98．新菌灵

出处：按学科分类—医药、卫生 军事医学科学出版社《临床常用进口药物手册》第545页（11746字）

【中文释文】：

(头孢呋辛片剂)

〔简介〕

新菌灵药片125mg：白色，薄膜包衣，胶囊形状的药片，一面刻上Glaxo字样，另一面则刻上125字样，每片含头孢呋辛125mg(头孢呋辛乙酰氧乙酯)。

新菌灵药片250mg：白色，薄膜包衣，胶囊形状的药片，一面刻上Glaxo字样，另一面则刻上250字样，每片含头孢呋辛250mg(头孢呋辛乙酰氧乙酯)。

新菌灵药片500mg：白色，薄膜包衣，胶囊形状的药片，一面刻上Glaxo字样，另一面则刻上500字样，每片含头孢呋辛500mg(形式为头孢呋辛乙酰氧乙酯)。

〔用途〕

头孢呋辛乙酰氧乙酯是杀菌性头孢菌素抗生素类头孢呋辛乙酰氧乙酯的一种口服的前体药物，对绝大多数的β内酰胺酶具抵抗力，并对系列的革兰阳性及革兰阴性细菌有效，适用于治疗由敏感性细菌所引发的感染。

〔适应证〕

下呼吸道感染：例如急性和慢性支气管炎及肺炎。

上呼吸道感染：例如耳、鼻和喉部感染，如中耳炎、窦炎、扁桃体炎和咽炎。

泌尿生殖道感染：例如肾盂肾炎、膀胱炎和尿道炎。

皮肤及软组织感染：例如疖病、脓性皮炎和脓疱病。

淋病：急性无并发病的淋球菌性尿道炎和子宫颈炎。

〔细菌学〕

头孢呋辛乙酰氧乙酯在活体内的杀菌功效归功于其母体化合物头孢呋辛。头孢呋辛是一种特性显赫和有效的抗菌药，对广泛的一般病原体，包括生产β内酰胺酶的菌株，具广谱杀菌功效。头孢呋辛具有对细菌β内酰胺酶的良好稳定性，因而对许多的耐氨苄西林或耐阿莫西林的菌株均奏效。头孢呋辛杀菌功效的发挥源于与首要的目标蛋白质结合，从而抑制细胞壁合成。

头孢呋辛一般都对下列在体外试验的细菌有效：需氧菌、革兰阴性：流感嗜血杆菌(包括耐氨苄西林的菌株)；副流感嗜血杆菌；卡他球菌；大肠杆菌；克雷伯菌属；奇异变形菌；雷氏变形杆菌；普罗威登斯菌属及淋病瑟球菌(包括生产和不生产青霉素酶的菌株)。

需氧菌，革兰阳性：金黄色葡萄球菌和表皮球菌(包括生产青霉素酶的菌株而不包括耐甲氧西林的菌株)；肺炎链球菌；酿脓链球菌(其他的β溶血链球菌)；乙簇链球菌(无乳链球菌)。

厌氧菌，革兰阳性及革兰阴性球菌属(包括消化球菌和消化链球菌种)；革兰阳性杆菌属(包括梭菌属)及革兰阴性杆菌属(包括拟杆菌属和梭杆菌属)；丙酸杆菌属。

对头孢呋辛不敏感：艰难梭菌；假单胞菌属；弯曲杆菌菌属；乙酸钙不动杆菌；耐甲氧西林的金黄色葡萄球菌株和表皮葡萄球菌株，以下各属有的菌株对头孢呋辛不敏感：类链球菌；摩氏摩根菌；普通变形菌；肠杆菌属；柠檬酸杆菌属；沙雷菌属；脆弱拟杆菌。

〔剂量与用法〕

成人：绝大多数感染对250mg，每天2次的剂量有反应；在轻度至中度下呼吸道感染如支气管炎，可投用每天2次250mg。部分严重下呼吸道感染，或怀疑是肺炎的情况，应投用每天2次500mg的剂量。一般泌尿道感染用125mg剂量亦已足够，肾盂肾炎，推荐剂量为每天2次250mg，而对无并发症的淋病，推荐剂量为1g单剂。

儿童：一般的剂量是每天2次125mg。在患中耳炎的儿童，年龄2岁或较大的，可用每天2次250mg。

一般的疗程为7d。(由5～10d不等)

头孢呋辛应该餐后服用，如此则吸收为最佳。

头孢呋辛味道苦涩，所以新菌灵药片不宜压碎，对那些不能吞服药片的病人如幼儿可能不适合使用。

〔禁忌证与警告〕

禁忌证：对头孢菌素抗生素类有过敏的病人。

注意：头孢菌素抗生素类一般都是可以安全地投用于对青霉素类过敏的病人，虽亦会有交叉反应的报告，已经历对青霉素类产生过敏反应的病人即表明有特别护理的需要。

一如其他的抗生素类，长期使用头孢呋辛乙酰氧乙酯可能会引致由非敏感微生物过度生长的情况(例如念珠菌属，肠球菌、梭菌)，因而可能需要中断疗法，曾有因使用广谱抗生素类而出现假膜性结肠炎的报告。故此，在于使用抗生素期间或期后而发生严重腹泻的病人，考虑这一诊断是重要的。

虽然没有实验室的证据显示头孢呋辛乙酰氧乙酯对胚胎及畸胎有影响，但一如所有药物，在妊娠的首数月中应小心投用，头孢呋辛乙酰氧乙酯会从人奶中排泄，所以当使用头孢呋辛乙酰氧乙酯于哺乳的母亲时应采取谨慎的措施。

正接受头孢呋辛乙酰氧乙酯的病人，推荐用作测定血／血浆葡萄糖水平的方法为葡萄糖氧化酶或己糖激酶，此抗生素不会干扰碱性苦味酸测定肌酸酐。

〔副作用〕

对头孢呋辛乙酰氧乙酯的不良反应本质上一般都是温和及短暂的。一小部分接受头孢呋辛乙酰氧乙酯的病人曾有经历胃肠失调情况，包括腹泻，恶心和呕吐。一如其他广谱的抗生素类，假膜性结肠炎罕见。头痛的报告亦有。过敏性反应的报告少有。

曾有在使用新菌灵疗法期间出现嗜酸性细胞增多及短暂增高肝酶水平(ALT和AST)的报告，曾有报告在头孢菌素类疗法中出现对库姆斯试验的阳性反应，而这现象则会干扰血液的交叉配合。

过量使用头孢菌素会引起大脑的刺激而导致抽搐。

头孢呋辛乙酰氧乙酯血药浓度可在腹膜透析中进行血液透析来降低。

〔药物注意事项〕

新菌灵药片应该贮藏于25℃以下，必要时贮于30℃以内达2个月对产品无损害。

〔其他资料〕

口服给药后，头孢呋辛乙酰氧乙酯在胃肠道被吸收，并在肠粘膜和血液迅速水解而释放循环中。进食后服药可达最佳吸收。服药后，其高峰血药浓度(剂量125mg为2～3mg／kg，250mg为4～6mg／kg，500mg为5～8mg／kg和1g为9～14mg／kg)，大约在2～3h达到。其血清半衰期为1～1．5h，与蛋白质结合量为33%～50%，视测试方法而定。头孢呋辛乙酰氧乙酯不被代谢，并经肾小球过滤和肾小管分泌排泄。同时并投丙磺舒即增加血药浓度—时间曲线下面积达50%。头孢呋辛乙酰氧乙酯的血清水平经透析便减退。

新菌灵为葛兰素集团所拥有的商标。

〔生产厂家〕

英国格林福德葛兰素集团

(附本品别名：头孢氨呋肟、头孢呋肟酯、头孢呋新酯)

【外文释文】：

Presentation

Zinnat tablets 125mg：white，film-coated，capsule-shaped tablets engraved with‘Glaxo’ on one side and‘125’on the other．Each tablet contains cefuroxime 125mg(as cefuroxime axetil)

Zinnat tablets 250mg：white，film-coated，capsule-shaped tablets engraved with‘Glaxo on one side and‘250on the other．Each tablet contains cefuroxime 250mg(as cefuroxime axetil)

Zinnat tablets 500mg：white，film-coated，capsule-shaped tablets engraved with‘Glaxo or one side and‘500on the other．Each tablet contains cefuroxime 500mg(as cefuroxime axetil)

Cefuroxime axetil is an oral prodrug of the bactericidal cephalosporin antibiotic cefuroxime，which is resistant to most beta-lactamases and is active against a wide range of Grampositive and Gram-negative organisms．It is indicated for the treatment of infections caused by sensitive bacteria．

Indications include

Lower respiratory tract infections for example，acute and chronic bronchitis，and pneumonia．

Upper respiratory tract infections for example ear，nose and throat infections，such as otitis media，sinusitis，tonsillitis and pharyngitis．

Genito-urinary tract infections for example，pyelonephritis，cystitis and urethritis．

Skin and soft tissue infections for example，furunculosis，pyoderma and impetigo．

Gonorrhoea，acute uncomplicated gonococcal urethritis，and cervicitis．

Bacteriology

Cefuroxime axetil owes its in vivo bactericidal activity to the parent compound cefuroxime．Cefuroxime is a well characterized and effective antibacterial agent which has broadspectrum，bactericidal activity against a wide range of common pathogens，including beta-lactamase-producing strains．Cefuroxime has good stability to bacterial beta-lactamase，and consequently is active against many ampicillin resistant or amoxycillin-resistant strains．The bactericidal action of cefuroxime results from inhibition of cell-wall synthesis by binding to essential target proteins．

Cefuroxime is usually active against the following organisms in vitro．

Aerobes，Gram-negative：Haemoph ilus influenzae(including ampicillin-resistant strains)；H．parainfluenzae；Branhamella catarrhalis；Escherichia coli，Klebsiella species，Proteus mirabillis，P．rettgeri；Providencia species and Neisseria gonorrhoeae(including penicillinase-and nonpenicillinase-producing strains)．

Aerobes，Gram-positive：Staphylococcus aureus and S．epidermidis(including penicillinase-producing strains but excluding methicillin-resistant strains)；Staphylcoccus pneumoniae，Streptococcus pyogenes(and other beta-haemolytic streptococcus)；Streptococcus Group B(S．agalactiae)．

Anaerobes，Gram-positive and Gram-negative cocci(including Peptococcus and Peptostreptococcus species)；Gram-positive bacilli(including Clostridium species)and Gram-negative bacilli(including Bacteroides and Fusobacterium species)，Propionibacterium species．

The following organisms are not susceptible to cefuroxime：Clostridium difficile；Pseudomonas species；Campylobacter species；Acinetobacter calcoaceticus；methicillin resistant strains of Staphylococcus aureus and S．epidermidis．

Some strains of the following genera are not susceptible to cefuroxime：Streptococcus faecalis；Morganella morganii；Proteus vulgaris；Enterobacter species；Citrobacter species；Serratia species；Bacteroides fragilis．

Dosage and administration

1．Adults Most infections will respond to 250mg bid．In mild to moderate lower respiratory tract infections e．g．bronchitis 250mg bid should be given．For some severe lower respiratory tract infections or if pneumonia is suspected then 500mg bid should be given．For urinary tract infections a dose of 125mg is usually adequate．In pyelonephritis the recommended dose is 250mg bid．A single dose of 1 gram is recommended for the treatment of uncomplicated gonorrhoea．

2．Children The usual dose is 125mg bid．In children with otitis media，aged two years or older，250mg bid．may be used．

The usual course of therapy is seven days(range 5-10 days)．

Cefuroxime axetil should be taken after food for optimum absorption．

Because of the bitter taste of cefuroxime axetil，Zinnat tablets should not be crushed and are therefore unsuitable for treatment of patients，such as younger children，who cannot swallow tablets．

Contra-indications，warnings etc．

Contra-indications

Patients with known hypersensitivity to cephalosporin antibiotics．

Precautions

Cephalosporin antibiotics may in general be given safely to patients who are hypersensitive to penicillins，although cross-reactions have been reported．Special care is indicated in patients who have experienced an anaphylactic reaction to penicillins．

As with other antibiotics，prolonged use of cefuroxime axetil may result in the overgrowth of non-susceptible organisms(e．g．Candida，Enterococci，Clostridium difficile)，which may require interruption of treatment．

Pseudomembranous colitis has been reported with the use of broad-spectrum antibiotics．therefore it is important to consider its diagnosis in patients who develop serious diarrhoea during or after antibiotics use．

There is no experimental evidence of embryopathic or teratogenic effects attributable to cefuroxime axetil but，as with all drugs，it should be adrnmistered with caution during the early months of pregnancy．Cefuroxime is excreted in hutnan milk and consequently caution should be exercised when cefuroxime axetil is administered to a nursing mother．It is recom mended that either the glucose oxidase or hexokinase methods are used to determine blood／ plasma glucose levets in patients receiving eefuroxime axetil．This antibiotic does not interfere in the alkaline picrate assay for creatinine．

Side effects

Advese reactions to cefuroxime axetil have been generally mild and transient in nature．

A small proportion of patients receiving cefuroxime axetil have experienced gastrointestinal disturbances，including diarrhoea，nausea and vomiting．As with other broad-spectrum antibiotics，there have been rare reports of pseudomembranous colitis．Headache has also been reported．There have been rare reports of hypersensitivity reactions．Eosinophilia and tran sient increases in hepatic enzyme levels，[ALT(SGPT)and AST(SGOT)]have been noted during Zinnat therapy．A positive Coombs’test has been reported during treatment with cephalosporins．This phenomenon can interfere with cross-matching of blood．

Overdosage

Overdosage of cephalosporins can cause cerebal irritation leading to convulsions．

Serum levels of cefuroxime can be induced by haemodiaysis in peritoneal dialysis．

Pharmaceutical precautions

Zinnat tablets should be stored below 25℃．Occasional storage at temperatures not higher than 30℃ for up to 2 months is not detrimental to the product．

Further information

After oral administration，cefuroxime axetil is absorbed from the gastro-intestinal tract and rapidly hydrolyzed in the intestinal mucosa and blood to release cefuroxime into the circulation．Optimum absorption occurs when it is administered after a meal．Peak serum levels(2-3mg／L for a 125mg dose，4-6mg／L for a 250mg dose，5-8mg／L for a 500mg dose arid 9-14mg／L for a 1 g dose)occur approximately two to three hours after dosing when taking after food．The serum half life is between 1 and 1．5 hours．Protein binding has been variously stated as 33-50%depending on the methodology used．Cefuroxime is not metabolized and is excreted by glomerular filtration and tubular secretion．Concurrent administration of probenecid increases the area under the mean serum concentration time curve by 50%．Serum levels of cefuroxime are reduced by dialysis．

Zinnat is a trade mark owned by the Glaxo Group of Companies．

Manufacturer

Glaxo Operations UK Ltd．，Greenford，England