AZTREONAM(AZACTAM)氨曲南干粉剂 【中文品名】氨曲南 【药效类别】抗生素类>单环β-内酰胺类 【通用药名】AZTREONAM 【别 名】Azactam, Azthreonam, Dynabiotic, Monobactam, Primbactam, SQ-26776, Urobactam 【化学名称】 Propanoic acid, 2-[[(Z)-[1-(2-amino-4-thiazolyl)-2-[[(2S,3S)-2-methyl-4-oxo-1-sulfo-3-azetidinyl]amino]-2-oxoethylidene]-amino]oxy]-2-methyl- 【CA登记号】[78110-38-0] 【结 构 式】 【分 子 式】C13H18N5O8S2 【功能作用】 抗菌谱主要包括革兰阴性菌,诸如大肠杆菌、克雷白杆菌、沙雷杆菌、奇异变形杆菌、吲哚阳性变形杆菌、枸橼酸杆菌、流感嗜血杆菌、绿脓杆菌及其他假单胞菌、某些肠杆菌属、淋球菌等。 与头孢他定、庆大霉素相比、对产气杆菌、阴沟肠杆菌的作用高于头孢他定,但低于庆大霉素;对绿脓杆菌的作用低于头孢他定、与庆大霉素相近;对于质粒传导的β-内酰胺酶,本品较第3代头孢菌素为稳定。 口服不吸收,肌注1g,1小时血浓度达峰值,约为46μg/ml,t1/2约1.8小时;静注1g,5分钟血药浓度约为125μg/ml,1小时约为49μg/ml,t1/2约1.6小时。 体内分布较广,在脓疱液、心包液、胸水、滑膜液、胆汁、骨组织、肾、肺、皮肤等部位有较高浓度;在前列腺、子宫肌肉、支气管分泌物中也有一定浓度、在脑脊液中浓度低。主要由尿排泄,在尿中原形药物的浓度甚高。在乳汁中的浓度甚低,为血药浓度的1%,平均0.3μg/ml,1日间母乳内总量约0.3mg。 主要用于敏感的革兰阴性留所致的感染、包括肺炎、胸膜炎、腹腔感染、胆道感染、骨和关节感染、皮肤和软组织炎症,尤适用于尿路感染,也用于败血症。由于本品有较好的耐酸性能,因此,当微生物对青霉素类、头孢菌素类、氨基糖苷类等药物不敏感时,应用本品常可有效。 【用法用量】 一般感染:3~4g/d,分2~3次给予。严重感染:1次2g,1日3~4次。无其他合并症的尿路感染:只需用1g,分成1~2次给予。肌注:药物每1g,加液3~4ml溶解。静注:药物每1g,加液10ml溶解,缓慢推注。静滴:药物1g,加液50ml以上溶解(浓度不超过2%),滴注时间20~60分。 注射时,下列药液可用作本品的溶解-稀释液:灭菌注射用水、等渗氯化钠注射液、林格液、乳酸钠林格液、5%~10%葡萄糖液、葡萄糖氯化钠注射液等。用于肌注时,还可用含苯甲醇的氯化钠注射液作溶剂。 【注意事项】 (1)本品与青霉素类之间不存在交叉过敏反应,但对于青霉素过敏者及过敏体质者仍须慎用。 (2)本品对肝脏毒性不大,但对肝功能已受损的病人应观察其动态变化。 (3)不良反应有皮肤症状、如皮疹、紫癜、瘙痒等(共约2%);消化道症状,如腹泻、恶心、呕吐、味觉改变、黄疸以及药物性肝炎(共约2%);局部刺激症状,如血栓性静脉炎。注射部位肿胀(共约2.4%);其他尚有神经系统症状、阴道炎、口腔损害、乏力、眩晕、出血等。 Aztreonam (trade name Azactam) is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum. It was approved by the U.S. Food and Drug Administration (FDA) in 1986. It is resistant to some beta-lactamases, but is inactivated by extended-spectrum beta-lactamases. ------------------------------------------------------------------------------------------ Contents 1 Mechanism of action;Indicationsandspectrumofactivity;3Administration;4Common ;adverse effects;5 References;6 External links ------------------------------------------------------------------------------------------ Mechanism of action Aztreonam is similar in action to penicillin. It inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidoglycan crosslinking. It has a very high affinity for penicillin-binding protein 3 (PBP-3) and mild affinity for PBP-1a. Aztreonam binds the penicillin-binding proteins of gram-positive and anaerobic bacteria very poorly and is largely ineffective against them.[1] Aztreonam is bactericidal but less so than some of the cephalosporins. ------------------------------------------------------------------------------------------ Indications and spectrum of activity Aztreonam has strong activity against susceptible gram-negative bacteria, including Pseudomonas aeruginosa. It has no useful activity against gram-positive bacteria or anaerobes. It is known to be effective against a wide range of bacteria including Citrobacter, Enterobacter, E coli, Haemophilus, Klebsiella, Proteus, and Serratia species. Synergism between aztreonam and arbekacin or tobramycin against Pseudomonas aeruginosa has been suggested. Aztreonam is often used in patients who are penicillin allergic or who can not tolerate aminoglycosides ------------------------------------------------------------------------------------------ Administration Aztreonam must be administered intravenously, as the compound is poorly absorbed when given via the oral route. Phase III trials took place to measure its delivery in inhaled form, using an ultrasonic nebulizer. In the United States the FDA approved Cayston, Aztreonam for inhalation, on February 22, 2010 for the suppression of Pseudomonas aeruginosa infections in patients with cystic fibrosis.[4] Cayston received conditional approval for administration in Canada and the European Union September 2009,[4] and has been fully approved in Australia. ------------------------------------------------------------------------------------------ Common adverse effects Reported side-effects include injection site reactions, rash, and rarely toxic epidermal necrolysis. Gastrointestinal side effects generally include diarrhea and nausea and vomiting. There may be drug-induced eosinophilia. There is limited cross-reactivity between aztreonam and other beta-lactam antibiotics, and it is generally considered safe to admininister aztreonam to patients with hypersensitivity (allergies) to penicillins. Aztreonam is considered Pregnancy category B.
アザクタム注射用0.5g/アザクタム注射用1g
商標名 Azactam 一 般 名 アズトレオナム (Aztreonam) 化 学 名 2‐{(Z )‐(2‐Aminothiazol‐4‐yl)‐[(2S,3S )‐2‐methyl‐4‐oxo‐1‐sulfoazetidin‐3‐ylcarbamoyl]methyleneaminooxy}‐2‐methyl‐1‐propanoic acid 略 号 AZT 分 子 式 C13H17N5O8S2 分 子 量 435.43 構 造 式
性 状 アズトレオナムは、白色~帯黄白色の結晶性の粉末である。本品はジメチルスルホキシドに溶けやすく、水又はメタノールに溶けにくく、エタノール(95)に極めて溶けにくい。 包装 注射用アズトレオナム アザクタム注射用0.5g:10バイアル 注射用アズトレオナム アザクタム注射用1g:10バイアル 製造販売元 エーザイ株式会社 注:卫材产品请参照原资料:http://www.info.pmda.go.jp/go/pack/6122400D1028_1_12/6122400D1028_1_12?view=body -------------------------------------------------------------------------------- 注:以下产品是德国和日本产品,不同规格和不同价格,购买以咨询为准! --------------------------------------------------------------------------------- 产地国家: 德国 原产地英文商品名: AZACTAM POWDER 5g/vial 原产地英文药品名: AZTREONAM 中文参考商品译名: AZACTAM干粉剂 5克/瓶 中文参考药品译名: 氨曲南 生产厂家中文参考译名: 百时美施贵宝 生产厂家英文名: BRISTOL MYERS SQUIBB ------------------------------------------------------------ 产地国家: 德国 原产地英文商品名: AZACTAM POWDER 5g/vial 原产地英文药品名: AZTREONAM 中文参考商品译名: AZACTAM干粉剂 5克/瓶 中文参考药品译名: 氨曲南 生产厂家中文参考译名: 百时美施贵宝 生产厂家英文名: BRISTOL MYERS SQUIBB ------------------------------------------------------------ 产地国家: 日本 原产地英文商品名: AZACTAM POWDER(アザクタム注射用)0.5g/vial 10vials/box 原产地英文药品名: AZTREONAM 中文参考商品译名: AZACTAM干粉剂(アザクタム注射用)0.5克/瓶 10瓶/盒 中文参考药品译名: 氨曲南 生产厂家中文参考译名: 卫材 生产厂家英文名: Eisai Co., Ltd.
------------------------------------------------------------ 产地国家: 日本 原产地英文商品名: AZACTAM POWDER(アザクタム注射用)1g/vial 10vials/box 原产地英文药品名: AZTREONAM 中文参考商品译名: AZACTAM干粉剂(アザクタム注射用)1克/瓶 10瓶/盒 中文参考药品译名: 氨曲南 生产厂家中文参考译名: 卫材 生产厂家英文名: Eisai Co., Ltd.
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