泰比培南小儿用10%细颗粒（Tebipenem pivoxil，オラペネム小児用細粒10％）-是第一个用于肺炎链球菌抗药株感染的治疗 【中文名称】 替比培南酯 【英文名称】 Tebipenem pivoxil 【商品名称】 Orapenem 【C  A  S】 161715-24-8 【分 子 量】 497.63 【分 子 式】 C22H31N3O6S2 【剂型规格】原料＋颗粒剂。0.5g每包 【适 应 症】肺炎、中耳炎、副鼻腔炎 【规    格】颗粒剂10%。 【上市时间】 2009年4月。 【原研厂家】替比培南酯最早由美国辉瑞公司研发，替比培南酯细粒剂由惠氏立达公司原研开发，之后转让给日本明治制果制药公司（2002年3月，范围包括日本在内的15个亚洲国家），2009年4月在日本获得厚生省批准。 【临床药理】 替比培南酯是泰吡培南的前药，对革兰阳性和革兰阴性菌均具有较强的抗菌活性，对金黄色酿脓葡萄球菌、链球菌属、肺炎球菌、粘膜炎莫拉菌( 布兰汉氏球菌属) 、流感菌敏感，对青霉素敏感或耐药肺炎链球菌和流感嗜血菌的疗效较好，用于儿科患者耳鼻喉和上呼吸道感染的治疗，包括持续性中耳炎和细菌性肺炎。 【产品特点】 该产品用于儿科病人耳鼻喉和上呼吸道感染的治疗。它是第一个用于肺炎链球菌抗药株感染的治疗，包括持续性中耳炎和细菌性肺炎的培南类药物。替比培南酯是替比培南的前体药物，口服后被酯酶水解释放出母体药物替比培南，与细菌青霉素结合蛋白（PBP）结合，抑制细菌细胞壁的合成，是目前唯一一个可以口服的碳青霉烯类抗生素。替比培南酯对抗肺炎链球菌、大肠杆菌、肺炎克雷白菌、流感嗜血菌、肺炎军团菌的抑制活性，强于对照药如亚胺培南、头孢地尼、阿莫西林和左氧氟沙星等。 替比培南的结构，特点是在C3位侧链为噻唑基取代的氮杂环丁烷基团，同时通过在C2位羧酸形成匹伏酯形成前药，提高了口服吸收性。本品的口服吸收性优于现在已经上市的大多数β-内酰胺类抗生素。 替比培南抗菌谱广。对大多数临床分离的菌株（除Enterococcus faecium（屎肠球菌）及Pseudomonas aeruginosa（绿脓杆菌）等少部分菌种外），替比培南均表现出比青霉素系列及头孢系列更强的抗菌性，而与其他注射用的碳青霉烯类抗生素相比，替比培南也表现出同程度或更强的抗菌效果。 特别是针对近几年引起儿童感染主要原因的PRSP（耐青霉素肺炎链球菌）、MRSP（耐红霉素肺炎链球菌）及Haemophilus influenzae（流感嗜血杆菌）表现出极强的抗菌效果。 由PRSP（耐青霉素肺炎链球菌）、MRSP（耐红霉素肺炎链球菌）及Haemophilus influenzae（流感嗜血杆菌）所引起的儿童患者包括中耳炎在内的上呼吸道感染及细菌性肺炎，是临床上最常见的儿童感染。由于耐药现象日趋严重，目前临床上常使用的抗生素对于儿童感染的治疗效果已日渐减弱，因此有必要开发新的抗菌效果更强的药物。 オラペネム小児用細粒10％ 治疗类别名称 欧文商標名 ORAPENEM FINE GRANULES 10% FOR PEDIATRIC 性　状 Tebipenemu酯是一种白色结晶性粉末。 该产品可以自由在甲醇和乙腈，乙醇（99.5）稍溶于水，不溶于乙醚和非常易溶于水 一般名 テビペネム　ピボキシル　Tebipenem Pivoxil 略　号 TBPM-PI 化学名 (＋)-hydroxymethyl(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3-{[1-(2-thiazolin-2-yl)-3-azetidinyl]thio}-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate,2-pivalate 分子式 C22H31N3O6S2 分子量 497.63 構造式 融　点 134℃ 分配係数 （１-オクタノール/薄めたMcIlvaine緩衝液） （下表参照） pH3.0  pH4.0  pH5.0  pH6.0  pH7.0  0.0216  0.123  0.977  7.82  64.0 取扱い上の注意 防湿のため、ボトル入製剤は調剤後必ず密栓すること。ボトル入製剤を分包した場合は、湿気を避けて保存すること。また、分包製剤は湿気を避けて保存し、服用時に開封するよう指示すること。 承認条件 使用施設を把握すると共に施設の抽出率、施設数を考慮して以下の対策を講ずること。 1. 適切な製造販売後調査（感受性調査を含む）を継続し、情報を収集すること。 2. 収集した情報を解析し、適正な使用を確保するために医療機関に対し、必要な情報提供を継続すること。 包装规格 含1克在100毫克 瓶：50克，100G 0.5克×120包（2×60连包） Meiji Seika ファルマ株式会社 完整处方资料附件：http://www.info.pmda.go.jp/go/pack/6139002C1026_1_07/ ORAPENEM FINE GRANULES 10% FOR PEDIATRIC（オラペネム小児用細粒10％）  Brand name : ORAPENEM FINE GRANULES 10% FOR PEDIATRIC 　Active ingredient: Tebipenem pivoxil 　Dosage form: yellowish pale red fine granule 　Print on wrapping:  Effects of this medicine This medicine is a carbapenem antibiotic to inhibit bacterial cell wall synthesis, and shows antimicrobial effect. It is usually used to treat pneumonia, otitis media and sinusitis. Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reactions (itch, rash etc.) to any medicines. If you or any of your parents or siblings are prone to allergic symptoms such as bronchial asthma, rash or hives. If you are a patient with renal disorder, poor ingestion or parenteral nutrition, or poor general status. If you have a history of convulsive diseases such as epilepsy. •If you are pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>> •For children: In general, take 0.04 gram per kilogram of body weight (g/kg) (4 mg of the active ingredient [titer]/kg) at a time, twice a day, after meals. The dosage may be increased up to 0.06 g/kg (6 mg [titer]/kg) as needed. Strictly follow the instructions. •Standard duration of administration is for 7 days or less. •If you miss a dose, take a dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose and follow your regular dosing schedule. You should never take two doses at one time. •If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist. •Do not stop taking this medicine unless your doctor instructs you to do so. Precautions while taking this medicine • Possible adverse reactions to this medicine The most commonly reported adverse reactions include diarrhea and loose stool. If any of these symptoms occur, consult with your doctor or pharmacist. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •convulsion, disturbed consciousness [hypoglycemia associated with hypocarnitinemia] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information •Keep out of reach of children. Store away from direct sunlight, heat and moisture. •Discard the remainder. Do not store them. Meiji Seika Pharma Co., Ltd.Internal Revised: 1/2013 The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.