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Fosfomycin
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Pregnancy/Breast-Feeding Implications
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Administration
Monitoring Parameters
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Dosage Forms
References

Pronunciation
(fos foe MYE sin)

U.S. Brand Names
Monurol™

Generic Available

No


Synonyms
Fosfomycin Tromethamine

Pharmacological Index

Antibiotic, Miscellaneous


Use

A single oral dose in the treatment of uncomplicated urinary tract infections in women due to susceptible strains of E. coli and Enterococcus; multiple doses have been investigated for complicated urinary tract infections in men; may have an advantage over other agents since it maintains high concentration in the urine for up to 48 hours


Pregnancy Risk Factor

B


Pregnancy/Breast-Feeding Implications

Breast-feeding/lactation: Milk concentration approximates 10% of plasma


Adverse Reactions

>1%:

Central nervous system: Headache

Dermatologic: Rash

Gastrointestinal: Diarrhea (2% to 8%), nausea, vomiting, epigastric discomfort, anorexia

<1%: Dizziness, drowsiness, fatigue, pruritus


Overdosage/Toxicology

Symptomatic and supportive treatment is recommended in the event of an overdose.


Drug Interactions

Decreased effect: Antacids or calcium salts may cause precipitate formation and decrease fosfomycin absorption

Metoclopramide: Increased gastrointestinal motility may lower fosfomycin tromethamine serum concentrations and urinary excretion. This drug interaction possibly could be extrapolated to other medications which increase gastrointestinal motility.


Mechanism of Action

As a phosphonic acid derivative, fosfomycin inhibits bacterial wall synthesis (bactericidal) by inactivating the enzyme, pyruvyl transferase, which is critical in the synthesis of cell walls by bacteria; the tromethamine salt is preferable to the calcium salt due to its superior absorption


Pharmacodynamics/Kinetics

Absorption: Well absorbed

Distribution: Vd: 2 L/kg; high concentrations in urine; distributed well into other tissues, crosses maximally into CSF with inflamed meninges

Protein binding: Minimal (<3%)

Metabolism: None

Bioavailability: 34% to 58%

Half-life: 4-8 hours; prolonged in renal failure (50 hours with Clcr <10 mL/minute)

Time to peak serum concentration: 2 hours

Elimination: High urinary levels persist for >48 hours (100 mcg/mL); excreted unchanged


Usual Dosage

Adults: Urinary tract infections: Oral:

Male: 3 g once daily for 2-3 days for complicated urinary tract infections

Dosing adjustment in renal impairment: Decrease dose; 80% removed by dialysis, repeat dose after dialysis

Dosing adjustment in hepatic impairment: No dosage decrease needed


Administration

Always mix with water before ingesting; do not give in its dry form; pour contents of envelope into 90-120 mL of water (not hot), stir to dissolve. Drink immediately after dissolving.


Monitoring Parameters

Signs and symptoms of urinary tract infection


Mental Health: Effects on Mental Status

May cause drowsiness


Mental Health: Effects on Psychiatric Treatment

None reported


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

May be taken with or without food; avoid use of antacids or calcium salts within 4 hours before or 2 hours after taking fosfomycin; contact your physician if signs of allergy develop; if symptoms do not improve after 2-3 days, contact your healthcare provider


Dosage Forms

Powder, as tromethamine: 3 g, to be mixed in 4 oz of water


References

Patel SS, Balfour JA, and Bryson HM, "Fosfomycin Tromethamine. A Review of Its Antibacterial Activity, Pharmacokinetic Properties, and Therapeutic Efficacy as a Single-Dose Oral Treatment for Acute Uncomplicated Lower Urinary Tract Infections," Drugs, 1997, 53(4):637-56.


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