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部分中文Ceftizoxime sodium Suppositories处方资料（仅供参考）

一、品种的基本情况
1 、新药名称： 头孢唑肟钠栓剂
2 、新药类别： 化学药品注册分类 3 。
3 、适应症： 本品适用于对头孢唑肟敏感的链球菌属（肠球菌除外）、肺炎球菌、流感杆菌、大肠杆菌、克雷白氏菌、变形杆菌、沙雷氏菌、肠杆菌属、柠檬酸杆菌属、消化球菌、消化链球菌属和拟杆菌属菌株引起的（1）支气管炎、肺炎；（2）尿路感染症（肾盂肾炎、膀胱炎）。
4 、剂 型： 栓剂。
5 、规 格： 1克/ 瓶 ( 头孢唑肟计 ) 。
6 、用法与用量： 小儿常用剂量： 20-70 毫克（效价）/公斤/天，分 3-4 次插入肛门内。

二、药理与临床
1 、药理
    本品属于第三代半合成头孢菌素，作用方式是杀菌，通过抑制细菌细胞壁合成而产生杀菌作用。本品具有广泛抗菌作用，对各种需氧和厌氧的革兰氏阳性菌和革兰氏阴性菌有显著抗菌活性，尤其对革兰氏阳性菌的肺炎球菌、链球菌（肠球菌除外）和革兰氏阴性杆菌的大肠杆菌、克雷伯氏菌、奇异变形杆菌、吲哚阳性变形杆菌和流感杆菌有强大抗菌作用。
2 、临床
    临床疗效：头孢唑肟钠栓剂对 261 例患儿的有效率为 95.4% （249/261）其中肺炎 96.1% （73/76 例）、支气管炎 93.2% ，扁桃体炎和咽喉炎 95.2% （59/62 例），猩红热 100% （2/2 例），中耳炎 100% （5/5 例），尿路感染 95.9% （47/49 例），其他 100% （8/8 例）。 故 头孢唑肟钠栓剂直肠内给药在儿科感染治疗方面，疗效显著，安全性高。

三、国内外关于本品的生产、开发情况
    头孢唑肟钠栓由日本藤泽药品工业公司开发、生产、上市的，用于小儿由头孢唑肟敏感 的链球菌属等引起的（1）支气管炎、肺炎；（2）尿路感染症（肾盂肾炎、膀胱炎）。小儿常用剂量：20-70毫克（效价）/公斤/天，分3-4次插入肛门内。头孢唑肟钠栓在日本上市有125mg/枚和250mg/枚两种规格，为日本药典所收载，其英文名称为：Ceftizoxime sodium Suppositories ； 商品名为： Epocelin Suppositories。

四、市场分析 
    头孢唑肟钠在临床应用广泛，对小儿多种感染疗效显著，但目前国内只有 无菌粉，其用法为静脉滴注，该剂型对小儿尤其对婴幼儿的应用，受到一定的限制。头孢唑肟钠栓是经直肠粘膜吸收， 50 %～ 75%的药物可直接进入血液循环系统，不仅克服小儿注射给药困难的问题，又克服了肝脏的首过效应减轻药物对肝脏的损害，而且并应用于临床取得了与肌肉注射相似的治疗效果。
抗生素也是儿科的重点用药。我国人口基数大，每年出生近 2000万人，儿童占人口总数的1/3，达4亿，抗生素在儿科的市场也非常巨大。但目前国内市场上还缺乏适于儿童使用的头孢类栓剂品种。本品的开发可以填补国内空白，并且以其剂型在儿童中使用的优越性，必将有非常可观的市场前景。

Epocelin - General Information:
A semisynthetic cephalosporin antibiotic which can be administered intravenously or by suppository. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative organisms. It has few side effects and is reported to be safe and effective in aged patients and in patients with hematologic disorders. [PubChem]

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Efficacy / Effectiveness : 1. Effective species (Such as streptococci), pneumococcal bacteria, influenza bacteria, Escherichia coli, Klebsiella, Proteus, Serratia, Enterobacter, Citrobacter, Peptococcus, 2. Indications 1) sepsis, infective endocarditis 2) meningitis 3) Secondary infection of burns and burns 4) bronchitis, bronchiectasis (infection), secondary infection of chronic respiratory disease, pneumonia, lung abscess, empyema 5) Cholecystitis, cholangitis 6) Peritonitis 7) pyelonephritis, cystitis, prostatitis 8) uterine appendicitis, intrauterine infection, pelvic quadriplegia Usage / Capacity : 1. Intravenous injection 1) Adult: Intravenous injection of 0.5 ~ 2g (potency) twice or four times a day as a sedative center. 2) Pediatric patients (6 months or more): Intravenous injections 2 to 4 times a day for 40 ~ 80mg / kg body weight. 3) Intractable or severe infectious diseases: Increase the dose to 4g (titer) for adult on day 1 and 120mg (titer) per kg body weight for pediatric (6 months or more). 2. Intramuscular injection 1) Adult: Cefotin is the intellectual center of the body 0.5 ~ 2g (titer) per day is injected 2 ~ 4 times divided muscle. 2) Appropriate increase or decrease according to age and symptoms. 3) Preparation of this drug For intravenous injection, dissolve in injection water, saline solution or glucose injection solution and inject slowly. For intravenous injection, dissolve in the solution of sugar solution, electrolyte solution, amino acid preparation, etc., and inject for 30 minutes to 2 hours, but do not use the injection water when it dissolves (not the solution). For intramuscular injection, inject 2 mL of 0.25 g (potency) vial and 0.5 g (potency) vial and 1 g (potency) vial in 3 mL of water for injection or 0.5% lidocaine injection. Precautions for use : 1. Do not administer to the following patients. 1) Patients with a history of shock due to this drug 2) Patients who have a history of hypersensitivity to anilide-based local anesthetics such as lidocaine (for muscle injections only). 2. The following patients should be administered with caution. 1) It should not be administered to patients who have a history of hypersensitivity reactions to this drug or chemotherapy antibiotics, but should be administered with caution in case of unavoidable administration. 2) Patients with a history of hypersensitivity to penicillin antibiotics 3) Patients whose parents or siblings are susceptible to allergic symptoms such as bronchial asthma, rash, or urticaria. 4) Patients with severe renal disease 5) Patients with poor oral intake or parenteral nutrition, elderly patients, and patients with poor general condition (Observe vitamin K deficiency symptoms enough.) 6) Patients with a history of gastrointestinal disease (especially colitis) 3. Adverse reaction 1) Shock: Rarely can cause shock or anaphylactic reactions. Observe it carefully. If discomfort, irritability, wheezing, dizziness, paralysis, tinnitus, sweating, etc. appear, discontinue administration and take appropriate measures. 2) Hypersensitivity: Occasional rash, urticaria, erythema, fever, itching. Inflammation of the lymph nodes, arthralgia, paralysis may occur rarely. 3) Digestive system: In rare cases, severe colitis accompanied by stool such as pseudomembranous colitis may occur. If abdominal pain and frequent diarrhea occur, take appropriate measures such as stopping the administration immediately. Sometimes diarrhea, rarely vomiting, and other symptoms can occur. 4) Respiratory system: Intermittent pneumonia accompanied by fever, cough, dyspnea, chest x-ray abnormality, eosinophilia, eosinophilic lung infiltration may occur. If such symptoms occur, discontinue administration and discontinue administration of corticosteroids Take appropriate action. 5) Blood system: Sometimes anemia, granulocyte reduction, thrombocytopenia, eosinophilia, leukocytosis, and transient thrombocytosis are rarely observed. Hemolytic anemia may occur. 6) Skin: Stevens-Johnson syndrome was reported using deprived dermatitis, toxic epidermal mass. 7) Hepatic: Sometimes AST, ALT, ALP, bilirubin, LDH elevation may be rarely observed. If the abnormality is recognized, stop the administration and take appropriate measures. 8) Kidney: In rare cases, severe renal impairment such as acute renal failure, transient BUN, elevation of blood creatinine may occur. If the abnormality is observed, the patient should be observed regularly. 9) Hypoglycemia: In rare cases, stomatitis and candidiasis may occur. 10) Vitamin Deficiency: Rarely, there may be symptoms of vitamin K deficiency (hypoprothrombinemia, bleeding tendency, etc.), vitamin B deficiency syndrome (sulphitis, stomatitis, anorexia and neuritis). 11) Others: Headache and vaginitis may occur rarely. 4. General caution 1) In order to prevent the expression of resistant bacteria in the use of this drug, it is preferable to confirm the sensitivity and administer only the minimum period necessary for the treatment. 2) It is desirable to conduct a skin reaction test beforehand enough to predict the reaction such as shock. 3) Prepare for first aid in case of shock, and observe patient in stable state after administration. 5. Interaction 1) Caution should be exercised in combination with other cephalosporins and aminoglycoside antibiotics that renal toxicity may increase. 2) In combination with probenecid, the rate of tubular excretion of this drug may be reduced and the blood concentration may be sustained. 3) Combination with warfarin sodium may enhance the action of warfarin. 4) When administered in combination with a diuretic such as furosemide, renal toxicity may be increased. 6. Administration to pregnant and lactating women 1) Since the safety of administration during pregnancy has not been established, it should only be given to women who are pregnant or likely to be pregnant only when the therapeutic benefit exceeds the risk. 2) Since breastfeeding has been reported, care should be taken in breastfeeding. 7. Administration to children 1) Safety is not established for neonates, premature infants, and infants less than 6 months old. 2) There may be an increase in transient eosinophilia, AST, ALT, and CPK when administered to children over 6 months. The rise in CPK appears to be associated with intramuscular injections. 8. Administration to elderly people In the case of the elderly, pay attention to the following points and pay attention to the patient's condition such as the dose and the interval of administration. 1) In general, physiological function is deteriorated, and many adverse reactions are likely to occur. 2) Vitamin K deficiency may lead to bleeding tendency. 9. Influence on clinical examination 1) Be careful that false positives may occur in Benedict's reagents, test reagents, and urine tests by a clinical test except for the test tape reaction. 2) Be cautious because it can directly test positive coombs. 10. Application Precautions 1) Intravenous administration may cause vasoconstriction and thrombophlebitis rarely. Therefore, pay attention to injection preparation, injection site, injection method and so on, and make the scanning speed as slow as possible. 2) Intramuscular injection should be used only when it is inevitable. 3) Pain may appear on the injection site during muscle injection. 4) Do not inject muscles into newborns, premature babies, infants and children. 5) In order to avoid the influence on tissues, nerves, etc. during muscle injection, pay attention to the following points. ① Avoid repeated injections at the same site as much as possible. ② Be careful to avoid the nerve running area. ③ When piercing the needle, complain of intense pain, or if blood reflux occurs, remove the needle immediately and change the site. 6) In principle avoid mixing with other drugs. 11. Storage and Handling Precautions If it needs to be used and stored promptly after dissolution, it should be used within 12 hours since it can form precipitates when stored at room temperature, and within 48 hours when stored in refrigeration. Do not use if deposits are visible. The dissolving solution may be slightly yellowish with the lapse of time, but it may be used. However, if the color is blurred, it should be discarded. 12. Other Interactions with oral contraceptives have been reported. Storage : sealed container at room temperature Packing units : 1, 5, 10 vials