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

auxiliary substances (core): lactose monohydrate 16.0 mg; cellulose microcrystalline 26.95 mg; povidone-K30 1.75 mg; corn starch 12.5 mg; sodium carboxymethyl starch type A 9.6 mg; silicon dioxide colloid 1.6 mg; magnesium stearate 1.6 mg;

film sheath: InstacoatUniversal A05R00878 orange 8.0 mg: hypromellose 65.00%, macrogol 13.00%, talc 2.00%, titanium dioxide (E 171) 16.92%, coloring sunset yellow sunset (E 110) 3.08%.

Description:

Round, biconvex tablets, covered with a film shell of orange color.

On the cross-section - the core is from white to light yellow color.

Pharmacotherapeutic group:antimicrobial and antiprotozoal agent

ATX: & nbsp

P.01.A.B Nitroimidazole derivatives

P.01.A.B.01 Metronidazole

Pharmacodynamics:

Metronidazole is a derivative of 5-nitroimidazole. The mechanism of action of metronidazole 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 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 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).

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:

Ingestion metronidazole quickly and almost completely absorbed (about 80% per hour). The intake of food does not affect the absorption of metronidazole. Bioavailability of at least 80%. After oral administration of 500 mg of metronidazole, the plasma concentration after 1 hour is 10 μg / ml, and after 3 hours - 13.5 μg / ml. The half-life (T_1/2) is 8-10 hours, the connection with blood proteins is insignificant and does not exceed 10-20%. Metronidazole quickly penetrates into tissues (lungs, kidneys, liver, skin, bile, cerebrospinal fluid, saliva, seminal fluid, vaginal secret), into breast milk and prodrugdit through the placental barrier. Metabolized about 30-60% of metronidazole by hydroxylation, oxidation and glucuronidation. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effects.Metronidazole is excreted by 40-70% of the kidneys (unchanged about 35% of the dose).

Indications:

Infections caused by Bacteroides spp. (including AT. fragilis, AT. ovatus, AT. distasonis, AT. thetaiotaomicron, AT. vulgatus): infection of bones and joints, sepsis, meningitis, brain abscess, bacterial endocarditis, pneumonia, pleural empyema, lung abscess.

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

Trichomoniasis in women (urethritis and vaginitis) and men (urethritis).

Amoebasis of the intestinal (including amoebic dysentery), extraintestinal (including liver abscess).

Pseudomembranous colitis (associated with the use of antibiotics).

A peptic ulcer associated with Helicobacter pylori (as part of complex therapy).

Prevention of postoperative infections (mainly surgery on the large intestine, gynecological operations).

Contraindications:

Hypersensitivity to metronidazole, other components of the drug, to imidazoles, as well as to the derivatives of nitroimidazole; organic lesions of the central nervous system (including epilepsy); leukopenia (including in the anamnesis); hereditary lactose intolerance, lactase deficiency or malabsorption syndrome,pregnancy; the period of breastfeeding; liver failure; children under 10 years old.

Carefully:

Renal failure, elderly age.

Dosing and Administration:

Inside, during or after a meal, without chewing, squeezed with enough water.

Anaerobic infections

Usually, treatment begins with intravenous infusions of metronidazole followed by a switch to taking Metronidazole-Teva, 250 mg tablets.

Adults and children over 10 years of age: 500 mg 3 times a day. The duration of treatment is up to 7 days.

Trichomoniasis

Adults and children over 10 years of age: with trichomoniasis in women (urethritis and vaginitis) the drug is used once in a dose of 2 g or in the form of course treatment for 10 days: 250 mg twice a day.

For trichomoniasis in men (urethritis), the drug is used once in a dose of 2 g or as a course of treatment for 10 days: 250 mg twice a day.

Pseudomembranous colitis: 500 mg 3-4 times a day. The duration of treatment is determined by the doctor.

Intestinal amebiasis

Adults and children over 15 years of age: 1500 mg / day in three divided doses for 7 days.

In acute amoebic dysentery - the daily dose is 2250 mg / day, divided into three doses. Children from 10 to 15 years: a dose of 500 mg / day, divided into 2 doses.

Abscess of the liver and other extraintestinal forms of amoebiasis

Adults and children over 15 years of age: the maximum daily dose is 2500 mg / day, divided into 3 doses, for 3-5 days, in combination with tetracycline antibiotics and other therapies.

Children from 10 to 15 years: a dose of 500 mg / day, divided into 2 doses.

A peptic ulcer associated with Helicobacter pylori

Adults and children over 10 years of age: 500 mg 3 times a day as part of a combination therapy, for example, with amoxicillin.

Prevention of postoperative infections

750-1500 mg / day in 3 divided doses 3-4 days before the operation. In 1-2 days after the operation (when already allowed ingestion) - 750 mg / day for 7 days.

With renal insufficiency correction of the dose is not required.

Side effects:

Disorders from the gastrointestinal tract: pain in the epigastrium, 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 / for proliferation 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 (impaired 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 disturbances such as diplopia, myopia, blurred contours of objects, blurred vision, impaired color perception: neuropathy / optic neuritis.

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

Disturbance of 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,treated with metronidazole in combination with other antibacterial agents, there were cases of liver failure that required liver transplantation.

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, congestion or swelling at the injection site) (for parenteral dosage forms).

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

Overdose:

The cases of a single administration of metronidazole up to 12 g, accompanied by vomiting, nausea, ataxia and insignificant disorientation are described.

Treatment: symptomatic therapy.

Interaction:

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

Alcohol intake during treatment with Metronidazole-Teva can have an effect similar to the effect of disulfiram (heat, vomiting, tachycardia, lowering blood pressure). Patients should be warned that, during treatment and 48 hours after discontinuation of treatment with Metronidazole-Teva, alcoholic beverages or drugs containing ethyl alcohol should not be consumed.

An increase in the anticoagulant effect and an increased risk of hemorrhagic complications may be associated with a slowdown in hepatic metabolism with simultaneous use of metronidazole and anticoagulants of indirect actionwarfarin). In case of simultaneous use, monitoring of prothrombin time and, if necessary, correction of anticoagulant doses are required.

With simultaneous administration of metronidazole with lithium preparations, the concentration of lithium in blood plasma can increase.At simultaneous application it is necessary to monitor plasma concentrations of lithium, the concentration of creatinine and the content of electrolytes in the blood plasma.

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 the serum concentration of cyclosporine and creatinine is required.

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

The simultaneous use of metronidazole with drugs, which are inducers of microsomal oxidation enzymes in the liver (phenobarbital, phenytoin) can accelerate the excretion of metronidazole, as a result of which its concentration in the blood plasma decreases. Metronidazole slows the metabolism of phenytoin (increase in the concentration of phenytoin in the blood plasma). Primidone accelerates the metabolism of metronidazole and causes a decrease in its concentration in the blood plasma.

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

Metronidazole increases the concentration of busulfan in the blood plasma, which can lead to the development of severe toxic effects of busulfan.

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

Sulfonamides increase the antimicrobial effect of metronidazole.

It is possible to reduce the contraceptive effect of estrogens in the use of metronidazole.

Special instructions:

During the treatment with Metronidazole-Teva, the clinical status and results of laboratory tests (in particular, the number of white blood cells) should be regularly analyzed, especially if the drug is used for more than 10 days.

It should stop treatment when ataxia, dizziness, the development of hallucinations, with worsening neurological status of patients.

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.

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:

It is necessary to refrain from driving a car, from engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions due to the fact that drowsiness, dizziness, confusion, hallucinations, convulsions or transient visual impairment may develop.

Form release / dosage:

Tablets, film-coated, 250 mg.

Packaging:

For 10 tablets in a blister of PVC / aluminum foil.

1 or 2 blisters together with instructions for use in a cardboard bundle.

Storage conditions:

Store at a temperature of no higher than 25 ° C, in a place protected from light.

Keep out of the reach of children.

Shelf life:

2 of the year.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002531

Date of registration:15.07.2014

Expiration Date:15.07.2019

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

RUSAN PHARMA, Ltd. India

Representation: & nbspTeva Teva Israel

Information update date: & nbsp10.09.2016

Illustrated instructions

Instructions

Metronidazole-Teva (Metronidazole-Teva)