Trichopol - instructions for use, doses, side effects, contraindications

The drug shows a high activity in a relationship 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.

To Metronidazole not sensitive 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.

Metronidazole is excreted by the kidneys - 63% dose (20% of the drug is unchanged). The half-life of metronidazole is 6-7 hours. The renal clearance is 10.2 ml / min.

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

Indications:

Metronidazole, an infusion solution, is indicated for the treatment of infections caused by drug-susceptible microorganisms:

- prevention and treatment of anaerobic infections in 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 the skin and soft tissues, bones and joints.

Contraindications:

- Hypersensitivity to metronidazole or other nitroimidazole derivatives;

- organic lesions of the central nervous system (including epilepsy);

- leukopenia (including in the anamnesis);

- hepatic failure (in the case of the appointment of large doses);

- I trimester of pregnancy;

- lactation period.

Carefully:

- Pregnancy II and III trimesters (only for life indications);

- renal and / or liver failure.

Pregnancy and lactation:

Metronidazole penetrates the placenta, so do not prescribe the drug in the first trimester of pregnancy, then should be used only if the potential benefit of using the drug for the mother exceeds the possible risk to the fetus.

Because the metronidazole penetrates into breast milk, reaching in it the concentrations close to the concentrations in the blood plasma, it is recommended to stop breastfeeding during treatment with the drug.

Dosing and Administration:

Intravenously.

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.

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 pelvic organs and urinary tract adults and children over 12 years Metronidazole is administered 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.

Children under the age of 12 years it is recommended the administration of metronidazole intravenously drip on the same schedule in a single dose of 7.5 mg / kg body weight. The maximum daily dose in children under 12 years of age is 22.5 mg / kg body weight.

For patients with severe renal dysfunction (creatinine clearance less than 30 ml / min) and / or liver The daily dose of metronidazole is 1000 mg, the frequency of administration is 2 times.

Metronidazole, a solution for infusions, is not recommended to be mixed with other medicinal products!

Side effects:

From the gastrointestinal tract: epigastric pain, nausea, vomiting, diarrhea, constipation, intestinal colic, decreased appetite, anorexia, a taste disorder, an unpleasant "metallic" taste in the mouth,dry mouth, glossitis, stomatitis; very rarely - a deviation from the norm results of tests for the functional state of the liver, cholestatic hepatitis, jaundice, pancreatitis.

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

From the genitourinary system: dysuria, cystitis, polyuria, urinary incontinence, vulvovaginal candidiasis, pain in the vagina, staining the urine in a red-brown color.

Allergic reactions: skin rash, itching, urticaria, multi-form exudative erythema, nasal congestion, fever.

From the side of the musculoskeletal system: myalgia, arthralgia.

From the hematopoietic system: leukopenia; rarely - agranulocytosis, neutropenia, thrombocytopenia, pancytopenia.

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

Other: flattening of the T wave on the ECG; extremely rare - ototoxicity; pustular eruptions; gynecomastia.

Overdose:

Too high doses can cause increased side effects, mainly nausea, vomiting and dizziness; in more severe cases, there may be ataxia, paresthesia and seizures.

Treatment: symptomatic. There is no specific antidote.

Interaction:

When using metronidazole, a solution for infusions, interaction with other drugs is negligible, but caution should be exercised when concomitant administration with certain medicines:

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 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 use 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.

With the combined administration of metronidazole and cyclosporine there may be an increase in the concentration of cyclosporine in the blood plasma.

Metronidazole reduces clearance fluorouracil, which can cause an increase in the toxicity of the latter.

With simultaneous application metronidazole can increase plasma concentrations bisulfan.

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

Special instructions:

With caution appoint for diseases of the kidneys, liver.

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

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

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. During the administration of metronidazole, a red-brown staining of urine can be observed.

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

There is no information.

Form release / dosage:

Solution for infusion, 5 mg / ml.

Packaging:

To 20 ml in ampoules of colorless glass of hydrolytic class I. 10 ampoules together with the instruction for use are placed in a cardboard box.

100 ml in bottles of high-density polyethylene with an adapter for infusion set. One bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

Ampoules - 3 years.

Bottles - 2 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014710 / 02

Date of registration:20.08.2009 / 31.03.2014

Expiration Date:Unlimited

Date of cancellation:2018-04-12

The owner of the registration certificate:Pharmaceutical factory "POLFARMA" JSCPharmaceutical factory "POLFARMA" JSC Poland

Manufacturer: & nbsp

POLPHARMA PHARMACEUTICAL WORKS, S.A. Poland

Representation: & nbspAKRIKHIN OJSC AKRIKHIN OJSC Russia

Information update date: & nbsp12.04.2018

Illustrated instructions

Instructions

Trichopolol® (Trichopol®)