Metronidazole solution for infusion 5mg/ml vials, 100ml

Composition

of 1 fl. metronidazole 5 mg

Auxiliary substances:

sodium chloride 900 mg,

sodium dihydrogen phosphate dihydrate (sodium phosphoric acid monosubstituted 2-water) 300 mg,

d/i water (up to 100 ml).

Pharmacological action

An antiprotozoal and antimicrobial drug derived from 5-nitroimidazole. The mechanism of action consists in the biochemical reduction of the 5-nitro group of 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 their nucleic acids, which leads to the death of bacteria.

Active against Trichomonas vaginalis, Entamoeba histolytica, and obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., some Gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus niger, Peptostreptococcus spp. ).

The minimum inhibitory concentration for these strains is 0.125-6.25 micrograms / ml.

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 works synergistically with antibiotics that are effective against conventional aerobes.

Increases the sensitivity of tumors to radiation, causes sensitization to alcohol (disulfiram-like effect).

Indications

• protozoal infection (extraintestinal amoebiasis /including abscess of the liver/ intestinal amoebiasis, trichomoniasis, balantidiasis, giardiasis (Giardia), cutaneous leishmaniasis, Trichomonas vaginitis, Trichomonas urethritis);
• infections caused by Bacteroides spp., including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus (infection of bones and joints, Central nervous system infections including meningitis, abscess of the brain, bacterial endocarditis, pneumonia, empyema and lung abscess);
• infections caused by Bacteroides spp. (including Bacteroides fragilis), Clostridium spp., Peptococcus spp., Peptostreptococcus spp. (abdominal infections /peritonitis, liver abscess/, pelvic infections /endometritis, endomyometritis, fallopian tube and ovarian abscess, vaginal vault infections after surgery/, skin and soft tissue infections);
• sepsis caused by Bacteroides spp. (including Bacteroides fragilis), and Clostridium spp. ;
• pseudomembranous colitis (associated with the use of antibiotics);
• gastritis or peptic ulcer disease of the duodenum associated with Helicobacter pylori;
• alcoholism;
• as a radiosensitizing tools in radiation therapy (in cases where the resistance of tumors due to hypoxia in tumor cells);
• prevention of postoperative infections (especially after operations on the colon, colorectales region, appendectomy, gynecological interventions).

Contraindications

• leukopenia (including in the anamnesis);
• impaired coordination of movements,
• organic damage to the central nervous system (including epilepsy);
• liver failure (if prescribed in high doses);
• I trimester of pregnancy;
• lactation period;
• hypersensitivity to the components of the drug;
• hypersensitivity to nitroimidazole derivatives.

Use with caution in the second and third trimesters of pregnancy.

Side effects

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

From the hematopoietic system:  reversible neutropenia (leukopenia).

From the central nervous system:  peripheral neuropathy (feeling of numbness of the extremities), headaches, convulsions, drowsiness, dizziness, impaired coordination of movements, ataxia, confusion, depression, increased excitability, weakness, insomnia, hallucinations, irritability.

Allergic reactions:  skin rash, urticaria, pruritus, erythema multiforme, angioedema and anaphylactic reaction, skin hyperemia, nasal congestion, fever, arthralgia.

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

From the side of the hepatobiliary system:  increased activity of liver enzymes, cholestasis jaundice.

From the genitourinary system:  dysuria, cystitis, polyuria. urinary incontinence, candidiasis of the vaginal mucosa, red-brown staining of urine (causes a metronidazole metabolite, has no clinical significance).

Other services:  increased body temperature, flattening of the T wave on the ECG.

Interaction

When used concomitantly with antacids containing aluminum hydroxide, colestyramine slightly reduces the absorption of metronidazole from the gastrointestinal tract.

When used concomitantly, metronidazole potentiates the effect of indirect anticoagulants.

When used concomitantly with disulfiram, acute psychosis and impaired consciousness may develop.

It is impossible to exclude an increase in the concentration of carbamazepine in blood plasma and an increased risk of toxic effects when used simultaneously with metronidazole.

When used concomitantly with lansoprazole, glossitis, stomatitis and/or the appearance of dark coloration of the tongue are possible; with lithium carbonate, an increase in the concentration of lithium in blood plasma and the development of symptoms of intoxication is possible; with prednisone, the excretion of metronidazole from the body increases due to the acceleration of its metabolism in the liver under the influence of prednisone. It is possible to reduce the effectiveness of metronidazole.

When used concomitantly with rifampicin, the clearance of metronidazole from the body increases; with phenytoin, a slight increase in the concentration of phenytoin in blood plasma is possible, and a case of toxic action is described.

When used concomitantly with phenobarbital, the elimination of metronidazole from the body significantly increases, apparently due to the acceleration of its metabolism in the liver under the influence of phenobarbital. It is possible to reduce the effectiveness of metronidazole.

When used concomitantly with fluorouracil, the toxic effect increases, but not the effectiveness of fluorouracil.

A case of acute dystonia after taking a single dose of chloroquine in a patient receiving metronidazole is described.

When used concomitantly with cimetidine, it is possible to inhibit the metabolism of metronidazole in the liver, which may lead to a slowdown in its excretion and an increase in its concentration in blood plasma.

With the simultaneous use of ethanol in patients receiving metronidazole, disulfiram-like reactions may develop.

How to take, course of use and dosage

Intravenous

Intravenous use is indicated for severe infections, as well as in the absence of the possibility of oral use of the drug.

For adults and children over 12 years of age, the single dose is 500 mg, the rate of continuous (jet) or drip use is 5 ml/min. The interval between injections is 8 hours. The duration of the course of treatment is determined individually. The maximum daily dose is no more than 4 g. According to indications, depending on the nature of the infection, switch to maintenance therapy with oral forms of metronidazole.

Children under 12 years of age are administered 7.5 mg / kg of body weight in 3 doses at a rate of 5 ml / min.

To prevent anaerobic infection before elective surgery on the pelvic organs and urinary tract, adults and children over 12 years of age are prescribed the drug in the form of infusions at a dose of 500-1000 mg on the day of surgery, and the next day — at a dose of 1500 mg / day (500 mg every 8 hours). After 1-2 days, they usually switch to maintenance therapy with oral forms of metronidazole.

For patients with severe renal impairment (creatinine clearance less than 30 ml / min) and / or liver, the daily dose is 1000 mg (multiplicity of use-2 times).

Overdose

Symptoms:  nausea, vomiting, ataxia; when taken as a radiosensitizing agent – convulsions, peripheral neuropathy.

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

Special instructions

During the treatment period, taking ethanol is contraindicated (a disulfiram-like reaction may develop: spastic abdominal pain, 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 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 discontinuation of treatment.

May immobilize treponemes and result in a false positive Nelson test.

Stains urine in a dark color.

When treating trichomonas vaginitis in women and trichomonas urethritis in men, it is necessary to refrain from sexual activity. Simultaneous treatment of sexual partners is mandatory. Treatment does not stop during menstruation. After trichomoniasis therapy, follow-up tests should be performed for three consecutive cycles before and after menstruation.

After treatment of giardiasis, if symptoms persist, perform 3 stool tests in 3-4 weeks at intervals of several days (in some successfully treated patients, lactose intolerance caused by invasion may persist for several weeks or months, resembling the symptoms of giardiasis).

During the treatment period, it is recommended to stop breastfeeding.

Form of production

The solution for infusions is clear, slightly yellow in color with a greenish tinge.

Storage conditions

Store in a dark place at room temperature; do not freeze. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Metronidazole

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Stomach and Duodenal ulcers, Amoebiasis and Giardiasis, Alcoholism, Pneumonia, Trichomoniasis, Urinary Tract Infections, Vaginitis, Inflammation of the female genital organs, Urethritis, Skin Infections, Gastrointestinal Infections caused by Helicobacter Pylori, Osteomyelitis