medicalmeds.eu Medicines Antibiotic. Урофосфабол®

Урофосфабол®

Producer: LLC ABOLMED Russia

Code of automatic telephone exchange: J01XX01

Release form: Liquid dosage forms. Powder for preparation of solution for injections.

Indications to use: The infected burns. Osteitis. Lower respiratory tract infections. Pneumonia. Mucoviscidosis. Cholecystitis. Cholangitis. Peritonitis. Salpingitis. Endometritis. Pelviperitonitis. Pyelonephritis. Cystitis.

General characteristics. Structure:

Active ingredient: 1,0 g фосфомицин dinatrium (in terms of фосфомицин).
Excipient: succinic acid.

Antibiotic of a broad spectrum of activity with effective treatment of the infections caused by steady activators.

Pharmacological properties:

Pharmacodynamics. Bactericidal action of a fosfomitsin is based on disturbance (at early stages) synthesis of a peptidoglikan of a cell wall of bacteria. Getting into a microbic cell on systems of transport of D - glucose-6-phosphate, drug it is irreversible inhibits УДФ-N-ацетилглюкозамиенолпирувилтрансферазу enzyme which catalyzes reaction of education UDF-N-atsetil-3-0-(1 carboxyvinyl) - a D-glycosamine from a fosfoyenolpiruvat and an UDF-N-atsetil-D-glyukozamina.

Fosfomitsin is active concerning gram-positive aerobes - Staphylococcus aureus, Staphylococcus epidermidis (including some strains steady against Methicillinum), Staphylococcus spp., Streptococcus pyogenes, Streptococcus spp. viridans groups, streptococci of the groups C, F, G, Streptococcus pneumoniae, Enterococcus faecalis, Bacillus anthracis; gram-negative aerobes - Aeromonas hydrophila, Citrobacter spp., Campylobacter jejuni, Escherichia coli, Enterobacter spp. (are moderately sensitive), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca (are moderately sensitive), Morganella morganii (the majority of strains are moderately sensitive), Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri (are moderately sensitive), Pseudomonas aeruginosa, Serratia marcescens, Salmonella spp., Shigella spp., Vibrio spp. (are moderately sensitive), Yersinia enterocolitica; and also some anaerobe bacterias - Actinomyces spp., Peptococcus spp., Peptostreptococcus spp., Fusobacterium spp., Veillonella spp., Clostridium perfringens and Prevotella spp are moderately sensitive.

Enterococcus faecium, Acinetobacter spp are steady., Legionella spp., Borrelia spp., Listeria monocytogenes, Mycobacterium spp., Bacteroides spp., majority of intracellular activators (Coxiella burnetii, Rickettsia spp., Chlamydia spp., Mycoplasma pneumoniae, Ureaplasma urealyticum).

Secondary resistance of microorganisms to Urofosfabolu® develops seldom. Valuable property of drug is lack of cross resistance with other antibacterial agents. At a combination to beta lactams, ftorkhinolona, glycopeptides or aminoglycosides the expressed synergism of antimicrobic action concerning a wide range of gram-positive and gram-negative aerobic bacteria is noted.

Pharmacokinetics. After intramuscular introduction the maximum serumal concentration (Cmax) are reached in 1 hour and make 17,1 mg/l and 28 mg/l after introduction of 0,5 g and 1 g of a fosfomitsin, respectively. At introduction in the mode of 1 g each 6 hours it is possible to maintain stable serumal concentration at the level of 8 mg/l.

Extent of linkng of a fosfomitsin with proteins of a blood plasma low - 1% of the entered dose.

Thanks to low molecular weight, фосфомицин it is well distributed in many bodies and body tissues. Bactericidal concentration are defined in tissue of a lung, pleural liquid, peritoneal liquid, bile, podkozhnozhirovy cellulose, muscles, bones, synovial fluid, eye tissues, an endocardium of valves of heart; quickly gets through a blood-brain barrier. Concentration of drug considerably increases in cerebrospinal fluid at an inflammation of a meninx. Gets and collects in cells phagocytes (neutrophils and macrophages). Gets through a placenta. In small concentration gets into breast milk.
The elimination half-life (Т½) makes, on average, 1,5-2 hours at adults and from 0,69 to 1,04 hours, depending on a dose, at children. The main way of excretion of a fosfomitsin - renal (90-100% of the entered dose within a day); with urine the active form of drug is removed. A small part of the entered antibiotic is excreted through intestines, however, this way of elimination has no essential value. Fosfomitsin can be easily removed from plasma at a hemodialysis.

Indications to use:

The infectious and inflammatory diseases caused by activators, sensitive to drug, at children, since 2,5 years, and adults:
- infections of soft tissues, including at patients with disturbances of peripheric circulation (a diabetes mellitus, diseases of arteries of the lower extremities), infections of burn wounds;
- infections of bones and joints;
- lower respiratory tract infections, including pneumonia and infections at patients with a mucoviscidosis;
- intraabdominal infections: acute cholecystitis, cholangitis, peritonitis;
- infectious and inflammatory diseases of bodies of a small pelvis: salpingitis, endometritis, pelviperitonitis;
- infections of urinary tract, including acute and exacerbation of chronic pyelonephritis.

Route of administration and doses:

Intramusculary!
Average dose ^{of Urofosfabola®} for introduction in oil at adult 1-2 g 3 times a day.

At children 2,5 years - 500-1000 mg 3 times a day are more senior.

Correction of the modes of introduction ^{Urofosfabola®} is required from patients with a renal failure and the patients who are on a hemodialysis (see the table):

Clearance of creatinine	40-20 ml/min.	20-10 ml/min.	<10 ml/min.
Dose/mode	To 2-4 g there are each 12 hours	To 2-4 g there are each 24 hours	To 2-4 g there are each 48 hours

The patient who is on a hemodialysis enter 1-2 g after each procedure of dialysis.

Intramuscular injections of a fosfomitsin are painful. For preparation of solution of 1 g of drug dissolve in 2 ml of water for injections, and then add 2 ml of 2% of solution of lidocaine, mix.

Features of use:

Necessary precautionary measures. It is necessary to observe the way of introduction specified on packaging and a bottle; not to use a form for introduction in oil intravenously and a form for in/in introductions - intramusculary.

As Urofosfabol® contains 14,5 мЭкв sodium on 1 g of drug, electrolytic disturbances are possible. It is necessary to be careful at the choice of a dose at administration of drug by the elderly patient which need reduction of consumption of sodium owing to a heart or renal failure, arterial hypertension, etc.

It is necessary to be careful at the choice of a dose at elderly patients as at them function of kidneys is usually reduced.

The precautionary measures concerning administration of drug. For the prevention of morbidity in an injection site it is recommended to use local anesthetic as solvent (see the Route of administration and doses), and rate of administering has to be slow.

Other precautionary measures. In case of prolonged treatment this medicine recommends to control function of a liver and kidneys periodically (including according to biochemical analysis of blood: to content of electrolytes, urea nitrogen, bilirubin, activity of liver enzymes), and also indicators of the general blood test.

There are no data indicating influence of a fosfomitsin on ability to driving of motor transport and to control of mechanisms.

At lidocaine solution use as solvent it is necessary to be careful when driving motor transport and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

For a fosfomitsin the minimum toxicity is inherent; therapy is usually well transferred, undesirable medicinal reactions are observed seldom.

Allergic reactions: a small tortoiseshell, a fever or fever, rash, an itch, cough, a bronchospasm, it is very rare - an acute anaphylaxis (<1%).

From a liver and biliary tract: the abnormal liver function in the form of the taking place increase in activity of alaninaminotranspherase, an aspartaminotransferaza, an alkaline phosphatase, a lactate dehydrogenase and concentration of bilirubin in blood serum, is very rare - jaundice.

From the alimentary system: diarrhea, it is rare - stomatitis, nausea, vomiting, an abdominal pain, anorexia.

From system of blood: a granulocytopenia, an eosinophilia, a leukopenia, it is very rare - anemia, thrombocytopenia, a pancytopenia and an agranulocytosis (<1%).

From an urinary system: seldom - a renal failure, increase in concentration of urea in blood, a proteinuria, an imbalance of electrolytes (sodium and potassium).

From a nervous system: dizziness, is very rare - spasms (at introduction in high doses).

Local reactions: morbidity and infiltrate in the place in oil of introduction.

Others: seldom - a headache, thirst, fever, an indisposition, peripheral hypostases, a sensation of discomfort in breasts, feeling of squeezing in a thorax, a cardiopalmus.

Interaction with other medicines:

In combinations with penicillin, cephalosporins, karbapenema, aminoglycosides, glycopeptides and ftorkhinolona фосфомицин shows the expressed sinergidny effect; this property of drug is used at therapy of heavy infections, and also the infections caused by polyresistant activators (metitsillinustoychivy stafilokokka, enterococci, enterobakteriya, Pseudomonas aeruginosa, etc.).

In view of physical and chemical incompatibility it is not necessary to mix in one syringe with ampicillin, gentamycin, streptomycin, Kanamycinum and rifampicin.

Contraindications:

- individual hypersensitivity to a fosfomitsin, amide anesthetics (at lidocaine solution use as solvent);
- children's age up to 2,5 years.

With care: allergic reactions to medicines in the anamnesis, a serious illness of a liver, a heart and renal failure, at elderly patients, at arterial hypertension.

Use of Urofosfabola® for pregnant women perhaps in cases when the estimated advantage for mother exceeds potential risk for a fruit, and has to be carried out under observation of the specialist.

Fosfomitsin in very small concentration gets into breast milk. At purpose of Urofosfabola® in the period of a lactation it is necessary to stop breastfeeding.