フィニバックス点滴用0.25g／フィニバックスキット点滴用0.25g
多尼培南是由日本盐野义公司研发的β-内酰胺类抗生素,强生公司从日本盐野义公司获得了该药的开发上市权.2005年9月多尼培南首次在日本上市,商品名为Finibax.
【药品名】多尼培南
【英文名】Doripenem，S-4661
【日 文 名】ドリペネム
【商 品 名】フィニバックス
【化学结构式】        
【规格】250mg/支，500mg/支冻干粉针（静脉注射）
【适应症】广谱抗生素，抗细菌感染
【产品简介】
多尼培南（Doripenem，S-4661）为日本盐也义公司开发的碳青酶烯类新广谱抗生素，具有抗菌谱广、对绝大多数β-内酰胺酶稳定的特点。目前本品在日本已完成Ⅲ期临床研究，已于2005年7月25日在日本取得药品生产许可。2003年5月，盐也义公司与Peninsula Pharmaceuticals Inc公司达成协议，Peninsula Pharmaceuticals Inc公司获得本品在北美的市场开发权利。本品已经获得美国 FDA的快速审批待遇，用于治疗医院获得性肺炎，包括呼吸器相关性肺炎（VAP）。 2007年10月15日，美国FDA批准了强生公司的多尼培南 (doripenem，Doribax) 注射剂用于治疗复杂性腹内感染与复杂性尿道感染如肾盂肾炎，规格为500mg。本品对广范的革兰阳性菌与革兰阴性菌都有抗菌作用，包括能引起严重感染的假单胞菌属。     
强生公司从日本盐野义公司获得了该药的开发上市权，多尼培南已于2005年9月在日本上市，商品名为Finibax。
【药理作用特点】
多尼培南的抗菌机理与其他β-内酰胺抗生素相同，通过与细菌青霉素结合蛋白（penicillin binding proteins,PBPs）结合抑制细菌细胞壁合成。本品与S. aureus、 E. coli、 P. aeruginosa 及其他敏感菌PBPs具有极高的亲和力。
多尼培南对绝大多数β-内酰胺酶稳定，包括青霉素酶、头孢菌素酶以及超广谱β-内酰胺酶（ESBLs）。
多尼培南对人脱氢肽酶（DHP-1）稳定，在体内不被DHP-1水解，可单独使用。 多尼培南对厌氧或需氧的革兰氏阳性和革兰氏阴性细菌都有强大的抗菌活性。总体上多尼培南的抗菌活性与伊米培南、美罗培南以及ertapenem相当。但多尼培南对金黄色葡萄球菌、铜绿假单胞菌以及耐青霉素的肺炎链球菌的活性明显强于美罗培南。体外研究显示：多尼培南对耐甲氧西林葡萄球菌和链球菌的活性与伊米培南相当，MIC90值为0.5mg/ml或更低；对肠杆菌、嗜血流感杆菌以及Moraxella catarrhalis菌科细菌具有很高的活性，MIC90值为0.032~0.5mg/ml；对伊米培南耐药Pseudomonas aeruginosa菌也有较好的抗菌作用，MIC90值为8mg/ml，强于meropenem, biapenem, cefpirome, and ceftazidime；多尼培南对ceftazidime-, ciprofloxacin-, and gentamicin耐药菌也有很好的抗菌效果。
多尼培南对临床分离的常见妇科及产科感染细菌有很好的抗菌作用，MIC50和MIC90分别为0.25和1mg/ml，对这些细菌子宫感染的大鼠具有良好的治疗作用，提示多尼培南应用于临床妇科及产科的前景。多尼培南对来自人、犬、猪、豚鼠、大鼠、小鼠以及兔的DHP-1均稳定，动物模型研究显示，小鼠皮下注射多尼培南后可以达到很高的血药水平，对革兰氏阳性以及革兰氏阴性细菌（包括耐药细菌）感染小鼠模型有很好的保护作用。 多尼培南临床研究显示：本品在人体内稳定，不受人DHP-1酶影响，静脉注射125mg的半衰期（t1/2）为0.85h，主要经尿液排除，24h尿中药物回收率为75%，其药代动力学特点与美罗培南相似，不受多剂量给药影响。 250mg~1000mg，每天给药一次、两次或三次，对复杂性尿路感染和慢性呼吸道感染的有效率为93.8%~95.2，细菌清除率为87.5%~98.2%，显示本品良好的抗菌作用。
INDICATIONS AND USAGE
To reduce the development of drug-resistant bacteria and maintain the effectiveness of DORIBAX™ and other antibacterial drugs, DORIBAX™ should be used only to treat infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting and modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.DORIBAX™ (doripenem for injection) is indicated as a single agent for the treatment of complicated intra-abdominal infections caused by Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Bacteroides caccae, Bacteroides fragilis, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus, Streptococcus intermedius, Streptococcus constellatus and Peptostreptococcus micros.Complicated Urinary Tract Infections, Including Pyelonephritis
DORIBAX™ (doripenem for injection) is indicated as a single agent for the treatment of complicated urinary tract infections, including pyelonephritis caused by Escherichia coli including cases with concurrent bacteremia, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, and Acinetobacter baumannii.
DOSAGE AND ADMINISTRATION
Recommended Dosage
The recommended dosage of DORIBAX™ is 500 mg administered every 8 hours by intravenous infusion over one hour in patients ≥18 years of age.
Duration includes a possible switch to an appropriate oral therapy, after at least 3 days of parenteral therapy, once clinical improvement has been demonstrated.
Duration can be extended up to 14 days for patients with concurrent bacteremia.
Storage of Constituted Solutions
Upon constitution with sterile water for injection or 0.9% sodium chloride (normal saline) injection, DORIBAX suspension in the vial may be held for 1-hour prior to transfer and dilution in the infusion bag.
CONTRAINDICATIONS
DORIBAX™ is contraindicated in patients with known serious hypersensitivity to doripenem or to other drugs in the same class or in patients who have demonstrated anaphylactic reactions to beta-lactams.
WARNINGS AND PRECAUTIONS
1 Hypersensitivity Reactions
Serious and occasionally fatal hypersensitivity (anaphylactic) and serious skin reactions have been reported in patients receiving beta-lactam antibiotics. These reactions are more likely to occur in individuals with a history of sensitivity to multiple allergens. Before therapy with DORIBAX™ is instituted, careful inquiry should be made to determine whether the patient has had a previous hypersensitivity reaction to other carbapenems, cephalosporins, penicillins or other allergens. If this product is to be given to a penicillin- or other beta-lactam-allergic patient, caution should be exercised because cross-hyperreactivity among beta-lactam antibiotics has been clearly documented.If an allergic reaction to DORIBAX™ occurs, discontinue the drug. Serious acute hypersensitivity (anaphylactic) reactions require emergency treatment with epinephrine and other emergency measures, including oxygen, IV fluids, IV antihistamines, corticosteroids, pressor amines and airway management, as clinically indicated.
2 Interaction with Valproic Acid
Due to a drug interaction, patients with seizure disorders controlled with valproic acid or sodium valproate will be at an increased risk for breakthrough seizures when treated with DORIBAX™ concomitantly. Reduction in serum valproic acid concentrations to below the therapeutic concentration range (50 to 100 mcg/mL) was observed by 12 hours after the initiation of doripenem in healthy subjects co-administered both drugs. A similar drug interaction involving other carbapenem antibacterials and valproic acid has been described in published case reports. In some of these reports, increasing the dose of valproic acid or sodium valproate did not result in increased valproic acid serum concentrations. Alternative antibacterial therapies should be considered for patients receiving valproic acid or sodium valproate. If administration of DORIBAX™ is necessary, supplemental anti-convulsant therapy should be considered.
3 Clostridium difficile-Associated Diarrhea
Clostridium difficile-associated diarrhea (CDAD) has been reported with nearly all antibacterial agents and may range in severity from mild diarrhea to fatal colitis.Treatment with antibacterial agents alters the normal flora of the colon and may permit overgrowth of C. difficile.C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.
If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile, and surgical eva luation should be instituted as clinically indicated.
4 Development of Drug-Resistant Bacteria
Prescribing DORIBAX™ 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.
5 Pneumonitis with Inhalational Use
When DORIBAX™ has been used investigationally via inhalation, pneumonitis has occurred. DORIBAX™ should not be administered by this route.

强生（Doribax 500 mg IV Susp）

包装
フィニバックス点滴静注用0.25g：10瓶（10mL容量瓶）


フィニバックス点滴静注用0.5g：10瓶（20mL容量瓶）

フィニバックスキット点滴静注用0.25g：10キット

製造販売元
塩野義製薬株式会社
完整（日文）资料附件：http://www.info.pmda.go.jp/go/pack/6139402D1032_1_04/