Flagyl - instructions for use, doses, side effects, contraindications

Metronidazole is a derivative of nitro-5-imidazole. The mechanism of action of metronidazole is biochemical reduction of 5-nitro group of metronidazole intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group Metronidazole interacts with the DNA of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of microorganisms.

Active in a relationship Trichomonas vaginalis, Entamoeba histolytica, as well as Gram-negative anaerobes Bacteroides spp. (incl. AT. fragilis, AT. ovatus, AT. distasonis, AT. thetaiotaomicron, AT. vulgatus), Fusobacterium spp.,and some Gram-positive anaerobes (sensitive strains Eubacterium spp., Clostridium spp., Peptococcus niger, Peptostreptococcus spp.). The MIC for these strains is 0.125-6.25 μg / ml.

In combination with amoxicillin shows activity against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).

To Metronidazole insensitive Aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.

Pharmacokinetics:

Approximately 20% of the intravaginally administered dose of metronidazole (0.5 g) undergoes systemic absorption, resulting in a concentration of the drug in the blood plasma of approximately 12% of that after ingestion of a single dose of 0.5 g. Half-life (elimination established in systemic use with normal function of the liver) is 8-10 hours. The association with plasma proteins is less than 20%.

Indications:

Local treatment of trichomoniasis and nonspecific vaginitis.

Prevention of the occurrence of anaerobic infections in surgical interventions on the abdominal and pelvic organs.

Contraindications:

- Hypersensitivity to imidazoles, as well as to derivatives of nitroimidazole;

- organic lesions of the central nervous system (including epilepsy);

- Violations of coordination of movements;

- Lakopenia (including in the anamnesis);

- liver failure (in the case of taking large doses);

- pregnancy;

- the period of breastfeeding.

- children and adolescents under the age of 18 (for this dosage form).

Carefully:

- Hepatic encephalopathy;

- acute and chronic diseases of the peripheral and central nervous system (risk of weighting of neurological symptoms);

- Renal failure.

Dosing and Administration:

The drug is used only in adults.

Adults

- Trichomonal vaginitis: 1 suppository per day, in the vagina, for 10 days in combination with metronidazole ingestion.

- Nonspecific vaginitis: 1 suppository 2 times a day for 7 days, if necessary in combination with metronidazole ingestion.

It is necessary to simultaneously treat the sexual partner metronidazole inside, regardless of whether he has manifestations of the disease.

Treatment with metronidazole should not be administered for more than 10 days and should be repeated more than 2-3 times per year. Preliminarily releasing the suppository from the contour package using scissors, cut the film along the contour of the suppository and insert it deep into the vagina.

Side effects:

Disorders from the gastrointestinal tract

- Pain in epigastrium, nausea, vomiting, diarrhea.

- Inflammation of the oral mucosa (glossitis, stomatitis), taste disorders ("metallic" taste in the mouth), decreased appetite, anorexia, dryness of the oral mucosa, constipation.

- Pancreatitis (reversible cases).

- Changing the color of the tongue / "lined tongue" (due to the growth of fungal microflora).

Immune system disorders

- Angioedema, anaphylactic shock.

Disturbances from the nervous system

- Peripheral sensory neuropathy.

- Headache, cramps, dizziness.

- The development of encephalopathy (for example, confusion) has been reported and subacute cerebellar syndrome (impaired coordination and synergy of movements, ataxia, dysarthria, gait disorders, nystagmus and tremor), which undergo reverse development after metronidazole withdrawal.

- Aseptic meningitis.

Disorders of the psyche

- Psychotic disorders, including confusion, hallucinations.

- Depressed mood, insomnia, irritability, increased excitability.

Disturbances on the part of the organ of sight

- Transient visual impairments, such as diplopia, myopia, vagueness of contours of subjects, reduced visual acuity, violation of color perception.

- Neuropathy / optic neuritis.

Violations of the blood and lymphatic system

- Agranulocytosis, leukopenia, neutropenia and thrombocytopenia.

Disturbances from the liver and bile ducts

- Increased activity of "hepatic" enzymes (aspartate aminotransferase (ACT) and alanine aminotransferase (ALT), alkaline phosphatase), the development of cholestatic or mixed hepatitis and hepatocellular liver damage, sometimes accompanied by jaundice.

- In patients treated with metronidazole in combination with other antibiotics, cases of hepatic impairment were observed, requiring liver transplantation.

Disturbances from the skin and subcutaneous tissues

- Rash, itchy skin, skin hyperemia, urticaria.

- Pustular skin rash.

- Stevens-Johnson syndrome, toxic epidermal necrolysis.

Disorders from the kidneys and urinary tract

- It is possible to stain urine in a brownish-reddish color, due to the presence in the urine of a water-soluble metabolite of metronidazole.

- Dysuria, polyuria, cystitis, urinary incontinence, candidiasis.

General disorders and disorders at the site of administration

- Fever, nasal congestion, arthralgia, weakness.

- Burning sensation or irritation of the penis in the sexual partner, burning sensation or frequent urination, vulvitis (itching, burning pain or hyperemia of the mucous membrane in the external genital area).

Infectious and parasitic diseases

- After cancellation of the drug, the development of candidiasis of the vagina is possible.

Laboratory and instrumental data

- Compaction of the T wave on the ECG.

Interaction:

With disulfiram

It was reported about the development of psychotic reactions in patients receiving concomitantly metronidazole and disulfiram (the interval between taking these two drugs should be at least 2 weeks).

FROM ethanol

Possible occurrence of difulfiramoid-like reactions (flushing of the skin, vomiting, tachycardia).

With indirect anticoagulants (warfarin)

Increased anticoagulant effect and increased hemorrhagic risk associated with a slowdown in their hepatic metabolism, which may lead to an increase in prothrombin time. In the case of simultaneous use, more frequent monitoring of prothrombin time and, if necessary, dose adjustment anticoagulants.

With lithium preparations

With the simultaneous administration of metronidazole with lithium preparations, the concentration of the latter in the blood plasma can increase. With simultaneous use, plasma concentrations of lithium, creatinine and electrolytes should be monitored.

With cyclosporine

With the simultaneous administration of metronidazole with cyclosporine, the serum concentration of cyclosporine can increase. If simultaneous use of these two drugs is required, monitoring of serum concentrations of cyclosporine and creatinine is required.

With cimetidine

Cimetidine suppresses the metabolism of metronidazole, which can lead to an increase in its concentration in the blood serum and an increased risk of side effects.

With drugs that induce enzymes microsomal oxidation in the liver (phenobarbital, phenytoin)

Simultaneous use of drugs that stimulate enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin), can accelerate the elimination of metronidazole, as a result of which its concentration in the plasma decreases.

FROM fluorouracil

Metronidazole reduces the clearance of fluorouracil, leading to an increase in its toxicity.

With busulfan

Metronidazole increases the concentration of busulfan in the blood plasma, leading to an increase in its toxicity in severe form.

With nondepolarizing muscle relaxants (vecuronium bromide)

It is not recommended to combine with nondepolarizing muscle relaxants (vecuronium bromide).

Special instructions:

Since simultaneous administration of the drug with alcohol (ethanol) can have an effect similar to the effect of disulfiram (feeling of heat, vomiting, tachycardia), patients should be warned that during treatment with Flagil®, do not consume alcoholic drinks or medicines containing ethanol.

You should carefully weigh the indications for long-term use of metronidazole and, without strict indications, avoid prolonged treatment with Flagil®. If, in the presence of strict indications, the drug is used for a longer period than is generally recommended, then treatment should be monitored by hematological indicators and adverse reactions such as peripheral or central neuropathy, manifested by paresthesia, ataxia, dizziness, convulsions, in the event of which treatment should be discontinued .

In the treatment of trichomonas vaginitis in women, it is necessary to abstain from sexual intercourse. It is necessary to simultaneously treat sexual partners. Treatment does not stop during menstruation. After therapy with trichomoniasis, control tests should be performed for 3 consecutive cycles before and after menstruation.

It is necessary to take into account that metronidazole can immobilize treponemy, which leads to a false positive test of Nelson.

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

Given the profile of side effects (dizziness, visual impairment and others), it is recommended during treatment to refrain from driving, from practicing other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Vaginal suppositories, 500 mg.

Packaging:

5 suppositories of vaginal in a contour cell pack (PVC / PE).

2 contour squares, together with instructions for use, are placed in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014269 / 01

Date of registration:11.12.2008 / 12.03.2013

Expiration Date:Unlimited

The owner of the registration certificate:Sanofi-Aventis FranceSanofi-Aventis France France

Manufacturer: & nbsp

UNITHER LIQUID MANUFACTURING France

Representation: & nbspSanofi Aventis GroupSanofi Aventis Group

Information update date: & nbsp18.09.2016

Illustrated instructions

Instructions

Flagil® (Flagyl®)