53．头孢必

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292页（7171字）

【中文释文】：

头孢哌酮针剂

〔概述〕

头孢必(头孢哌酮)为第三代头孢类供静脉及肌肉注射的无菌半合成的广谱抗生素，其分子式为：7-〔D(-)-a-(4-乙基-2，3-双氧-1-哌嗪)羰酰氨〕氨基〕(4-羟基苯)乙酰基〕氨基〕-3-〔〔(1-甲基-1H-四唑-5-基)硫代〕甲基〕-8-氧代-，单钠盐。

〔适应证〕

1．呼吸道感染 由肺炎双球菌、流感杆菌、金黄色葡萄球菌、β-溶血性链球菌、克雷白杆菌、变形菌属、肠杆菌属、绿脓杆菌等所致感染等。

2．腹膜炎及其他腹内感染 由大肠杆菌、绿脓杆菌、肠球菌、革兰阳性厌氧球菌、革兰阳性厌氧杆菌及革兰阳性厌氧杆菌等所致感染。

3．细菌性败血症 由肺炎双球菌、绿脓杆菌、金黄色葡萄球菌、肠球菌、流感杆菌、大肠杆菌、奇异变形杆菌、梭状芽胞杆菌以及革兰厌氧阳性球菌等所致感染。

4．皮肤及皮肤组织感染 由金黄色葡萄球菌，绿脓杆菌等所致感染。

5．骨盆炎症，子宫内膜炎及女性生殖道感染 由淋球菌、金黄色葡萄球菌、表皮葡萄球菌、无乳链球菌、大肠杆菌、梭状芽胞杆菌、类杆菌属(包括脆弱类杆菌)以及革兰阳性厌氧球菌所致感染。

尿道感染 由肠球菌、大肠杆菌、绿脓杆菌所致感染。

〔剂量及给药方法〕

一般成人剂量：成人为2～4g／d，分次给药，每隔12h1次，对严重感染或不敏感组织器官的感染每日总剂量和给药次数可以增加(6～12g／d，分2～4次给药)。

小儿剂量：儿童及婴儿的总剂量为50～200mg／(kg·d)，分2～4次给药，该剂量适合中、轻度感染。

〔配制〕

肌肉注射液的配制(建议分下述两步稀释配制)：

1．加入所需量的无菌注射用水，摇动至头孢必完全溶解；

2．加入所需量的2%利多卡因，混合即可(请见下表)。

表17 头孢必肌肉注射液的配制

〔静脉注射液配制〕

最初稀释液的配制：

每克头孢必至少加2．8ml(5ml更好些)下述任何一种溶液：

5%葡萄糖注射液；

5%葡萄糖和0．9%(或0．2%)氯化钠注射液；

10%葡萄糖注射液；

0．9%氯化钠注射液；

无菌注射用水(不能作为静脉输液辅助药液用)。

配制好的初始溶液，再加上述任何一种辅药液稀释即可。

〔禁忌证〕

对头孢类抗生素过敏者的禁用。

〔副作用〕

据报道头孢哌酮有头孢类抗生素常见的副作用，过敏反应(如发热，抗蛋白试验的变化)，血液等反应(如，中性粒细胞减少，短暂性嗜伊红细胞增多)，以及腹泻，恶心、呕吐，稀便等。

〔妊娠〕

妊娠期不应使用该药。

〔配伍禁忌〕

β-内酰胺类抗生素(青霉素类和头孢类)与氨基糖甙类抗生素混合，可彼此失活，因此如需同时应用，应分别在不同部位给药。不能将两类药物在同一静脉输液袋(瓶)中混合。

〔药物相互作用〕

头孢哌酮与酒精可引起戒酒硫样反应，口服抗凝血药以及其它影响凝血的药物相互作用。

〔贮存及稳定性〕

头孢必无菌粉剂应在25℃或25℃以下保存，配制注射液前应避光，配制成注射液后不必再避光，配制的注射液室温下24h稳定，如冷藏(5℃)可贮存5d。

〔可供产品〕

1g供静脉注射、肌肉注射用粉针剂。

2g供静脉注射、肌肉注射用粉针剂。

〔生产厂家〕

塞浦路斯麦道甘美大药厂

(附本品别名：先锋必素，先锋哌酮，氧哌羟苯唑头孢菌素钠，先锋哌唑酮，头孢氧哌羟苯唑，先锋松，Cefobid，Cefobis，T-1551，Dardum，Cefozone，kiphazon)

【外文释文】：

Cefoperazone Broad spectrum antibiotic

Description

Medocef(cefoperazine sodium)is a sterile，semisynthetic broad spectrum parenteral cephalosporin antibiotic for intravenous or intramuscular administration．It is the sodium salt of 7-[D(-)-a-(4-ethyl-2，3-dioxo-1-piperazine-carboxamido)-a-(4-hydroxyphenyl)acetamido]-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid．

Indications

Respiratory tract infections caused by S．pneumoniae，H．influenzae，S．aureus(penicillinase and non-penicillinase producing strains)，S．pyogenes(Group A betahemolytic streptococci)，P．aeruginosa，Klebsiella pneumoniae，E．coli，Proteus species，and Enterobacter species．

Peritonitis and other Intra-abdominal Infections caused by E．coli，P．aeruginosa，enterococci，anaerobic gram-positive cocci，and anaerobic gram-positive and gramnegative bacilli．

Bacterial Septicemia caused by S．pneumoniae，S．pyogenes，S．aqalactiae，S．aureus，enterococci enterococci，H．influenzae，Pseudomonas aeruginosa，E． coli， Klebsiella spp．，Proteus species，Clostridium spp．and anaerobic gram-positive cocci．

Infections of the skin and skin structures caused by S．aureus(penicillinase and nonpenicillinase producing strains)，S．pyogenes and S．aeruginosa．

Pelvic inflammatory disease，endometritis，and other infections of the female genital tract caused by N．gonorrhoeae，S．aureus and epidermidis，S．agalactiae，E．coli，Clostridium spp．，Bacteroides species(including Bacteroides frgilis)and anaerobic gram-positive cocci．

Urinary tract infections caused by Enterococcus，Escherichia coli，and Pseudomonas aeruginosa．

Dosage and Administration

Usual adult dosage：The usual adult daily dose of Medocef is 2 to 4 grams per day administered in divided doses every 12 hours．In severe infecgtions or infections caused by less sensitive organisms，the total daily dose and／or frequency may be increased(6-12 g daily divide into 2，3 or 4 administrations)．

Pediatric dosage：In children and infants，a total dosage of 50mg to 200mg per kg of body weight divided into 2-4 equal doses，is effective for most mild to moderately severe infectiosn．

Reconstitution

Intramuscular amdinistration．A two step silution process as follows is recommended：First，add the required amount of sterile water for injection and agitate until Medocef powder is completely dissolved．Second，add the required amount of 2% lidocaine and mix(See table below)．

Table 17

Intravenous administration．To prepare initial dilution for intravenous use，add a minimum of 2．8ml(5ml prefered)per gram of cefoperazone of any of the following solutions：5% of dextrose injection，5% dextrose and 0．9% or 0．2% sodium chloride injecion，10%dextrose injection，0．9% sodium chloride injection and sterile water for injection(not to be used as a vehicle for intravenous infusion)．The resulting solution should then be wihtdrawn for further dilution and administration using any of the above vehicles．

Contraindications

Medocef is contraindicated in patients with known allergy to the cephalosporin-class of antibiotics．

Side Effects

The usual adverse reactions ascribed to the cephalosporins have been reported for cefoperazone．Hypersensitivity reactions(e．g．fever，a change in Goombs′test)and hematologic reactions(e．g．neutropenia，transient eosingophilia)have been reported．Diarrhea，nausea，vomitting or loose stools have also been observed．

Pregnancy

Medocef should not be administered during Pregnancy．

Incompatibilities

Extemporaneous admixtures of beta-Lactam antibacterials(Penicillins and Cephalosporins)and Aminoglycosides may result in substantial mutual inactivation．If they are administered concurrently，they should be administered in separate sites．Do not mix them in the same intravenous bag or bottle．

Drug Interactions

Cefoperazone interacts with alcohol(disulfiram like reaction)，oral anticoagulants and other medication which affect blood clotting．

Storage and Stability

Medocef sterile powder is to be stored at or below 25℃ and protected from light prior to reconstitution．After reconstitution，protection form light is not necessary．Reconstituted Medocef and dilutions of Medocef in the commonly used intravenous fluids are stable for 24 hours at room temperature and 5 days if stored under refrigeration(5℃)．

Availability

Vials containing cefoperazone sodium equivalent to 1 gram cefoperazone，and 2 gram cefoperazone for intramuscular and intravenous administration．

Manufacturer

Medochemie Ltd．，Limassol，Cyprus