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

Pharmacodynamics:Antiprotozoal and antibacterial drug, a derivative of 5-nitroimidazole. The mechanism of action is the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic bacteria and protozoa. Reduced 5-nitrothe metronidazole group interacts with the DNA of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active in a relationship Trichomonas vaginalis, Entamoeba histolytica, as well as Gram-negative anaerobes Bacteroides spp. (including V. fragilis, AT. distasonis, AT. ovatus, AT. thetaiotaomicron, AT. vulgatus), Fusobacterium spp. and some Gram-positive anaerobes (sensitive strains Eubacterium spp., Clostridium spp., Peptococcus niger, Peptostreptococcus spp.). The minimum inhibitory concentration (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 bacteria and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.

Increases the sensitivity of tumors to irradiation, causes disulfiram-like reactions.

Pharmacokinetics:

Absorption is high (bioavailability is not less than 80%). It has a high penetrating ability, reaching bactericidal concentrations in most tissues and body fluids, including lungs, kidneys, liver, skin, CSF, brain, bile, saliva, amniotic fluid, abscess cavities, vaginal secretion, seminal fluid, breast milk, penetrates the BBB and the placental barrier.

The volume of distribution: adults - about 0.55 l / kg, newborns - 0.54-0.81 l / kg. FROM_mOhis between 6 and 40 μg / ml, depending on the dose. TFROM_mOh- 1-3 hours. Connection with plasma proteins - 10-20%.

In the body, about 30-60% of metronidazole is metabolized by hydroxylation, oxidation and glucuronation. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effects.

T_1/2with normal liver function - 8 hours (6 to 12 hours), with alcohol damage of the liver - 18 hours (10 to 29 hours), in newborns: those born at the gestational age of 28-30 weeks.- approximately 75 hours, 32-35 weeks. - 35 hours, 36-40 weeks. - 25 hours.

It is excreted by the kidneys 60-80% (20% unchanged), through the intestine - 6-15%. Kidney clearance - 10.2 ml / min.

In patients with impaired renal function after repeated administration of metronidazole cumulation in serum can be observed (hence patients with severe renal impairment receiving frequency to be reduced). Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T_1/2is reduced to 2.6 hours). When peritoneal dialysis is withdrawn in small quantities.

Indications:

Protozoal infections: extraintestinal amebiasis, including amoebic liver abscess, intestinal amoebiasis (amoebic dysentery), trichomoniasis (including trichomonas vaginitis, trichomonas urethritis).

Infections caused by Bacteroides spp. (incl. B. fragilis, AT. distasonis, AT. ovatus, AT. thetaiotaomicron, AT. vulgatus): infections of bones and joints, infection of the central nervous system, incl. meningitis, brain abscess, bacterial endocarditis, pneumonia, empyema and lung abscess, sepsis.

Infections caused by the species Clostridium spp., Peptococcus niger and Peptostreptococcus spp.: infection of the abdominal cavity (peritonitis, liver abscess), pelvic infection (endometritis, abscess of the fallopian tubes and ovaries, vaginal vaginal infection).

Pseudomembranous colitis (associated with the use of antibiotics).

Gastritis or duodenal ulcer associated with Helicobacter pylori.

Prevention of postoperative complications (especially interference on the colon, paraectal area, appendectomy, gynecological operations).

Radiation therapy of patients with tumors as a radiosensitizing drug in cases where tumor resistance is due to hypoxia in tumor cells.

Contraindications:

Hypersensitivity to the components of the drug and other derivatives of nitroimidazole, leukopenia (including in the anamnesis), organic lesions of the central nervous system (including epilepsy), liver failure (in the case of high doses), pregnancy (I trimester), lactation .

Children's age (up to 3 years).

Carefully:

Pregnancy (II-III trimesters), renal / hepatic insufficiency.

Pregnancy and lactation:

The use of the drug during pregnancy and during breastfeeding is contraindicated.

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

Dosing and Administration:

Inside. Inside, during or after a meal (or squeezed milk), without chewing.

With trichomoniasis - 250 mg twice a day for 10 days or 400 mg twice a day for 5-8 days. Women need to be additionally appointed metronidazole in the form of vaginal suppositories or tablets. If necessary, you can repeat the course of treatment or increase the dose to 0.75-1 g / day. Between the courses should be a break in 3-4 weeks. with the conduct of repeated control laboratory tests. An alternative scheme of therapy is the appointment of 2 g once to the patient and his sexual partner. Children 3-5 years - 250 mg / day .; 5-10 years - 250-375 mg / day; over 10 years - 500 mg / day. The daily dose should be divided into 2 divided doses. The course of treatment is 10 days.

With giardiasis (giardiasis) - 500 mg twice a day for 5-7 days. Children 3-5 years - 250 mg / day, 5-8 years - 375 mg / day, over 8 years - 500 mg / day. (in 2 admission). The course of treatment is 5 days.

With chronic amebiasis daily dose - 1,5 g in 3 admission for 5-10 days, with acute amoebic dysentery - 2.25 g in 3 divided doses until symptoms stop.

With liver abscess the maximum daily dose is 2.5 g in 1 or 2-3 doses, for 3-5 days, in combination with antibiotics (tetracyclines) and other therapies. Children 3-7 years - 1/3 of the dose of an adult, 7-10 years - 1/2 dose adult.

With ulcerative stomatitis adults are prescribed 500 mg twice a day for 3-5 days; children in this case, the drug is not shown.

With pseudomembranous colitis - 500 mg 3-4 times a day.

For eradication Helicobacter pylori - 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 infectious complications - 750-1500 mg / day. in 3 admission for 3-4 day before surgery or once 1 g on the first day after surgery. In 1-2 days after the operation (when already allowed ingestion) - 750 mg / day. within 7 days.

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

Anaerobic bacterial infections: children - 7 mg / kg every 8 hours, the course of treatment - 7-10 days. The course of treatment can be repeated after 10-15 days.

Side effects:

Disorders from the gastrointestinal tract: epigastric pain, nausea, vomiting, diarrhea, glossitis, stomatitis, metallic taste in the mouth, decreased appetite, anorexia, dryness of the oral mucosa, constipation, pancreatitis (reversible cases), discoloration of the tongue / "lipped tongue" ( because of the growth of fungal microflora).

Immune system disorders: angioedema, anaphylactic shock.

Disturbances from the nervous system: peripheral sensory neuropathy, headache, convulsions, dizziness, reported on the development of encephalopathy and subacute cerebellar syndrome (disruption of coordination and synergy of movements, ataxia, dysarthria, gait disorders, nystagmus, tremor) that are reversible after metronidazole withdrawal, aseptic meningitis.

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

Disturbances on the part of the organ of sight: transient visual impairment, 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, thrombocytopenia.

Disturbances from the liver and bile ducts: increase 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 treated with metronidazole in combination with other antibacterial agents, cases of hepatic insufficiency that required liver transplantation were observed.

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

Disorders from the kidneys and urinary tract: staining 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 (for oral and parenteral dosage forms), thrombophlebitis (pain, hyperemia or swelling at the injection site) (for parenteral dosage forms).

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

Overdose:

Symptoms: nausea, vomiting, ataxia; when taken as a radiosensitizing agent - convulsions,peripheral neuropathy.

Treatment: there is no specific antidote, symptomatic and supportive therapy.

Interaction:

Pharmacodynamic: joint oral administration of metronidazole with antibiotics-aminoglycosides (neomycin, streptomycin, gentamicin , etc.), 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, it is possible to enhance the effects of anticoagulants indirect action.

Under the influence of barbiturates, it is possible to reduce the effect of metronidazole, since its inactivation in the liver is accelerated.

The spectrum of action of metronidazole expands when combined with sulfanylamides and cephalosporins. Sulfonamides increase the antimicrobial effect of metronidazole.

With the combined use of metronidazole and ethyl alcohol, due to the blockade of metronidazole enzyme aldehyde dehydrogenase, it is possible to redden the face, vomiting, abdominal pain,

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

Simultaneous use with disulfiram can lead to the development of various neurologic symptoms (the interval between appointments is at least 2 weeks).

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 to increase its concentration in the blood serum and increase the risk of side effects.

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

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

Special instructions:

In the period of treatment, the use of ethanol is contraindicated (development of disulfiram-like reactions is possible: abdominal pain of a spastic nature, nausea, vomiting, headache, sudden "tide" of blood to the face).

In combination with amoxicillin it is not recommended to use in patients younger than 18 years.

With prolonged therapy, it is necessary to monitor the picture of peripheral blood. With leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process.

The appearance of ataxia, dizziness and any other deterioration in the neurological status of patients requires discontinuation of treatment.

Can immobilize treponema and lead to Nelson's false positive test. Stains urine in a dark color.

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. After therapy with trichomoniasis, control tests should be performed for 3 consecutive cycles before and after menstruation.

Effect on the ability to drive transp. cf. and fur:Investigations of the drug on the reaction rate when driving vehicles or working with other mechanisms were not carried out.

Form release / dosage:Pills, 250 mg.

Packaging:

For 10 tablets in a contour mesh package or in a contour non-jawed package.

1, 2 contour packs together with instructions for use are placed in a cardboard pack.

Contour non-cellular packages are allowed together with instructions for use in group packaging.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000862

Date of registration:14.10.2011

Expiration Date:14.10.2016

The owner of the registration certificate:Tyumen Chemical - Pharmaceutical Plant, OJSC Tyumen Chemical - Pharmaceutical Plant, OJSC Russia

Manufacturer: & nbsp

Tyumen Chemical - Pharmaceutical Plant, OJSC Russia

Information update date: & nbsp11.09.2016

Illustrated instructions

Instructions

Metronidazole-LekT (Metronidazol-LekT)