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

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

Has a wide range of action against anaerobic microorganisms - Peptostreptococcus, Clostridium sp., Bacteroides sp., Fusobacterium, Prevotella, Veillonella. Suppresses development protozoa - Trichomonas vaginalis, Giardia intestinalis, Lamblia spp., Entamoeba histolytica.

Increases the sensitivity of tumors to radiation, causes disulfiram-like reactions, stimulates reparative processes.

Pharmacokinetics:

Ingestion Metronidazole quickly and almost completely absorbed. Eating does not affect the absorption of the drug.The half-life is 8-10 hours, the connection with blood proteins is insignificant and does not exceed 10-20%. The drug quickly penetrates into tissues (lungs, kidneys, liver, skin), bile, cerebrospinal fluid, saliva, seminal fluid, vaginal secretion, into breast milk and passes through the placental barrier. Metronidazole metabolized by oxidation in the liver and binding to glucuronic acid. Excretion is carried out on 40-70% through the kidneys (in unchanged form - about 20% of the dose) and with feces.

In patients with hepatic insufficiency the elimination half-life remains unchanged.

Indications:

Trichomonas vaginitis and urethritis in women, trichomoniasis urethritis in men, giardiasis, amoebic dysentery; Anaerobic infections caused by microorganisms that are sensitive to the drug.

Combined therapy of severe mixed aerobic-anaerobic infections.

Prevention of anaerobic infection during surgical interventions (especially on the organs of the abdominal cavity, urinary tract).

In combination with amoxicillin: chronic gastritis in the exacerbation phase, peptic ulcer of the stomach and duodenum in the acute phase, associated with Helicobacter pylori.

Contraindications:

- Hypersensitivity to imidazoles;

- organic lesions of the central nervous system;

- abnormal liver function;

- pregnancy and the period of breastfeeding;

- leukopenia (including in the anamnesis);

- Children under 3 years old (for this dosage form).

Carefully:Pkidney failure.

Pregnancy and lactation:If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside, during or after eating, without chewing.

With amebiasis - within 7 days of 1.5 g per day in 3 doses (adults) and 30-40 mg / kg per day, as well as in 3 doses (children).

With giardiasis - for 5 days - adults 750-1000 mg per day, children 3-5 years 250 mg per day, children 5-10 years - 375 mg per day and children 10-15 years - 500 mg per day. Take 2-3 times a day after meals.

With trichomoniasis in women (urethritis and vaginitis) Metronidazole appoint once in a dose of 2 g or as a course of treatment for 10 days, 1 tablet (250 mg) 2 times a day. Parallel with ingestion, one evening vaginal suppository or a vaginal tablet containing 250 mg of metronidazole is prescribed in the evening.

To exclude possible reinfection, it is necessary to treat simultaneously sexual partners.

The course of treatment is repeated if necessary in 4-6 weeks.

With trichomoniasis in men (urethritis) Metronidazole appoint once in a dose of 2 g or as a course of treatment for 10 days, 1 tablet (250 mg) 2 times a day.

With nonspecific vaginitis Apply 500 mg of Metronidazole 2 times a day for 7 days.

In the treatment of gastritis and peptic ulcer associated with Helicobact pylori Metronidazole is prescribed for 500 mg 3 times a day for 7 days (as part of combination therapy, for example, combination with amoxicillin 2.25 g / day).

For the prevention of anaerobic infection in surgical interventions appoint Metronidazole on 750 -1500 mg / day in 3 doses for 3-4 days before the operation. In 1-2 days after the operation (when already allowed ingestion) - 750 mg / day for 7 days.

In the treatment of anaerobic infections adults are appointed Metronidazole 1-1.5 g per day, children - at a rate of 20-30 mg / kg per day.

With severe renal dysfunction (creatinine clearance less than 10 ml / min) daily dose should be reduced by 2 times.

Side effects:

Disorders from the gastrointestinal tract: pain in epigastrium. nausea, vomiting. diarrhea, glossitis, stomatitis, "metallic" taste in the mouth, decreased appetite, anorexia, dryness of the oral mucosa.constipation, pancreatitis (reversible cases), changing the language of color, coated tongue "(because of the proliferation of fungal microflora).

Immune system disorders: angioedema, anaphylactic shock.

Impaired nervous system: Peripheral sensory neuropathy, headache, convulsions, dizziness, reported on the development of encephalopathy and subacute cerebellar syndrome (loss of coordination and synergy of movements, ataxia, dysarthria, gait disturbance, nystagmus, tremor), which are reversible after discontinuation of metronidazola, aceptichesky meningitis.

Disorders of the psyche: psychotic disorders, including confusion, hallucinations; depression, insomnia, irritability, increased excitability.

Disorders from the side of the organ of vision: transient visual disturbances such as diplopia, myopia, blurred contours of objects, blurred vision, impaired color perception: neuropathy / optic neuritis.

Violations from the blood and lymphatic system: agranulocytosis, leukopenia, neutropenia, thrombocytopenia.

Disturbances from the liver and bile ducts: increased activity of "hepatic" enzymes (aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase), development of cholestatic or mixed hepatitis and hepatocellular liver damage, sometimes accompanied by jaundice; in patients who have been treated with metronidazole in combination with other antibacterial agents, there have been cases of liver failure that required liver transplantation.

Disturbances from the skin and subcutaneous tissues: rash, itching, skin flushing, hives, pustular skin rash, Stevens-Johnson syndrome. toxic epidermal necrolysis.

Disorders from the kidneys and urinary tract: staining of urine in a brownish-reddish color, due to the presence in the urine of a water-soluble metronidazole metabolite, dysuria, polyuria. cystitis, urinary incontinence, candidiasis.

General disorders and disorders at the site of administration: fever, nasal congestion, arthralgia, weakness.

Laboratory and instrumental data: flattening of the T wave on the electrocardiogram.

Interaction:

Pharmacodynamic: combined oral administration of metronidazole with antibiotics-aminoglycosides (neomycin, streptomycin, gentamicin and others), erythromycin depresses the pathogenic flora in the digestive tract, which reduces the likelihood of complications after surgery on the colon and rectum.

Under the influence of metronidazole, there may be an increase in the effects of indirect anticoagulants.

Under the influence of barbiturates, the effect of metronidazole may decrease, since its inactivation in the liver is accelerated.

With the combined use of metronidazole and ethanol due to the blockade of metronidazole enzyme aldehyde dehydrogenase, the development of disulfiram-like reactions (including facial flushing, vomiting, abdominal pain) is possible.

Do not combine metronidazole with disulfiram, since the interaction of these drugs may inhibit consciousness, psychotic disorders.

Pharmacokinetic: adsorbents, colestramine, astringent and enveloping agents reduce the absorption of metronidazole in the gastrointestinal tract.

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 simultaneous reception with drugs Li+ The concentration of the latter in the plasma and the development of symptoms of intoxication may increase.

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

Sulfonamides increase the antimicrobial effect of metronidazole.

Special instructions:

During the treatment period, ethanol intake is contraindicated.

In combination with amoxicillin, it is not recommended for patients under the age of 18 years. With prolonged therapy, it is necessary to monitor the blood picture.

With leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process.

When treating trichomonadal vaginitis in women and trichomoniasis in men, it is necessary to abstain from sexual activity. 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.

After treatment of Giardiasis, if symptoms persist, after 3 to 4 weeks, 3 feces should be analyzed at intervals of several days.

Can immobilize treponema and lead to Nelson's false positive test.

Form release / dosage:Tablets, 250 mg.

Packaging:

10 tablets per contour cell pack.

2 contour mesh packs together with instructions for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001401 / 01

Date of registration:29.10.2008 / 08.12.2015

Expiration Date:Unlimited

The owner of the registration certificate:TATHIMFARMPREPARATY, JSC TATHIMFARMPREPARATY, JSC Russia

Manufacturer: & nbsp

TATHIMFARMPREPARATY, JSC Russia

Representation: & nbspTATHIMFARM PREPARATIONS OJSC TATHIMFARM PREPARATIONS OJSC Russia

Information update date: & nbsp25.04.2018

Illustrated instructions

Instructions

Metronidazole (Metronidazole)