Fosfomycin
Fosfomycin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Fosfomycin
ATX code: J01XX01
Active ingredient: fosfomycin (fosfomycin)
Producer: Krasfarma, JSC (Russia)
Description and photo updated: 22.11.2018
Prices in pharmacies: from 182 rubles.
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Fosfomycin is an antibacterial drug.
Release form and composition
Dosage form - powder for preparation of a solution for intravenous administration: hygroscopic, white or white with a yellowish tinge color (0.5 g - in 10 ml vials, in a cardboard box 1 or 10 vials; 1 g - in 10 or 20 ml vials, in a cardboard box 1 or 10 bottles; packaging for hospitals - in a cardboard box 50 bottles).
The composition of the powder contained in 1 bottle:
- active substance: disodium fosfomycin - 0.5 or 1 g (in terms of fosfomycin);
- auxiliary component: succinic acid - 0.0128 or 0.0255 g.
Pharmacological properties
Pharmacodynamics
Fosfomycin has bactericidal properties. The mechanism of its action is due to the ability to disrupt the synthesis of peptidoglycan of the bacterial cell wall in the early stages. Penetrating into the microbial cell through the transport systems of D-glucose-6-phosphate, fosfomycin irreversibly inhibits UDP-N-acetylglucosamienolpyruvyltransferase, an enzyme that catalyzes the formation of UDP-N-acetyl-3-0- (1-carboxyvinyl) -D-glucosamine from phosphoenolpyruvate and UDP-N-acetyl-D-glucosamine.
In vitro fosfomycin is active against the following microorganisms:
- gram-positive aerobes: Staphylococcus spp., including Staphylococcus aureus, Staphylococcus pyogenes, Staphylococcus epidermidis (including some methicillin-resistant strains), Streptococcus pneumoniae, Streptococcus antrum, Enterococillus antis, Faccalis, Enterococcus G, G and G
- gram-negative aerobes: Aeromonas hydrophila, Citrobacter spp., Campylobacter jejuni, Escherichia coli, Enterobacter spp. (moderately susceptible), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca (moderately susceptible), Morganella morganii (most strains are moderately susceptible), Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus mirabilis, Proteus retgaris, Providencia moderately susceptible marcescens, Salmonella spp., Shigella spp., Vibrio spp. (moderately sensitive), Yersinia enterocolitica;
- some anaerobes: Actinomyces spp., Peptococcus spp., Peptostreptococcus spp., Fusobacterium spp., Veillonella spp., Prevotella spp. and Clostridium perfringens (moderately sensitive).
The following microorganisms are resistant to the action of fosfomycin: Bacteroides spp., Mycobacterium spp., Listeria monocytogenes, Borrelia spp., Legionella spp., Acinetobacter spp., Enterococcus faecium.
Secondary resistance of bacteria to fosfomycin is rare.
Pharmacokinetics
After intravenous administration of fosfomycin at a dose of 1 g, the maximum plasma concentration is 46 mg / l and is noted after 15 minutes.
The drug is characterized by a very low binding to plasma proteins (1%).
Fosfomycin has a low molecular weight, due to which it is well distributed in many tissues and organs. In bactericidal concentrations, it is determined in the tissues of the eye, pleural fluid, tissues of the lungs, bile, peritoneal fluid, synovial fluid, muscles, subcutaneous fat, bones, endocardium of the heart valves.
In the case of inflammation of the meninges, the concentration of the drug in the cerebrospinal fluid increases significantly.
Fosfomycin penetrates and accumulates in phagocytes (macrophages and neutrophils). Quickly penetrates the blood-brain barrier. Penetrates the placenta. In small amounts excreted in breast milk.
Depending on the dose, the elimination half-life averages 1.5-2 hours in adults, 0.69-1.04 hours in children.
It is excreted mainly by the kidneys (from 90 to 100% of the dose) in the form of an active form during the day. A small part of the drug is excreted by the intestines, but this way of elimination is not essential.
Easily removed from plasma by hemodialysis.
Indications for use
According to the instructions, Fosfomycin is used to treat infectious and inflammatory diseases of the following body systems caused by susceptible microorganisms:
- lower respiratory tract (including pneumonia and infections in patients with cystic fibrosis);
- urinary tract (including acute pyelonephritis and exacerbation of chronic pyelonephritis);
- soft tissues (including burn wounds), including in patients with impaired peripheral circulation (diabetes mellitus, diseases of the arteries of the lower extremities);
- bones and joints;
- pelvic organs: endometritis, salpingitis, pelvioperitonitis;
- gastrointestinal tract: peritonitis, cholangitis, acute cholecystitis.
In combination with antibiotics of other groups, Fosfomycin is used to treat sepsis, bacterial endocarditis, infections of the central nervous system (bacterial meningitis, including postoperative).
Contraindications
- severe chronic renal failure (creatinine clearance <10 ml / min);
- children under 12 years old;
- hypersensitivity to the drug.
With care: chronic renal failure, liver disease, arterial hypertension, chronic heart failure, a history of allergic diseases, old age.
Instructions for the use of Fosfomycin: method and dosage
Fosfomycin is administered intravenously (IV) after preparation from a powder solution.
Adults are prescribed 2-4 g, the drug is administered at intervals of 6-8 hours.
For adolescents over 12 years old, the recommended daily dose is 0.2-0.4 g / kg, it is divided into 3 injections at intervals of 8 hours.
Correction of the dosage regimen is required for patients with renal failure: creatinine clearance 20-40 ml / min - 2-4 g every 12 hours, creatinine clearance 10-20 ml / min - 2-4 g every 24 hours.
Patients on hemodialysis require one additional dose (2–4 g) after each dialysis procedure.
Methods for preparing solutions and their introduction:
- direct jet intravenous injection: powder from one bottle (0.5 or 1 g) is dissolved in 20 ml of water for injection or 5% dextrose solution, administered within 5 minutes;
- rapid intravenous infusion: powder from one bottle is dissolved in water for injection, the resulting solution is added to 100-200 mg of infusion solution (sodium chloride solution 0.9%, dextrose 5%, Ringer's or Ringer's solution with lactate), injected within 30-60 minutes;
- long-term drip intravenous injection: powder from one bottle is dissolved in water for injection, the resulting solution is added to 200-500 ml of infusion solution, administered within 1-3 hours.
It should be borne in mind that when the drug dissolves, an exothermic reaction may occur.
Side effects
Possible common side effects (0.1–5%):
- from the digestive system: diarrhea;
- from the hepatobiliary system: liver dysfunction, including hyperbilirubinemia, increased lactate dehydrogenase, alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase;
- local reactions: soreness at the injection site, exanthema.
Possible rare side effects (<0.1%):
- from the digestive system: stomatitis, abdominal pain, nausea, vomiting, pseudomembranous colitis, anorexia, jaundice;
- from the nervous system: dizziness, paresthesia; when using high doses of the drug - convulsions;
- from the urinary system: impaired renal function, including an increase in the plasma concentration of urea, proteinuria, an increase / decrease in the concentration of sodium and potassium ions;
- on the part of the cardiovascular system: a feeling of palpitations;
- from the circulatory system: anemia, pancytopenia, leukopenia, agranulocytosis, thrombocytopenia, granulocytopenia, eosinophilia;
- allergic reactions: itching of the skin, urticaria, erythema, anaphylactic shock, cough, bronchospasm;
- local reactions: soreness along the vein, phlebitis;
- others: thirst, feeling of tightness in the chest, chest discomfort, malaise, fever, headache, peripheral edema.
Overdose
In case of overdose, diarrhea usually occurs.
Symptomatic treatment is performed. Drinking plenty of fluids is recommended to increase urine output.
special instructions
In severe infectious diseases, Fosfomycin is used in combination with other antibacterial agents (usually beta-lactam).
Before administering the drug, the doctor should study the patient's allergic history to assess the risk of developing anaphylactic shock.
Fosfomycin contains sodium ions (14.5 meq per 1 g). This must be taken into account when treating patients with chronic heart failure and chronic renal failure.
During treatment, all patients are recommended to periodically monitor the biochemical blood test, kidney and liver function.
Slow administration of the drug reduces the risk of pain at the injection site and the development of phlebitis.
Influence on the ability to drive vehicles and complex mechanisms
There is no information on the effect of Fosfomycin on psychophysical functions. However, there are known cases of side effects from the central nervous system, therefore, it is recommended to be careful when driving and working with complex mechanisms.
Application during pregnancy and lactation
During pregnancy, the use of Fosfomycin is possible if the expected benefits are higher than the potential risks.
Lactating women are advised to stop breastfeeding for the period of treatment.
Pediatric use
Fosfomycin is contraindicated in children under 12 years of age.
With impaired renal function
In chronic renal failure, the drug should be used with caution. In severe cases (creatinine clearance <10 ml / min), fosfomycin is contraindicated.
For violations of liver function
With caution, an antibiotic should be prescribed if the patient has concomitant liver diseases.
Use in the elderly
The antibacterial agent should be used with caution in the treatment of elderly patients.
Drug interactions
A pronounced synergistic effect is noted with the simultaneous use of cephalosporins, benzylpenicillins, aminoglycosides, fluoroquinolones, glycopeptides, carbapenems. This property of Fosfomycin is used in the treatment of severe infectious diseases and infections caused by multidrug-resistant pathogens (methicillin-resistant staphylococci, enterobacteria, enterococci, Pseudomonas aeruginosa).
Fosfomycin has physicochemical incompatibility with rifampicin, kanamycin, gentamicin, ampicillin and streptomycin, so they cannot be mixed in the same syringe / infusion system.
Analogs
Fosfomycin analogues are Ovea, Fosforal Rompharm, Monural, Urofoscin, Fosfomycin Esparma, Uronormin-F, Urofosfabol, Ekofomural.
Terms and conditions of storage
Shelf life is 2 years.
Store at temperatures up to 25 ° C in a dark place out of the reach of children.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Fosfomycin
According to reviews, Fosfomycin is an effective antibiotic most often used in the treatment of infectious diseases of the urinary system.
The price of Fosfomycin in pharmacies
The approximate price for Fosfomycin (1 g) is 487 rubles. per bottle.
Fosfomycin: prices in online pharmacies
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Drug name Price Pharmacy |
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Fosfomycin Esparma 3 g powder for oral solution 1 pc. 182 r Buy |
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Fosfomycin Esparma 3 g powder for prig. solution for internal reception package 8 g No. 1 378 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
