美国FDA批准布洛芬静脉注射液（ibuprofen，Caldolor）上市，是首个治疗疼痛和发热的布洛芬静脉注射新制剂。本品剂量规格：布洛芬100 mg/mL，4 mL/瓶、8 mL/瓶。

中文名：布洛芬

通用名：ibuprofen

国外商品名：Caldolor

性状描述：白色结晶性粉末。熔点75-77℃。不溶于水，易溶于乙醇、氯仿、乙醚、丙酮。有异臭，无味。在氢氧化钠或碳酸钠试液中易溶。

剂型：注射液
CALDOLOR（布洛芬）注射液
[坎伯兰制药公司]

初始美国批准：1974

心血管风险
非甾体抗炎药（NSAIDs）可能会增加严重心血管血栓事件，心肌梗死和中风，这可能是致命的危险。风险可能会增加使用的持续时间。
Caldolor是禁忌的围手术期的冠状动脉搭桥术（CABG）手术治疗疼痛的设置。
胃肠道风险
NSAIDs的增加严重胃肠道（GI），包括出血，溃疡，胃或肠穿孔，可致命的不良事件的风险。事件可以发生在任何时候不经警告症状。老年患者面临更大的风险。
 
适应症
Caldolor是为成人表示有类固醇消炎药：

管理的轻度至中度疼痛
管理适度作为阿片类镇痛药辅助剧烈疼痛
发热减少
 
剂量和用法
疼痛：400毫克至800毫克必要时超过30分钟每6小时静脉注射。 （2.1）
热：400毫克静脉注射超过30分钟，由400毫克，每4至6小时或100-200毫克，必要时每4个小时之后。
患者必须有充分的水合前Caldolor管理。
Caldolor给药前必须稀释。
 
剂型和规格
样品瓶：400毫克/ 4毫升或800毫克/ 8毫升
 
禁忌
已知过敏或其他NSAIDs布洛芬
哮喘，荨麻疹​​，或在服用阿司匹林或其他NSAIDs过敏型反应
期间，在冠状动脉搭桥术（CABG）手术设置围手术期使用.

警告和注意事项
严重和可能致命的CV血栓事件：使用尽可能短的时间最低的Caldolor有效剂量。 
严重和可能致命的胃肠道反应：使用尽可能短的时间最低的Caldolor有效剂量。谨慎使用与溃疡病或胃肠道出血病史的患者。
肝效果：范围从转氨酶升高肝功能衰竭。如有异常立即停止Caldolor肝功能持续或恶化。 
高血压：可发生与类固醇消炎药治疗。密切监测血压在与Caldolor治疗。
充血性心力衰竭及水肿：液体潴留和水肿可发生类固醇消炎药治疗。使用与水肿或心脏衰竭患者慎用Caldolor。
肾功能的影响：长期NSAIDs的管理可能导致肾乳头坏死等肾脏损伤。使用与患者慎用的风险（例如，老年人，肾功能不全，心功能衰竭，肝损害，服用利尿剂或ACE抑制剂者）Caldolor。 
过敏性反应：可能发生在与阿司匹林黑社会或在没有事先接触Caldolor患者。立即停止Caldolor如果发生过敏性反应。
严重的皮肤反应：包括剥脱性皮炎，史蒂文斯 - 约翰逊综合征和中毒性表皮坏死松解症，这可能是致命的。停止Caldolor如果局部皮肤反应的发生皮疹或其他迹象。
不良反应
最常见的不良反应有恶心，胀气，呕吐，头痛，出血和头晕（> 5％）。
药物相互作用
ACE抑制剂：NSAIDs的可能减少了ACE抑制剂的降压作用。
阿司匹林：布洛芬和阿司匹林同时服用一般不推荐，因为增加的不利影响的可能性。 
 
特殊族群使用
怀孕：避免在30周妊娠的使用，因为过早的动脉导管闭合的胎儿可能发生。 
哺乳母亲：谨慎使用，因为它不知道，如果布洛芬在人乳中排出。
儿童用药：安全性和有效性的患者不小于17岁的建立。

修订：06/2009

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！

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原产地英文商品名:
CALDOLOR 800mg/8ml/vial 25vials/box
原产地英文药品名:
IBUPROFEN
中文参考商品译名:
CALDOLOR 800毫克/8毫升/瓶 25瓶/盒
中文参考药品译名:
布洛芬
生产厂家中文参考译名:
美国Cumberland制药公司
生产厂家英文名:
Cumberland Pharmaceuticals Inc（USA）
---------------------------------------------------------------
原产地英文商品名:
CALDOLOR 400mg/4ml/vial 25vials/box
原产地英文药品名:
IBUPROFEN
中文参考商品译名:
CALDOLOR 400毫克/4毫升/瓶 25瓶/盒
中文参考药品译名:
布洛芬
生产厂家中文参考译名:
美国Cumberland制药公司
生产厂家英文名
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美国FDA批准布洛芬静脉注射液上市

布洛芬静脉注射液（ibuprofen，Caldolor）由 Cumberland公司研制，已在美国FDA批准布上市，为首个治疗疼痛和发热的布洛芬静脉注射新制剂。本品剂量规格：布洛芬100 mg/mL，4 mL/瓶、8 mL/瓶。   Cumberland公司负责人称，布洛芬静脉注射液（Caldolor）是获得FDA批准在美国市场销售，用于治疗疼痛和发烧的第一种注射剂，无论对该公司的产品线还是对目前市场上的止痛产品来说都是一个有力的补充。

Cumberland公司曾获得FDA的优先审批权。布洛芬静脉注射液可用于治疗中-重度疼痛，也可作为辅助药物与阿片类止痛剂联用治疗中-重度疼痛，还可以用于成人患者治疗发烧，但适用人群主要为需要住院治疗，且无法采用口服药物医治的患者。

临床实验结果显示，与安慰剂对照组相比较，发烧患者用药治疗之后，体温显著降低。在用药过程中，未出现严重不良反应。  

布洛芬静脉注射液（Caldolor）主要用于不能口服的住院患者解除疼痛和退热。目前市售减轻疼痛的注射剂仅有阿片类药物吗啡和哌替啶和非甾体消炎药酮咯芬。阿片类药物会造成镇静、恶心、呕吐、认知损伤和抑制呼吸。酮咯芬有增加出血的危险，胃肠道和肾并发症。尽管出现这些不良反应，美国治疗疼痛的注射剂市场2008年仍达约 6.79亿单元。

临床研究显示，布洛芬静脉注射液对14 00例住院患者减轻疼痛和退热安全有效。在Ⅲ期临床研究中，使用Caldolor患者显著减轻术后首个24小时疼痛的强度，同时也显著减少他们使用的吗啡量。临床研究包括病危和非病危发热患者较安慰剂显著降低体温。在这些临床研究中，布洛芬静脉注射液未出现严重不良反应。

FDA官员说道：“注射型布洛芬与其它非甾体抗炎药注射剂是一种有前景的疼痛治疗药。但是现在大多数此类药物都为口服药物。布洛芬注射剂可用于减轻那些不能使用口服产品患者的疼痛与发热症状。”

Caldolor的使用剂量为400mg或800mg，经30分钟以上输注，每隔6小时一次用于急性疼痛；用于退烧时，剂量为400mg经30分钟以上输注，如果需要，每4-6小时再给予400m g，可每4小时给予100-200mg剂量。

Generic Name: ibuprofen
Date of Approval: June 11, 2009
Company: Cumberland Pharmaceuticals

Treatment for: Pain and Fever
Caldolor
FDA Approves Caldolor 
The U.S. Food and Drug Administration has approved Caldolor, the first injectable dosage form of the common pain medication ibuprofen, to treat pain and fever.

"Injectable ibuprofen and other nonsteroidal anti-inflammatory drugs (NSAIDs) are promising pain management options," said Bob Rappaport, M.D., director, Division of Anesthesia, Analgesia and Rheumatology Drug Products in the FDA's Center for Drug Evaluation and Research. "But until now there were only oral forms of most NSAIDs. An injectable ibuprofen product can provide patients with relief from pain and fever when they cannot take oral products."

Caldolor will be available for hospital use only. It is approved to be administered in 400 mg to 800 mg doses, over 30 minutes, every 6 hours for acute pain. To treat fever, the drug is approved in a 400 mg dose administered over 30 minutes, followed by 400 mg every 4 to 6 hours, or 100-200 mg every 4 hours, as necessary.

In a clinical trial of 319 women who had undergone an elective abdominal hysterectomy, patients were less likely to request morphine for pain on an as-needed basis when administered Caldolor.

Caldolor should be used with caution in patients with congestive heart failure, kidney impairment, at risk of blood clots and those who have a prior history of ulcers or gastrointestinal bleeding. When used in such patients, attention to using the lowest effective dose for the shortest time period is important to reduce the risk of serious adverse events. The drug has also been associated with high blood pressure, serious skin reactions, and serious allergic reactions.

The most common adverse reactions reported in the controlled clinical trials were nausea, flatulence, vomiting, and headache.

Caldolor is manufactured by Cumberland Pharmaceuticals Inc., Nashville, Tenn

Source: FDA

Highlights of Caldolor Prescribing Information
These highlights do not include all the information needed to use Caldolor safely and effectively. See full prescribing information for Caldolor.

WARNING: RISK OF SERIOUS CARDIOVASCULAR AND GASTROINTESTINAL EVENTS

See full prescribing information for complete boxed warning

Cardiovascular Risk

Non-steroidal anti-inflammatory drugs (NSAIDs) may increase the risk of serious cardiovascular (CV) thrombotic events, myocardial infarction, and stroke, which can be fatal. Risk may increase with duration of use.
Caldolor is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery.
Gastrointestinal Risk

NSAIDs increase the risk of serious gastrointestinal (GI) adverse events including bleeding, ulceration, and perforation of the stomach or intestines, which can be fatal. Events can occur at any time without warning symptoms. Elderly patients are at greater risk.
Caldolor Indications and Usage
Caldolor is an NSAID indicated in adults for the:

Management of mild to moderate pain
Management of moderate to severe pain as an adjunct to opioid analgesics
Reduction of fever
Dosage and Administration
Pain: 400 mg to 800 mg intravenously over 30 minutes every 6 hours as necessary.
Fever: 400 mg intravenously over 30 minutes, followed by 400 mg every 4 to 6 hours or 100-200 mg every 4 hours as necessary.
Patients must be well hydrated before Caldolor administration.
Caldolor must be diluted before administration.
Dosage Forms and Strengths
Vials: 400 mg/4 mL or 800 mg/8 mL

Contraindications
Known hypersensitivity to ibuprofen or other NSAIDS
Asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs
Use during the peri-operative period in the setting of coronary artery bypass graft (CABG) surgery
Warnings and Precautions
Serious and potentially fatal CV thrombotic events: Use lowest effective dose of Caldolor for shortest possible duration.
Serious and potentially fatal GI reactions: Use lowest effective dose of Caldolor for shortest possible duration. Use with caution in patients with prior history of ulcer disease or GI bleeding.
Hepatic effects: Range from transaminase elevations to liver failure. Discontinue Caldolor immediately if abnormal liver tests persist or worsen.
Hypertension: Can occur with NSAID treatment. Monitor blood pressure closely during treatment with Caldolor.
Congestive heart failure and edema: Fluid retention and edema can occur with NSAID treatment. Use Caldolor with caution in patients with fluid retention or heart failure.
Renal effects: Long-term administration of NSAIDs can result in renal papillary necrosis and other renal injury. Use Caldolor with caution in patients at risk (e.g., the elderly, those with renal impairment, heart failure, liver impairment, and those taking diuretics or ACE inhibitors.
Anaphylactoid reactions: May occur in patients with the aspirin triad or in patients without prior exposure to Caldolor. Discontinue Caldolor immediately if an anaphylactoid reaction occurs.
Serious skin reactions: Include exfoliative dermatitis, Stevens-Johnson Syndrome, and toxic epidermal necrolysis, which can be fatal. Discontinue Caldolor if rash or other signs of local skin reaction occur.
Caldolor Adverse Reactions
The most common adverse reactions are nausea, flatulence, vomiting, headache, hemorrhage and dizziness (>5%). (6.1) To report SUSPECTED ADVERSE REACTIONS, contact Cumberland Pharmaceuticals Inc. at 1-877-484-2700 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Drug Interactions
ACE-inhibitors: NSAIDs may diminish the antihypertensive effect of ACE-inhibitors.
Aspirin: Concomitant administration of ibuprofen and aspirin is not generally recommended because of the potential for increased adverse effects.
Use in Specific Populations
Pregnancy: Avoid use after 30 weeks gestation because premature closure of the ductus arteriosus in the fetus may occur.
Nursing Mothers: Use with caution as it is not known if ibuprofen is excreted in human milk.
Pediatric Use: Safety and effectiveness not established in patients less than 17 years of age.
Patient Counseling Information
Patients should be informed of the following information before initiating therapy with an NSAID.

Cardiovascular Effects Ibuprofen, like other NSAIDs, may cause serious CV events such as myocardial infarction or stroke, which may result in hospitalization and even death. Although serious CV events can occur without warning symptoms, advise patients to be alert for the signs and symptoms of chest pain, shortness of breath, weakness, and slurring of speech, and to ask for medical advice when observing any indicative sign or symptoms.
Gastrointestinal Effects Ibuprofen, like other NSAIDs, can cause GI discomfort and, rarely, serious GI side effects such as ulcers and bleeding, which may result in hospitalization and even death. Although serious GI tract ulcerations and bleeding can occur without warning symptoms, advise patients to be alert for the signs and symptoms of ulcerations and bleeding, and to ask for medical advice when observing any indicative signs or symptoms including epigastric pain, dyspepsia, melena, and hematemesis.
Hepatotoxicity Inform patients of the warning signs and symptoms of hepatotoxicity (e.g., nausea, fatigue, lethargy, pruritus, jaundice, right upper quadrant tenderness, and "flulike" symptoms). Instruct patients to stop therapy with Caldolor and seek immediate medical therapy if any of these occur.
Adverse Skin Reactions Ibuprofen, like other NSAIDs, can cause serious skin side effects such as exfoliative dermatitis, SJS and TEN, which may result in hospitalization and even death. Although serious skin reactions may occur without warning, advise patients to be alert for the signs and symptoms of skin rash and blisters, fever, or other signs of hypersensitivity such as itching, and to ask for medical advice when observing any indicative sign or symptoms. Advise patients to stop Caldolor immediately if they develop any type of rash, and to contact a physician as soon as possible.
Weight Gain and Edema Advise patients to promptly report to their physicians signs or symptoms of unexplained weight gain or edema during treatment with Caldolor.
Anaphylactoid Reactions Inform patients of the signs of an anaphylactoid reaction (e.g. difficulty in breathing, swelling of the face or throat). If these occur, therapy should be discontinued and medical therapy initiated.
Effects During Pregnancy Starting at 30 weeks gestation, Caldolor and other NSAIDs should be avoided by pregnant women as premature closure of the ductus arteriosus in the fetus may occur.