Uronormin-F - instructions for use, dose, side effects, contraindications

	for a dosage of 2 grams	for a dosage of 3 grams
Active substance:
Phosphomycin trometamol	- 3.754 g	- 5.61 g
in terms of phosphomycin	- 2.0 g	- 3.0 g
Excipients:
Sucrose	- 2,100 g	- 2.213 g
Aromatic tangerine	0.070 g	0.070 g
Orange flavors	0.060 g	0.070 g
Sodium saccharinate	- 0.016 g	- 0.016 g
Mass of contents of the package	- 6,000 g	- 8,000 g

Description:

The granular powder is white or almost white in color, with a characteristic fruity odor.

Pharmacotherapeutic group:Antibacterial synthetic preparations

ATX: & nbsp

J.01.X.X.01 Phosphomycin

Pharmacodynamics:

URONORMIN-F contains phosphomycin [mono (2-ammonium-2-hydroxymethyl-1,3-propanediol) (2Rcis) - (3-methyloxiranyl) phosphonate] is a broad spectrum antibacterial agent, a phosphonic acid derivative for the treatment of urinary tract infections.

The mechanism of action is associated with the suppression of the first stage of bacterial cell wall synthesis. As a structural analog of phosphoenolpyruvate competitively irreversibly inhibits the enzyme UDP-N-atsetilglyukozamienolpiruviltransferazu that catalyzes the reaction for the formation of UDP-N-acetyl-3-O- (1-carboxyvinyl) -D-glucosamine from phosphoenolpyruvate and UDP-N-acetyl-D-glucosamine . Also, the drug is able to reduce the adhesion of bacteria with the mucous membranes of the bladder, which can play a role as 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, with beta-lactam antibiotics.

Fosfomycin is active against a wide range of Gram-positive and Gram-negative microorganisms commonly released from infections of the urinary tract, such as Escherichia coli, Citrobacter spp., Klebsiella spp., Proteus spp., Serratia spp., Pseudomonas aeruginosa, Enterrococcus faecalis.

The emergence of resistance in the laboratory is due to gene mutation glpT and uhp, which control the transport L-alpha-glycerophosphates and glucosophosphates, respectively.

Pharmacokinetics:

Suction:

Ingestion phosphomycin well absorbed from the intestine and reaches bioavailability of about 50%. The maximum concentration in plasma is observed after 2-2,5 hours after oral administration and is 22-32 mg / l. The half-life of the plasma is 4 hours. Admission with food slows down absorption, without affecting the concentration in the urine.

Distribution:

Fosfomycin is distributed in the kidneys, the walls of the bladder, the prostate and the seminal glands. The constant concentration of phosphomycin in the urine, exceeding the Minimum Bacteriostatic Concentration (MBcK), is reached 24-48 hours after oral administration. Phosphomycin does not bind to plasma proteins and overcomes the placental barrier. After a single administration phosphomycin is excreted in breast milk in small amounts.

Excretion:

Phosphomycin is excreted unchanged, mainly kidney, by glomerular filtration (40-50% of the dose is detected in the urine), with a half-life of about 4 hours, and to a lesser extent - with feces (18-28% dose).

The occurrence of a second peak concentration in the serum after 6 and 10 hours after taking the drug suggests that the drug is susceptible to enteric-liver recirculation.

The pharmacokinetic properties of phosphomycin are independent of age and pregnancy. The drug is cumulated in patients with renal insufficiency; the pharmacokinetic parameters of phosphomycin and the rate of glomerular filtration are linear.

Indications:

Infectious-inflammatory diseases caused by microorganisms susceptible to phosphomycin:

- acute bacterial cystitis, acute attacks of recurrent bacterial cystitis;

- bacterial nonspecific urethritis;

- asymptomatic massive bacteriuria in pregnant women;

- postoperative urinary tract infections;

Prevention of infections during surgical intervention on the urinary tract and in transurethral diagnostic studies.

Contraindications:

- Hypersensitivity to phosphomycin and other components of the drug;

- severe renal failure (creatinine clearance <10 mL / min);

- children under 5 years (for a dosage of 2 g), children under 12 years (for dosage 3 g);

- hemodialysis;

- deficiency of sugar / isomaltase;

- intolerance to fructose;

- glucose-galactose malabsorption.

Pregnancy and lactation:

During pregnancy the drug is prescribed only when the potential benefit to the mother exceeds the potential risk to the fetus. The data of a limited number of examined pregnancies do not show undesirable effects on the pregnancy, fetus or on the health of the newborn.

If it is necessary to administer the drug in the period of breastfeeding should stop breastfeeding for the duration of treatment.

Dosing and Administration:

Inside.

The powder is dissolved in 1/2 a glass of water (50-75 ml) or another beverage, mixed until completely dissolved, taken immediately after dissolution. URONORMIN-F apply once a day inwardly on an empty stomach 1 hour before or 2-3 hours after eating, preferably before going to bed, previously emptying the bladder.

Adults and children from 12 to 18 years: 1 packet (3 g) 1 time per day once.

In order to prevent infection of the urinary tract during surgery, transurethral diagnostic procedures phosphomycin take 1 times 3 g: 3 hours before the intervention and 24 hours after the intervention.

Children from 5 to 12 years: 1 packet (2 g) 1 time per day once.

In order to prevent infection of the urinary tract during surgery, transurethral diagnostic procedures phosphomycin take 2 times 2 grams: for 2 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.

Side effects:

The most common adverse reactions to a single dose of phosphomycin are disorders of the gastrointestinal tract, most often diarrhea. These reactions are short-lived and pass spontaneously.

The following are adverse adverse reactions that have been reported with the use of phosphomycin, during clinical trials or post-registration follow-up.

The reaction frequency 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); it is not known - the incidence of adverse reactions can not be estimated on the basis of available data.

In each group, adverse reactions are presented in descending order of severity.

Infectious and parasitic diseases:

Infrequently: vulvovaginitis

Rarely: superinfection

Immune system disorders:

Unknown: anaphylactic reactions, including anaphylactic shock, hypersensitivity

Disturbances from the nervous system:

Infrequent: headache, dizziness

Rarely: paresthesia

Heart Disease:

Very rarely: tachycardia

Disturbances from the respiratory system, organs of the chest and mediastinum:

Unknown: asthma, bronchospasm, dyspnea

Disorders from the gastrointestinal tract:

Infrequent: diarrhea, nausea, indigestion

Rarely: abdominal pain, vomiting

Unknown: antibiotic-associated colitis, decreased appetite

Disturbances from the skin and subcutaneous tissues:

Rare: rash, hives, itching

Unknown: angioedema

General disorders and disorders at the site of administration:

Rarely: fatigue

Vascular disorders:

Unknown: lowering blood pressure, petechiae

Disturbances from the liver and bile ducts:

It is not known: a short-term increase in the activity of alkaline phosphatase and "liver" transaminases

Violations of the blood and lymphatic system:

Rarely: aplastic anemia

Unknown: eosinophilia, thrombocytosis (petechiae).

Overdose:

Data on overdose of phosphomycin during ingestion are limited. In patients who took an excessive dose of the drug, the following reactions were observed: violations of the function of the vestibular apparatus, hearing impairment, "metallic" taste in the mouth, and a general decrease in taste perception.

Treatment with an overdose - symptomatic and supportive.

In case of an overdose, it is recommended to take the liquid inside to increase diuresis.

Interaction:

When combined with phosphomycin metoclopramide reduces the concentration of phosphomycin in serum and urine.

Simultaneous use of antacids or calcium salts leads to a decrease in the concentration of phosphomycin in blood plasma and urine.

Drugs that increase the motor activity (motility) of the gastrointestinal tract, can cause a similar effect (decrease in the concentration of phosphomycin in blood plasma and urine).

Possible specific problems associated with the change in the international normalized relationship (INR). In patients receiving antibiotics, numerous cases of increased activity of antivitamin K antagonists have been reported. In the presence of such risk factors as severe infection, inflammation, age or poor overall health, the change in INR may be due to both an infectious disease and the consequence of its treatment. Similar changes are considered more characteristic for the following classes of antibiotics: fluoroquinolones, macrolides, cyclins, cotrimoxazole and some cephalosporins.

Special instructions:

During treatment with phosphomycin, hypersensitivity reactions may occur, including anaphylaxis and anaphylactic shock, which are life-threatening. In such cases, it is necessary to exclude the repeated use of phosphomycin and to conduct adequate treatment.

The use of almost all antibacterial agents, including phosphomycin, can lead to antibiotic-associated diarrhea. Its severity can range from mild diarrhea to colitis with fatalities. Diarrhea, especially severe, persistent and / or blood-mixed, observed during or after treatment with phosphomycin (including several weeks after treatment) may be a symptom of pseudomembranous colitis caused by Clostridium difficile. With a presumed or confirmed diagnosis of pseudomembranous colitis, treatment should be initiated immediately. Drugs that suppress the intestinal peristalsis are contraindicated in this clinical situation.

Application for renal failure: the concentration of phosphomycin in the urine is maintained for 48 hours after the usual dose, if the creatinine clearance is above 10 ml / min. The drug is contraindicated in patients undergoing hemodialysis.

Patients with diabetes should take into account that in 1 package 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.

Patients with rare hereditary diseases, such as fructose intolerance, glucose-galactose malabsorption or insufficiency of isomaltase sucrose, this drug is contraindicated.

Effect on the ability to drive transp. cf. and fur:

Patients should be warned about the possibility of developing dizziness, and when dizziness occurs, one should refrain from performing these activities.

Form release / dosage:

Powder for solution for oral administration, 2 g and 3 g.

Packaging:

By 6.0 g (for a dosage of 2 g) or 8.0 g (for a dosage of 3 g) in heat-sealing bags (buffers) made of four-layer laminated foil (paper-polyethylene-aluminum-polyethylene).

For 1, 2 or 3 bags together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004180

Date of registration:15.03.2017

Expiration Date:15.03.2022

The owner of the registration certificate:OTISIFARM, OJSC OTISIFARM, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp05.04.2017

Illustrated instructions

Instructions

Uronormin-F (Uronormin-F)