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

Excipients: lactose monohydrate (sugar milk) - 22.5 mg, povidone (polyvinylpyrrolidone) 9 mg, methylcellulose (methylcellulose water soluble) 0.5 mg, potato starch 6 mg, calcium stearate 3 mg,crospovidone (collidone CL-M) - 9 mg.

Description:

Tablets are white or white with a yellowish-greenish shade of color, flat-cylindrical shape, with a facet and a risk.

Pharmacotherapeutic group:Antimicrobial and antiprotozoal drug

ATX: & nbsp

P.01.A.B Nitroimidazole derivatives

P.01.A.B.01 Metronidazole

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. 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.

Active in a relationship Trichomonas vaginalis, Entamoeba histolytica, as well as Gram-negative anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteriodes ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp. and some Gram-positive anaerobes (sensitive strains Eubacterium spp., Clostridium spp., Peptococcus niger, Peptostreptococcus spp.). The minimum inhibitory concentration 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).

Metronidazole is insensitive to aerobic bacteria and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.

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, cerebrospinal fluid, brain, bile, saliva, amniotic fluid, abscess cavities, vaginal secretion, seminal fluid, breast milk, penetrates the blood-brain and placental barrier. Distribution: adults - approximately 0.55 l / kg.

The maximum concentration of the drug in the blood (C_m_Oh) is from 6 to 40 μg / ml, depending on the dose. The time to reach the maximum concentration (TC_max) - 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.

The half-life (T_1/2) with normal liver function - 8 hours (6 to 12 hours), with alcohol damage of the liver - 18 hours (10 to 29 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, cumulation of metronidazole in serum can be observed (therefore, the frequency of admission should be reduced in patients with severe renal insufficiency).

Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T_1/2 is reduced to 2.6 hours). When peritoneal dialysis is withdrawn in small quantities.

Indications:

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

Infections caused by Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus): infections of bones and joints, central nervous system infections, including meningitis, cerebral 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 fallopian tubes and ovaries, vaginal vaginal infection).

Pseudomembranous colitis associated with the use of antibiotics.

Treatment of infections caused by Helicobacter pylori, are performed as part of a combination therapy.

Gastritis or duodenal ulcer associated with Helicobacter pylori.

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

Contraindications:

Hypersensitivity to the components of the drug, leukopenia (including in the history), organic lesions of the central nervous system (including epilepsy), liver failure (in the case of the appointment of large doses).

Deficiency of lactose, lactose intolerance, glucose-galactose malabsorption.

Children's age (up to 3 years).

Carefully:

Renal / hepatic insufficiency.

Pregnancy and lactation:

Metronidazole has a high penetrating ability in breast milk, it penetrates the blood-brain and placental barrier. Therefore, the use of the drug during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

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

With trichomoniasis - 250 mg (1 tablet) 2 times a day for 10 days. Women are additionally appointed metronidazole in the form of vaginal suppositories or vaginal tablets containing 500 mg of metronidazole.

If necessary, you can repeat the course of treatment or increase the dose to 750 - 1000 mg / day (3-4 tabs / 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 (8 tablets) once to the patient and his sexual partner.

Children 3-5 years - 250 mg / day (1 table / day); 5-10 years - 250-375 mg / day (1-1,5 tablets / day), more than 10 years - 500 mg / day (2 tables / day). The daily dose should be divided into 2 divided doses. The course of treatment is 10 days.

With giardiasis (giardiasis) - 500 mg (2 tablets) 2 times a day for 5-7 days.

Children 3-5 years - 250 mg / day (1 table / day), 5-8 years - 375 mg / day (1.5 tablets / day), older than 8 years - 500 mg / day (2 tablets / day) 2 times a day for 5 days.

With chronic amebiasis daily dose of 1.5 g (6 tablets) in 3 divided doses for 5-10 days, with acute amoebic dysentery - 2.25 g (9 tablets) in 3 divided doses until symptoms stop.

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

For children 7-10 years the maximum daily dose is 1.25 g (5 tablets).

For the treatment of infectious diseases caused by anaerobic bacteria adults and children over 13 years - 500 mg (2 tablets) 3 times a day. The course of treatment is 7 days or more.

With pseudomembranous colitis - 500 mg (2 tablets) 3-4 times a day. Children in this case, the drug is not shown.

For eradication Helicobacter pylori - 500 mg (2 tablets) 3 times daily for 7 days (in combination therapy, e.g., a combination of amoxicillin with 2.25 g / d). Children in this case, the drug is not shown.

For the prevention of infectious complications - at 750-1500 mg / day (3 to 6 tablets) in 3 divided doses for 3-4 days before the operation or single 1 g (4 tablets) for the first day after the operation. 1-2 days after the operation (when it is already allowed to enter) - 750 mg / day (3 tablets / day) for 7 days.

Children from 5 to 12 years of 125 mg (0.5 tablets) every 8 hours for 2 days

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

Side effects:

Disturbances from the gastrointestinal tract: epigastric pain, nausea, vomiting, diarrhea, glossitis, stomatitis, "metallic" aftertaste in the mouth, reduced appetite, anorexia, dryness of the oral mucosa, constipation, pancreatitis (reversible cases), changes in language color / "coated tongue" (from for the growth of fungal flora).

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 metronidazole; aseptic 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 impairments, such as diplopia, myopia, vagueness of contours of subjects, reduced visual acuity, violation of color perception; Neuropathy / optic neuritis.

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

Disorders from the liver and bile ducts: increased activity of "liver" 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 liver failure 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 of 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.

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

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

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: nausea, vomiting, ataxia.

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

Interaction:

Increases the effect of indirect anticoagulants, which leads to an increase in prothrombin time.

Similarly, disulfiram causes intolerance to ethanol.

The interval between the use of disulfiram and metronidazole should be at least 2 weeks because of the possible development of various neurological symptoms.

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.

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

Together with the admission lithium drugs may increase the plasma concentration of the latter and the development of symptoms of intoxication.

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

Sulfonamides increase the antimicrobial effect of metronidazole.

The drug interaction with metronidazole with disulfan is noted.

Metronidazole reduces the clearance of fluorouracil, and therefore, can increase its toxicity.

With simultaneous use of metronidazole and cytotoxic immunosuppressive drugs significantly increases the risk of leukopenia and thrombocytopenia, which requires more careful monitoring of blood parameters.

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 reddish-brown 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. 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 (for some successfully cured patients lactose intolerance caused by the invasion may persist for several weeks or months, recalling the symptoms of giardiasis).

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

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, 250 mg.

Packaging:

10 tablets per contour cell packaging made of polyvinylchloride film and foil of aluminum printed lacquered or paper packaging with polymer coating.

For 20, 30, 40, 50, 60, 80,100 tablets in cans of polymer.

Each bank or 1, 2, 3, 4, 5 contour squares with instructions for use are placed in a cardboard pack.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

2 years.

The drug can not be used after the date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001459

Date of registration:20.10.2011 / 11.01.2016

Expiration Date:Unlimited

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Representation: & nbspURALBIOFARM, OJSCURALBIOFARM, OJSCRussia

Information update date: & nbsp25.04.2018

Illustrated instructions

Instructions

Metronidazole-UBF (Metronidazole-UBF)