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药品详细

Fosfomycin (磷霉素 )

化学结构式图
中文名
磷霉素
英文名
Fosfomycin
分子式
Not Available
化学名
[(2R,3S)-3-methyloxiran-2-yl]phosphonic acid
分子量
Average: 138.059
Monoisotopic: 138.008195224
CAS号
23155-02-4
ATC分类
J01X Other Antibacterials
药物类型
small molecule
阶段
商品名
Monurol;Veramina;
同义名
Fosfocina;Fosfomycin disodium salt;Fosfomycin sodium;Fosfonomycin;Phosphomycin;phosphomycin disodium salt;Phosphonomycin;
基本介绍

An antibiotic produced by Streptomyces fradiae. [PubChem]

生产厂家
  • Zambon spa italy
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
Form Route Strength
Powder Oral
规格
Unit description Cost Unit
Monurol 3 gm Packets 50.87 USD packet
Monurol 3 gm sachet 47.07 USD each
Viramune 200 mg tablet 9.48 USD tablet
化合物类型
Type small molecule
Classes
  • Phosphonic Acids and Derivatives
Substructures
  • Hydroxy Compounds
  • Phosphonic Acids and Derivatives
  • Ethers
  • Heterocyclic compounds
  • Phosphinic Acids and Derivatives
  • Epoxides
适应症
antibacterials 抗细菌;
药理
Indication For the treatment of uncomplicated urinary tract infections (acute cystitis) in women due to susceptible strains of Escherichia coli and Enterococcus faecalis.
Pharmacodynamics Fosfomycin is a broad spectrum antibiotic that concentrates in kidney and bladder and is used to treat uncomplicated urinary tract infections. Fosfomycin also reduces nephrotoxicity and ototoxicity of platinum-containing anti-tumor agents.
Mechanism of action Fosfomycin is a phosphoenolpyruvate analogue produced by Streptomyces that irreversibly inhibits enolpyruvate transferase (MurA), which prevents the formation of N-acetylmuramic acid, an essential element of the peptidoglycan cell wall.
Absorption Fosfomycin tromethamine is rapidly absorbed following oral administration and converted to fosfomycin. Oral bioavailability under fasting conditions is 37%. When given with food, oral bioavailability is reduced to 30%
Volume of distribution
  • 136.1 卤44.1 L
Protein binding 0% (not bound to plasma proteins)
Metabolism

No transformation, excreted unchanged

Route of elimination Fosfomycin is excreted unchanged in both urine and feces.
Half life 5.7 (± 2.8) hours. The elimination half-life is 40 hours in anuric patients undergoing hemodialysis.
Clearance
  • 16.9 +/- 3.5 L/hr
Toxicity LD50>5 g/kg (rats). Side effects may include diarrhea
Affected organisms
  • Enteric bacteria and other eubacteria
Pathways Not Available
理化性质
Properties
State solid
Melting point 94 oC
Experimental Properties
Property Value Source
water solubility 50 mg/mL (Sodium salt) PhysProp
logP -1.6 PhysProp
Predicted Properties
Property Value Source
water solubility 4.69e+01 g/l ALOGPS
logP -0.86 ALOGPS
logP -0.74 ChemAxon Molconvert
logS -0.47 ALOGPS
pKa 7.82 ChemAxon Molconvert
hydrogen acceptor count 4 ChemAxon Molconvert
hydrogen donor count 2 ChemAxon Molconvert
polar surface area 70.06 ChemAxon Molconvert
rotatable bond count 1 ChemAxon Molconvert
refractivity 25.87 ChemAxon Molconvert
polarizability 10.81 ChemAxon Molconvert
药物相互作用
食物相互作用
  • Food decreases Cmax slightly.
  • Take without regard to meals.

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