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
Henan Tengmao Chemical Technology Co. LTD	+8615238638457	salesvip2@hntmhg.com	China	415	58
Shaanxi TNJONE Pharmaceutical Co., Ltd	+8618740459177	sarah@tnjone.com	China	893	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21691	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9348	55
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
HubeiwidelychemicaltechnologyCo.,Ltd	18627774460	faith@widelychemical.com	CHINA	742	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
SIMAGCHEM CORP	+86-13806087780	sale@simagchem.com	China	17367	58
Hefei TNJ Chemical Industry Co.,Ltd.	0551-65418671	sales@tnjchem.com	China	34572	58
Shaanxi Dideu Medichem Co. Ltd	+86-029-89586680 +86-18192503167	1026@dideu.com	China	9320	58

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