头孢他洛林酯(ceftaroline fosamil,商品名：Teflaro)是一种新的注射用头孢类抗生素，2010年10月29日经美国FDA批准,该药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软组织感染(ABSSSI),包括耐甲氧西林金黄色葡萄球菌(MRSA)所致感染。这两种适应症都属于严重并可能威胁生命的感染,尤其是社区获得性肺炎发病率和死亡率都较高。 头孢他洛林酯由日本武田制药公司开发,美国Forest Laboratories获得市场授权。头孢洛林是第五代头孢菌素，临床III期实验显示其对于MRSA具有强大的抗菌活性，对照实验显示在对于MRSA的治疗中，头孢洛林与万古霉素和氨曲南合用的治疗效果没有显著的差异。在对于小区获得性肺炎的治疗中，头孢洛林也与头孢曲松的治疗效果相当，也没有显示更多的副作用。头孢洛林还可以有效的与PBP-2a结合，这种蛋白通常由MRSA产生而且不易与现在临床广泛使用的β-内酰胺类抗生素结合。因此，头孢洛林对于MRSA具有有效的抗菌活性，优于其它β-内酰胺类抗生素。 Teflaro(taroline fosamil)注射剂使用说明 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 【药品名】头孢洛林酯（ceftaroline fosamil） 【商品名】Teflaro 【分子式】C22H21N8O8PS4.C2H4O2.H2O 【分子量】762.75 【作用机制】Ceftaroline是一种抗菌药[见临床药理学]。 【剂型及规格】 无菌粉针剂，规格：400mg、600mg。 【适应症】 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)。 【用法用量】 静脉滴注，大于的18岁的患者每次600mg，每12小时一次，于一小时内滴注完成。肾功能不全患者的使用剂量详见说明书。 Teflaro (Ceftaroline Fosamil Injection for Intravenous (IV) Use) INDICATIONS AND USAGE TEFLARO is indicated 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. TEFLARO is also indicated 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. 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 and anaphylactoid reactions have 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 antibacterials. Before therapy with TEFLARO is instituted, careful inquiry about previous hypersensitivity reactions to other cephalosporins, penicillins, or carbapenems should be made. If this product is to be given to a penicillin- or other beta-lactam-allergic patient, caution should be exercised because cross sensitivity among beta-lactam antibacterial agents has been clearly established. If an allergic reaction to TEFLARO occurs, the drug should be discontinued. Serious acute hypersensitivity (anaphylactic) reactions require emergency treatment with epinephrine and other emergency measures that may include airway management, oxygen, intravenous fluids, antihistamines, corticosteroids, and vasopressors as clinically indicated. 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 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 Phase 3 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 the four pooled Phase 3 clinical trials, serious adverse events 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 events 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 events 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. No adverse reactions occurred in greater than 5% of patients receiving TEFLARO. The most common adverse reactions occurring in >2% of patients receiving TEFLARO in the pooled Phase 3 clinical trials were diarrhea, nausea, and rash. 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 TEFLARO has not been studied in pregnant women. Therefore, TEFLARO should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. It is not known whether ceftaroline is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when TEFLARO is administered to a nursing woman. Safety and effectiveness in pediatric patients have not been established. 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 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). The pharmacokinetics of ceftaroline in patients with hepatic impairment have not been established. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=3ecde48b-75a2-4beb-9999-369f3f61bb8a --------------------------------------------------------------- 注：以下产品不同的规格和不同的价格，请以咨询为准！ --------------------------------------------------------------- 产地国家：美国 原产地英文商品名: TEFLARO 400mg/20ml/vial 10vials/box 原产地英文药品名: CEFTAROLINE FOSAMIL ACETATE 中文参考商品译名: TEFLARO 400毫克/20毫升/瓶 10瓶/盒 中文参考药品译名: 醋酸头孢洛林酯 生产厂家中文参考译名: CEREXA 生产厂家英文名: CEREXA ------------------------------------------------------------------- 产地国家：美国 原产地英文商品名: TEFLARO 600mg/20ml/vial 10vials/box 原产地英文药品名: CEFTAROLINE FOSAMIL ACETATE 中文参考商品译名: TEFLARO 600毫克/20毫升/瓶 10瓶/盒 中文参考药品译名: 醋酸头孢洛林酯 生产厂家中文参考译名: CEREXA 生产厂家英文名: CEREXA ------------------------------------------------------------------ 产地国家：美国 原产地英文商品名: TEFLARO 600mg/20ml/vial 原产地英文药品名: CEFTAROLINE FOSAMIL ACETATE 中文参考商品译名: TEFLARO 600毫克/20毫升/瓶 中文参考药品译名: 醋酸头孢洛林酯 生产厂家中文参考译名: CEREXA 生产厂家英文名: CEREXA ------------------------------------------------------------------ 产地国家：美国 原产地英文商品名: TEFLARO 400mg/20ml/vial 原产地英文药品名: CEFTAROLINE FOSAMIL ACETATE 中文参考商品译名: TEFLARO 400毫克/20毫升/瓶 中文参考药品译名: 醋酸头孢洛林酯 生产厂家中文参考译名: CEREXA 生产厂家英文名: CEREXA