Metrolakar - instructions for use, dose, side effects, contraindications

Active substance:
Metronidazole	0.500 grams
Excipients:
Sodium chloride	0.720 g
Lemon acid	0.023 g
Sodium dihydrogen phosphate (sodium phosphate monosubstituted)	0.060 g
Water for injections	up to 100 ml

Description:

Transparent solution from colorless to slightly yellow in color.

Pharmacotherapeutic group:Antimicrobial and antiprotozoal drug

ATX: & nbsp

P.01.A.B Nitroimidazole derivatives

P.01.A.B.01 Metronidazole

Pharmacodynamics:

Antiprotozoal and antibacterial 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 reacts with the DNA of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Active in a relationship Trichomonas vaginalis, Entamoeba histolytica, as well as Gram-negative anaerobes Bacteroides spp. (including W. fragilis, AT. distasonis, AT. ovatus, 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).

Metronidazole is insensitive to aerobic microorganisms and facultative anaerobes, 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 irradiation, causes disulfiram-like reactions.

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, abscess cavities, vaginal secretion, seminal fluid, breast milk, penetrates the blood-brain barrier and placental barrier.

The volume of distribution: adults - about 0.55 l / kg, newborns - 0.54-0.81 l / kg.

The maximum concentration of the drug in the blood (FROM_mOh) is from 6 to 40 μg / ml, depending on the dose. Time to reach the maximum concentration of the drug in the blood (TFROM_mOh) - 30-60 minutes, the therapeutic concentration is maintained for 6-8 hours. The connection with plasma proteins is 10-20%.

With intravenous administration of 500 mg for 20 minutes FROM_mOhin the blood serum after 1h - 35.2 μg / ml. The concentration of the drug in the blood after 4 hours was 33.9 μg / ml, after 8 hours 25.7 μg / ml; minimum concentration (C_min) with subsequent administration of 18 μg / ml.With normal bile formation, the concentration of metronidazole in the bile after IV injection can significantly exceed the concentration in the plasma.

B The body metabolizes about 30-60% of metronidazole by hydroxylation, oxidation and glucuronidation. The main metabolite (2-oxymetronidazole) also indicates antiprotozoal and antibacterial action.

Half-life of blood (T_1/2) with normal liver function - 8 hours (6 to 12 hours), with alcoholic liver damage - 18 hours (from 10 to 29 hours), in newborns: those born at the time of pregnancy - 28-30 weeks - about 75 hours, 32- 35 weeks - 35 hours, 36-40 weeks - 25 hours.

It is excreted by the kidneys 60-80% (20% unchanged), intestines - 6-15%. Kidney clearance - 10.2 ml / min.

In patients with impaired renal function after repeated administration, cumulation of metronidazole in serum can be observed (therefore, the frequency of admission should be reduced in patients with severe renal insufficiency).

Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T_1/2is reduced to 2.6 h). When peritoneal dialysis is withdrawn in small quantities.

Indications:

Protozoal infections: extraintestinal amebiasis, including amoebic liver abscess, intestinal amoebiasis (amoebic dysentery), trichomoniasis (including trichomonas vaginitis, trichomonas urethritis).

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

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

Pseudomembranous colitis (associated with the use of antibiotics).

Gastritis or duodenal ulcer associated with Helicobacter pylori.

Prevention of postoperative complications (especially interference on the colon, paraectal area, appendectomy, gynecological operations).

Radiation therapy of patients with tumors - as a radiosensitizer in cases where tumor resistance is caused by hypoxia of tumor cells.

Contraindications:

Hypersensitivity, leukopenia (including in the anamnesis), organic lesions of the central nervous system (including epilepsy), liver failure (in the case of high doses), pregnancy (I trimester), lactation.

Carefully:

- II and III trimesters of pregnancy - only for life reasons;

- renal / hepatic insufficiency.

Pregnancy and lactation:

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

For prophylactic purposes, adults and children over 12 years of age are prescribed intravenously / intravenously drip 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 inside.

Patients with CRF and KK less than 30 ml / min and / or liver failure the maximum daily dose - no more than 1 g, the frequency of reception - 2 times a day.

As a radiosensitizing drug is injected IV drip at the rate of 160 mg / kg or 4-6 g / m2 body surface for 0.5-1 h before the start of irradiation. Apply before each irradiation session for 1-2 weeks. In the remaining period of radiation treatment metronidazole do not apply. The maximum single dose should not exceed 10 grams, the course dose should be 60 g. To remove intoxication caused by irradiation, a 5% solution of dextrose, povidone or 0.9% sodium chloride solution is used.

With cancer of the cervix and uterus body, skin cancer is used in the form of local applications (3 g is dissolved in a 10% solution of dimethylsulfoxide), wet tampons that are applied topically,for 1.5-2 hours before irradiation). With a poor regression of the tumor, the appliqués are carried out throughout the course of radiotherapy. With a positive dynamics of purification of the tumor from necrosis - during the first 2 weeks of treatment.

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

For adults and children over 12 years a single dose of 500 mg, the rate of intravenous continuous (jet) or dropwise administration - 5 ml per minute. The interval between administrations is 8 hours. The duration of treatment is determined individually. The maximum daily dose is no more than 4 g. According to the indications, depending on the nature of the infection, a transition to maintenance therapy with oral forms of metronidazole is carried out. When purulent-septic diseases are usually conducted 1 course of treatment.

Children under the age of 12 years metronidazole 7.5 mg / kg of body weight is administered in 3 divided doses at a rate of 5 ml per minute.

For the prevention of anaerobic infection before the planned operation on the pelvic organs and urinary tract adults and children over 12 years metronidazole prescribe in the form of infusions in a dose of 500-1000 mg, on the day of the operation and the next day - at a dose of 1500 mg / day (500 mg every 8 hours).After 1-2 days usually go to maintenance therapy with oral forms of metronidazole.

For patients with severe renal dysfunction (creatinine clearance less than 30 ml / min) and / or liver The daily dose of metronidazole is 1000 mg (multiplicity of intake 2 times a day).

Metronidazole for intravenous fluids should not be mixed with other medications!

Side effects:

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, increased excitability, weakness, insomnia, headache, convulsions, hallucinations, peripheral neuropathy.

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

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

Local Reactions: thrombophlebitis (pain, flushing or swelling at the injection site).

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

Overdose:

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

Treatment: there is no specific antidote, symptomatic and supportive therapy is indicated. With the help of hemo- or peritoneal dialysis, only a small amount (less than 10%) of the drug can be excreted.

Interaction:

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

Similarly, disulfiram causes intolerance to ethanol.

The simultaneous use of metronidazole with disulfiram can lead to the development of various neurological symptoms (the interval between appointments is at least 2 weeks).

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

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

Simultaneous appointment with inductors of microsomal liver enzymes (for example, phenobarbital, phenytoin), can accelerate the elimination of metronidazole, as a result of which its concentration in the plasma decreases.

When taken concomitantly with Li preparations⁺ may increase the concentration of the latter in the plasma and develop symptoms of intoxication.

It is not recommended to combine with nondepolarizing muscle relaxants (for example, vecuronium bromide).

Special instructions:

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

In combination with amoxicillin it is not recommended to use in patients younger than 18 years.

With prolonged 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.

Can immobilize treponema and lead to Nelson's false positive test. Stains urine in a dark color.

During treatment of trichomonas 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.

Form release / dosage:Solution for infusion, 5 mg / ml.

Packaging:

For 100 ml of the drug in a polyethylene bottle made of high-quality polyethylene.

One bottle together with the instruction for use is placed in a pack of cardboard.

Storage conditions:

AT dry, protected from light, at a temperature of no higher than 25 ° C. Do not freeze

Shelf life:

5 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N013902 / 01

Date of registration:22.12.2009

Expiration Date:Unlimited

The owner of the registration certificate:La Car Pharma LimitedLa Car Pharma Limited India

Manufacturer: & nbsp

LA CARE FARMA, Ltd. India

Representation: & nbspJodas Expoim, Open CompanyJodas Expoim, Open Company

Information update date: & nbsp11.05.2018

Illustrated instructions

Instructions

Metrolacker (Metrolacare)