药品详细

Cefmetazole(头孢美唑)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

头孢美唑

英文名

Cefmetazole

分子式

C₁₅H₁₇N₇O₅S₃

化学名

(6R,7S)-7-{2-[(cyanomethyl)sulfanyl]acetamido}-7-methoxy-3-{[(1-methyl-1H-1,2,3,4-tetrazol-5-yl)sulfanyl]methyl}-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid

分子量

Average: 471.534
Monoisotopic: 471.045328759

CAS号

56796-20-4

ATC分类

J01D Other Beta- lactam Antibacterials

药物类型

small molecule

阶段

approved

商品名

Zefazone;

同义名

Cefmetazole sodium;Cefmetazolo [INN-Spanish];Cefmetazolum [INN-Latin];

基本介绍

A semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. It has a high rate of efficacy in many types of infection and to date no severe side effects have been noted. [PubChem]

生产厂家

Pharmacia and upjohn co

封装厂家

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Ethers
Nitriles and Derivatives
Cephalosporins

Substructures

Ethers
Hydroxy Compounds
Acetates
Amino Ketones
Carboxylic Acids and Derivatives
Nitriles and Derivatives
Aliphatic and Aryl Amines
Aminals and Derivatives
Beta Lactams
Enamines
Cyanides
Tetrazoles
Heterocyclic compounds
Aromatic compounds
Carboxamides and Derivatives
Cephalosporins
Lactams
Azetidines
Cyanamides

适应症

antibacterials 抗细菌;

药理

Indication	For the treatment of infections caused by susceptible organisms.
Pharmacodynamics	Cefmetazole is a second-generation cephalosporin. The cephalosporins are bactericidal drugs with both gram-positive and gram-negative activity. They inhibit bacterial cell wall synthesis in a way similar to the penicillins. Cefmetazole is more active than 1st-generation cephalosporins against indole-positive Proteus, Serratia, anaerobic gram-negative bacilli (including B. fragilis), and some E. coli, Klebsiella, and P. mirabilis, but is less active than cefoxitin or cefotetan against most gram-negative bacilli.
Mechanism of action	The bactericidal activity of cefmetazole results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs).
Absorption	Bioavailability is approximately 100% following intramuscular injection.
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	No appreciable metabolism.
Route of elimination	Not Available
Half life	1.50 ±0.14 hours
Clearance	Not Available
Toxicity	Oral LD₅₀ in rats is 3,204 mg/kg. With other b-lactam antibiotics, adverse effects following overdosage have included nausea, vomiting, epigastric distress, diarrhea, and convulsions.
Affected organisms	Enteric bacteria and other eubacteria
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
water solubility	94.2 mg/L	Not Available
logP	-0.60	SANGSTER (1993)

Predicted Properties

Property	Value	Source
water solubility	2.16e+00 g/l	ALOGPS
logP	-0.38	ALOGPS
logP	-0.65	ChemAxon
logS	-2.3	ALOGPS
pKa (strongest acidic)	3.38	ChemAxon
pKa (strongest basic)	-1.7	ChemAxon
physiological charge	-1	ChemAxon
hydrogen acceptor count	9	ChemAxon
hydrogen donor count	2	ChemAxon
polar surface area	163.33	ChemAxon
rotatable bond count	9	ChemAxon
refractivity	124.57	ChemAxon
polarizability	44.5	ChemAxon

药物相互作用

Drug	Interaction
Probenecid	Probenecid may increase the serum level of cefmatzole.

食物相互作用

Not Available

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