Metrogyl solution for infusion instructions, use. Metrid, solution for infusion Metrogyl for intravenous administration instructions

Rosacea (including post-steroid acne);

Vulgar acne;

Oily seborrhea, seborrheic dermatitis;

Trophic ulcers lower limbs(on the background varicose veins veins, diabetes);

Poorly healing wounds;

Bedsores;

Hemorrhoids, anal fissures.

Release form of the drug Metrogyl

solution for intravenous administration 5 mg/ml; polyethylene bottle (bottle) 100 ml, box (box) 1;
solution for intravenous administration 5 mg/ml; ampoule 20 ml, box (box) 5;
solution for intravenous administration 5 mg/ml; polyethylene bottle (bottle) 100 ml, film wrapper 1, cardboard pack 1;
solution for intravenous administration 5 mg/ml; ampoule 20 ml, cardboard pack 5;
solution for intravenous administration 5 mg/ml; ampoule 20 ml, thermal container 5, cardboard pack 1;

Pharmacodynamics of the drug Metrogyl

Antiprotozoal and antimicrobial 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 microorganisms and protozoa. The reduced 5-nitro group of metronidazole interacts with the DNA of microbial cells, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active against Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardiai ntestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevolella spp. (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp). In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).

Aerobic microorganisms and facultative anaerobes are insensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes), metronidazole acts synergistically with antibiotics effective against common aerobes. Increases the sensitivity of tumors to radiation, causes disulfiram-like reactions, and stimulates reparative processes.

Pharmacokinetics of the drug Metrogyl

With intravenous administration of 500 mg of Metrogyl over 20 minutes, the concentration of the drug in the blood serum was 35.2 μg/ml after an hour, 33.9 μg/ml after 4 hours, and 25.7 μg/ml after 8 hours. With normal bile formation, the concentration of metronidazole in bile after intravenous administration can significantly exceed the concentration in plasma. About 30-60% of metronidazole is metabolized in the body by hydroxylation, oxidation and glucuronidation. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effect.

T1/2 with normal liver function - 8 hours (from 6 to 12 hours), with alcoholic liver damage - 18 hours (from 10 to 29 hours), in newborns: those born during pregnancy - 28-30 weeks - approximately 75 hours, 32-35 weeks - 35 hours, 36-40 weeks - 25 hours. 60-80% is excreted by the kidneys (20% unchanged), through the intestines - 6-15%. Renal clearance – 10.2 ml/min. In patients with impaired renal function, after repeated administration, accumulation of metronidazole in the blood serum may occur (therefore, in patients with severe renal failure the frequency of administration should be reduced). Metronidazole and its main metabolites are quickly removed from the blood during hemodialysis (T1/2 is reduced to 2.6 hours). During peritoneal dialysis, it is excreted in small quantities.

Using Metrogyl during pregnancy

I trimester of pregnancy is contraindicated; II and III trimesters of pregnancy - only for health reasons;

For nursing mothers - according to indications with simultaneous cessation of breastfeeding.

Contraindications to the use of the drug Metrogyl

Organic lesions of the central nervous system (including epilepsy);

Liver failure (in case of high doses);

Blood diseases;

Pregnancy (first trimester);

Lactation period;

Hypersensitivity to metronidazole or other nitroimidazole derivatives.

Caution - renal failure.

Side effects of the drug Metrogyl

From the outside digestive system: diarrhea, loss of appetite, nausea, vomiting, intestinal colic, constipation, metallic taste in the mouth, dry mouth, glossitis, stomatitis, pancreatitis.

From the outside nervous system: dizziness, impaired coordination of movements, ataxia, confusion, irritability, depression, increased excitability, weakness, insomnia, headache, seizures, hallucinations, peripheral neuropathy.

Allergic reactions: urticaria, skin rash, skin hyperemia, nasal congestion, fever, arthralgia.

From the urinary system: dysuria, cystitis, polyuria, urinary incontinence, candidiasis, red-brown coloration of urine.

Local reactions: thrombophlebitis (pain, hyperemia or swelling at the injection site).

Other: neutropenia, leukopenia, flattening of the T wave on the ECG.

Method of administration and dosage of the drug Metrogyl

IV administration of the drug is indicated for severe course infections, as well as in the absence of the possibility of taking the drug orally.

Adults and children over 12 years old - an initial dose of 0.5-1 g intravenously (duration of infusions - 30-40 minutes), and then every 8 hours, 500 mg at a rate of 5 ml/min. If well tolerated, after the first 2-3 infusions they switch to jet administration. The course of treatment is 7 days. If necessary, intravenous administration is continued for a longer time. Maximum daily dose- 4 g. According to indications, switch to maintenance oral administration at a dose of 400 mg 3 times a day.

Children under 12 years of age are prescribed according to the same regimen in a single dose of 7.5 mg/kg.

At purulent-septic diseases usually carry out 1 course of treatment.

For preventive purposes, adults and children over 12 years of age are prescribed 0.5-1 g intravenously on the eve of surgery, on the day of surgery and the next day - 1.5 g / day (500 mg every 8 hours). After 1-2 days, they switch to maintenance therapy orally.

Patients with chronic renal failure and CC less than 30 ml/min and/or liver failure The maximum daily dose is no more than 1 g, the frequency of administration is 2 times a day.

Overdose of Metrogyl

Symptoms: nausea, vomiting, ataxia, in severe cases - peripheral neuropathy and epileptic seizures.

Treatment: symptomatic; There is no specific antidote.

Interactions of the drug Metrogyl with other drugs

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

Similar to disulfiram, it causes ethanol intolerance. Simultaneous use with disulfiram can lead to the development of various neurological symptoms(the interval between appointments is at least 2 weeks).

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

Simultaneous administration medicines, stimulating enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin), can accelerate the elimination of metronidazole, resulting in a decrease in its concentration in plasma.

At simultaneous administration with lithium preparations, the concentration of the latter in plasma may increase and symptoms of intoxication may develop.

Sulfonamides enhance the antimicrobial effect of metronidazole.

Special instructions when taking the drug Metrogyl

During the treatment period, alcohol intake is contraindicated (disulfiram-like reactions may develop: abdominal pain of a spastic nature, nausea, vomiting, headache, sudden rush of blood to the face).

With long-term 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.

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

May immobilize treponemes and lead to false positive test Nelson.

Colors urine dark.

Storage conditions for the drug Metrogyl

List B.: In a place protected from light, at a temperature not exceeding 30 °C (do not freeze).

Shelf life of the drug Metrogyl

The drug Metrogyl belongs to the ATX classification:

G Genitourinary system and sex hormones

G01 Antiseptics and antimicrobials for treatment gynecological diseases

G01A Antiseptics and antimicrobials for the treatment of gynecological diseases (excluding combinations with corticosteroids)

G01AF Imidazole derivatives

Instructions for medical use

medicine

METRID

Tradename

International nonproprietary name

Metronidazole

Dosage form

Solution for infusion, 0.5% 100 ml

Compound

100 ml of solution contains

active substance: metronidazole 500 mg,

Excipients: sodium chloride, citric acid monohydrate, disodium hydrogen phosphate anhydrous, water for injection.

Description

Transparent colorless or light yellow color solution

Pharmacotherapeutic group

Antibacterial drugs for systemic use. Other antibacterial drugs. Imidazole derivatives. Metronidazole

ATX code J01XD01

Pharmacological properties

Pharmacokinetics

Distribution

After intravenous administration at a dose of 500 mg for 20 minutes, the maximum concentration in the blood serum after 1 hour is 35.2 μg/ml, after 4 hours - 33.9 μg/ml, after 8 hours - 25.7 μg/ml; minimum concentration with subsequent administration - 18 mcg/ml. With intravenous administration, the maximum concentration is reached after 30-60 minutes, the therapeutic concentration remains for 6-8 hours. With normal bile formation, the concentration of metronidazole in bile after intravenous administration can significantly exceed the concentration in plasma.

Plasma protein binding - 10-20%. The volume of distribution in adults is 0.55 l/kg, in newborns - 0.54-0.81 l/kg.

Metronidazole has high penetrating ability. Reaches bactericidal concentrations in the lungs, kidneys, liver, brain, skin, cerebrospinal fluid, bile, saliva, amniotic fluid, abscess cavities, vaginal secretions, seminal fluid, breast milk. Penetrates the blood-brain barrier and passes through the placental barrier.

Metabolism

Metabolized (about 30-60%) by hydroxylation, oxidation and glucuronidation. The main metabolite - 2 oxymetronidazole - has antiprotozoal and antimicrobial effects.

Removal

Excreted by the kidneys (60-80%), 20% - unchanged; 6-15% is excreted through the intestines. The half-life is 8 hours (6-12 hours). Renal clearance - 10.2 ml/min.

Pharmacokinetics in special clinical situations

With alcoholic liver damage, the half-life is 18 hours (10-29 hours), in newborns born at a gestational age of 28-30 weeks - 75 hours, at a period of 32-35 weeks - 35 hours, at a period of 36-40 weeks - 25 hours .

In patients with impaired renal function, accumulation of metronidazole in the blood serum may occur after repeated administration.

Pharmacodynamics

Antiprotozoal and antimicrobial drug, a derivative of 5-nitroimidazole. The mechanism of action is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group interacts with DNA, inhibiting its synthesis, which leads to the death of bacteria.

A drug active against protozoa: Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp.; anaerobic bacteria: Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella spp. (Prevotella bivia, Prevotella buccae, Prevotella disiens), Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp. The minimum inhibitory concentration for these strains is 0.125-6.25 μg/ml.

In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).

To the drug stable aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes), metronidazole acts synergistically with antibiotics effective against aerobes.

The drug increases the sensitivity of tumors to radiation, has a disulfiram-like effect, and stimulates reparative processes.

Indications for use

Treatment of infectious and inflammatory diseases caused by pathogens sensitive to the drug, including:

• severe forms of hepatic and intestinal amebiasis
• infections of bones and joints, including osteomyelitis
• central nervous system infections, including meningitis, brain abscess
• bacterial endocarditis
• necrotizing pneumonia, empyema, lung abscess
• infections abdominal cavity, including peritonitis, liver abscess
• infections of the pelvic organs (endometritis, endomyometritis, abscess fallopian tubes and ovaries, infections of the vaginal vault after surgical interventions)
• skin and soft tissue infections
• sepsis, gas gangrene
• as a radiosensitizing agent for radiation therapy(in cases where tumor resistance is due to hypoxia in tumor cells)
• prevention and treatment of postoperative infections (especially after operations on colon, perirectal area, appendectomy, gynecological interventions)

Mode of applicationAnddoses

The drug is intended for intravenous infusion.

Adults and children over 12 years old the drug is prescribed in an initial dose of 0.5-1 g (infusion duration 30-40 minutes). Then every 8 hours, 500 mg at a rate of 5 ml/min. If well tolerated, after the first 2-3 infusions they switch to jet administration. The course of treatment is 7 days. The maximum daily dose is 4 g. According to indications, switch to maintenance oral administration at a dose of 400 mg 3 times a day.

Children under 12 years of age prescribed according to the same regimen in a single dose of 7.5 mg/kg (1.5 ml).

At purulent-septic diseases usually carry out 1 course of treatment.

IN for preventive purposes adults and children over 12 years old Prescribe 0.5-1 g drips on the eve of surgery, on the day of surgery and the next day - 1.5 g per day (500 mg every 8 hours). After 1-2 days, they switch to maintenance therapy (metronidazole taken orally).

For patients with chronic renal failure (with CC less than 30 ml/min) and/or with liver failure the maximum daily dose is 1 g (with a frequency of administration 2 times a day).

IN as a radiosensitizing agent the drug is administered intravenously at a rate of 160 mg/kg or 4-6 g/m2 of body surface 0.5-1 hour before the start of irradiation. Apply before each irradiation session for 1-2 weeks. During the remaining period of radiotherapy, metronidazole is not used. Maximum single dose- 10 g, coursework - 60 g.

Side effects

Often(≥1/10)

Headache

Nausea

Often(≥1/100 to<1/10)

Abdominal pain, abdominal cramps

Infrequently(≥1/1000 to<1/100)

Anorexia, vomiting, coated tongue

Peripheral neuropathy (numbness of the extremities), dizziness, incoordination, drowsiness, dysgeusia (metallic taste)

Increased temperature, fever

Skin hyperemia

Nasal congestion

Arthralgia

Flattening of the T wave on the ECG

Dysuria, cystitis, polyuria, urinary incontinence, candidiasis

Quincke's edema, itching, rash, urticaria

Rarely(≥1/10000 to<1/1000)

Confusion, ataxia, irritability, depression, increased excitability, weakness, insomnia, convulsions, hallucinations, peripheral neuropathy

Decreased appetite, constipation

Dry mucous membrane, glossitis, stomatitis

Pancreatitis

Darkening of urine

Very pcaustically(<1/10000)

Neutropenia (leukopenia)

Anaphylactic reactions

Thrombophlebitis

Cholestasis, jaundice

Erythema multiforme

Increased liver enzyme activity

These phenomena usually disappear with a reduction in the administered dose or after completion of the course of therapy.

Contraindications

Hypersensitivity to the components of the drug and other nitroimidazole derivatives

Leukopenia (including history)

Organic lesions of the central nervous system, including epilepsy

Liver failure (when using the drug in high doses)

Pregnancy (1st trimester)

Lactation period

Severe renal failure

Drug interactions

With simultaneous use of Metrid:

With indirect anticoagulants, an increase in prothrombin time is observed;

With preparations of lithium salts, it is possible to increase the concentration of lithium in the blood plasma and develop symptoms of intoxication;

With prednisolone - the excretion of metronidazole from the body increases due to the acceleration of its metabolism in the liver under the influence of prednisolone;

With cimetidine - inhibition of the metabolism of metronidazole is noted, which can lead to an increase in the concentration of metronidazole in the blood plasma and an increased risk of adverse reactions;

With drugs that stimulate microsomal liver enzymes (phenytoin, phenobarbital), the elimination of metronidazole may be accelerated, resulting in a decrease in its concentration in the blood plasma;

With rifampicin - the clearance of metronidazole from the body increases,

With phenytoin - a slight increase in the concentration of phenytoin in the blood plasma is possible; a case of toxic effects has been described;

With fluorouracil - the toxic effect is enhanced, but not the effect of fluorouracil;

With ethanol, disulfiram-like reactions develop;

With disulfiram - can lead to the development of neurological reactions (the interval between prescriptions should be at least 2 weeks).

Sulfonamides and antibiotics enhance the antimicrobial effect of metronidazole.

Pharmaceutical interactions

Metronidazole for intravenous administration is not recommended to be mixed with other drugs.

special instructions

It should be taken into account that during the period of use of the drug, alcohol intake is contraindicated, since the development of a disulfiram-like reaction (cramping abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face) is possible.

During long-term therapy, blood counts should be monitored. With leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process. Use with caution for liver and kidney diseases.

If neurological symptoms develop (ataxia, dizziness and any other symptoms of deterioration of neurological status), the use of the drug should be discontinued.

The drug can immobilize treponemes and lead to a false-positive Nelson test.

Pregnancy and lactation

In the second and third trimesters of pregnancy, the drug should be prescribed only for health reasons, carefully assessing the expected benefits of therapy for the mother and the potential risk for the fetus.

Use in pediatrics

Features of the influence on the ability to drive a vehicle and potentially dangerous mechanisms

It is necessary to warn the patient that the drug may reduce concentration when driving vehicles or other potentially dangerous mechanisms.

Overdose

Symptoms: increased side effects.

Treatment: carry out symptomatic treatment. Metronidazole and its main metabolites are removed by hemodialysis (the half-life is reduced to 2.6 hours). During peritoneal dialysis, it is excreted in small quantities.

Release form, composition and pack

The solution for intravenous administration is transparent, colorless to pale yellow.

1 ml. metronidazole 5 mg.

1 amp. metronidazole 100 mg.

The solution for intravenous administration is transparent, colorless to pale yellow.

1 ml. metronidazole 5 mg.

1 fl. metronidazole 500 mg.

Excipients: sodium chloride, citric acid monohydrate, sodium hydrogen phosphate (anhydrous), water for injection.

Clinical and pharmacological group: Antiprotozoal product with antibacterial activity

pharmachologic effect

A drug with antiprotozoal and antibacterial action, the mechanism of which is the biochemical reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group interacts with the DNA of the microbial cell, inhibiting the synthesis of nucleic acids, which leads to the death of bacteria. Active against Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., also obligate anaerobes Bacteroides spp. (Bacteroides Ovatae, Bacteroides Thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (Prevotella Bivia, Prevotella BuccAe gram -positive microorganisms (Eubacter spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp. ).

In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).

Aerobic microorganisms and facultative anaerobes are insensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes), metronidazole exhibits synergism with antibiotics active against common aerobes. Metronidazole increases the susceptibility of tumors to radiation, causes disulfiram-like reactions, and stimulates reparative processes.

Pharmacokinetics

Distribution

After intravenous administration of Metrogyl at a dose of 500 mg for 20 minutes, the concentration of metronidazole in the blood serum was 35.2 μg/ml after 1 hour, 33.9 μg/ml after 4 hours, and 25.7 μg/ml after 8 hours. With normal bile formation, the concentration of metronidazole in bile after intravenous administration can significantly exceed the concentration in plasma.

Metabolism

Biotransformed within 30-60% of metronidazole by hydroxylation, oxidation and glucuronidation. The main metabolite (2-oxymetronidazole) has antiprotozoal and antimicrobial activity.

Removal

T1/2 is 8 hours (from 6 to 12 hours). 60-80% is excreted by the kidneys (within 20% unchanged), through the intestines - 6-15%. Renal clearance - 10.2 ml/min.

Pharmacokinetics in special clinical situations

With alcoholic liver damage, T1/2 is 18 hours (from 10 to 29 hours).

In newborns born during the gestation period from 28 to 30 weeks - 75 hours, from 32 to 35 weeks - 35 hours, from 36 to 40 weeks - 25 hours.

In patients with impaired renal function, accumulation of metronidazole may occur after repeated administration (therefore, in patients with severe renal failure, the frequency of use of the product should be reduced).

Metronidazole and its metabolites are excreted during hemodialysis (T1/2 - 2.6 hours). During peritoneal dialysis they are excreted in minor amounts.

Indications

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the product:

severe infections caused by mixed aerobic-anaerobic microflora (as part of combination therapy);

severe forms of intestinal and hepatic amebiasis;

• peritonitis;

  osteomyelitis;

  gynecological infections;

  pelvic abscesses;

  abscess pneumonia;

  brain abscesses;

  gas gangrene;

  infections of the skin and soft tissues, bones and joints.

Prevention and treatment of infections caused by aerobic microflora during surgical interventions (mainly on the abdominal organs, urinary tract).

Radiation therapy of tumors (as a radiosensitizing agent in cases where tumor resistance is due to hypoxia in tumor cells).

Dosage regimen

The drug is intended for intravenous infusion, which is indicated for severe infections, also when it is impossible to take metronidazole orally.

For adults and children over 12 years of age, the product is administered intravenously by drip at an initial dose of 0.5-1 g (infusion duration 30-40 minutes), and then after 8 hours, 500 mg at a rate of 5 ml/min.

If therapy is well tolerated, after the first 2-3 infusions they switch to jet administration. The course of treatment is 7 days. If necessary, intravenous administration is carried out for a longer time. The maximum daily dose is 4 g. According to indications, it is possible to switch to taking the substance orally in a maintenance dose of 400 mg 3 times a day.

Children under 12 years of age are prescribed according to the same regimen in a single dose of 7.5 mg/kg.

For purulent-septic diseases, 1 course of therapy is usually sufficient.

For prophylaxis in adults and children over 12 years of age, the product is prescribed intravenously in a dose of 0.5-1 g on the eve of surgery, every day of surgery and the next day - 1.5 g/day (500 mg every 8 hours). After 1-2 days, they switch to maintenance therapy (metronidazole taken orally).

For chronic renal failure (creatinine clearance less than 30 ml/min) and/or for liver failure, the highest daily dose is 1 g with a frequency of administration of 2 times a day.

When used as a radiosensitizing agent, the product is administered intravenously at a dose of 160 mg/kg body weight or 4-6 g/m2 of body surface 0.5-1 hour before the start of the irradiation session. The drug is used before each session for 1-2 weeks, and during the remaining period of radiation therapy, metronidazole is not used. The maximum single dose should not exceed 10 g, a course dose - 60 g. To reduce intoxication caused by radiation, infusions of a 5% dextrose (glucose) solution, hemodez or 0.9% sodium chloride solution are performed.

For cervical and uterine cancer, skin cancer, it is used in the form of local applications. In this case, 3 g is dissolved in a 10% solution of dimethyl sulfoxide, and tampons are moistened with the resulting solution, which are used topically 1.5-2 hours before irradiation. In case of poor tumor regression, applications are carried out throughout the entire course of therapy; with positive dynamics of tumor clearance from necrosis - during the first 2 weeks of therapy.

Side effect

From the digestive system: diarrhea, loss of appetite, nausea, vomiting, intestinal colic, constipation, metallic taste in the mouth, dry mouth, glossitis, stomatitis, pancreatitis.

From the central nervous system and peripheral nervous system: dizziness, impaired coordination of movements, ataxia, confusion, irritability, depression, high excitability, weakness, insomnia, headache, convulsions, hallucinations, peripheral neuropathy.

From the urinary system: dysuria, cystitis, polyuria, urinary incontinence, candidiasis, red-brown coloration of urine. Allergic reactions: urticaria, skin rash, skin hyperemia, nasal congestion, fever, arthralgia.

Local reactions: thrombophlebitis, pain, hyperemia, swelling.

Other: neutropenia, leukopenia, flattening of the T wave on the ECG.

Contraindications

organic lesions of the central nervous system (including epilepsy);

renal failure (when used in large doses);

diseases of the hematopoietic system;

I trimester of pregnancy;

lactation (breastfeeding);

high susceptibility to the product and other nitroimidazole derivatives.

Pregnancy and lactation

The drug is contraindicated for use in the first trimester of pregnancy. Use in the second and third trimesters is possible only for health reasons. If it is necessary to prescribe during lactation, the issue of stopping breastfeeding must be resolved.

special instructions

When used in combination with amoxicillin, Metrogyl should not be prescribed to patients under 18 years of age.

When carrying out long-term therapy, the peripheral blood picture should be monitored.

If leukopenia occurs, the question of continued use of the product is decided individually, depending on the course of the infectious process.

If ataxia, dizziness or other neurological symptoms occur, use of the product should be discontinued.

While using Metrogyl, you should not drink alcohol, because Disulfiram-like reactions may occur (spasmodic abdominal pain, nausea, vomiting, headache, hot flashes).

Against the background of using the product, it is possible to obtain a false-positive Nelson test (due to immobilization of treponemes).

Overdose

Symptoms: nausea, vomiting, anorexia.

Treatment: carry out symptomatic therapy. There is no specific antidote. Metronidazole and its metabolites are readily excreted by hemodialysis.

Drug interactions

The drug can enhance the effect of oral anticoagulants, and the prothrombin time increases.

Concomitant use of ethanol causes disulfiram-like reactions.

The combined use of Metrogyl with disulfiram can lead to the development of neurological reactions (the interval between administration should be at least 2 weeks).

Cimetidine inhibits the metabolism of metronidazole, which may lead to increased serum concentrations and an increased risk of side effects.

Hepatic enzyme inducers (phenytoin, phenobarbital) can accelerate the elimination of metronidazole, which will lead to a decrease in its plasma concentration.

When Metrogyl is used simultaneously with lithium products, the level of lithium in the blood may increase, which increases the likelihood of toxic effects.

When used together, sulfonamides enhance the antimicrobial effect of metronidazole.

Pharmaceutical interactions

Metrogyl solution should not be mixed with other medicinal products.

Storage conditions and periods

The drug should be stored in a place protected from light and inaccessible to children at a temperature not exceeding 30°C; do not freeze.

Shelf life - 3 years.

Attention!
Before using the medication "Metrogyl for intravenous administration" You should consult your doctor.
The instructions are provided for informational purposes only. Metrogyl for intravenous administration».

Part Metrogyl solution active ingredient included metronidazole and also: sodium chloride, sodium hydrogen phosphate (anhydrous), citric acid, water.

Metrogyl tablets contain active ingredient metronidazole , as well as: corn starch, magnesium stearate, colloidal silicon dioxide, hydrogenated castor oil, Opadry II dye, water.

Gel Metrogyl includes metronidazole and additional components: propyl parahydroxybenzoate, methyl parahydroxybenzoate, disodium edetate, carbomer 940, sodium hydroxide, propylene glycol, water.

Release form

Currently, Metrogyl solution is produced for intravenous administration, as well as tablets, vaginal gel and gel for external use.

• Solution for intravenous administration can be colorless or pale yellow, transparent, packaged in transparent ampoules of 20 ml (100 mg solution) and in polyethylene bottles of 100 ml (500 mg solution). The containers are placed in cardboard packs.
• Tablets 200 mg– pink, biconvex, film-coated, round, packaged in blisters of 10 pcs., in cardboard packs of 2 blisters.
• Ttablets 400 mg– orange, biconvex, film-coated, round, packaged in blisters of 10 pcs., in cardboard packs of 2 blisters.
• Vaginal gel Metrogyl homogeneous, colorless or has a yellow tint, contained in tubes of 30 g.

pharmachologic effect

The broad-spectrum medicine contains metronidazole , a 5-nitroimidazole derivative.

The drug has antimicrobial and antiprotozoal effects. The mechanism of action is based on the reduction of the 5-nitro group of metronidazole by intracellular transport proteins of anaerobic microorganisms and protozoa. The 5-nitro group of metronidazole interacts with the DNA of microbial cells, inhibiting the synthesis of their nucleic acids. As a result, the bacteria die.

Metrogyl demonstrates activity towards Gardnerella vaginalis, Trichomonas vaginalis, Giardiai intestinalis, Entamoeba histolytica, Lamblia spp.. The drug is also active against obligate anaerobes and a number of gram-positive microorganisms.

If metronidazole is combined with, activity against Helicobacter pylori.

Facultative anaerobes and aerobic microorganisms do not show sensitivity to metronidazole, however, in the presence of mixed flora, a synergistic effect of metronidazole with antibiotics , which are effective against aerobes.

It provokes disulfiram-like reactions, under its influence the sensitivity of tumors to radiation increases, and reparative processes are stimulated.

When applied externally, an anti-acne effect is observed, the mechanism of which is not fully known. Metrogyl ointment appears to demonstrate antioxidant activity. Under the influence of this drug, the production of active oxygen, hydrogen peroxide, and hydroxyl radicals by neutrophils is reduced, that is, potential oxidants that contribute to tissue damage in the place where the inflammatory process develops.

The external form of the drug is active against telangiectasias with .

Pharmacokinetics and pharmacodynamics

After a patient has been administered Metrogyl intravenously, approximately 30-60% of the substance is metabolized through hydroxylation, oxidation and glucuronidation. As a result, a metabolite, 2-oxymetronidazole, is formed, which also produces an antiprotozoal and antimicrobial effect. The half-life is 8 hours (subject to normal liver function), up to 18 hours (if the liver is damaged by alcohol).

Approximately 60-80% of the administered dose is excreted through the kidneys, another 6-15% is excreted through the intestines. Both metronidazole and its metabolites are eliminated from the blood by.

If the antibiotic is taken orally, it is quickly absorbed, and its maximum concentration in the blood is observed after 2 hours. The product has a high ability to penetrate tissues and body fluids. 10-20% bound to plasma proteins. About 60-80% is excreted through the kidneys, while approximately 20% is excreted unchanged. Half-life is 8 hours.

When the product is used externally, a minimal amount is absorbed, so only traces of the active component are detected in the blood. It should be taken into account that the absorbed active substance passes the blood-brain and placental barriers.

Indications for use

The instructions define the following indications for the use of Metrogyl intravenously:

• protozoal infections: (, extraintestinal and intestinal amoebiasis , balantidiasis , giardiasis , , vaginitis And Trichomonas);
• infectious diseases caused by Bacteroides spp.: infections of the abdominal cavity, pelvic organs, skin, soft tissues;
• infections caused by Bacteroides spp.: infections of the nervous system, joints, bones, including brain abscess , empyema , lung abscess , pneumonia ;
• infectious diseases caused by Bacteroides spp., including Clostridium spp., V. fragilis: sepsis ;
• pseudomembranous colitis as a result of treatment with antibiotics;
• or ulcer , as a consequence of the action Helicobacter pylori;
• prevention of complications after surgery.

It is advisable to prescribe tablets in the following cases:

• to prevent the development of postoperative complications (in particular gynecological);
• for protozoal infections ( giardiasis , trichomoniasis , amoebic dysentery , amoebiasis and etc.);
• anaerobic infections (those that were provoked Bac.fragilis, and clostridia , fusobacteria , anaerobic cocci , eubacteria );
• period after operations;
• infectious diseases of the respiratory tract;
• gas;
• septicemia ;
• meningitis , brain abscess ;

Metrogyl cream is prescribed for the following diseases and conditions:

• acne vulgar;
• , oily seborrhea;
• trophic ulcers which appear on the lower extremities as a consequence varicose veins , ;
• bedsores ;
• wounds that heal poorly;

Metrogyl vaginal gel is indicated for therapy vaginitis which are caused by metronidazole-sensitive microflora, as well as for the treatment of urogenital .

Contraindications

Metrogyl IV Contraindicated for use in the following conditions and diseases:

• organic lesions of the nervous system ( and etc.);
• blood diseases;
• liver failure (you cannot take large doses);
• blood diseases;
• lactation and pregnancy (first trimester);
• severe sensitivity to metronidazole, derivatives nitroimidazole .

Intravenous injections are given with caution to people suffering from renal failure.

Metrogyl tablets should not be taken in the following cases:

• with organic lesions of the nervous system, in particular epilepsy ;
• for blood diseases;
• at liver failure (large doses of tablets);
• under the age of 12;
• during pregnancy (first trimester);
• high sensitivity to the active substance, to other derivatives nitroimidazole .

Prescribed with caution to people with liver and kidney diseases.

Vaginal gel not prescribed for the following diseases and conditions:

• impaired coordination of movements;
• leukopenia (also in the anamnesis);
• damage to the nervous system of an organic nature, including epilepsy ;
• pregnancy (first trimester);
• liver failure ;
• high sensitivity, also sensitivity to nitroimidazole derivatives.

Side effects

When using the drug intravenously and orally, the following side effects may develop:

• Gastrointestinal tract: loss of appetite, nausea , intestinal colic, vomit , , dryness or metallic taste in the mouth;
• nervous system: impaired coordination, impaired consciousness, ataxia , severe excitability, irritability, weakness, headache , convulsions ;
• allergy: rash, hyperemia , nasal congestion, arthralgia ;
• urinary system : , dysuria , urinary incontinence , polyuria , change in urine color to red-brown;
• local manifestations: , development of pain, swelling, redness at the injection site;
• other manifestations: leukopenia , neutropenia .

When using Metrogyl gel for topical use, a small amount of the active component is absorbed into the blood, so systemic side effects are unlikely. Rarely, the development of allergic manifestations, lacrimation, dryness and burning of the skin is possible.

Instructions for use of Metrogyl (Method and dosage)

Metrogyl solution, instructions for use

A Metrogil dropper is indicated in cases of severe infectious diseases, as well as in cases where the patient is unable to take the medicine orally.

Adolescents over 12 years of age and children receive the drug intravenously (duration of administration is about 40 minutes), the initial dose is 0.5-1 g. Then 500 mg should be administered every 8 hours (rate 5 ml/min.). If a person tolerates the injection normally, then after 2-3 infusions the drug can be administered in a stream. The injections must be taken for 7 days.

If necessary, a longer administration of the medicine is practiced. The permissible dose per day is 4 g. If indicated, maintenance doses can be used - 400 mg three times a day.

A similar regimen of use is practiced for children under 12 years of age, a single dose is 7.5 mg/kg.

For treatment purulent-septic diseases One course of therapy is sufficient.

For prevention, adolescents over 12 years of age and adults are given 0.5-1 g of medication intravenously before surgery, and 1.5 g per day on the day after surgery, that is, 500 mg every 8 hours. After 1-2 days, the patient can be transferred to maintenance oral medication.

At liver and kidney dysfunctions You should not take more than 1 g of medication per day; the dose should be divided into 2 doses.

Metrogyl tablets, instructions for use

You can take the tablets both during and after meals; they do not need to be chewed.

The dose for adults and adolescents over 15 years of age is 200-400 mg two to three times a day. per day

Both the dosage and duration of the course depend on the infection.

At trichomoniasis you need to drink 200 mg 3 times for 7 days, while women take additional vaginal products with metronidazole. You can increase the dose or repeat the course of therapy if necessary.

At amoebiasis adults receive 400 mg 3 times. per day, children - 30-40 mg per 1 kg/day, the dose is divided into three doses. You need to take Metrogyl for up to 10 days.

At amoebic liver abscess adults receive 400 mg or 800 mg three times a day, the drug is combined with tetracyclines. Children - 30-35 mg per 1 kg/day, the dose is divided into three doses. Therapy lasts up to 10 days.

At anaerobic bacterial infections adults receive 200-400 mg 2-3 times. per day, children should receive 7 mg per 1 kg of weight every 8 hours. Therapy lasts up to 10 days.

For the purpose of prevention before operations, you need to take 1000 mg once, then 200 mg three times a day.

If Metrogyl is combined with amoxicillin, the dose of metronidazole per day should be 1.5 g, divided into three doses.

Vaginal gel Metrogyl, instructions for use

The ointment is applied intravaginally, once in a dose of 2 g or 500 mg twice a day, 10 days. During this time, sexual activity is not allowed.

Gel Metrogyl from used as prescribed by a doctor.

The gel is applied externally to cleansed skin twice a day, treatment lasts from 3 to 9 weeks, it is possible to use the product for a longer time - up to 4 months. An occlusive dressing can be applied if necessary.

Metrogyl for acne

Often those who use Metrogyl gel on their face give positive reviews for acne. Despite the fact that the official instructions do not provide detailed information about the use of this medicine for the face, Metrogyl gel for acne is still used very often, since metronidazole has a bactericidal and bacteriostatic effect. Accordingly, it helps to get rid of dermatological problems. If the patient has single pimples, it is enough to apply the ointment several times.

In the case of acne, treatment may take longer. However, after the first use, the severity of negative symptoms decreases. Metrogyl is used as the main remedy for the treatment of acne, and in combination with other drugs. Apply the gel twice a day to areas affected by acne.

Metrogyl and Differin

The product, which is a synthetic retinoid, contains the active component adapalene. This drug has a beneficial effect on the skin; when used with Metrogyl, users note a more pronounced effect.

Overdose

When taking large doses of tablets, it is possible to develop nausea , vomiting , ataxia , in severe poisoning develops peripheral neuropathy , possible epileptic seizures . There are no specific antidotes; symptomatic treatment is carried out.

No cases of overdose have been recorded when using Metrogyl gel.

Interaction

The dropper with Metrogyl should not contain other medications - it is not recommended to mix the product with other drugs.

Metronidazole activates the effect of indirect anticoagulants, as a result, the formation time increases prothrombin .

Causes intolerance ethanol . When used concomitantly, a variety of neurological symptoms may develop. It is important to keep the interval between taking these medications at least 2 weeks.

When taken, the metabolism of metronidazole is suppressed, so the concentration of the latter may increase, which leads to the development of side effects.

When used simultaneously , , that is, drugs that stimulate microsomal oxidation enzymes in the liver, it is possible to accelerate the elimination of metronidazole. As a result, its plasma concentration decreases.

If metronidazole is taken simultaneously with lithium preparations, the concentration of the latter in plasma may increase. In this case, signs of intoxication of the body may appear.

Metrogyl should not be combined with non-depolarizing drugs. muscle relaxants .

The antimicrobial effect of metronidazole is enhanced sulfonamides .

When the gel is applied topically, there is no significant interaction with other drugs, but it should be used with caution with other indirect anticoagulants, since an increase in prothrombin time is possible.

Terms of sale

On prescription.

Storage conditions

Belongs to list B. Metrogil storage temperature is no more than 30°C. Keep away from light and away from children.

Best before date

The solution and tablets can be stored for 3 years, Metrogyl gel for 2 years.

special instructions

Long-term therapy requires constant monitoring of the blood picture.

If the patient develops leukopenia , continuation of therapy depends on whether there is a risk of an infectious process.

Therapy should be discontinued if the patient develops dizziness , ataxia and other symptoms indicating a deterioration in neurological status.

Under the influence of the drug, immobilization of treponema may occur, which leads to a false-positive Nelson test.

During treatment, the urine turns dark.

During the treatment period trichomonas vaginitis And urethritis you need to abstain from sexual intercourse. It is important that both sexual partners undergo therapy at the same time. During menstruation, treatment is not stopped.

Do not allow the gel to get into your eyes. If this happens, you need to rinse your eyes with warm water.

The Metrogyl dropper in gynecology is used only as prescribed by the attending physician.

In cosmetology, Metrogyl gel for the face is used to treat acne and other skin lesions. You can use it on your face only on the recommendation of a specialist.

Analogues

Level 4 ATX code matches:

Currently, numerous analogues of Metrogyl gel, tablets and solution are produced. These are drugs Deflamon , Klion , Metrovagin , Metrolacare , Metron , Orvagil , Trichobrol , , Cyptrogyl , etc. Suppositories with the active substance are also sold metronidazole .

For children

The use of the solution, if necessary, is carried out in accordance with the instructions. Tablets are not prescribed to children under 12 years of age.

With alcohol

Drinking alcohol is contraindicated during treatment with all forms of Metrogyl, as disulfiram-like reactions may occur.

Metrogyl during pregnancy and lactation

The use of this drug during pregnancy is contraindicated; it can be used in later stages only for health reasons. Lactation during treatment with Metrogyl should be stopped.

APPROVED

By order of the chairman

Committee for Control of Medical and
pharmaceutical activities

Ministry of Health

Republic of Kazakhstan

From "____"__________20___

№ ______________

Instructions for medical use

Medicine

Metrogil

Tradename

Metrogil

International nonproprietary name

Metronidazole

Dosage form

Solution for intravenous administration 5 mg/ml

Compound

1 ml of solution contains

active substance- metronidazole……5 mg

Excipients: sodium chloride, citric acid monohydrate, disodium hydrogen phosphate anhydrous, water for injection.

Description

Transparent solution from colorless to pale yellow

Pharmacotherapeutic group

Antibacterial drugs for systemic use. Imidazole derivatives

PBX code J01XD01

pharmachologic effect

Pharmacokinetics

With intravenous administration of 500 mg of metronidazole over 20 minutes, the concentration of the drug in the blood serum was 35.2 μg/ml after an hour, 33.9 μg/ml after 4 hours, and 25.7 μg/ml after 8 hours. With normal bile formation, the concentration of metronidazole in bile after intravenous administration can significantly exceed the concentration in the blood plasma. About 30-60% of metronidazole is metabolized in the body by hydroxylation, oxidation and glucuronidation. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effects. T1/2 with normal liver function - 8 hours (from 6 to 12 hours), with alcoholic liver damage - 18 hours (from 10 to 29 hours), in newborns: those born during pregnancy - 28-30 weeks - approximately 75 hours, 32-35 weeks - 35 hours, 36-40 weeks - 25 hours. 60 - 80% is excreted by the kidneys (20% unchanged), through the intestines - 6 - 15%. Renal clearance - 10.2 ml/min. In patients with impaired renal function, accumulation of metronidazole in the blood serum may occur after repeated administration (therefore, the frequency of dosing should be reduced in patients with severe renal impairment). Metronidazole and its main metabolites are quickly removed from the blood during hemodialysis (T1/2 is reduced to 2.6 hours). During peritoneal dialysis, it is excreted in small quantities.

Pharmacodynamics

Metrogyl is an antiprotozoal and antimicrobial 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 microorganisms and protozoa. The reduced 5-nitro group of metronidazole interacts with the DNA of microbial cells, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active against Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some gram-positive microorganisms (Eubacter spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.).

In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin suppresses the development of resistance to metronidazole).

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 common aerobes.

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

Prevention and treatment of anaerobic infections during surgical interventions, mainly on the abdominal organs and urinary tract

Combination therapy for severe mixed aerobic-anaerobic infections

Severe form of intestinal and hepatic amebiasis

Peritonitis

Osteomyelitis

Gynecological infections

Pelvic abscesses

Brain abscesses

Abscess pneumonia

Gas gangrene

Infections of the skin and soft tissues, bones and joints

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

Directions for use and doses

Intravenous administration of the drug is indicated for severe infections, as well as in the absence of the possibility of taking the drug orally.

Adults and children over 12 years old in an initial dose of 0.5 - 1 g intravenously (duration of infusions - 30 - 40 minutes), and then every 8 hours, 500 mg at a rate of 5 ml/min. If well tolerated, after the first 2 - 3 infusions, switch to jet administration. The course of treatment is 7 days. If necessary, intravenous administration is continued for a longer time. The maximum daily dose is 4 g. According to indications, switch to maintenance oral administration at a dose of 400 mg 3 times a day.

Children under 12 years of age prescribed according to the same scheme in a single dose - 7.5 mg/kg.

For preventive purposes, adults and children over 12 years of age are prescribed intravenous drips of 0.5 - 1 g on the eve of surgery, on the day of surgery and the next day - 1.5 g / day (500 mg every 8 hours). After 1 - 2 days, they switch to maintenance therapy orally. For patients with chronic renal failure and creatinine clearance less than 30 ml/min and/or liver failure, the maximum daily dose is no more than 1 g, the frequency of administration is 2 times a day.

As a radiosensitizing drug, it is administered intravenously at a rate of 160 mg/kg or 4-6 g/sq.m of body surface 0.5 - 1 hour before the start of irradiation. Apply before each irradiation session for 1-2 weeks. During the remaining period of radiation treatment, metronidazole is not used. The maximum single dose should not exceed 10 g, course dose - 60 g. To relieve intoxication caused by radiation, drip administration of a 5% dextrose solution, hemodez or 0.9% sodium chloride solution is used.

For cervical and uterine cancer, skin cancer, they are used in the form of local applications (3 g dissolved in a 10% solution of dimethyl sulfoxide), moisten tampons, which are used topically, 1.5 - 2 hours before irradiation). In case of poor tumor regression, applications are carried out throughout the entire course of radiation therapy. If the dynamics of tumor cleansing from necrosis is positive - during the first 2 weeks of treatment.

Side effects

Nausea, dry mouth, loss of appetite, abdominal pain, metallic taste in the mouth

Diarrhea, vomiting, constipation, glossitis, stomatitis

Dizziness, impaired coordination of movements, ataxia, irritability, depression, increased excitability, weakness, insomnia, headache, peripheral neuropathies (with long-term use in large doses)

Urticaria, skin rash, skin flushing, nasal congestion, fever, arthralgia

Dysuria, cystitis, polyuria, urinary incontinence, candidiasis, red-brown urine color

Thrombophlebitis (pain, redness or swelling at the injection site)

Neutropenia, leukopenia

Flattening of the T wave on the ECG

Very rarely:

Seizures, confusion, hallucinations

Rarely:

Pancreatitis

Contraindications

Hypersensitivity to metronidazole or other nitroimidazole derivatives

Organic lesions of the central nervous system, including epilepsy

Liver failure (in case of high doses)

Blood diseases, including a history of leukopenia

Pregnancy (first trimester) and lactation period

Drug interactions

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

Similar to disulfiram, it causes intolerance to ethyl alcohol.

Concomitant use with disulfiram can lead to the development of various neurological symptoms (the interval between prescriptions is at least 2 weeks).

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

The simultaneous administration of drugs that stimulate microsomal oxidation enzymes in the liver (phenobarbital, phenytoin) can accelerate the elimination of Metrogyl, resulting in a decrease in its concentration in the blood plasma.