Fosfomycin trometamol - 5,631 g
in terms of fosfomycin - 3,0 g
Sucrose - 2,213 g
Tangerine flavor - 0,070 g
Orange flavor - 0,070 g
Sodium saccharin - 0,016 g
Package weight - 8,000 g
URONORMIN-F contains phosphomycin [mono (2-ammonium-2-hydroxymethyl-1,3-propanediol) (2R-cis) - (3-methyloxyranyl) phosphonate] - a broad-spectrum antibacterial agent, a derivative of phosphonic acid, designed to treat infections urinary tract.
The mechanism of action is associated with the suppression of the first stage of the synthesis of the bacterial cell wall. Being a structural analogue of phosphoenolpyruvate, it competitively inhibits the enzyme UDP-N-acetylglucosaminololpyruvyltransferase, which catalyzes the formation of UDP-N-acetyl-3-O- (1-carboxyvinyl) -D-glucosamine from phosphoenolpyruvate and UDP-N-glucose . Also, the drug is able to reduce the adhesion of bacteria to the mucous membranes of the bladder, which can play the role of a predisposing factor for recurrent infections.
The mechanism of action of the drug explains the lack of cross-resistance with other classes of antibiotics and the mutual enhancement of action with antibiotics of other classes, for example, beta-lactam antibiotics.
Fosfomycin is active against a wide range of gram-positive and gram-negative microorganisms, usually excreted in urinary tract infections, such as Escherichiacoli, Citrobacterspp., Klebsiellaspp., Proteusspp., Serratiaspp., Pseudomonasaeruginosa, Enterrococcusfaecalis.
The emergence of resistance in the laboratory is due to a mutation of the glpT and uhp genes that control the transport of L-alpha-glycerophosphates and glucose phosphates, respectively.
When taken orally, fosfomycin is well absorbed from the intestine and reaches a bioavailability of about 50%. The maximum plasma concentration is observed
2-2.5 hours after oral administration and is 22-32 mg / L. The plasma half-life is 4 hours. Food intake slows down absorption, without affecting the concentration in the urine.
Fosfomycin is distributed in the kidneys, bladder walls, prostate and seminal glands. A constant concentration of fosfomycin in urine, exceeding the Minimum Bacteriostatic concentration (MBsK), is achieved 24-48 hours after oral administration. Fosfomycin does not bind to plasma proteins and crosses the placental barrier. After a single injection, fosfomycin is excreted in breast milk in small quantities.
Fosfomycin is excreted unchanged, mainly by the kidneys, by glomerular filtration (40-50% of the dose taken is found in the urine), with a half-life of about 4 hours, and to a lesser extent with feces (18-28% of the dose). The occurrence of a second peak concentration in serum after 6 and 10 hours after taking the drug suggests that the drug is susceptible to enterohepatic recirculation.The pharmacokinetic properties of fosfomycin are independent of age and pregnancy. The drug is cumulated in patients with renal failure; between the pharmacokinetic parameters of fosfomycin and glomerular filtration rate a linear relationship was established.
Prevention of urinary tract infections during surgical interventions and transurethral diagnostic examinations.
Pregnancy and lactation
Data from a limited number of pregnancies studied does not show adverse effects on pregnancy, the fetus, or the health of the newborn.
If necessary, the appointment of the drug during breastfeeding should stop breastfeeding during treatment.
- severe renal failure (creatinine clearance <10 ml / min);
- children's age up to 5 years (for a dosage of 2 g), children's age up to 12 years (for a dosage of 3 g);
- deficiency of sucrose / isomaltase;
- fructose intolerance;
- glucose-galactose malabsorption.
The following are adverse reactions that have been reported with fosfomycin during clinical trials or post-registration observation.
The frequency of reactions is indicated as follows: very often (≥ 1/10); often (≥ 1/100 - <1/10); infrequently (≥ 1/1 000 - <1/100); rarely (≥ 1/10 000 - <1/1 000); very rarely (<1/10 000); unknown - the incidence of adverse reactions cannot be estimated based on available data.
In each group, adverse reactions are presented in decreasing order of severity.
Infectious and parasitic diseases:
Immune system disorders:
Unknown: anaphylactic reactions, including anaphylactic shock, hypersensitivity
Disorders of the nervous system:
Infrequent: headache, dizziness
Very Rare: Tachycardia
Disorders from the respiratory system, chest and mediastinal organs:
Unknown: asthma, bronchospasm, shortness of breath
Disorders of the gastrointestinal tract:
Infrequently: diarrhea, nausea, dyspepsia
Rarely: abdominal pains, vomiting
Unknown: antibiotic-associated colitis, decreased appetite
Disorders of the skin and subcutaneous tissue:
Rarely: rash, urticaria, pruritus.
General disorders and disorders at the injection site:
Unknown: decrease in blood pressure, petechiae
Disorders from the liver and biliary tract:
Unknown: short-term increase in the activity of alkaline phosphatase and “liver” transaminases
Disorders from the blood and lymphatic system:
Rarely: aplastic anemia.
Unknown: eosinophilia, thrombocytosis (petechiae).
The simultaneous use of antacids or calcium salts leads to a decrease in the concentration of fosfomycin in blood plasma and urine. Drugs that increase motor activity (motility) of the gastrointestinal tract can cause a similar effect (a decrease in the concentration of fosfomycin in blood plasma and urine).
There may be specific problems associated with a change in the international normalized ratio (INR). In patients receiving antibiotics, numerous cases of increased activity of antivitamin K antagonists have been reported.
In the presence of risk factors such as severe infection, inflammation, age, or poor general health, an INR change can be due to both an infectious disease and a consequence of its treatment. Such changes are considered more characteristic for the following classes of antibiotics: fluoroquinolones, macrolides, cyclins, cotrimoxazole and some cephalosporins.
How to take, course of administration and dosage
The powder is dissolved in 1/2 cup of water (50-75 ml) or another drink, mixed until completely dissolved, taken immediately after dissolution. Uronormin-F is used once a day inside an empty stomach 1 hour before or 2-3 hours after a meal, preferably before bedtime, after emptying the bladder.
Adults and children from 12 to 18 years: 1 packet (3 g) once a day once.
In order to prevent urinary tract infection during surgery, transurethral diagnostic procedures, fosfomycin is taken 2 times 3 g each: 3 hours before the intervention and 24 hours after the intervention.
Children from 5 to 12 years: 1 packet (2 g) once a day once. In order to prevent urinary tract infection during surgery, transurethral diagnostic procedures, fosfomycin is taken 2 times 2 g: 3 hours before the intervention and 24 hours after the intervention.
In more severe cases (elderly patients, recurrent infections) take another 1 packet after 24 hours.
In patients with mild or moderate severity of renal failure, dose adjustment is not required.
In patients with severe renal failure or on hemodialysis, the use of the drug is contraindicated. In patients with hepatic insufficiency, dose adjustment is not required.
Overdose treatment is symptomatic and supportive.
In case of an overdose, it is recommended that fluid be taken orally to increase urine output.
The use of almost all antibacterial agents, including fosfomycin, can lead to antibiotic-associated diarrhea. Its severity can range from mild diarrhea to fatal colitis.
Diarrhea, especially severe, persistent and / or blood-streaked, observed during or after treatment with phosphomycin (including, within a few weeks after treatment), may be a symptom of pseudomembranous colitis caused by Clostridium difficile.
With a suspected or confirmed diagnosis of pseudomembranous colitis, treatment should be started immediately. Drugs that suppress intestinal motility, are contraindicated in this clinical situation.
Application for renal failure: the concentration of fosfomycin in the urine is maintained for 48 hours after taking the usual dose if creatinine clearance is higher than 10 ml / min. The drug is contraindicated in patients undergoing hemodialysis.
Patients with diabetes should be aware that 1 packet of the drug with a dosage of 2 g or 3 g of phosphomycin contains 2,100 g or 2,213 g of sucrose, respectively.
For patients with rare hereditary diseases such as fructose intolerance, glucose-galactose malabsorption, or sucrose-isomaltase deficiency, this drug is contraindicated.Influence on the ability to drive vehicles, mechanisms.
Patients should be warned about the possibility of developing dizziness, and when dizziness occurs, one should refrain from performing these types of activities.
Store at a temperature not exceeding 25 ° C.Keep out of the reach of children.