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。

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原产地英文商品名:
Epocelin 250mg/piece 20pieces/box
原产地英文药品名:
ceftizoxime sodium Suppositories
中文参考商品译名:
益保世灵 250毫克/粒 20粒/盒
中文参考药品译名:
头孢唑肟钠栓剂
生产厂家中文参考译名:
安斯泰来，藤泽
生产厂家英文名:
Astellas Pharma Inc，Tanabe mitsubishi
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原产地英文商品名:
Epocelin 125mg/piece 20pieces/box
原产地英文药品名:
ceftizoxime sodium Suppositories
中文参考商品译名:
益保世灵 125毫克/粒 20粒/盒
中文参考药品译名:
头孢唑肟钠栓剂
生产厂家中文参考译名:
安斯泰来，藤泽
生产厂家英文名:
Astellas Pharma Inc，Tanabe mitsubishi

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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Pharmacology:
Epocelin 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.

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Epocelin Interactions
Although the occurrence has not been reported with Cefizox, nephrotoxicity has been reported following concomitant administration of other cephalosporins and aminoglycosides.

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Epocelin Contraindications
Cefizox (ceftizoxime for injection, USP) is contraindicated in patients who have known allergy to the drug.

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Additional information about Epocelin
Epocelin Indication: For the treatment of infections due to susceptible strains of microorganisms.

Mechanism Of Action: Epocelin is an aminothiazolyl cephalosporin with an extended spectrum of activity against many gram-negative, nosocomially acquired pathogens. It has excellent beta-lactamase stability, with good in vitro activity against Haemophilus influenzae, Neisseria gonorrhoeae and Klebsiella pneumoniae. Epocelin, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that ceftizoxime interferes with an autolysin inhibitor.

Generic Name: Ceftizoxime

Synonyms: Ceftizoxima [inn-spanish]; Ceftizoximum [inn-latin]

Drug Category: Cephalosporins; Anti-Bacterial Agents

Drug Type: Small Molecule; Approved

Other Brand Names containing Ceftizoxime: Cefizox; Cefizox in plastic container; Ceftix; Epocelin;

Protein Binding: 30% protein bound

Biotransformation: Ceftizoxime is not metabolized, and is excreted virtually unchanged by the kidneys in 24 hours.

Chemical IUPAC Name: (6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

Chemical Formula: C13H13N5O5S2

Organisms Affected: Enteric bacteria and other eubacteria

EPOCELIN Suppositories 125 エポセリン坐剤125／エポセリン坐剤250

*有効成分に関する理化学的知見

一般名

セフチゾキシムナトリウム，Ceftizoxime Sodium(JAN)

化学名

Ｍonosodium(6R ,7R )-7-[(Z )-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetylamino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

分子式

Ｃ₁₃Ｈ₁₂Ｎ₅ＮａＯ₅Ｓ₂

分子量

405.38

構造式

性状

白色～淡黄色の結晶又は結晶性の粉末である．
水に極めて溶けやすく，メタノールに溶けにくく，エタノール（95）にほとんど溶けない．

取扱い上の注意

1.

15℃以下で保存することが望ましい．

2.

アルミ袋開封後は，光及び湿気により黄変することがあるため，冷暗所で保存することが望ましい．

包装

エポセリン坐剤125：20個

エポセリン坐剤250：20個