Fosfomycin sodium, a broad-spectrum antibiotic of Gram-positive and Gram-negative bacteria with excellent curative effect

Fosfomycin sodium is a compound with the appearance of white or off-white powder at room temperature, hygroscopic, freely soluble in water or aqueous solution.

Mechanism

Fosfomycin Sodium, is a derivate of fosfomycin, a type of macrolide antibiotics, which was first isolated from Streptomyces fradicle in 1960s and has been used as human medicine and veterinary medicine for over 50 years. Fosfomycin Sodium is a competitive inhibitor of a bacterial cell wall synthesis enzyme, inhibiting the first synthesis reaction of the bacterial cell wall by hindering the utilization of related substances.

Features

· Broad spectrum antibiotic

Fosfomycin sodium is a broad-spectrum antibiotic of Gram-positive and Gram-negative bacteria, for instance E. coli, S. aureus, Serratia, Klebsiella, Citrobacter, Enterococcus, and Enterobacter etc. and is wildly used in the treatment of infection of respiratory, urinary, intestinal, genital systems etc..

· Rapid sterilization

With the characteristics of low molecular weight and high hydrophilicity Fosfomycin Sodium appears good distribution in fluid and strong penetration. So this medicine can widely distribute in body fluid and tissue to increase curative effect. About 25% of the E. coli were killed at 1 hour after exposured to Fosfomycin Sodium (12.5μg/ml), and all died within 4-6 hours. Pseudomonas aeruginosa and Staphylococcus aureus were also all killed at 4 and 8 hours.

· Low toxicity and residue

Fosfomycin Sodium shows little irritation on the body, no acute toxicity and adverse reactions. Single dose will be eliminated by kidney in 18-72 hours for muscles and organs to reach the residual standard with no increasing burden on the kidney.

· Extensive usage

Fosfomycin Sodium is wildly used for human and livestock in all countries with no restriction in regulation.

Sythesis

The Synthesis of Fosfomycin Sodium starts from fosfomycin phenylethylamine. Basic fosfomycin sodium (PH 9.0-10.5) was obtained through the reaction between fosfomycin phenylethylamine with NaOH or MeONa. Basic crude production recrystallizes in acetone to obtain neutral fosfomycin phenylethylamine.

Clinical Application

Fosfomycin Sodium is wildly use for the treatment of infections caused by Staphylococcus aureus, Escherichia coli, Proteus and Shigella etc.. It is usually used to treat uncomplicated urinary tract infections and to reduce nephrotoxicity and ototoxicity of platinum-containing anti-tumor agents. It is also used for susceptibility studies of Klebsiella pneumoniae and to study in vitro susceptibility testing procedures for fosfomycin tromethamine.

Usage and dosage

· Fosfomycin Sodium For Human

I.v.drip: dissolve in sterilized water, then dilute it into 250-500ml 5% glucose injection or sodium chloride injection for intravenous infusion.

Adult: 4-12g/day in 2-3 times;

Child: 0.1-0.3 per kg/day in 2-3 times.

· Fosfomycin Sodium On Veterinary

Drinking water：5-10g/100kg in water, twice daily for 3 days;

Mixed feed: 10-15g/100kg in feed, twice daily for 3 days.

Combination therapy

Intestinal infections: combine with β-lactam, aminoglycoside;
Respiratory and lung infections: combine with macrolides, β-lactam;
Staph infections: combine with erythromycin, rifampin;
Acute respiratory infections, sepsis, peritonitis etc.: increase the dose and combine with β-lactams or aminoglycosides.

Cautions

It may cause mild gastrointestinal reaction as Fosfomycin Sodium‘s Side Effects, for instance nausea, anorexia, epigastric discomfort, loose stools or mild diarrhea, which generally does not affect the continuous dosing.

Phlebitis is occasionally reported at high dose and rapid drip in i.v.drip, so the speed of drip should be in control.

Liver function should be monitored in large-dose therapy.

When use as veterinary medicine, Fosfomycin Sodium used for pigs, chickens and fish mainly; therapy for other animals should be under veterinary guidance.