Ovea - instructions for use, dose, side effects, contraindications

Ovea's drug contains phosphomycin [mono (2-amino-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 cell wall synthesis bacteria.Being a structural analogue of phosphoenolpyruvate, competitively irreversibly inhibits the enzyme UDF-N-acetylglucosaminolpyruvyl transferase, which catalyzes the formation of UDP-N-acetyl-3-0- (1-carboxyvinyl) -D- glucosamine from phosphoenolpyruvate and UDF-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 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, Enterococcus 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 the blood plasma is observed after 2-2,5 hours after ingestion and is 22-32 mg / l. The half-life of 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 is not bound by plasma proteins and overcomes the placental barrier. After a single injection phosphomycin is excreted in breast milk in small amounts.

Excretion

Fosfomycin is excreted unchanged, mainly by the kidneys by glomerular filtration (40-50% of the dose is detected in the urine), and the period half-life is about 4 hours, and to a lesser extent - with feces (18-23% dose).

The appearance of a second peak concentration in the serum at 6 and 10 hours after taking the drug suggests that the drug is prone to intestinal hepatic 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 (CK) <10 ml / min); deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption; hemodialysis; children under 12 years.

Carefully:Diabetes mellitus, elderly age, impaired renal function (QC more than 10 ml / min).

Pregnancy and lactation:

When pregnancy is used only if the intended benefit for the mother exceeds the potential risk to the fetus.

Fosfomycin penetrates into breast milk at very low concentrations.

If it is necessary to prescribe Ovea during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside.

The granules are dissolved in 1/2 cup water (50-75 ml) or other beverage, mixed until completely dissolved, taken immediately after dissolution. The drug Ovea is taken 1 time per day inside fasting for 1 hour before or 2-3 hours after meals, preferably before going to bed, pre-emptying the bladder.

Adults and children over 12 years. For 1 packet (3 g) 1 time per day once.

In order to prevent infection of the urinary tract during surgery, transurethral diagnostic procedures, the drug is taken 2 times 3 g: 3 hours before surgery and 24 hours after the intervention.

In more severe cases (elderly patients, recurrent infections) take another 1 packet (3 g) in 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 table below shows adverse adverse reactions that were registered with the use of phosphomycin, during clinical trials or post-registration observations.

The frequency of reactions is indicated as follows: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1/1000 to <1/100), rarely (> 1/10000 to <1 / 1000), very rarely (<1/10000) and unknown (frequency can not be estimated based on available data).

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

System-Organ Class	Undesirable reactions
System-Organ Class	infrequently (> 1/1000 to <1/100)	rarely (> 1/10000 to <1/1000)	very rarely (<1/10000)	unknown
Infectious and parasitic diseases	Vulvovaginitis	Superinfection
Immune system disorders				Anaphylactic reactions, including anaphylactic shock, hypersensitivity
Disturbances from the nervous system	Headache, dizziness	Paresthesia
Heart Disease			Tachycardia
Disturbances from the respiratory system in the chest and mediastinal organs				Asthma, bronchospasm, dyspnea
Violations from hand gastrointestinal tract	Diarrhea, nausea, dyspepsia	Abdominal pain, vomiting		Antibiotic-associated colitis, decreased appetite
Disturbances from the skin and subcutaneous tissues		Rash, hives, pruritus		Angioedema edema
Are common disorders and disorders at the site of administration		Fatigue
Vascular disorders				Reduction of blood pressure, petechiae
Disturbances from the liver and bile ducts				A short-term increase in the activity of alkaline phosphatase and "liver" transaminases
Violations of the blood and lymphatic system		Aplastic anemia		Eosinophilia, thrombocytosis (petechiae)

Overdose:

Data on overdose of phosphomycin for oral administration are limited.In patients who took an excessive dose of Ovea, the following reactions were observed: vestibular apparatus dysfunction, hearing impairment, "metallic" taste in the mouth, as well as a general decrease in taste perception.

Treatment for overdose is 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.

Other drugs that increase the motor activity of the gastrointestinal tract can cause a similar effect.

Possible specific problems associated with the change in international normalized relationship (INR). Patients receiving antibiotics were Numerous cases of increased activity of antagonists have been reported antivitamin K. The risk factors include severe infection or inflammation, age and poor overall health. Under these conditions, it is difficult to determine whether a change in INR resulting from an infectious disease or its treatment. Nevertheless, certain classes of antibiotics are more often mentioned in this 2 communication; namely: 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. If such a reaction occurs, it is necessary to exclude the repeated administration of phosphomycin and to conduct adequate treatment.

Antibiotic-associated diarrhea was noted with the use of almost all antibacterial agents, including phosphomycin. Its severity can range from mild diarrhea to fatal colitis. Diarrhea, especially severe, persistent and / or with blood, on time or after treatment with Ovea (including several weeks after treatment) may be a symptom of a disease caused by Clostridium difficile (pseudomembranous colitis). This diagnosis is important to consider when treating patients on time or after taking Ovea. With a presumed or confirmed diagnosis of pseudomembranous colitis, appropriate treatment should be started immediately.Drugs that suppress the intestinal peristalsis are contraindicated in this clinical situation.

Renal failure: the concentration of phosphomycin in the urine persists for 48 hours after taking 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 a package of Ovea with a dosage of 3 g contains 2.107 g of sucrose.

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:

No special studies have been conducted, but patients should be informed that use of the drug may cause dizziness. When dizziness occurs, you should refrain from performing these activities.

Form release / dosage:

Granules for solution for ingestion 3 g.

Packaging:

For 8 g of the drug in a package of composite material (polyethylene terephthalate - aluminum foil - polyethylene film).Each package is placed in a cardboard box with instructions for use.

Storage conditions:

Store at a temperature of no higher than 25 ° C, in the original packaging.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004217

Date of registration:29.03.2017

Expiration Date:29.03.2022

The owner of the registration certificate:Aspharma-Ros, Open CompanyAspharma-Ros, Open Company Russia

Manufacturer: & nbsp

Drogsan Ilaclari Sanayi ve Ticaret A.S. Turkey

Information update date: & nbsp23.04.2017

Illustrated instructions

Instructions

Ovea (Ovea)