Fosfomycin

Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[1][2].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

Fosfomycin (80 mg/kg; i.v. or p.o.) displays the protective effect on the nephrotoxicity of double beckacin, and is not affected by different administration routes in rats[3]. Pharmacokinetic of Fosfomycin in Rats[4] Dibekacin Dose (mg) Vdss (l/kg) β (min-1) T1/2 (min) Urinary recovery (%) 30 0.261 0.0244 28.4 85 Animal Model: Fischer 344 rats[3] Dosage: 320 mg/kg Administration: Intramuscular injection, 5 schedules: 1 h, 0.5 h earlier than dibekacin, concomitantly, 0.5 h later and 1 h later; 11 days Result: Reduced polyuria, proteinuria, enzymes and cytosine caused by dibecacin (40 mg/kg), followed by the previous treatment. Animal Model: Dehydrated Wistar rat with acute renal failure (8-week-old)[4] Dosage: 120 mg/kg Administration: Intravenous injection; once Result: Recovered the exclusion rate of rats basically to normal, and improved the nephrotoxicity parameters. Protects proximal tubular lysosomes from aminoglycosides by inhibiting myeloid formation and protecting the integrity of lysosomal membrane of rats treated with double bekacin.

[1]. Falagas ME, et al. Fosfomycin. Clin Microbiol Rev. 2016 Apr. 29(2):321-47.

[2]. Dijkmans AC, et al. Fosfomycin: Pharmacological, Clinical and Future Perspectives. Antibiotics (Basel). 2017 Oct 31. 6(4):24.

[3]. Inouye S, et al. Mode of protective action of fosfomycin against dibekacin-induced nephrotoxicity in the dehydrated rats. J Pharmacobiodyn. 1982 Dec. 5(12):941-50.

DATA ITEMS CITED :

3

MOLECULAR FORMULA :

C3-H7-O4-P

MOLECULAR WEIGHT :

138.07

WISWESSER LINE NOTATION :

T3OTJ BPQQO C1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

4 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

MUTATION DATA

TYPE OF TEST :

Mutation in microorganisms

TEST SYSTEM :

Microorganism - not otherwise specified

DOSE/DURATION :

10 gm/L

REFERENCE :

MILEDM Microbios Letters. (Faculty Press, 88 Regent St., Cambridge, UK) V.1- 1976- Volume(issue)/page/year: 8,27,1978