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

The drug exhibits high activity with respect to Trichomonas vaginalis, Giardia intestinalis (Lamblia intestinalis), Entamoeba histolytica, as well as in respect of obligate anaerobes (sporo- and non-spore-forming) Bacteroides spp. (B.fragilis. B.ovatus, B.distasonis, B.thetaiotaomicron, B.vulgatus), Fusobacterium spp., Clostridium spp., Peptostreptococcus spp., Peptococcus spp., sensitive strains Eubacterium.

Metronidazole is not sensitive to aerobic microorganisms and facultative anaerobes, but in the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional anaerobes.

Pharmacodynamics

The mechanism of action of metronidazole 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.

Pharmacokinetics:

ATSucks: when intravenously administered 500 mg of metronidazole for 20 minutes to patients with an anaerobic infection, the concentration of the drug in the blood serum was 35.2 μg / ml an hour later,after 4 hours, 33.9 μg / ml, after 8 hours - 25.7 μg / ml.

Distribution: the drug 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. Binding to blood proteins is weak and does not exceed 10-20%. With normal bile formation, the concentration of metronidazole in the bile after intravenous administration may significantly exceed the concentration of metronidazole in the blood plasma.

Metabolism and excretion: 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 with a gestation period of 28-30 weeks - about 75 hours, 32-35 weeks - 35 hours, 36-40 weeks - 25 hours. Metronidazole is excreted by the kidneys - 63% of the dose (20% of the drug is unchanged). The renal clearance is 10.2 ml / min.

In patients with impaired renal function after repeated administration of the drug cumulation of metronidazole in the serum can be observed (therefore, the frequency of metronidazole administration should be reduced in patients with severe renal insufficiency). Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T_1/2 is reduced to 2.6 hours). When peritoneal dialysis is withdrawn in small quantities.

Indications:

Metronidazole is recommended for the treatment of infections caused by microorganisms that are sensitive to the drug:

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

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

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

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

Contraindications:

Hypersensitivity to the components of the drug, leukopenia (including in history), liver failure (in the case of high doses), organic lesions of the central nervous system (including epilepsy), blood diseases, I trimester of pregnancy, lactation.

Carefully:

Pregnancy (II-III trimesters), renal / hepatic insufficiency.

Pregnancy and lactation:

The drug should be given to pregnant women in the II and III trimesters only if the expected benefit for the mother exceeds the potential risk to the fetus.

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

Dosing and Administration:

Intravenously sprayed or drip. 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, the transition to maintenance therapy with oral forms of metronidazole is carried out.

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 on the eve of surgery on pelvic organs and urinary tract adults and children over 12 years metronidazole Assign in the form of infusions in 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 usually go to maintenance therapy with oral forms of metronidazole.

For patients with severe renal dysfunction (CC (creatinine clearance) less than 30 ml / min) and / or liver the maximum daily dose of metronidazole is not more than 1000 mg (multiplicity of intake 2 times).

Metronidazole for intravenous administration is not recommended to be mixed with other medications!

Side effects:

Very Frequent -> 10%; Frequent -> 1% and <10%; not frequent -> 0,1% and <1%; rare -> 0.01% and <0.1%; very rare - <0.01%.

From the digestive system: very rarely - nausea, vomiting, diarrhea, lack of appetite, unpleasant "metallic" taste in the mouth, epigastric pain, intestinal colic, constipation, dryness of the oral mucosa, glossitis, stomatitis, pancreatitis;

From the nervous system: with prolonged use very rarely - headache, dizziness, increased excitability, depression, sleep disturbance, weakness, confusion, hallucinations, convulsions, impaired coordination of movements, ataxia, irritability, peripheral neuropathy.

From the urinary system: very rarely - a burning sensation in the urethra, excessive development of fungal flora of the vagina (candidiasis), during the administration of metronidazole, reddish brown staining of urine, dysuria, cystitis, polyuria, incontinence can be observed.

Allergic reactions: very rarely - skin rash, itching, hives, skin hyperemia, nasal congestion, fever;

From the side of the musculoskeletal system: very rarely - arthralgia;

On the part of the organs of hematopoiesis: very rarely - leukopenia.

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

Other: very rarely - neutropenia, flattening of the T wave on the ECG.

Overdose:

Symptoms: nausea, vomiting, ataxia.

Treatment: symptomatic and supportive therapy. There is no specific antidote.

Interaction:

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

When using metronidazole, interaction with other drugs is negligible, but caution should be exercised when concomitant administration with certain medications.

Warfarin and other indirect anticoagulants. Metronidazole increases the effect of indirect anticoagulants, which leads to an increase in the time of prothrombin formation.

Disulfiram (Esperal). Simultaneous application can lead to the development of various neurological symptoms, so one should not prescribe metronidazole patients who took disulfiram in the last two weeks. Similarly, disulfiram causes intolerance to ethanol.

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.

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

With the simultaneous administration of metronidazole with drugs lithium may increase the concentration of the latter in blood plasma and the development of symptoms of intoxication.

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

The antimicrobial effect of metronidazole is enhanced in combination with sulfonamides.

Special instructions:

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

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.

When treating trichomonadal vaginitis in women and trichomoniasis in men, it is necessary to abstain from sexual activity. It is necessary to simultaneously treat sexual partners. After therapy with trichomoniasis, control tests should be performed for 3 consecutive cycles before and after menstruation.

Long-term use of the drug is desirable to be carried out under the control of peripheral blood.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Form release / dosage:

Solution for infusion, 5 mg / ml.

Packaging:

For 100 ml of the drug in a bottle of polyethylene. For 1 bottle with the drug, along with instructions for use in a cardboard bundle.

For hospitals: For 100 ml of the drug in a bottle of polyethylene. For 50 bottles in a box of cardboard with an equal number of instructions for use.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 30 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014437 / 01

Date of registration:29.10.2009 / 20.08.2013

Expiration Date:Unlimited

The owner of the registration certificate:Alkem Laboratories LtdAlkem Laboratories Ltd India

Manufacturer: & nbsp

ALKEM LABORATORIES, Ltd. India

Representation: & nbspPharmaReg Ltd.PharmaReg Ltd.Russia

Information update date: & nbsp11.05.2018

Illustrated instructions

Instructions

Metron (Metron)