Universal reference book for medicines
Name of the drug: UROFOSFABOL ® (UROFOSFABOL)

Active substance: fosfomycin

Type: Antibiotic group of phosphonic acid derivatives

Manufacturer: АБОЛмед (Russia)
Composition, form of production and packaging
Powder for the preparation of a solution for intravenous administration of
white or white with a yellowish hue.

1 f.

phosphomycin (in the form of a disodium salt) 1 g

Auxiliary substances: succinic acid 0.0255 g.

1 g - bottles (1) - packs of cardboard.

Powder for the preparation of a solution for intravenous administration of white or white with a yellowish hue.

1 f.

phosphomycin (in the form of a disodium salt) 2 g

Auxiliary substances: succinic acid 0.04 g.

2 g - vials (1) - packs of cardboard.

Powder for the preparation of a solution for intravenous administration of white or white with a yellowish hue.

1 f.

phosphomycin (in the form of a disodium salt) 4 g

Auxiliary substances: succinic acid 0.102 g.

4 g - bottles (1) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2010.

PHARMACHOLOGIC EFFECT

Antibiotic group of phosphonic acid derivatives.

The bactericidal effect of phosphomycin is based on the disturbance at the early stages of peptidoglycan synthesis of the bacterial cell wall.
Penetrating into the microbial cell via D-glucose-6-phosphate transport systems, the drug irreversibly inhibits the uridine-diphospho-N-acetylglucosamine-3-0-enolpyruvattransferase (MurA) enzyme, which is involved in the synthesis of uridine-diphospho-N-acetylmuraminic acid from uridine - N-acetylglucosamine.
It is active against gram-positive aerobes: Staphylococcus aureus, Staphylococcus epidermidis (including some strains resistant to methicillin), Staphylococcus spp., Streptococcus pyogenes, Streptococcus viridans, Streptococcus groups C, F, G, Streptococcus pneumoniae, Enterococcus faecalis, Bacillus anthracis;
Gram-negative aerobes: Aeromonas hydrophila, Citrobacter spp., Campylobacter jejuni, Escherichia coli, Enterobacter spp. (moderately sensitive), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca, Morganella morganii (most strains are moderately sensitive), Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri (moderately sensitive), Pseudomonas aeruginosa, Serratia marcescens, Salmonella spp., Shigella spp., Vibrio spp.(moderately sensitive), Yersinia enterocolitica; anaerobes: Actinomyces spp., Peptococcus spp., Peptostreptococcus spp., Fusobacterium spp., Veillonella spp.
The drug is moderately sensitive Clostridium perfringens, Prevotella spp.

The drug is resistant to Legionella spp., Borrelia spp., Listeria monocytogenes, Mycobacterium spp., Bacteroides spp., The majority of intracellular pathogens (Coxiella burnetii, Rickettsia spp., Chlamydia spp., Mycoplasma pneumoniae, Ureaplasma urealyticum).

The secondary resistance of microorganisms to Urophosfabol is rare.
A valuable property of the drug is the lack of cross-resistance with other antibacterial agents. It exhibits synergism in combination with beta-lactam antibiotics, aminoglycosides and vancomycin.
PHARMACOKINETICS

Distribution

15 minutes after intravenous administration of the drug at a dose of 500 mg and 1 g, serum phosphomycin concentration is 28 mg / L and 46 mg / L, respectively;
after 1 h they are halved. With a slow (within 30-40 min) infusion of large doses of the drug (4 g every 6 h) C max is more than 250 mg / l. In the intervals between administrations, the phosphomycin content in the plasma is not less than 20 mg / l.
The binding of phosphomycin to plasma proteins is low - 1%.

Due to its low molecular weight, phosphomycin is well distributed in many organs and tissues of the body.
Bactericidal concentrations are determined in the tissues of the lung, pleural fluid, peritoneal fluid, bile, subcutaneous fat, muscle, bones, synovial fluid, eye tissues, endocardial valvular valves. Rapidly penetrates the BBB. The concentration of the drug in the cerebrospinal fluid increases significantly with inflammation of the meninges. It penetrates and accumulates in phagocyte cells (neutrophils and macrophages). Passes through the placenta. In small concentrations excreted in breast milk.
Excretion

T 1/2 is, on average, 1.5-2 hours in adults and 0.69 to 1.04 hours, depending on the dose, in children.
The main way to excrete phosphomycin is renal (90-100% of the administered dose during the day). With the urine, the active form of the drug is displayed. A small part of the injected antibiotic is excreted with bile, however this way of elimination does not have a significant significance. Fosfomycin can be easily removed from the plasma during hemodialysis.
Pharmacokinetics in special clinical cases

In children with a slow (within 60 min) IV infusion at the rate of 25 mg / kg and 50 mg / kg after 30 minutes, the serum concentrations are 55.5 mg / l and 118.8 mg / l;
after 1 h - 34.2 mg / l and 89.7 mg / l, respectively.
INDICATIONS

- Central nervous system infection: bacterial meningitis (primary and secondary, including postoperative), ventriculitis;

- Infections of soft tissues, incl.
in patients with impaired peripheral circulation (diabetes mellitus, arterial diseases of the lower extremities), infection of burn wounds;
- Infections of bones and joints: acute and chronic hematogenous osteomyelitis in children and adults, post-traumatic and postoperative osteomyelitis, infectious arthritis;

- infections of the lower respiratory tract: bacterial pneumonia requiring in-patient treatment, especially in cases of isolation of penicillin-resistant pneumococci, as well as Gram-negative pathogens from the Enterobacteriaceae family;
pulmonary infections in patients with cystic fibrosis;
- infections of the abdominal cavity: acute cholecystitis, cholangitis, secondary peritonitis;

- Infectious and inflammatory diseases of the pelvic organs in women: salpingitis, endometritis, pelvioperitonitis;

- urinary tract infections: acute pyelonephritis with moderate and severe course, complicated and exacerbation of chronic urinary tract infections (pyelonephritis against a background of urolithiasis, infectious complications of hydronephrosis, postoperative infections in urology);

bacterial endocarditis.

Indications for the use of combinations of Urophosfabol with antibiotics of other groups are severe infections, incl.
caused by mixed flora, as well as the failure of previous therapy:
- septicemia caused by enterobacteria (Klebsiella spp., Proteus spp., Enterobacter spp., Serratia mercesens) and Pseudomonas aeruginosa - combination with cephalosporins, penicillins (active against Pseudomonas aeruginosa), aminoglycosides or fluoroquinolones;

- bacterial meningitis - a combination with cephalosporins, ampicillin or rifampicin;

- Severe infections caused by methicillin-sensitive strains of Staphylococcus aureus, Staphylococcus epidermidis or Enterococcus spp.
- combination with oxacillin or ampicillin;
- infections caused by methicillin-resistant strains of Staphylococcus aureus or Staphylococcus epidemidis - combinations with glycopeptides;

- intra-abdominal infections and pelvic infections in women - combination with antibiotics active against anaerobes (metronidazole) or with aminoglycosides;

- infections in patients with blood diseases and neutropenia - combinations with cefoperazonom / sulbactam, fourth generation cephalosporins or carbapenems;

- infections caused by multiresistant strains of Pseudomonas aeruginosa - combinations with cephalosporins of the fourth generation, aztreonam or carbapenems.

DOSING MODE

The drug is administered iv.

The average dose of Urophosfabol in adults is 2-4 g, which is administered every 6-8 hours.

In children, beginning with the newborn period, Urophosphabol ® is administered at a rate of 200-400 mg / kg body weight / day.
The daily dose is divided into 3 injections; intervals between administrations are 8 hours.
In patients with renal insufficiency and patients on hemodialysis, correction of the regimens for Urophosphatol administration is required.

Creatinine clearance Dose / multiplicity of administration

50-90 ml / min 2-4 g every 6-8 h

30-50 ml / min 2-4 g every 12 h

10-30 ml / min 2-4 g every 24 hours

<10 ml / min 2-4 g every 48 h

Patients on hemodialysis are given 2-4 g after each dialysis procedure.

Rules for the preparation of solutions and administration

For intravenous administration, 2 g of Urophosfabol is dissolved in 20 ml of water for injection (10 ml of solvent per 1 g of the preparation).
Enter slowly for 5 minutes (the recommended dosing regimen is 2 g every 6-8 h).
For rapid IV infusion, 4 g of Urophosfabol is dissolved in 20 ml of water for injection;
the resulting solution is added to 100-250 ml of a compatible infusion medium.Enter for 0.5-1 h (the recommended dosing regimen is 4 g every 6-8 h).
For long-term drip administration, 4 g (in some clinical cases, 8 g) of Urophosfabol is dissolved in 20 ml of water for injection.
The resulting solution is added to 250-500 ml of a compatible infusion fluid and injected for 1-3 hours (the recommended regimen is 4 g every 6-8 hours).
When dissolving Urophosfabol, an exothermic reaction is possible.

Compatible infusion liquids: 0.9% solution of sodium chloride (saline), 5% dextrose (glucose) solution, Ringer's solution, Ringer's solution with lactate.

SIDE EFFECT

For phosphomycin, a minimum toxicity is characteristic.
Therapy is usually well tolerated, undesirable drug reactions are rare.
On the part of the liver and bile ducts: a violation of liver function in the form of a passing increase in activity of ALT, AST, APF, lactate dehydrogenase and bilirubin in blood serum;
very rarely - jaundice.
From the digestive system: diarrhea;
rarely - stomatitis, nausea, vomiting, abdominal pain, anorexia.
From the nervous system: dizziness, headache;
very rarely - convulsions (when administered in high doses).
From the hemopoietic system: granulocytopenia, eosinophilia, leukopenia;
Very rarely - anemia, thrombocytopenia, pancytopenia and agranulocytosis (<1%).
From the cardiovascular system: peripheral edema, a feeling of discomfort in the chest, a feeling of constriction in the chest, heart palpitations,

From the urinary system: rarely - a violation of kidney function, increased urea concentration in the blood, proteinuria.

Local reactions: soreness and infiltration at the site of the / m introduction, tenderness along the vein;
rarely phlebitis.
Allergic reactions: urticaria, chills or fever, rash, itching, cough, bronchospasm;
very rarely - anaphylactic shock (<1%).
Other: rarely - thirst, fever, malaise, imbalance of electrolytes (sodium and potassium).

CONTRAINDICATIONS

- Hypersensitivity to fosfomycin.

With caution should prescribe the drug with a predisposition to allergic diseases, with liver disease, heart and kidney failure, hypertension, in elderly patients.

PREGNANCY AND LACTATION

The use of Urophosfabol in pregnant women is possible in cases where the intended benefit to the mother exceeds the potential risk to the fetus , and should be carried out under the supervision of a specialist.

Fosfomycin in very small concentrations is excreted in breast milk.
When appointing Urophosphatol Care should be taken during lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be given to the drug in case of kidney failure.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With caution should prescribe the drug for liver disease.

APPLICATION FOR CHILDREN

For the / m administration, children are prescribed 100-200 mg / kg in 3 injections (one of the indications for the / m administration are phlebitis, especially after using iv phosphomycin sodium salt forms).
It should be remembered that in / m injections are painful, so the drug is dissolved in 3 ml of water for injection, and then add 2 ml of a 2% solution of lidocaine, mix. In children, calculate the dose as presented in the table.
Age of introduction

in / m w / in

Newborns Not used 100-400 mg / kg / day in 3 injections

Children under 1 year Not used 100-400 mg / kg / day in 3 injections

Children over 1 year of age 100-200 mg / kg / day in 3 injections 100-400 mg / kg / day in 3-4 injections

APPLICATION IN ELDERLY PATIENTS

Caution should be given to the drug in elderly patients.

SPECIAL INSTRUCTIONS

Because Urophosfabol ® contains 14.5 mEq of sodium per gram of the drug, electrolyte disturbances are possible.
Care must be taken when choosing a dose when administering the drug to elderly patients who need to reduce sodium intake due to cardiac or renal insufficiency, arterial hypertension.
Care must be taken when choosing a dose in elderly patients, because they usually have a reduced kidney function.

To prevent the development of phlebitis or soreness at the injection site, it is recommended to use large amounts of a solvent for IV administration, and the rate of administration should be as slow as possible.

Urofosfabol ® in high doses is recommended to be administered iv in drip.

In the case of prolonged treatment, it is recommended to periodically monitor liver and kidney function, as well as general and biochemical blood tests.

OVERDOSE

Data on drug overdose are not provided.

DRUG INTERACTION

In combinations with penicillins, cephalosporins, carbapenems, aminoglycosides, glycopeptides and fluoroquinolones, phosphomycin shows a pronounced synergism of action.
This property of the drug is used in the treatment of infections caused by multiresistant pathogens (methicillin-resistant staphylococci, enterococci, enterobacteria, Pseudomonas aeruginosa).
Pharmaceutical interaction

In solutions it is compatible with penicillin, carbenicillin, chloramphenicol and streptomycin.
In view of the possible pharmaceutical incompatibility, one should not mix the Urophosphatol solution with solutions of other antibiotics.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
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