用户名： 密   码：
注册 | 忘记密码？
药品详细

Cloxacillin(氯唑西林)

化学结构式图
中文名
氯唑西林
英文名
Cloxacillin
分子式
C19H18ClN3O5S
化学名
(2S,5R,6R)-6-[3-(2-chlorophenyl)-5-methyl-1,2-oxazole-4-amido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
分子量
Average: 435.881
Monoisotopic: 435.065569098
CAS号
61-72-3
ATC分类
J01C Beta-lactam Antibacterials, Penicillins;J01C Beta-lactam Antibacterials, Penicillins;J01C Beta-lactam Antibacterials, Penicillins
药物类型
small molecule
阶段
approved
商品名
Novo-Cloxin;Nu-Cloxi;
同义名
Cloxacillin Sodium;
基本介绍

A semi-synthetic antibiotic that is a chlorinated derivative of oxacillin. [PubChem]

生产厂家
  • Apothecon inc div bristol myers squibb
  • Glaxosmithkline
  • Teva pharmaceuticals usa inc
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
  • Phenylpropenes
  • Penicillins
  • Polypeptides
  • Cinnamaldehydes
Substructures
  • Hydroxy Compounds
  • Acetates
  • Amino Ketones
  • Phenylpropenes
  • Benzene and Derivatives
  • Aliphatic and Aryl Amines
  • Isoxazoles
  • Aryl Halides
  • Carboxylic Acids and Derivatives
  • Halobenzenes
  • Beta Lactams
  • Penicillins
  • Thiazoles
  • Polypeptides
  • Heterocyclic compounds
  • Aromatic compounds
  • Cinnamaldehydes
  • Carboxamides and Derivatives
  • Oxazoles
  • Lactams
  • Imines
  • Azetidines
  • Thiazolidines
适应症
antibacterials 抗细菌;
药理
Indication Used to treat infections caused by penicillinase-producing staphylococci, including pneumococci, group A beta-hemolytic streptococci, and penicillin G-sensitive and penicillin G-resistant staphylococci.
Pharmacodynamics Cloxacillin is a semisynthetic antibiotic in the same class as penicillin. Cloxacillin is for use against staphylococci that produce beta-lactamase.
Mechanism of action By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, cloxacillin inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cloxacillin interferes with an autolysin inhibitor.
Absorption Well absorbed from the gastrointestinal tract.
Volume of distribution Not Available
Protein binding 95%
Metabolism
Not Available
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Oral LD50 in rat and mouse is 5000 mg/kg. Intravenous LD50 in rat is 1660 mg/kg. Symptoms of overdose include wheezing, tightness in the chest, fever, itching, bad cough, blue skin color, fits, and swelling of face, lips, tongue, or throat.
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility 13.9 mg/L Not Available
logP 2.48 SANGSTER (1994)
pKa 2.78 SANGSTER (1994)
Predicted Properties
Property Value Source
water solubility 5.32e-02 g/l ALOGPS
logP 2.61 ALOGPS
logP 2.3 ChemAxon
logS -3.9 ALOGPS
pKa (strongest acidic) 3.75 ChemAxon
pKa (strongest basic) -0.41 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 112.74 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 106.64 ChemAxon
polarizability 41.64 ChemAxon
药物相互作用
Drug Interaction
Demeclocycline Possible antagonism of action
Doxycycline Possible antagonism of action
Ethinyl Estradiol This anti-infectious agent could decrease the effect of the oral contraceptive
Mestranol This anti-infectious agent could decrease the effect of the oral contraceptive
Methacycline Possible antagonism of action
Methotrexate The penicillin increases the effect and toxicity of methotrexate
Minocycline Possible antagonism of action
Oxytetracycline Possible antagonism of action
Rolitetracycline Possible antagonism of action
Tetracycline Possible antagonism of action
食物相互作用
  • Take on an empty stomach.

返回 | 收藏