option for acute moderate to moderately severe pain relief.Ketorolac tromethamine is a frequently administered non-narcotic injectable analgesic for moderately severe pain in U.S. hospitals today. The approval of SPRIX provides acute pain outpatients with a nonnarcotic and easy-to-administer alternative to commonly prescribed opioids. What Is Sprix? Sprix™ (ketorolac nasal spray) is a prescription medication approved to treat moderate to moderately severe pain for up to five days. (Click Sprix Uses for more information, including possible off-label uses.) Who Makes This Medication? Sprix is manufactured by Roxro Pharma, Inc. How Does Sprix Work? Sprix belongs to a group of medications called nonsteroidal anti-inflammatory drugs (NSAIDs). Like other NSAIDs, Sprix is thought to work by blocking the production of certain hormones that cause pain and inflammation in the body. These hormones are called prostaglandins. By blocking prostaglandins, Sprix helps to alleviate pain. Clinical Effects of Sprix Clinical studies have shown that Sprix can reduce pain from major surgery. In one study, people who were given Sprix experienced less intense pain in the two days after surgery, compared to those who received a placebo (a "sugar pill" that does not contain any active ingredients). The people who were given Sprix also used 36 percent less morphine, a strong opioid pain medicine, than those who received the placebo pill. When and How to Use It Some general considerations include the following: This medication comes in the form of a nasal spray. It is sprayed into the nostrils, usually every six to eight hours. Your healthcare provider will tell you how many sprays to use for each dose. You must activate the pump before using each Sprix bottle for the first time. Do this by holding the bottle away from your body, and pressing down on the flange five times. It is important to learn exactly how to use Sprix. Using a nasal spray is not always easy. Make sure to read the instruction guide that comes with the medication, and ask your healthcare provider or pharmacist if you have any questions. Sprix bottles do not contain preservatives. Therefore, it is important that you throw away each bottle within 24 hours after your first dose, even if there is medicine still left in the bottle. Do not use Sprix for more than five days in a row. Using this medicine for more than five days will increase your risk for serious side effects. You can take Sprix with food or on an empty stomach. If it bothers your stomach, try taking it with food. Make sure to drink plenty of fluids while you are using Sprix. You might want to take a sip of water after using this medication to reduce the chance of getting an irritated throat. For the medication to work properly, it must be used as prescribed. Dosing Information The dose of Sprix your healthcare provider recommends will vary, depending on a number of factors, including: Your age Your weight Whether you have kidney disease. As is always the case, do not adjust your dose unless your healthcare provider specifically tells you to do so. Side Effects of Sprix Just like any medicine, Sprix can cause side effects. However, not everyone who uses the medicine will have problems. In fact, most people tolerate it quite well. Some of the most common side effects of Sprix include but are not limited to: Nasal pain and discomfort Eye tearing Stuffy or runny nose Throat irritation. If reactions do occur, in most cases, they are minor and either require no treatment or are treated easily by you or your healthcare provider. Serious side effects are less common. (Click Sprix Side Effects to learn more, including potentially serious side effects that you should report immediately to your healthcare provider.) Drug Interactions Sprix can potentially interact with a number of other medicines (see Sprix Drug Interactions). Important Information for Your Healthcare Provider You should talk with your healthcare provider prior to using this medication if you have: Asthma Congestive heart failure or other heart or circulatory problems High blood pressure (hypertension) or are taking medication to treat high blood pressure Liver disease, such as hepatitis, cirrhosis, or liver failure Kidney disease or kidney failure Dehydration, which occurs when you lose a large amount of fluids, such as when you experience vomiting or diarrhea Bleeding problems, or are taking medicine that decreases your blood's ability to clot Inflammatory bowel disease, such as ulcerative colitis or Crohn's disease, or a history of these conditions Stomach ulcers, stomach bleeding, or a history of these conditions An allergic reaction to aspirin, another NSAID, or ethylenediaminetetraacetic acid (EDTA) Plans for surgery A pattern of frequent alcohol use or currently smoke Any allergies, including allergies to foods, dyes, or preservatives. Also, let your healthcare provider know if you are: Pregnant or thinking of becoming pregnant (see Sprix and Pregnancy) Breastfeeding (see Sprix and Breastfeeding). Make sure to tell your healthcare provider about any other medications you are taking, including prescription and nonprescription medicines, any other NSAIDs, vitamins, and herbal supplements. What If I Take an Overdose? People who use too much Sprix may experience symptoms that could include but are not limited to: Nausea Vomiting Abdominal (stomach) pain Stomach or intestinal bleeding Excessive sleepiness or drowsiness Kidney failure Excessive rapid or deep breathing (hyperventilation) Increased blood pressure (hypertension) Coma. How Should Sprix Be Stored? Unopened Sprix bottles should be stored upright, in a cool, dry location, such as the refrigerator. Do not let the bottles become frozen. During use, Sprix can be stored at room temperature, out of direct sunlight. Keep this and all other medications out of the reach of children. What Should I Do If I Miss a Dose? If you forget to take your Sprix dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose or use two doses within six hours. Available Strengths Sprix nasal spray only comes in one form and strength -- Sprix 15.75 mg in each spray. There are eight sprays in each Sprix bottle.