近日，美国FDA批准注射用抗生素ceftaroline fosamil（商品名 Teflaro）用于治疗成人社区获得性细菌性肺炎（CABP）和急性细菌性皮肤和皮肤结构感染（ABSSSI），包括耐甲氧西林金黄色葡萄球菌（MRSA）。
MRSA是一种葡萄球菌，它对某些抗生素耐药。这些抗生素包括甲氧西林和其他许多常用的抗生素，如苯唑西林、青霉素和阿莫西林。社区中，大多数MRSA感染是皮肤感染。而根据美国疾病控制与预防中心统计，严重或潜在威胁生命的MRSA感染最常发生在与卫生保健机构接触的患者中。
“那些严重和潜在威胁生命的感染需要新的治疗方案”，FDA药物评价和研究中心抗菌药物办公室主任考克斯（Edward·Cox）博士说。“FDA正致力于促进新型抗生素药物的发展。
批准日期：2010年10月29日；公司:Forest Laboratories, Inc. 武田制药和Forest Laboratories合作开发
TEFLARO（头孢洛林[ceftaroline fosamil]）注射， 用于静脉注射
美国初步批准：2010年
最近的主要变化
适应症及用法：5/2016 
剂量及管理：5/2016 
警告和注意事项：5/2016
作用机制
头孢洛罗是一种头孢菌素抗菌药物[见微生物学]。 
适用范围及用途
Teflaro®是2月龄以下的成人和儿科患者中指定的头孢菌素抗菌剂，用于治疗由指定的易感细菌引起的以下感染：
急性细菌性皮肤和皮肤结构感染（ABSSSI）。
社区获得性细菌性肺炎（CABP）。
为了减少耐药细菌的发展，保持Teflaro和其他抗菌药物的有效性，Teflaro只能用于治疗被证实或强烈怀疑是由细菌引起的感染。
剂量和管理
18岁以上的成年患者：通过静脉滴注施用5〜60分钟，每12小时600mg。
儿科患者从2岁到<18岁，体重≤33公斤：每8小时12毫克/公斤静脉输注5到60分钟。儿科患者从2岁到<18岁，体重> 33公斤：每8小时400毫克，每12小时600毫克，静脉输注5到60分钟。
2个月至<2岁的儿科患者：静脉输注5〜60分钟，每8小时8 mg / kg。
成人肌酐清除率（CrCl）<50mL/min和终末期肾脏疾病（ESRD）包括血液透析需要调整剂量
对于CrCL <50mL/min/1.73 m2的儿科患者，没有足够的信息推荐给药方案。
使用Cockcroft-Gault公式计算
估计肌酐清除率
（mL/min）Teflaro剂量方案成人
> 50无需调整剂量
> 30至≤50400mg IV（超过5至60分钟）每12小时
每12小时≥15至≤30 300mg IV（超过5至60分钟）
终末期肾病（ESRD），包括每12小时血液透析200mg IV（5-60分钟）
剂量形式和强度
用于注射：在单剂量20 mL小瓶中600毫克或400毫克无菌头孢洛林粉末粉末。构成粉末并进一步稀释用于静脉内注射。
禁忌症
已知对头孢洛林或头孢菌素类的其他成员的严重超敏反应。
警告和注意事项
已经报道了β-内酰胺抗菌药物（包括Teflaro）的严重超敏反应（过敏）反应。如果发生超敏反应，请停止Teflaro。
已经报道了具有几乎所有全身抗菌剂（包括Teflaro）的艰难梭菌相关性腹泻（CDAD）。评估腹泻是否发生。
Teflaro已经报道了直接库姆氏血清学检测。如果在治疗期间或之后发生贫血，应进行药物诱导的溶血性贫血的诊断处理，并考虑停止Teflaro。
不良反应
发生在> 2％的成年患者和≥3％的儿科患者中最常见的不良反应是腹泻，恶心和皮疹。儿童患者≥3％的其他不良反应包括呕吐和发热。
如何提供/存储和处理
600MG 10小瓶/盒  NDC: 00456-0600-10
未经重组的Teflaro小瓶应储存在25ºC（77ºF）; 游览允许为15-30ºC（59-86ºF）[见USP受控室温]。
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3ecde48b-75a2-4beb-9999-369f3f61bb8a
TEFLARO(ceftaroline fosamil) for injection, for intravenous use
Dosing for ABSSSI and CABP in adult patients: Can administer in 5 minutes
600 mg IV (over 5 to 60 minutes) every 12 hours for CABP 5-7 days and for ABSSSI 5-14 days
For patients with CrCl >50 mL/min. Duration of therapy should be guided by the severity and site of infection and the patient’s clinical and bacteriological progress
Patients with renal impairment should receive TEFLARO 5 to 60 minute IV infusion every 12 hours at the following dosages: 
•>50 CrCl† (mL/min): 600 mg
•>30 to ≤50 CrCl† (mL/min): 400 mg
•≥15 to ≤30 CrCl† (mL/min): 300 mg
•End-stage renal disease, including hemodialysis‡: 200 mg§
Creatinine clearance (CrCl) estimated using the Cockcroft-Gault formula.
End-stage renal disease is defined as CrCl <15 mL/min.
TEFLARO is hemodialyzable; thus TEFLARO should be administered after hemodialysis on hemodialysis days.
INDICATIONS AND USAGE
—TEFLARO® (ceftaroline fosamil) is indicated in adult and pediatric patients 2 months of age and older for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible isolates of the following Gram-positive and Gram-negative microorganisms: Staphylococcus aureus (including methicillin-susceptible and ‑resistant isolates), Streptococcus pyogenes, Streptococcus agalactiae, Escherichia coli, Klebsiella pneumoniae, and Klebsiella oxytoca.
TEFLARO is also indicated in adult and pediatric patients 2 months of age and older for the treatment of community-acquired bacterial pneumonia (CABP) caused by susceptible isolates of the following Gram-positive and Gram-negative microorganisms: Streptococcus pneumoniae (including cases with concurrent bacteremia), Staphylococcus aureus (methicillin-susceptible isolates only), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca, and Escherichia coli.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of TEFLARO and other antibacterial drugs, TEFLARO should be used to treat only ABSSSI or CABP that are proven or strongly suspected to be caused by susceptible bacteria. Appropriate specimens for microbiological examination should be obtained in order to isolate and identify the causative pathogens and to determine their susceptibility to ceftaroline. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.
IMPORTANT SAFETY INFORMATION
Contraindications
—TEFLARO is contraindicated in patients with known serious hypersensitivity to ceftaroline or other members of the cephalosporin class. Anaphylaxis has been reported with ceftaroline.
Warnings and Precautions
Hypersensitivity Reactions
—Serious and occasionally fatal hypersensitivity (anaphylactic) reactions and serious skin reactions have been reported with beta-lactam antibacterial drugs. Before therapy with TEFLARO is instituted, careful inquiry about previous hypersensitivity reactions to other cephalosporins, penicillins, or carbapenems should be made. Maintain clinical supervision if this product is to be given to a penicillin- or other beta-lactam-allergic patient, because cross sensitivity among beta-lactam antibacterial agents has been clearly established.
—If an allergic reaction to TEFLARO occurs, discontinue TEFLARO and institute appropriate treatment and supportive measures.
Clostridium difficile-Associated Diarrhea
—Clostridium difficile-Associated Diarrhea (CDAD) has been reported for nearly all systemic antibacterial agents, including TEFLARO, and may range in severity from mild diarrhea to fatal colitis. Careful medical history is necessary because CDAD has been reported to occur more than 2 months after the administration of antibacterial agents. If CDAD is suspected or confirmed, antibacterials not directed against C. difficile should be discontinued, if possible.
Direct Coombs' Test Seroconversion
—In adults, seroconversion from a negative to a positive direct Coombs’ test result occurred in 120/1114 (10.8%) of patients receiving TEFLARO and 49/1116 (4.4%) of patients receiving comparator drugs in the four pooled adult Phase 3 trials.
—In children, seroconversion from a negative to a positive direct Coombs’ test result occurred in 42/234 (17.9%) of patients receiving TEFLARO and 3/93 (3.2%) of patients receiving comparator drugs in the three pooled pediatric trials.
—No adverse reactions representing hemolytic anemia were reported in any treatment group. If anemia develops during or after treatment with TEFLARO, drug-induced hemolytic anemia should be considered. If drug-induced hemolytic anemia is suspected, discontinuation of TEFLARO should be considered and supportive care should be administered to the patient if clinically indicated.
Development of Drug-Resistant Bacteria
— Prescribing TEFLARO in the absence of a proven or strongly suspected bacterial infection is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.
Adverse Reactions in Adults
—In the four pooled adult Phase 3 clinical trials, serious adverse reactions occurred in 98/1300 (7.5%) of patients receiving TEFLARO and 100/1297 (7.7%) of patients receiving comparator drugs. Treatment discontinuation due to adverse reactions occurred in 35/1300 (2.7%) of patients receiving TEFLARO and 48/1297 (3.7%) of patients receiving comparator drugs with the most common adverse reactions leading to discontinuation being hypersensitivity for both treatment groups at a rate of 0.3% in the TEFLARO group and 0.5% in the comparator group.
—The most common adverse reactions occurring in >2% of patients receiving TEFLARO in the adult pooled Phase 3 clinical trials were diarrhea (5%) nausea (4%), and rash (3%).
Adverse Reactions in Pediatrics
—In the three pooled pediatric clinical trials, serious adverse reactions occurred in 10/257 (4%) of patients receiving TEFLARO and 3/102 (3%) of patients receiving comparator drugs. Treatment discontinuation due to adverse reactions occurred in 10/257 (3.9%) of patients receiving TEFLARO and 2/102 (2%) of patients receiving comparator drugs with the most common adverse reaction leading to discontinuation being rash in 2/257 (0.8%) of patients treated with TEFLARO.
—The most common adverse reactions occurring in ≥3% of patients receiving TEFLARO in the pooled pediatric clinical trials were diarrhea (8%), rash (7%), vomiting (5%), pyrexia (3%) and nausea (3%).
Drug Interactions
—No clinical drug-drug interaction studies have been conducted with TEFLARO. There is minimal potential for drug-drug interactions between TEFLARO and CYP450 substrates, inhibitors, or inducers; drugs known to undergo active renal secretion; and drugs that may alter renal blood flow.
Use in Specific Populations
—There have been no adequate and well-controlled studies with TEFLARO in pregnant or nursing women. TEFLARO should only be used if the potential benefit justifies the potential risk in these populations.
—Safety and effectiveness in pediatric patients below the age of 2 months have not been established as no data are available.
—Because elderly patients, those ≥65 years of age, are more likely to have decreased renal function and ceftaroline is excreted primarily by the kidney, care should be taken in dose selection in this age group and it may be useful to monitor renal function. Dosage adjustment for elderly patients should therefore be based on renal function.
—Dosage adjustment is required in adult patients with moderate (CrCl >30 to ≤50 mL/min) or severe (CrCl ≥15 to ≤30 mL/min) renal impairment and in patients with end-stage renal disease (CrCl <15 mL/min). There is insufficient information to recommend a dosage regimen for pediatric patients with CrCl <50 mL/min/1.73m2.