Metrogyl solution for intravenous administration 5mg / ml, 100ml

• Protozoal infections: extraintestinal amebiasis, including amoebic liver abscess, intestinal amebiasis (amoebic dysentery), trichomoniasis, giardiasis, balantidiasis, giardiasis, cutaneous leishmaniasis, trichomonas vaginitis, trichomonas urethritis;

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

• infections caused by species of Bacteroides spp., including group B. fragilis, Clostridium spp.,, Peptococcus spp., and Peptostreptococcus spp .: infections of the abdominal cavity (peritonitis, liver abscess), pelvic infections (endometritis, endomyometritis, abscess of the fallopian tubes and ovaries, vaginal vault infections after surgery), skin and soft tissue infections;

• infections caused by species of Bacteroides spp., including the group B. fragilis, Clostridium spp .;

• sepsis;

• pseudomembranous colitis (associated with the use of antibiotics);

• gastritis or duodenal ulcer associated with Helicobacter pylori; alcoholism;

• prevention of postoperative complications (especially interventions on the colon, near-rectal region, apendectomy, gynecological operations).

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 - in 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 tolerance, 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. The maximum daily dose is 4 g. According to indications, a transition is made to a maintenance intake at a dose of 400 mg 3 times / day.

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

With purulent-septic diseases, 1 course of treatment is usually carried out.

For prophylactic purposes, adults and children over 12 years of age are prescribed intravenous drip, 0.5-1 g on the eve of the operation, on the day of the operation and the next day - 1.5 g / day (500 mg every 8 hours). After 1-2 days, they switch to supportive therapy inside.

For 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 / day.

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

1 ml 1 fl.

metronidazole 5 mg 500 mg

Excipients: sodium chloride, citric acid (monohydrate), sodium hydrogen phosphate anhydrous, water d / i.

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

• hepatic impairment (in the case of large doses);

• blood diseases;

• pregnancy (I trimester);

• lactation period;

• hypersensitivity to metronidazole or other nitroimidazole derivatives.

• With caution: renal failure.

pharmachologic effect

Antiprotozoal and antimicrobial drug derived from 5-nitroimidazole. The mechanism of action consists in 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 the cell of microorganisms, 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 inhibits 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 conventional aerobes. Increases the sensitivity of tumors to radiation, causes disulfiram-like reactions, and stimulates reparative processes.

Pharmacokinetics

With intravenous administration of 500 mg of Metrogyl for 20 minutes, the concentration of the drug in the blood serum was 35.2 ?g / ml after an hour, 33.9 ?g / ml after 4 hours, and 25.7 ?g / ml after 8 hours. With normal bile formation, the concentration of metronidazole in bile after intravenous administration can significantly exceed the plasma concentration. In the body, about 30-60% of metronidazole is metabolized 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 at a gestational age of 28-30 weeks - about 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%. Renal clearance - 10.2 ml / min. In patients with impaired renal function, after repeated administration, accumulation of metronidazole in the blood serum may be observed (therefore, in patients with severe renal insufficiency, the frequency of administration should be reduced). Metronidazole and the main metabolites are rapidly removed from the blood during hemodialysis (T1 / 2 is reduced to 2.6 hours). With peritoneal dialysis, it is excreted in small quantities.

Side effect

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

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

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

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

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

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

Application during pregnancy and lactation

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

Nursing mothers - according to indications with the simultaneous termination of breastfeeding.

Application for violations of liver function

For patients with hepatic insufficiency, the maximum daily dose is no more than 1 g, the frequency of administration is 2 times / day.

Application for impaired renal function

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

Application in children

Children over 12 years old - in 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 tolerance, 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. The maximum daily dose is 4 g. According to indications, a transition is made to a maintenance intake at a dose of 400 mg 3 times / day.

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

With purulent-septic diseases, 1 course of treatment is usually carried out.

For prophylactic purposes, children over 12 years of age are prescribed intravenous drip, 0.5-1 g on the eve of the operation, on the day of the operation and the next day - 1.5 g / day (500 mg every 8 hours). After 1-2 days, they switch to supportive therapy inside.

special instructions

During the period of treatment, 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).

In combination with amoxicillin, it is not recommended for use in patients under 18 years of age.

With prolonged therapy, it is necessary to control 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 discontinuation of treatment.

May immobilize treponemas and lead to false positive Nelson's test.

Stains urine dark.

Drug interactions

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

Enhances the action of indirect anticoagulants, which leads to an increase in the time of prothrombin formation.

Similar to disulfiram, it causes intolerance to ethanol. 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 can 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 enzymes of microsomal oxidation 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 the plasma may increase and the development of symptoms of intoxication.

It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).

Sulfonamides enhance the antimicrobial effect of metronidazole.