INSTRUCTIONS for medical use of the drug
Tradename: METROGIL ®
Composition per 1 ml of solution
Active ingredient: metronidazole – 5.0 mg. Auxiliary substances: sodium chloride 7.9 mg, citric acid monohydrate 0.229 mg, sodium hydrogen phosphate 0.467 mg, water for injection – sk. required, up to 1 ml.
Description: Clear solution from colorless to light yellow color.
ATX code: [J01XD01]
Pharmacodynamics. Anti-protozoan and antimicrobial drug derived from 5-nitroimidazole. 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 recovered 5-nitro group of metronidazole interacts with the microbial cell DNA, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.
Active against Trichomonas vaginalis, Entamoeba histolytica, as well as Gram-negative anaerobes Bacteroides spp. (at
In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin inhibits the development of metronidazole resistance).
Aerobic microorganisms and facultative anaerobes are insensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes), metronidazole acts synergistically with antibiotics that are effective against ordinary aerobes. It increases the sensitivity of tumors to radiation, causes disulfiram-like reactions, stimulates reparative processes.
Pharmacokinetics 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, abscesses, vaginal secretions, seminal fluid, breast milk, passes through . hemato-encephalic and placental barrier. Volume of distribution: adults – approximately
Communication with plasma proteins -10-20%.
With intravenous administration of 500 mg of the drug for 20 minutes, the maximum concentration (C max) in the serum is: after 1 h.
In the body, about 30-60% of metronidazole is metabolized by hydroxylation, oxidation and glucuronidation. The main metabolite (2-hydroxymetronidazole) also has an antiprotozoal and antimicrobial effect.
The elimination half-life with normal liver function is 8 hours (from 6 to 12 hours), with alcoholic liver damage – 18 hours (from 10 to 29 hours), in newborns: born during the gestation period – 28-30 weeks – approximately 75 hours, 32 -35 weeks – 35 hours, 36-40 weeks – 25. hours
Excreted by the kidneys 60-80% (20% unchanged), through the intestines – 6-15%. Kidney clearance –
Metronidazole and the major metabolites are rapidly removed from the blood during hemodialysis (the half-life is reduced to
Indications for use Protozoal infections: extraintestinal amebiasis, including amebic liver abscess, intestinal amebiasis (amebic dysentery), trichomoniasis (in
Infections caused by Bacteroides spp. (at
Infections caused by Clostridium spp., Peptococcus, Peptostreptococcus: abdominal infections (peritonitis, liver abscess), pelvic infection (endometritis, endomyometritis, abscess of the fallopian tubes and ovaries, vaginal arch infection).
Prevention of postoperative complications (especially interventions on the colon, near-rectal area, appendectomy, gynecological surgery).
Radiation therapy of patients with tumors – as a radiosensitizing drug in cases when tumor resistance is due to hypoxia in the tumor cells.
Contraindications Hypersensitivity to metronidazole or components that make up the drug, as well as to other nitroimidazole derivatives; I trimester of pregnancy, lactation, organic lesions of the central nervous system (in
Carefully Pregnancy (II-III trimesters), renal / hepatic failure.
Pregnancy and lactation.
- I trimester of pregnancy is contraindicated;
- nursing mothers – according to indications, with the simultaneous termination of breastfeeding.
Dosage and administration Intravenous administration of the drug is indicated in severe infections, as well as in the absence of the possibility of taking the drug inside.
Adults and children over 12 years old have an initial dose of 0.5 – 1 g, intravenous drip (duration of infusion – 30 – 40 minutes), and then every 8 hours 500 mg at a rate of 5 ml / min. With good portability after the first 2-3 infusions go on jet injection. The course of treatment is 7 days. If necessary, intravenous administration is continued for a longer time. The maximum daily dose is 4 g. With the improvement of the patient’s condition, according to the indications, a transition is made to supporting the oral administration of the drug at a dose of 400 mg 3-5 times a day.
Children under the age of 12 are prescribed according to the same scheme in a single dose – 7.5 mg / kg. When purulent-septic diseases usually spend 1 course of treatment.
For prophylactic purposes, adults and children over 12 years of age are prescribed intravenously in a dose of 0.5 -1 g on the eve of the operation, on the day of surgery and the next day – 1.5 g / day (500 mg every 8 hours). After 1-2 days, go to maintenance therapy inside. Patients with chronic renal insufficiency and creatinine clearance less than 30 ml / min and / or liver failure have a maximum daily dose of not more than 1 g, the dose rate is 2 times a day.
As a radiosensitizing drug, the drug is administered intravenously at the rate of 160 mg / kg or 4-6 g / sq m of body surface 0.5-1.0 hours before the start of irradiation. Apply before each session for 1-2 weeks. In the remaining period of radiation treatment, metronidazole is not used. The maximum single dose should not exceed 10 g, the course one 60 g. To relieve the intoxication caused by irradiation, apply a drip of a 5% solution of dextrose, hemodez or 0.9% sodium chloride solution.
Side effect. On the part of the digestive system: diarrhea, anorexia, nausea, vomiting, intestinal colic, constipation, “metallic” taste in the mouth, dry mouth, glossitis, stomatitis, pancreatitis.
Nervous system disorders: dizziness, incoordination, ataxia, confusion, irritability, depression, irritability, weakness, insomnia, headache, convulsions, hallucinations, peripheral neuropathy.
Allergic reactions: urticaria, skin rash, skin flushing, nasal congestion, fever, arthralgia.
On the part of the urinary system: dysuria, cystitis, polyuria, urinary incontinence, candidiasis, urine staining in red-brown color.
Local reactions: thrombophlebitis (pain, hyperemia or swelling at the injection site).
Other: neutropenia, leukopenia, flattening of the T wave on the ECG.
Overdose. Symptoms: nausea, vomiting, ataxia; when taken as a radiosensitizing agent – convulsions, peripheral neuropathy. Treatment: specific antidote – absent, symptomatic and supportive therapy.
Interaction with other drugs Metronidazole for intravenous administration is not recommended to be mixed with other medications.
It enhances the effect of indirect anticoagulants, which leads to an increase in prothrombin time.
Similarly, disulfiram causes intolerance to ethanol. Simultaneous use with disulfiram can lead to the development of various neurological symptoms (the interval between administration is at least 2 weeks).
Cimetidine inhibits the metabolism of metronidazole, which can lead to an increase in its concentration in serum and an increase in the risk of side effects.
The simultaneous administration of drugs that stimulate microsomal oxidation enzymes in the liver (phenobarbital, phenytoin) can accelerate the elimination of metronidazole, as a result of which its concentration in plasma decreases.
When taken simultaneously with lithium preparations, the concentration of the latter in plasma and the development of symptoms of intoxication may increase.
It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).
Sulfonamides enhance the antimicrobial action of metronidazole.
special instructions During the treatment period: ethanol is contraindicated (possibly, the development of disulfiram-like reactions: abdominal pain of a spastic nature, nausea, vomiting, headache, sudden flushing of the face). In combination with amoxicillin is not recommended for use in patients younger than 18 years. When treating Trichomonas vaginitis in women and Trichomonas urethritis in men, it is necessary to refrain from sex. Necessarily simultaneous treatment of sexual partners. After treating trichomoniasis, control tests should be carried out for 3 consecutive cycles before and after menstruation. With prolonged therapy, it is necessary to control the picture of peripheral blood. The appearance of ataxia, dizziness, and any other deterioration in the neurological status of patients requires discontinuation of treatment. It can immobilize treponema and lead to a false-positive Nelson test. It paints urine in a dark color.
Influence pa ability to drive and working mechanisms During the period of treatment, care must be taken when driving vehicles and when engaging in other potentially hazardous activities that require increased concentration and psychomotor speed (dizziness, impaired consciousness, hallucinations, convulsions, impaired coordination of movements, ataxia are possible).
Release form Solution for intravenous administration of 5 mg / ml. By 20 ml in a glass ampoule (type 1,
Storage At a temperature not higher than 30 ° C in a dark place. Do not freeze. Keep out of the reach of children.
Released from pharmacies: by prescription
Manufacturer “Unic Pharmaceutical Laboratories” (Branch of the company “
Addresses of production sites Plot number 4, Phase IV,
Representative office in Russia Moscow 121059, st. Bryansk, 5