药品信息: 中文品名】头孢克洛
【药效类别】抗生素>头孢菌素类
【通用药名】Cefaclor
【别 名】头孢氯氨苄, Cephaclor, Ceclor, Alfatil, Distaclor, Gliamin, Keflor, Kefral, Panacef, Muco Panoral, Panoral, Lilly 99638, Ceclor CD, Distaclorin, Kefoclor, Kefolor, Kloclor, L-Kefral,
【CA 名 称】
5-Thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid, 7-[[(2R)-aminophenylacetyl]amino]-3-chloro-8-oxo-, (6R,7R)-
【CA登记号】[53994-73-3]、[70356-03-5](一水合物)
【结 构 式】
【分 子 式】C15H14ClN3O4S
【分 子 量】367.806
【收录药典】JP14, USP23
【开发单位】礼来
【首次上市】1979年,美国、南非、英国和德国
【性 状】
【用 途】半合成高效口服头孢类抗生素,结晶带一分子结晶水。由于在C3-位引入了氯,增强了抗菌作用。和临床常用的口服头孢菌素如头孢氨苄、头孢拉定比较,本品抑制革兰氏阴、阳性菌包括大肠杆菌、流感杆菌、奇异变性杆菌、伤寒杆菌、肺炎球菌、金黄色葡萄球菌有较强的抗菌作用,一般比头孢氨苄、头孢拉定为佳。对流感杆菌及一些肠道细菌头孢氨苄、头孢拉定比头孢氨苄强4--16倍,对β-内酰胺酶的稳定性随酶的类别而异。
不同适应症和各年龄组别患者的用法用量
口服给药
适用于尿道感染, 上下呼吸道感染, 皮肤感染, 中耳炎
成人: 头孢克洛一水化物:250-500 mg,每8小时一次。最大剂量:4 g/天。
儿童: >1个月:20 mg/kg/天,分3次服用,必要时增加至40 mg/kg/天。<1岁:62.5mg,每天3次;1-5岁:125 mg,每天3次;>5岁:250 mg,每天3次。
服药与进食
服药不受进食影响
禁忌
已知对头孢菌素类过敏者禁用。
注意事项
慎用于严重肾脏损伤者,有青霉素过敏史者,孕妇和哺乳期妇女。
不良反应
过敏反应,腹泻,恶心,呕吐,念珠菌病,嗜酸粒细胞增多,血转氨酶升高。严重不良反应: 过敏性反应,伪膜性结肠炎。
药物相互作用
丙磺舒会降低本药的肾小管分泌。严重药物相互作用: 会增加氨基糖甙类和呋赛米的肾毒性。与抗凝剂同用可能引起出血。
对实验室检查结果的影响
导致直接血清抗人球蛋白试验和尿糖测试(Benedict,Fehling或非酶检测方法)结果假阳性。干扰Jaffe法血清肌酐测定结果。
与食物的相互作用
食物会引起本药血浆浓度轻微降低。
贮藏/有效期
口服给药: 存于15-30°C。
药理作用
头孢克洛与一个或多个青霉素结合蛋白结合,抑制细菌细胞壁内肽聚糖合成过程中的转肽作用,干扰肽聚糖的生物合成,使细胞壁的组装停止,导致细菌死亡。对革兰阴性菌,如致病大肠杆菌、肺炎链球菌、淋病奈瑟菌、奇异变形杆菌和流感嗜血杆菌有抗菌活性。
吸收: 口服胃肠道吸收良好;吸收率因进食而改变,但吸收程度不受影响。
分布: 在体内广泛分布;可穿过胎盘和进入乳汁(低浓度)。蛋白结合率:25%。
排泄:
在8小时内通过肾脏经尿液排泄(85%为原形药);绝大部分在2小时以内排出。消除半衰期:0.5-1小时,会因肾功能损伤而略微延长。血液透析可清除。
Chinese Name] cefaclor
[Category] antibiotic efficacy> cephalosporins
[Generic drug name] Cefaclor
[Alias] cefaclor ampicillin, Cephaclor, Ceclor, Alfatil, Distaclor, Gliamin, Keflor, Kefral, Panacef, Muco Panoral, Panoral, Lilly 99638, Ceclor CD, Distaclorin, Kefoclor, Kefolor, Kloclor, L-Kefral,
Name [CA]
5-Thia-1-azabicyclo [4,2,0] oct-2-ene-2-carboxylic acid, 7 - [[(2R) -aminophenylacetyl] amino] -3-chloro-8-oxo-, (6R, 7R) -
[CA registration number] [53994-73-3], [70356-03-5] (monohydrate)
[Structural formula]
【Molecular formula】 C15H14ClN3O4S
[Molecular weight] 367.806
[Index] Pharmacopoeia JP14, USP23
[Developer] Eli Lilly
[Listed] in 1979 for the first time, the United States, South Africa, United Kingdom and Germany
[Character]
[Use] semi-synthetic cephalosporin antibiotic effective oral, with part of the crystalline water of crystallization. Since the introduction of chlorine C3- bit enhanced antibacterial effect. And clinical commonly used oral cephalosporins such as cephalexin, cephradine compare this product against Gram positive and negative bacteria, including E. coli, Haemophilus influenzae, singular degeneration, typhoid bacillus, pneumococcus, staphylococcus aureus has a strong antibacterial activity, generally higher than cephalexin, cephradine better. Influenza bacillus and some intestinal bacteria cephalexin, cephradine 4-16 times stronger than cephalexin, stability β- lactamase varies with the type of enzyme.
Indications and Dosage different age groups of patients each
Oral administration
Applied to a urinary tract infection, upper and lower respiratory tract infections, skin infections, otitis media
Adults: cefaclor monohydrate: 250-500 mg, every 8 hours. Maximum dose: 4 g / day.
Children:> 1 month: 20 mg / kg / day, 3 times daily, increased to 40 mg / kg / day if necessary. <1 year old: 62.5mg, 3 times a day; 1-5 years old: 125 mg, 3 times a day;> 5 years of age: 250 mg, 3 times a day.
Medication and eating
Medication is not eating
Contraindications
Disable known allergy to cephalosporins.
Precautions
Caution in severe renal impairment who have a history of penicillin allergy, pregnant and lactating women.
Adverse reactions
Allergic reactions, diarrhea, nausea, vomiting, candidiasis, eosinophilia, elevated serum transaminases. Serious adverse reactions: allergic reactions, pseudomembranous colitis.
Drug Interactions
Probenecid reduces the renal tubular secretion of the drug. Serious drug interactions: aminoglycosides and furosemide increased renal toxicity meter race. And with the use of anticoagulants may cause bleeding.
Effects on laboratory test results
The direct antiglobulin test serum and urine tests (Benedict, Fehling non-enzymatic detection method) false positive results. Jaffe method for the determination of serum creatinine interference results.
Interaction with food
Food will cause a slight decrease in plasma concentration of the drug.
Storage / valid
Oral administration: kept in a 15-30 ° C.
Pharmacological effects
Cefaclor with one or more of the penicillin binding proteins, inhibit the synthesis of bacterial cell wall peptide glycan in the process of Thr, interference of peptidoglycan biosynthesis, cell wall assembly is stopped, resulting in bacterial death. Gram-negative bacteria, such as pathogenic E. coli, Streptococcus pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis and Haemophilus influenzae have antibacterial activity.
Absorption: good oral gastrointestinal absorption; absorption rate due to the consumption and change, but the extent of absorption is not affected.
Distribution: widely distributed in the body; can cross the placenta and enter the milk (low concentration). Protein binding: 25%.
Excretion:
Within eight hours through the kidneys through urine excretion (85% for the prototype drug); majority discharged within two hours. Elimination half-life: 0.5 hours due to renal damage and slightly extended. Hemodialysis can be cleared. |