Composition
active ingredient: metronidazole

1 pill contains 250 mg of metronidazole

excipients: wheat starch, povidone, magnesium stearate shell: hypromellose, polyethylene glycol.
Dosage form

Coated tablets Flagyl.

Basic physical and chemical properties:

White to creamy white, round, film-coated tablets, embossed with F 250 on one side.
Pharmacological group

Antibacterial agents for systemic use. Antiprotozoal drugs. imidazole derivatives. ATX code J01X D01.

Means for the treatment of amebiasis and other protozoal diseases. Antiprotozoal drugs. ATX code P01A B01.
Pharmacological properties

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Pharmacological.

The prevalence of acquired resistance in certain types of microorganisms may differ depending on the geographical location and time. In this regard, it is useful to have information about the local prevalence of resistance, especially when treating severe infections. These data are only general guidelines indicating the likelihood of sensitivity of a particular bacterial strain to this antibiotic.

Sensitive to the drug: Peptostreptococcus spp., Clostridium spp., Bacteroides spp., Fusobacterium spp., Porphyromonas, Bilophila, Helicobacter pylori, Prevotella spp., Veilonella. Metronidazole inhibits the development of protozoa – Trichomonas vaginalis, Giardia intestinalis (Lamblia intestinalis), Entamoeba histolytica. Variably sensitive to the drug: Bifidobacterium spp., Eubacterium spp. Insensitive strains of microorganisms: Propionibacterium, Actinomyces, Mobiluncus

Pharmacokinetics.

Absorption. When taken orally, metronidazole is rapidly and almost completely absorbed (at least 80% per hour). The maximum concentration in blood serum, after oral administration of the drug, is similar to that achieved after the introduction of equivalent doses.

Oral bioavailability is 100% and does not decrease significantly with concomitant food intake.

Distribution. Approximately one hour after taking a single dose of 500 mg, the average maximum plasma concentration is 10 µg/ml. After 3:00, the mean plasma concentration is 13.5 µg/mL.

The half-life is 8-10 hours, binding to blood proteins is insignificant – no more than 20%. The volume of distribution is high (approximately 40 l, i.e. 0.65 l/kg).

Distribution is rapid and significant, reaching concentrations close to plasma levels in the lungs, kidneys, liver, skin, bile, cerebrospinal fluid, saliva, seminal fluid and vaginal secretions.

Metronidazole crosses the placental barrier and is excreted in breast milk.

Metabolism. Metabolism of metronidazole occurs by oxidation in the liver. Two metabolites are formed:

the main alcohol metabolite, which provides approximately 30% of the antibacterial activity of metronidazole against anaerobic bacteria, the half-life is approximately 11:00
an acid metabolite that is present in a smaller amount and provides about 5% of the antibacterial activity of metronidazole.

Significant concentration in the liver and bile, low concentration in the colon, slight elimination with feces. Excretion of the drug is carried out by 35-65% by the kidneys (in the form of metronidazole and oxidized metabolites).
testimony

Infections caused by microorganisms sensitive to the drug: amoebiasis urogenital trichomoniasis nonspecific vaginitis giardiasis surgical infections caused by metronidazole-sensitive anaerobic microorganisms replacement of intravenous treatment of infections caused by metronidazole-sensitive anaerobic microorganisms.

Contraindications

Interaction with other medicinal products and other forms of interaction

Disulfiram. Risk of developing acute psychotic episodes or confusion, which are reversible after discontinuation of the drug.

Busulfan. When using busulfan in high doses: doubling the concentrations of busulfan in patients receiving metronidazole.

Combinations that require precautions for use.

Enzyme-inducing anticonvulsants. Decreased plasma concentrations of metronidazole due to increased hepatic metabolism by an enzyme inducer. Clinical observation is indicated, and dose adjustment of metronidazole may be required during and after treatment with an inducer.

Rifampicin. Decreased plasma concentrations of metronidazole due to increased hepatic metabolism by rifampicin. Clinical observation is indicated, and dose adjustment of metronidazole may be required during and after treatment with rifampicin.

Lithium. Increased levels of lithium in the blood, which can reach toxic levels, with signs of lithium overdose. It is necessary to carefully monitor the level of lithium in the blood, dose adjustment may be required.

Combinations that require special attention.

Fluorouracil (and, by extrapolation, tegafur and capecitabine). An increase in the toxicity of fluorouracil due to a slowdown in its clearance.

Special problems for the Ministry of Emergency Situations (international normalized ratio).

In patients receiving antibiotic therapy, numerous cases of increased activity of oral anticoagulants were recorded. Risk factors include the severity of the infection or inflammation, the age of the patient, and general health. In these circumstances, it is difficult to determine to what extent the imbalance of the MES is affected by the infection itself or its treatment. However, some groups of antibiotics are more involved in this effect, especially fluoroquinolones, macrolides, cyclins, co-trimoxazole and some cephalosporins.
application features

From the side of the central nervous system. In the event of the appearance of symptoms characteristic of encephalopathy or cerebellar syndrome, the patient’s treatment should be immediately reviewed, and the use of metronidazole should be discontinued.

Patients should be monitored for possible signs of encephalopathy or exacerbation of symptoms in patients with disorders of the central nervous system.

If aseptic meningitis develops during treatment, re-administration of metronidazole is NOT recommended, and in patients with a serious infectious disease, a benefit / risk assessment should be carried out.

From the peripheral nervous system. It is necessary to monitor the condition of patients for possible signs of peripheral neuropathy, especially with prolonged treatment with the drug or in the presence of severe, chronic or progressive peripheral neurological disorders.

hematological effects. In patients with a history of hematological disorders or receiving the drug in high doses and / or for a long period, it is necessary to regularly perform blood tests, especially the determination of the content of leukocytes.

In patients with leukopenia, the decision to continue treatment depends on the severity of the infection.

Excipients with a known effect. This drug can be prescribed to patients with celiac disease. Wheat starch may contain gluten, but only in trace amounts, so it is considered safe for celiac patients.

pediatric patients. The use of tablets is contraindicated in children under 6 years of age due to the risk of suffocation. For young children, other dosage forms of drugs based on metronidazole are available.
Interaction with other drugs

Influence on the results of laboratory tests. Metronidazole can fix treponemas, thereby leading to false positive Nelson test results.
Use during pregnancy or lactation

Pregnancy. Animal studies have not shown a teratogenic effect. Since no teratogenic effect has been observed in animals, malformations are not expected to occur in humans. Substances that cause malformations in humans have been reported to be teratogenic in animals in adequately conducted studies in two species. Numerous clinical data have not demonstrated any specific teratogenic or fetotoxic effects associated with the administration of metronidazole during pregnancy..

However, further epidemiological studies are required to confirm that there is no risk. Therefore, metronidazole can be prescribed during pregnancy only if necessary, when the benefits of using the drug outweigh the potential risk.

Breastfeeding. Metronidazole passes into breast milk. Flagyl should not be used while breastfeeding.
The ability to influence the reaction rate when driving vehicles or operating other mechanisms

Persons who drive vehicles and work with mechanisms should be aware of the possible occurrence of confusion, dizziness, hallucinations, convulsions or visual disturbances while taking this drug and refrain from driving vehicles and working with other mechanisms during the period of treatment.
Dosage and administration

With amoebiasis, Flagyl is taken continuously for 7 days. Adults 1.5 g per day, that is, 500 mg (2 tablets) 3 times a day.

Children over the age of 6 years 30-40 mg / kg of body weight per day in 3 divided doses.

In the event of a liver abscess in amebiasis, drainage or aspiration of pus is carried out simultaneously with metronidazole therapy.

Giardiasis is treated within 5 days. Assign 750 mg-1 g of the drug Flagyl per day. Children 6-10 years old – 375 mg / day, 10-15 years old – 500 mg per day. To achieve the prescribed dosage, metronidazole is used in the appropriate dosage or other dosage forms.

With trichomoniasis in women (urethritis and vaginitis caused by Trichomonas), Flagyl is prescribed for a course of treatment for 10 days, combining 250 mg (1 tablet) 2 times a day and 1 vaginal suppository (500 mg) per day. The sexual partner should be treated at the same time, regardless of the presence or absence of clinical signs of trichomonas infection, even if the result of laboratory tests is negative.

With trichomoniasis in men (urethritis caused by Trichomonas), Flagyl is prescribed for a course of treatment for 10 days: 250 mg (1 tablet) 2 times a day.

In exceptional cases, it may be necessary to increase the daily dose to 750 mg or 1 g.

For nonspecific vaginitis, 500 mg (2 tablets) of Flagyl are prescribed 2 times a day for 7 days. The sexual partner should be treated at the same time.

For the treatment of anaerobic infections (first-line therapy or substitution treatment), 1.0-1.5 g (4-6 tablets) of Flagyl is prescribed per day, for children over 6 years old – 20-30 mg / kg of body weight per day, for 2 reception.
Children

The drug in the form of tablets of 250 mg can be used in children over the age of 6 years.
Overdose

A single dose of not more than 12 g has been observed in suicidal attempts and accidental overdose.

Symptoms included vomiting, ataxia, and mild disorientation. There is no specific antidote. In case of significant overdose, symptomatic therapy should be carried out.
Adverse reactions

From the gastrointestinal tract:

minor gastrointestinal disorders (pain in the epigastric region, nausea, vomiting, diarrhea)
glossitis with dry mouth, stomatitis, taste disturbance, anorexia
pancreatitis that is reversible after discontinuation of the drug
discoloration or change in the appearance of the tongue (mycosis).

From the skin and its derivatives:

hot flashes, itching of the skin, skin rash, in some cases accompanied by an increase in body temperature

toxic epidermal necrolysis
fixed toxicoderma
Stevens-Johnson syndrome.

From the nervous system:

  • peripheral sensory neuropathy
  • headache
  • dizziness
  • confusion
  • convulsions

Visual impairment:

temporary visual disturbances such as diplopia, myopia, decreased visual acuity, changes in color vision
neuropathy / optic neuritis.

From the side of the psyche:

hallucinations

depressed mood.

From the blood and lymphatic system:

neutropenia, agranulocytosis, thrombocytopenia.

Hepatobiliary system:

increased levels of liver enzymes (AST, ALT, alkaline phosphatase), very rarely reported cases of acute cholestatic or mixed hepatitis and hepatocellular liver damage, sometimes with the appearance of jaundice. Isolated cases of hepatocellular insufficiency have been reported, which may require liver transplantation.

From the organs of hearing and balance:

hearing loss and hearing loss (including sensorineural)
tinnitus.

other:

reddish-brown coloration of urine due to water-soluble pigments that are formed during the metabolism of this drug.

Best before date

3 years.
Storage conditions

Keep out of the reach of children. Store in original packaging.
Package

No. 20 (10×2): 10 tablets in a blister, 2 blisters in a cardboard box.
Holiday category

On prescription.