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注射用头孢洛林酯|Teflaro (ceftaroline fosamil)

2011-03-18 13:50:16 作者：新特药房来源：中国新特药网天津分站浏览次数：730 文字大小：【大】【中】【小】

简介： 制造商：森林实验室药理分类：抗生素（头孢菌素）。活性成分（补）： Ceftaroline fosamil 400mg/vial，600mg/vial;为重组后静脉输注粉指示（补）：易受细菌社区获得性肺炎和急性皮肤和皮肤结 ...

关键字：注射用头孢洛林酯

制造商：
森林实验室

药理分类：
抗生素（头孢菌素）。

活性成分（补）：
Ceftaroline fosamil 400mg/vial，600mg/vial;为重组后静脉输注粉
指示（补）：
易受细菌社区获得性肺炎和急性皮肤和皮肤结构感染。

药理作用：
Ceftaroline，一种广谱半合成头孢菌素的静脉注射，适应症是用于治疗急性细菌性皮肤和皮肤结构感染金黄色葡萄球菌（包括耐甲氧西林和甲氧西林敏感株），化脓性链球菌，无乳链球菌，大肠杆菌引起的大肠杆菌，肺炎克雷伯菌和K. oxytoca。它也用于治疗社区获得性肺炎的肺炎链球菌（包括并发菌血症的个案），金黄色葡萄球菌（甲氧西林敏感株只），流感嗜血杆菌，肺炎克雷伯菌，光oxytoca引起的，大肠杆菌。

Ceftaroline是积极对两克（ - ）和克（+）菌。它的行为有约束力的基本青霉素结合蛋白。这不是对革兰氏活动（ - ）细菌产生广谱β-内酰胺酶。有些菌株对其他头孢菌素耐药可能受到ceftaroline。

在静脉输注，ceftaroline fosamil转换由血浆中磷酸的生物活性形式，ceftaroline。这是不是细胞色素P450酶系统底物，因此不会调整剂量，肝功能不全必要的，而且由于药物的相互作用与代谢酶的干扰问题是不太可能。无论是活性药物及其代谢产物的消除由肾小球滤过肾脏，因此，对肾功能的评估是适当的剂量至关重要。

临床试验：
两项研究涉及1396年与复杂性皮肤和皮肤结构感染的成年人进行了比较ceftaroline对万古霉素加氨曲南。进行了分析，在797例病灶≥75平方厘米，要么主要脓肿，伤口感染，或深/广泛蜂窝组织炎。分析评价急救员对两个病灶蔓延和第3天出现发烧的情况下停止成就利率计算。在一次审判中，有反应的人数为148 200 ceftaroline，万古霉素和氨曲南+ 209 135。在其他审判，为ceftaroline反应人数为200 148再次相比，128的188万古霉素+氨曲南。

两项试验进行了比较ceftaroline对头孢曲松在1231成人社区获得性细菌性肺炎（钙结合蛋白）的治疗。与新的或严重的肺部浸润和标志，并与住院治疗的需要和第四钙结合蛋白症状病人。研究一，二口服克拉霉素剂量（500毫克每12小时），共为辅助的第一天开始治疗的病人。已知或怀疑患者葡萄球菌是从两个试验排除在外。在所有科目谁收到任何研究药量，30天的全因死亡率分别为1.8％，而ceftaroline组和2组的头孢曲松％。

法律分类：
接收

成人：
≥18yrs：给超过1小时的静脉输液。治疗皮肤和皮肤结构的5-14天，连续治疗5 - 7天肺炎。肌酐清除率> 50mL/minutes：600毫克每12小时。肾功能不全（CrCl为“30 - ≤50mL/min）：400毫克每12小时;（CrCl为≥15 - ≤30mL/min）：300毫克每12小时，终末期肾病（包括血液透析）：200毫克每12小时（天透析后透析剂量）。

儿童：
“18yrs：不推荐。

警告/注意事项：
青霉素或其他过敏。胃肠道疾病（特别是结肠炎）。妊娠（Cat.B）。哺乳的母亲。

不良反应（补）：
胃肠不适，皮疹，（+）库姆斯试验（溶血性贫血评估是否发生），伪膜性肠炎，二重感染。

如何提供：
样品瓶- 1，10

第五代”头孢菌素类抗生素头孢洛林酯获FDA批准全球首次上市

2010年10月29日，Forest Laboratories公司宣布，其“第五代”头孢菌素类抗生素头孢洛林酯（ceftaroline fosamil, 商品名Teflaro）获得美国FDA批准上市，用于治疗CABP(社区获得细菌性肺炎）和ABSSSI（急性细菌性皮肤及皮肤组织感染）,包括耐甲氧西林金黄色葡萄球菌（MRSA）所致感染。

Drug: Teflaro (ceftaroline fosamil)
Indication: Skin infections, bacterial pneumonia
Companies: Forest Laboratories
Approval Date: October 29

Drug type: Small molecule

Manufacturer:

Forest Laboratories

Pharmacological Class:

Antibiotic (cephalosporin).

Active Ingredient(s):

Ceftaroline fosamil 400mg/vial, 600mg/vial; powder for IV infusion after reconstitution.

Indication(s):

Susceptible bacterial community-acquired pneumonia and acute skin and skin structure infections.

Pharmacology:

Ceftaroline, a broad-spectrum semisynthetic cephalosporin for intravenous administration, is indicated for treating acute bacterial skin and skin structure infections caused by S. aureus (both methicillin-resistant and methicillin-susceptible strains), S. pyogenes, S. agalactiae, E. coli, K. pneumoniae, and K. oxytoca. It is also indicated for treating community-acquired pneumonia caused by S. pneumoniae (including cases with concurrent bacteremia), S. aureus (methicillin-susceptible isolates only), H. influenzae, K. pneumoniae, K. oxytoca, and E. coli.

Ceftaroline is active against both gram (–) and gram (+) bacteria. It acts by binding to essential penicillin-binding proteins. It is not active against gram (–) bacteria that produce extended-spectrum beta-lactamases. Some isolates resistant to other cephalosporins may be susceptible to ceftaroline.

During intravenous infusion, ceftaroline fosamil is converted by phosphatase in the plasma to the bioactive form, ceftaroline. It is not a substrate of the CYP450 enzyme system, so dosage adjustments are not necessary in hepatic dysfunction, and drug interactions due to interferences with metabolic enzymes are not likely. Both the active drug and its metabolites are eliminated by the kidneys by glomerular filtration; therefore, an evaluation of renal function is essential for proper dosing.

Clinical Trials:

Two studies involving 1396 adults with complicated skin and skin structure infections were conducted to compare ceftaroline to vancomycin plus aztreonam. An analysis was conducted in 797 patients with lesions ≥75cm² and either major abscess, wound infection, or deep/extensive cellulitis. The analysis evaluated responder rates based on the achievement of both cessation of lesion spread and absence of fever on day 3. In one trial, the number of responders was 148 of 200 for ceftaroline, and 135 of 209 for vancomycin + aztreonam. In the other trial, the number of responders for ceftaroline was again 148 of 200, compared to 128 out of 188 for vancomycin + aztreonam.

Two trials were conducted to compare ceftaroline to ceftriaxone in the treatment of 1231 adults with community-acquired bacterial pneumonia (CABP). Patients with new or progressive pulmonary infiltrates and signs and symptoms of CABP with the need for hospitalization and IV therapy were enrolled. In study 1, two doses of oral clarithromycin (500mg every 12hours) were given to patients as adjunctive therapy starting on the first day. Patients with known or suspected MRSA were excluded from both trials. Among all subjects who received any amount of study drug, the 30-day all-cause mortality rates were 1.8% for the ceftaroline group and 2% for the ceftriaxone group.

Legal Classification:

Adults:

≥18yrs: Give by IV infusion over 1hour. Treat skin and skin structure for 5–14 days; treat pneumonia for 5–7days. CrCl >50mL/minutes: 600mg every 12hours. Renal impairment (CrCl >30–≤50mL/min): 400mg every 12hours; (CrCl ≥15–≤30mL/min): 300mg every 12hours; ESRD (including hemodialysis): 200mg every 12hours (dose after dialysis on dialysis days).