Cefotaxime

Cefotaxime 속성

Cefotaxime C화학적 특성, 용도, 생산

개요

Like other third-generation cephalosporins, it has excellent anti-Gram-negative activity and is useful institutionally. It has a metabolically vulnerable acetoxy group attached to C-3 and loses approximately 90% of its activity when this is hydrolyzed. This metabolic feature also complicates the pharmacokinetic data, because both active forms are present and have different properties. Cefotaxime should be protected from heat and light and may color slightly without significant loss of potency. Like other third-generation cephalosporins, cefotaxime has less activity against staphylococci but has greater activity against Gram-negative organisms.

용도

Cefotaxime has a broad spectrum of antibicrobial use. It acts bactericidally. It is highly active with respect to Gram-negative microorganisms (E. coli, Citrobacter, Proteus mirabilis, P. indole, Providencia, Klebsiella, Serratia), and a few strains of Pseudomonas, H. influenzae that are resistant to other antibiotics. Cefotaxime is less active with respect to streptococci, pneumococci, meningococci, gonococci, and bacteroides. It is resistant to the majority of beta-lacatamases of Gram-positive and Gram-negative microorganisms.
This drug is used for severe bacterial infections caused by microorganisms that are sensitive to the drug such as peritonitis, sepsis, abdominal infections, infections of the pelvis minor, infections of the lower respiratory tract, urinary tract, bones, joints, skin, soft tissues, and infected wounds and burns. Synonyms of this drug are claforan, zarivis, and others.

Antimicrobial activity

The aminothiazoyl and methoximino groups at the 7-amino position confer, respectively, potent activity against many Gram-negative rods and cocci and stability to most β-lactamases. Ps. aeruginosa, Sten. maltophilia and other pseudomonads are often resistant. Brucella melitensis and some strains of Nocardia asteroides are susceptible. Activity against L. monocytogenes and B. fragilis is poor.

원료

Many enterobacteria resistant to other b-lactam agents are susceptible, but selection of resistant strains with derepressed chromosomal molecular class C cephalosporinases may occur. Gram-negative bacilli producing variants of the TEM enzymes (pp. 230–231) are resistant.

Pharmacokinetics

C_max 500 mg intramuscular: 10–15 mg/L after 0.5–1 h
1 g intravenous (15-min infusion): 90 mg/L end infusion
Plasma half-life: c.1 h
Volume of distribution: 32–37 L
Plasma protein binding: c. 40%
Distribution
It is widely distributed, achieving therapeutic concentrations in sputum, lung tissue, pleural fluid, peritoneal fluid, prostatic tissue and cortical bone. In patients receiving 2 g every 8 h, mean CSF concentrations in aseptic meningitis were 0.8 mg/L. Levels of 2–15 mg/L can be found in the CSF in the presence of inflammation after doses of 50 mg/kg by intravenous infusion over 30 min. A single intraventricular dose of 40 mg/kg produced levels at 2, 4 and 6 h of 6.4, 5.7 and 4.5 mg/L, respectively.
Metabolism
About 15–25% of a dose is metabolized by hepatic esterases to the desacetyl form, which may have some clinical importance because of its concentration in bile and accumulation in renal failure. Desacetylcefotaxime has about 10% of the activity of the parent against enterobacteria, less against Staph. aureus. Its half-life in normal subjects is around 1.5 h.
Excretion
Elimination is predominantly by the renal route, more than half the dose being recovered in the urine over the first 24 h, about 25% as the desacetyl derivative. Excretion is depressed by probenecid and declines in renal failure with accumulation of the metabolite. In patients with creatinine clearances in the range 3–10 mL/min, the plasma half-life rose to 2.6 h while that of the metabolite rose to 10 h.

Clinical Use

Cefotaxime is widely used in neutropenic patients, respiratory infection, meningitis, intra-abdominal sepsis, osteomyelitis, typhoid fever, urinary tract infection, neonatal sepsis and gonorrhea.

부작용

Minor hematological and dermatological side effects common to group 4 cephalosporins have been described. Superinfection with Ps. aeruginosa in the course of treatment has occurred. Occasional cases of pseudomembranous colitis have been reported.

Cefotaxime 준비 용품 및 원자재

원자재

준비 용품

Cefotaxime 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Taizhou Huaxi Technology Co. LTD	0576-89164227 13105618688	18323010@qq.com	China	39	58
Zhejiang Chenxi Technology Co., LTD	13552015630	3558143071@qq.com	China	510	58
Lanzhou Dawnrays Pharmaceutical Co Ltd	0931-0931-4910898 19913936884	sales@dawnrays.com	China	40	58
JinYan Chemicals(ShangHai) Co.,Ltd.	13817811078	sales@jingyan-chemical.com	China	9963	60
Adamas Reagent, Ltd.	4006009262 13023226327	hmj@titansci.com	China	14098	59
XiaoGan ShenYuan ChemPharm co,ltd	15527621225; 15527621225	1791901229@qq.com	China	6717	52
Beijing Isomersyn Technology CO;LTD	010-82954736 13391601435	sales@isomersyn.com	China	3294	57
Hunan Hui Bai Shi Biotechnology Co., Ltd.	0731-85526065 13308475853	ivy@hnhbsj.com	China	4999	62
ShangHai YuanYe Biotechnology Co., Ltd.	18916372613	shyysw007@163.com	China	4993	60
S.Z. PhyStandard Bio-Tech. Co., Ltd.	0755-83725681-603		China	4484	50

Cefotaxime 관련 검색: