Pharmacology Of Fosfomycin

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 ±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