Cefodizime
(Synonyms: 头孢地嗪) 目录号 : GC39537
Cefodizime (CEF, CDZ) is an aminothiazolyl cephalosporin with a broad spectrum of antibacterial activity.
Cas No.:69739-16-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cefodizime (CEF, CDZ) is an aminothiazolyl cephalosporin with a broad spectrum of antibacterial activity.
[1] L B Barradell, R N Brogden. Drugs. 1992 Nov;44(5):800-34. [2] J Barré. J Antimicrob Chemother. 1990 Nov;26 Suppl C:95-101.
| Cas No. | 69739-16-8 | SDF | |
| 别名 | 头孢地嗪 | ||
| Canonical SMILES | O=C(C(N12)=C(CSC3=NC(C)=C(CC(O)=O)S3)CS[C@]2([H])[C@H](NC(/C(C4=CSC(N)=N4)=N\OC)=O)C1=O)O | ||
| 分子式 | C20H20N6O7S4 | 分子量 | 584.67 |
| 溶解度 | DMSO: 20.83 mg/mL (35.63 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7104 mL | 8.5518 mL | 17.1037 mL |
| 5 mM | 0.3421 mL | 1.7104 mL | 3.4207 mL |
| 10 mM | 0.171 mL | 0.8552 mL | 1.7104 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Cefodizime. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use
Drugs 1992 Nov;44(5):800-34.PMID:1280568DOI:10.2165/00003495-199244050-00008.
Cefodizime is a third generation cephalosporin with a broad spectrum of antibacterial activity. Administered intravenously or intramuscularly, Cefodizime 1 to 4 g daily for an average of 7 to 10 days produced clinical cure in 80 to 100% of patients (adults, elderly or children) with upper or lower respiratory tract infections or urinary tract infections, and in comparative trials Cefodizime was as effective as other third generation cephalosporins. A single dose of Cefodizime 1 or 2 g is also useful in treating lower urinary tract infections, particularly uncomplicated infections, with a rate of clinical success of 72 to 88%. Urogenital gonorrhoea, whether caused by beta-lactamase producing or non-beta-lactamase producing Neisseria gonorrhoeae, is very effectively treated by single dose therapy with intramuscular Cefodizime 0.25 to 1 g (virtually 100% cured). Preliminary data from a small number of patients indicate that Cefodizime may also be useful in the treatment of otitis media, sinusitis and gynaecological infections, and for the prophylaxis or treatment of surgical infections. The clinical efficacy of Cefodizime in comparison with other third generation cephalosporins is superior to that predicted from in vitro results. This superior activity of Cefodizime may be related to the relatively long elimination half-life of the drug or its ability to modify some functions of the immune system--a potentially important finding awaiting further investigation. Cefodizime is well tolerated and has a tolerability profile similar to other members of its class with systemic adverse events being primarily gastrointestinal or dermatological. Thus, limited comparative studies indicate Cefodizime has the potential to become a useful alternative to current antimicrobial therapy for the treatment of a variety of infections. Cefodizime may be more convenient to administer than some other agents of its class as it may be given once or twice daily. While there are no trials comparing Cefodizime to other third generation cephalosporins in immunosuppressed populations, preliminary information indicates Cefodizime may be useful in this group.
The in-vitro activity of Cefodizime: a review
J Antimicrob Chemother 1990 Nov;26 Suppl C:13-21.PMID:2074248DOI:10.1093/jac/26.suppl_c.13.
For Enterobacteriaceae, MIC50s and MIC90s of Cefodizime (mg/l), respectively, were as follows, for naturally non-beta-lactamase-producing species: Escherichia coli 0.12 and 0.5, Salmonella spp. and Shigella spp. 0.25 and 0.5, Proteus mirabilis 0.016 and 0.03; for chromosomal penicillinase-producing species. Klebsiella spp. 0.25 and 64, and for chromosomal cephalosporinase-producing species. Enterobacter cloacae 1 and 64, Citrobacter freundii 1 and 128, Serratia marcescens 2 and 8: indole-positive Proteus spp. 0.06 and 0.5; and Providencia stuartii 0.5 and 1. The activity of Cefodizime was not modified by plasmid-mediated penicillinase-producing strains but Cefodizime was inactive against cephalosporinase hyper-producing strains and against expanded broad-spectrum beta-lactamase-producing strains. Cefodizime was noticeably less active against Pseudomonas aeruginosa and Acinetobacter baumannii with MICs ranging from 32 to more than 128 mg/l. Haemophilus spp. and Neisseria gonorrhoeae, regardless of beta-lactamase producing status, as well as N. meningitidis, were highly susceptible (MIC50s and MIC90s less than or equal to 0.008 mg/l). Cefodizime was moderately active against methicillin-susceptible staphylococci (MIC50 and MIC90 8 mg/l) but failed to inhibit methicillin-resistant strains. Enterococci were generally resistant: Streptococcus pyogenes and Str. pneumoniae were inhibited by low concentrations (MIC50 and MIC90 0.12 and 0.5 mg/l). A fairly wide range of MICs was found for anaerobes, with lower values for Clostridium perfringens (MIC50 and MIC90 0.5 and 1 mg/l) than for Bacteroides fragilis (8- greater than 128 mg/l). These results show that Cefodizime has similar properties to other third generation cephalosporins and suggest that Cefodizime would find a role in the management of hospital infections.
Pharmacokinetic profile of Cefodizime
Infection 1992;20 Suppl 1:S14-7.PMID:1526669DOI:10.1007/BF01709944.
The pharmacokinetics of Cefodizime (CDZ) were determined after i.v. and i.m. administration of single doses of up to 2 g and after i.v. administration of 2 g b.i.d. for six days. Serum concentrations were adequately described by three exponential functions, with a terminal half-life of about 4 h. Serum and urine levels and amounts excreted were dose-proportional, and derived pharmacokinetic characteristics were dose-independent. Steady state was established after the second dose (b.i.d.). CDZ is 100% bioavailable after i.m. administration. Concomitant administration of lidocaine did not alter either bioavailability or pharmacokinetic characteristics. Following administration of 1 and 2 g i.m., Cmax was reached after 1.2 h and amounted to 60 and 140 mg/l, respectively. CDZ is 88% bound to plasma proteins. CDZ was predominantly eliminated by the kidneys (80% of dose), a further 20% being excreted in the bile. Metabolites were not detectable in serum or urine. Dose adjustment does not seem warranted in the elderly. For renally impaired patients with CLcr between 30 and 10 ml/min, the daily dose should not exceed 2 g. For patients with CLcr below 10 ml/min, individual adjustment is suggested. CDZ showed good penetration into tissues and biological fluids (lung, bronchial secretions, pleural fluid, kidney, prostate, urine, bone, muscle, skin, Fallopian tube) with long-lasting concentrations. In urine, therapeutic concentrations were present for more than 24 h after administration of 1 and 2 g. Thus, on the basis of its pharmacokinetic profile, Cefodizime is appropriate for effective treatment with once-daily administration.
Cefodizime as a biological response modifier: a review of its in-vivo, ex-vivo and in-vitro immunomodulatory properties
J Antimicrob Chemother 1990 Nov;26 Suppl C:37-47.PMID:2074251DOI:10.1093/jac/26.suppl_c.37.
Immunomodulation by antibacterial agents shows promise as a novel strategy in the treatment of infectious diseases. Cefodizime, a new oxi-imino-amino-2-thiazolyl cephalosporin, is a particularly good candidate in this context. In-vivo models of experimental infections show that prophylactic administration of Cefodizime increases the survival of some strains of mice after challenge with Toxoplasma gondii or Candida albicans; its curative effect in infections due to members of the Enterobacteriaceae is better than that expected from in-vitro MIC determinations relative to other third-generation cephalosporins; this effect is even more marked in immunocompromised animals. Data obtained both in vivo and ex vivo show that Cefodizime enhances various immune parameters such as phagocyte function, B lymphocyte responsiveness and delayed hypersensitivity; it may restore natural killer (NK) and phagocyte activity, as well as interleukin 1 (IL-1) and interferon production, in immunocompromised patients and animals. The in-vitro effects of this drug include enhancement of phagocyte bactericidal activity and alteration of bacterial virulence factors. The chemical basis for these various immunomodulatory properties is related to the thio-thiazolyl side-chain at position 3 of the cephem nucleus. To date, the mechanisms underlying the immunomodulatory properties of Cefodizime have not been identified clearly, but it is likely that it interferes at different levels of specific and non-specific immune defences.
Cefodizime, a new 2-aminothiazolyl cephalosporin: physicochemical properties, toxicology and structure-activity relationships
J Antimicrob Chemother 1990 Nov;26 Suppl C:1-8.PMID:2074243DOI:10.1093/jac/26.suppl_c.1.
Cefodizime is a 2-aminothiazolyl cephalosporin for parenteral use. Cefodizime has a bisubstituted thiothiazole moiety in position 3 of the cephem nucleus. The presence of this moiety does not alter the in-vitro antibacterial activity, or safety in animal studies, which are similar to those of cefotaxime, but results in an apparent long elimination half-life in rodents and dogs, and in novel immunological properties.