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

The drug exhibits high activity with respect to Trichomonas vaginalis, Giardia intestinalis, Entamoeba histolytica, Lamblia intestinalis, 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 aerobes.

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:

With the intravenous administration of 500 mg of metronidazole for 20 minutes to patients with anaerobic infection, the concentration of the drug in the blood serum was 35.2 μg / ml in an hour, 33.9 μg / ml in 4 hours, 25.7 μg / ml after 8 hours . 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.

Excretion Metronidazole carried out by the kidneys - 63% of the dose (20% of the drug is unchanged). The half-life of metronidazole is 6-7 hours. Kidney clearance is 10,2 ml / min.

In patients with impaired renal function After repeated administration of the drug, accumulation of metronidazole in serum can be observed. Therefore, in patients with severe renal failure, the frequency of metronidazole should be reduced.

Indications:

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

- prevention and treatment of anaerobic infections during surgical interventions, mainly on the organs of the abdominal cavity and urinary tract;

- combined therapy of severe mixed aerobic-anaerobic infections;

- severe form of intestinal and hepatic amebiasis;

- sepsis;

- peritonitis;

- osteomyelitis;

- gynecological infections;

- abscesses of small pelvis and brain;

- abscessed pneumonia;

- gas gangrene;

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

Contraindications:

- Hypersensitivity to metronidazole or other nitroimidazole derivatives;

- organic lesions of the central nervous system;

- Diseases of the blood;

- I trimester of pregnancy;

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

Carefully:With caution appoint for diseases of the kidneys, liver.

II and III trimesters of pregnancy - only for life indications.

Dosing and Administration:

Intravenous administration Metronidazole It is indicated in cases of severe infection, as well as in the absence of the possibility of taking the drug inside.

For adults and children over 12 years single dose is 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.

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

For the prevention of anaerobic infection before the planned operation on pelvic organs and urinary tracts for adults and children over 12 years of age Metronidazole is prescribed 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 (SC less than 30 ml / min) and / or liver daily dose of metronidazole 1000 mg; (the frequency of reception 2 times).

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

Side effects:

From the gastrointestinal tract: nausea, vomiting, intestinal colic, constipation, dry mouth, glossitis, stomatitis, pancreatitis, diarrhea, lack of appetite, unpleasant metallic taste in the mouth, epigastric pain;

From the side of the neutral nervous system: with long-term use - headache, dizziness, movement coordination disorders, ataxia, irritability, peripheral neuropathy, increased excitability, depression, sleep disturbance, weakness; in some cases - confusion, hallucinations, convulsions;

From the genitourinary system: dysuria, cystitis, polyuria, urinary incontinence, burning sensation in the urethra, excessive development of the fungal flora of the vagina (candidiasis);

Dermatological reactions: allergic reactions (skin rash, itching, urticaria);

From the side of the musculoskeletal system: arthralgia;

From the hematopoietic system: leukopenia.

Allergic reactions: nasal congestion, fever;

Local Reactions: trhombo-phlebitis, (pain, congestion or swelling at the injection site).

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

During the reception of Metronidazole, a reddish-brown color of the urine may be observed.

Interaction:

In the application of metronidazole for injection interaction with other drugs slightly, but caution while the appointment with some drugs:

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

Disulfides (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.

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 that stimulate enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin), can accelerate the elimination of Metronidazole, resulting in reduced its concentration in the plasma.

In patients receiving long-term treatment with drugs lithium in high doses, with the admission of Metronidazole, an increase in the concentration of lithium in the blood plasma and the development of symptoms of intoxication are possible.

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

Special instructions:

Do not drink alcohol while taking the drug, since Metronidazole has the ability to induce aversion to alcoholic beverages.

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

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

With leukopenia, the possibility of continuing treatment depends on the risk of developing an infectious process.

The appearance of ataxia, dizziness and any other worsening of the neurological status of patients requires discontinuation of treatment.

Can immobilize treponema and lead to Nelson's false positive test.

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. 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:

100 ml of solution in a bottle of low density polyethylene.

Each vial is packed in a plastic bag or in a polypropylene bag and placed in a cardboard box along with instructions for use.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Do not freeze.

Shelf life:

3 years.

Do not use after the expiration of the period indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012969 / 01

Date of registration:01.08.2008

Expiration Date:Unlimited

The owner of the registration certificate:Ahlkon Parenteralis (India) LimitedAhlkon Parenteralis (India) Limited India

Manufacturer: & nbsp

AHLCON PARENTERALS, Limited India

Representation: & nbspAhlkon Parenteralis (India) LimitedAhlkon Parenteralis (India) LimitedIndia

Information update date: & nbsp25.04.2018

Illustrated instructions

Instructions

Metronidazole (Metronidazole)