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头孢克肟细粒剂(Cefspan fine granules,Cefixime)

2012-03-13 23:04:14  作者:新特药房  来源:中国新特药网天津分站  浏览次数:472  文字大小:【】【】【
简介: 部分中文Cefspan处方资料(仅供参考) 世福素 Cefspan 【分类】抗生素/β-内酰胺类/头孢菌素类 【别名】氨噻肟烯头孢菌素,世福素、头孢克肟 【外文名】Cefspan,Cefixime 【药理及应用】本品为广 ...

部分中文Cefspan处方资料(仅供参考)

世福素 Cefspan

药品英文名
Cefixime

药品别名
氨噻肟烯头孢菌素、世福素、头孢克肟、Cefiximum、Cefnixime、Cefspan、CFIX、FK-027、FR-17027
 
药物剂型
1.胶囊:50mg,100mg;
2.片剂:0.2g,0.4g。
3.世福素细粒剂:50mg(セフスパン)
药理作用
头孢克肟为口服用第三代头孢菌素。其抗菌作用机制与其他第三代头孢菌素相似,主要通过与细菌细胞的一个或多个青霉素结合蛋白(PBPs)相结合,抑制细菌分裂期的胞壁合成,从而起抗菌作用。
本药抗菌作用特点是:
1.对革兰阴性杆菌产生的广谱β-内酰胺酶高度稳定;
2.对革兰阴性杆菌抗菌作用明显超过第一代和第二代头孢菌素,但对革兰阳性球菌抗菌作用不如第一代和部分第二代头孢菌素。头孢克肟在体外和体内对肺炎链球菌、化脓性链球菌等革兰阳性球菌及流感嗜血杆菌(包括产酶株)、卡他莫拉菌(包括产酶株)、大肠杆菌、奇异变形杆菌、淋球菌(包括产酶株)等革兰阴性杆菌具有良好抗菌作用。头孢克肟在体外对副流感杆菌、普通变形杆菌、肺炎克雷白杆菌、多杀巴斯德菌、普罗威登菌、沙门菌属、志贺菌属、黏质沙雷菌、异型枸橼酸菌、丙二酸盐枸橼酸菌亦具有一定抗菌活性,但其临床有效性尚待确定。头孢克肟对葡萄球菌抗菌作用差,对铜绿假单胞菌、肠杆菌属、脆弱拟杆菌、梭菌属等无抗菌作用。
 
药动学
头孢克肟口服吸收良好(生物利用度约为60%),组织穿透力强,体内分布广。药物吸收后可在各组织、体腔液、体液中达到有效抗菌浓度,也可透过胎盘屏障进入胎儿血循环。药物在痰、扁桃体、上颌窦、中耳分泌物及胆汁中浓度较高。正常成人空腹一次服用50mg、100mg、200mg头孢克肟,4h后血药浓度达峰值,分别为0.69μg/ml、1.18μg/ml、1.95μg/ml。正常儿童空腹一次按1.5mg/kg、3.0mg/kg、6.0mg/kg服用,3~4h血药浓度达峰值,分别为1.14μg/ml、2.01μg/ml、3.97μg/ml。本药主要经肾排出,服药12h后尿排泄率为20%~25%。血清蛋白结合率为70%,半衰期为3~4h,肾功能不全者血清半衰期延长。血液透析或腹膜透析不能有效清除本药。
 
适应证
适用于治疗敏感菌所致的咽炎、扁桃体炎、急性支气管炎和慢性支气管炎急性发作、中耳炎、尿路感染、单纯性淋病(宫颈炎或尿道炎)等。
 
禁忌证
对本药或其他头孢菌素类药过敏者禁用。

注意事项
1.交叉过敏:对一种头孢菌素类药过敏者对其他头孢菌素也可能过敏;对青霉素类、青霉素衍生物过敏者也可能对头孢菌素类药过敏。
2.慎用:
(1)对青霉素类抗生素过敏者;
(2)孕妇、哺乳期妇女;
(3)早产儿、新生儿;
(4)肾功能不全者;
(5)高度过敏性体质者;
(6)抗生素相关性肠炎患者。
3.药物对检验值或诊断的影响:
(1)服药时用硫酸铜法测定尿糖可呈假阳性;
(2)直接抗人球蛋白(Coombs)试验可呈阳性反应。

不良反应
头孢克肟不良反应大多短暂而轻微。
1.最常见的不良反应为腹泻、腹痛、恶心、消化不良、腹胀等胃肠道反应。
2.其次可见皮疹、荨麻疹、药物热、瘙痒等过敏反应。
3.偶见头痛、头晕等中枢神经系统反应。
4.少数患者用药后有一过性血清丙氨酸氨基转移酶、天门冬氨酸氨基转移酶、碱性磷酸酶、血尿素氮、肌酐升高,血小板、白细胞计数减少,嗜酸粒细胞增多等。
5.长期用药可致菌群失调,发生二重感染;也有引起维生素缺乏的报道。

用法用量
口服给药:
1.成人:
(1)一般感染:每天400mg,可单次或分2次服用;
(2)单纯性淋病:宜用400mg单剂疗法;
(3)化脓性链球菌感染:每天400mg,可单次或分2次服用,疗程至少10天;
(4)肾功能不全时剂量:肾功能障碍者,需根据肌酐清除率调整用药剂量。肌酐清除率为每分钟21~60ml并进行血液透析者,给予标准剂量的75%,即每天给药300mg;肌酐清除率每分钟≤20ml并进行腹膜透析者,给予标准剂量的50%,即每天给药200mg。
2.儿童:
(1)体重50kg以下或年龄12岁以下的儿童:每天8mg/kg,分2次服用;
(2)体重50kg以上或年龄大于或等于12岁的儿童:用量同成人。
 
药物相应作用
1.与氨基糖苷类药联用对某些敏感菌株有协同抗菌作用。
2.丙磺舒能延长本药排泄,升高本药的血药浓度。
3.阿司匹林可能升高本药的血药浓度。
4.与氨基糖苷类或其他头孢菌素合用可增加肾毒性。
5.与呋塞米等强利尿剂合用可增强肾毒性。
6.与伤寒活疫苗同用可减弱伤寒活疫苗的免疫效应,其机制可能为本药对伤寒沙门菌有抗菌活性。
7.本药与氯霉素合用可能产生相互拮抗作用。
 
专家点评
本品是一种口服的第三代广谱头孢菌素。对金葡菌、粪链球菌、铜绿假单胞菌无效。用于敏感菌引起的支气管炎、支气管扩张、慢性呼吸道继发感染、肺炎、肾盂肾炎、膀胱炎、淋菌性尿道炎、胆管炎、胆囊炎、中耳炎、副鼻窦炎、猩红热等。国内报道应用本品治疗尿路感染患者30例,总有效率为96.7%,治愈率达90%。另有报道用本品治疗尿路感染,连续7~14天后总有效率为95.6%,其中对肾盂肾炎的治愈率为100%。本品对淋球菌感染疗效较好,单剂量400~800mg治疗无并发症的生殖器官、肛门、直肠淋病的治愈率达96%~100%。
Cefspan - General Information:
Cefspan, an antibiotic, is a third-generation cephalosporin like ceftriaxone and cefotaxime. Cefspan is highly stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and some cephalosporins due to the presence of beta-lactamases, may be susceptible to cefixime. The antibacterial effect of cefixime results from inhibition of mucopeptide synthesis in the bacterial cell wall.
Pharmacology:
Cefspan, an antibiotic, is a third-generation cephalosporin like ceftriaxone and cefotaxime. Cefspan is highly stable in the presence of beta-lactamase enzymes. As a result, many organisms resistant to penicillins and some cephalosporins due to the presence of beta-lactamases, may be susceptible to cefixime. The antibacterial effect of cefixime results from inhibition of mucopeptide synthesis in the bacterial cell wall.
Cefspan for patients
Cefixime is a cephalosporin antibiotic used to treat bacterial infections. Take at regular intervals and complete the entire course of therapy. Do not take this medication if you are allergic to any type of penicillin or cephalosporin. Notify your physician if you are pregnant or nursing. This antibiotic may decrease the effectiveness of birth control pills; use another form of birth control while taking this medication. Shake the suspension well before each use and store it in the refrigerator. May cause nausea, vomiting or diarrhea; notify your physician if these occur. Take with food or milk to avoid stomach upset. Cefixime may cause a false-positive reaction for nonspecific urine glucose tests in patients with diabetes. This medication does not interfere with enzyme-based urine glucose tests.
Cefspan Interactions
Carbamazepine: Elevated carbamazepine levels have been reported in postmarketing experience when SUPRAX is administered concomitantly. Drug monitoring may be of assistance in detecting alterations in carbamazepine plasma concentrations.
Warfarin and Anticoagulants: Increased prothrombin time, with or without clinical bleeding, has been reported when cefixime is administered concomitantly.
Drug/Laboratory Test Interactions
A false-positive reaction for ketones in the urine may occur with tests using nitroprusside but not with those using nitroferricyanide.
The administration of SUPRAX may result in a false-positive reaction for glucose in the urine using ClinitestÒ**, Benedictís solution, or Fehlingís solution. It is recommended that glucose tests based on enzymatic glucose oxidase reactions (such as Clinistix®** or Tes-TapeÒ**) be used. A false-positive direct Coombs test has been reported during treatment with other cephalosporin antibiotics; therefore, it should be recognized that a positive Coombs test may be due to the drug.
Cefspan Contraindications
SUPRAXÒ is contraindicated in patients with known allergy to the cephalosporin group of antibiotics.
Additional information about Cefspan
Cefspan Indication: For use in the treatment of the following infections when caused by susceptible strains of the designated microorganisms: (1) uncomplicated urinary tract infections caused by Escherichia coli and Proteus mirabilis, (2) otitis media caused by Haemophilus influenzae (beta-lactamase positive and negative strains), Moraxella catarrhalis (most of which are beta-lactamase positive), and S. pyogenes, (3) pharyngitis and tonsillitis caused by S. pyogenes, (4) acute bronchitis and acute exacerbations of chronic bronchitis caused by Streptococcus pneumoniae and Haemophilus influenzae (beta-lactamase positive and negative strains), and (5) uncomplicated gonorrhea (cervical/urethral) caused by Neisseria gonorrhoeae (penicillinase- and non-penicillinase-producing strains).
Mechanism Of Action: Like all beta-lactam antibiotics, cefixime binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of 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 cefixime interferes with an autolysin inhibitor.
Drug Interactions: Probenecid Probenecid increases the antibiotic's level
Food Interactions: Preferably on an empty stomach, rate of absorption is decreased but extenet of absorption remains the same: not really problematic.
Generic Name: Cefixime
Synonyms: Cefixima [Spanish]; Cefixime Anhydrous; Cefiximum [Latin]; Cefixim
Drug Category: Anti-Bacterial Agents; Cephalosporins
Drug Type: Small Molecule; Approved
Other Brand Names containing Cefixime: CFIX; Cefixoral; Cefspan; Cephoral; Oroken; Suprax; Unixime;
Absorption: About 40%-50% absorbed orally whether administered with or without food, however, time to maximal absorption is increased approximately 0.8 hours when administered with food.
Toxicity (Overdose): Symptoms of overdose include blood in the urine, diarrhea, nausea, upper abdominal pain, and vomiting.
Protein Binding: 65% (concentration independent)
Biotransformation: Hepatic. Approximately 50% of the absorbed dose is excreted unchanged in the urine in 24 hours.
Half Life: 3-4 hours (may range up to 9 hours). In severe renal impairment (5 to 20 mL/min creatinine clearance), the half-life increased to an average of 11.5 hours.
Dosage Forms of Cefspan: Tablet Oral
Powder, for suspension Oral
Chemical IUPAC Name: (6R,7R)-7-[[2-(2-amino-1,3-thiazol-4-yl)-2-(carboxymethyloxyimino)acetyl]amino]-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Chemical Formula: C16H15N5O7S2
Organisms Affected: Enteric bacteria and other eubacteria

セフスパン

抗生物質で、細菌による感染症の治療薬 
 
主成分名: セフィキシム
 
製薬会社: アステラス
 
薬価: 77.90円 (50mg1g)
 
主な作用 
 
セフェム系といわれる抗生物質で、細菌を直接殺す作用があります。レンサ球菌、肺炎球菌、リン菌、大腸菌、クレブシエラなどの腸内細菌、インフルエンザ菌などによる感染症に効力を現すので、呼吸器系、尿路、胆のう・胆管系、耳鼻科領域などの感染症に用いられます。 
 
副作用
 
発疹、じんま疹などの過敏症状が起こることがあります。ペニシリン系の抗生物質に過敏な人は、この薬でも過敏症が発生する可能性があるので、わかっていたらあらかじめ医師に伝えてください。 
服用上の注意
 
効果が比較的持続するので、服用は1日2回でよいとされています。
附件:



---------------------------------------------------------------
原产地英文商品名:
Cefspan fine granules 50mg(セフスパン) 100g/bottle
原产地英文药品名:
Cefixime
中文参考商品译名:
世福素细粒剂50毫克(セフスパン) 100克/瓶
中文参考药品译名:
头孢克肟
生产厂家中文参考译名:
安斯泰来
生产厂家英文名:
Astellas

责任编辑:admin


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