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

Round, flat-cylindrical tablets of white with a yellowish shade of color; with a facet on both sides and a risk on one side. The tablets turn yellow under the influence of light.

Pharmacotherapeutic group:antimicrobial and antiprotozoal agent

ATX: & nbsp

P.01.A.B Nitroimidazole derivatives

P.01.A.B.01 Metronidazole

Pharmacodynamics:

Metronidazole is a 5-nitroimidazole derivative with antiprotozoal and antibacterial action. The mechanism of action is the biochemical reduction of the 5-nitro group by intracellular transport proteins of anaerobic microorganisms and protozoa. The reduced 5-nitro group interacts with the DNA of a cell of microorganisms, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.

Metronidazole is active against: Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., as well as obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp., Prevotella (Prevotella bivia, Prevotella buccae, Prevotella disiens) and some Gram-positive microorganisms (Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The minimum inhibitory concentration (MIC) 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 has no bactericidal action against most aerobic bacteria and facultative anaerobes, fungi and viruses.In the presence of mixed flora (aerobes and anaerobes) metronidazole acts synergistically with antibiotics effective against conventional aerobes.

Increases the sensitivity of tumors to radiation, causes sensitization to alcohol (disulfiram-like action), stimulates reparative processes.

Pharmacokinetics:

Metronidazole - quickly and almost completely absorbed from the digestive tract, bioavailability of at least 80%. The presence of food reduces the rate of absorption and maximum concentration of metronidazole in the blood serum. Less than 20% of the drug binds to serum proteins.

Metronidazole penetrates 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 and placental barrier. The volume of distribution in adults is about 0.55 l / kg, in newborns - 0.54-0.81 l / kg.

The maximum concentration of metronidazole in the blood is reached in 1-3 hours.

About 30-60% of metronidazole is metabolized by hydroxylation, oxidation and interaction with glucuronic acid.The main metabolite of metronidazole (2-oxymetronidazole) also exhibits antibacterial and antiprotozoal effects.

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

Metronidazole and major metabolites are rapidly removed from the blood during hemodialysis (T_1/2is reduced to 2.6 hours). When peritoneal dialysis is withdrawn in small quantities. Kidney cancer 60-80% of metronidazole (20% unchanged), through the intestine - 6-15% of the dose applied. Kidney clearance of the drug is 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).

The renal excretion of metronidazole decreases in elderly patients.

Indications:

- Trichomoniasis;

- bacterial vaginosis;

- all forms of amoebiasis (diseases of intestinal and extraintestinal localization, including amoebic liver abscess, amoebic dysentery,as well as asymptomatic amoebiasis);

- giardiasis;

- Periodontal infections (including acute ulcerative gingivitis, acute odontogenic infections);

- anaerobic bacterial infections (gynecological and abdominal infections, central nervous system infections, bacteremia, sepsis, endocarditis, infections of bones and joints, skin and soft tissues, respiratory tract infections) caused by Bacteroides spp., Clostridium spp., Eubacterium spp., Peptococcus spp., Peptostreptococcus spp. and other anaerobes, sensitive to metronidazole.

- Treatment of infections Helicobacter pylori with peptic ulcer of the duodenum or stomach in combination with bismuth preparations and an antibiotic, for example, amoxicillin.

- Prophylactic appointment before surgical intervention on the gastrointestinal tract and reproductive organs.

Contraindications:

- Hypersensitivity to metronidazole and other nitroimidazole derivatives, as well as to any other ingredients of the drug;

- leukopenia (including in the anamnesis);

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

- hepatic insufficiency (in case of administration of large doses of the drug);

- pregnancy (1 trimester);

- lactation period;

- Children under 3 years old (for this dosage form).

Carefully:BVariability (II-III trimesters), renal / hepatic insufficiency.

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:

Inside, during or after eating, without chewing.

Trichomoniasis

Adults and children over 10 years of age:

250 mg (1 tablet) 3 times a day or 500 mg (2 tablets) 2 times a day for 7 days. Women need to be additionally appointed metronidazole in the form of vaginal suppositories or tablets. If necessary, you can repeat the course of treatment. Between the courses should be a break in 3-4 weeks with the conduct of repeated control laboratory tests.

An alternative therapy scheme is the administration of 750 mg (3 tablets) in the morning and 1250 mg (5tablets) in the evening or 2000 mg (8 tablets) as a single daily dose. Duration of treatment is 2 days.

Treatment is carried out at the same time for both sexual partners.

Children: from 3 to 7 years - 125 mg (1/2 tablet) 2 times a day; from 7 to 10 years - 125 mg (1/2 tablet) 3 times a day.

The course of treatment is 7 days.

Bacterial vaginosis

Adults:

For 500 mg (2 tablets) 2 times a day for 7 days or 2000 mg (8 tablets) as a single dose.

Simultaneous treatment of the sexual partner is not required.

Amebiasis

Invasive forms of intestinal amebiasis in susceptible patients (including amoebic dysentery)

Adults and children over 10 years of age:

For 750 mg (3 tablets) 3 times a day.

Children: from 3 to 7 years - 250 mg (1 tablet) 4 times a day; from 7 to 10 years - 375 mg (1.5 tablets) 3 times a day.

The course of treatment is usually 5 days.

Amoebiasis of the intestine in less susceptible patients and with chronic amoebic hepatitis

Adults and children over 10 years of age:

For 375 mg (1.5 tablets) 3 times a day.

Children: from 3 to 7 years - 125 mg (1/2 tablets) 4 times a day; from 7 to 10 years - 250 mg (1 tablet) 3 times a day.

The duration of treatment is 5-10 days.

Amoebic liver abscess and other forms of extraintestinal amebiasis

Adults and children over 10 years of age:

For 375 mg (1.5 tablets) 3 times a day.

Children: from 3 to 7 years -125 mg (1/2 tablet) 4 times a day; from 7 to 10 years - 250 mg (1 tablet) 3 times a day.

The course of treatment is 5 days.

Asymptomatic carriage of cysts

Adults and children over 10 years of age:

For 375-750 mg (1.5 - 3 tablets) 3 times a day.

Children: from 3 to 7 years - 125 mg (1/2 tablet) 4 times a day; from 7 to 10 years - 250 mg (1 tablet) 3 times a day.

The duration of the course of treatment is 5 to 10 days.

Lambliasis

Adults and children over 10 years of age:

For 500 mg (2 tablets) 2 times a day for 5-7 days;

By 2000 mg (8 tablets) once a day for 3 days.

Children: from 3 to 7 years - 250 - 375 mg (1 - 1.5 tablets) once a day for 5 days or 500-750 mg (2-3 tablets) once a day for 3 days; from 7 to 10 years - 250 mg (1 tablet) twice a day for 5 days or

1000 mg (4 tablets) once a day for 3 days.

Infections of periodontal disease

Acute Ulcerative Gingivitis

Adults and children over 10 years of age:

For 250 mg (1 tablet) 3 times a day.

Children: from 3 to 7 years - 125 mg (1/2 tablet) twice a day; from 7 to 10 years - 125 mg (1 tablet) 3 times a day.

The duration of treatment is 3 days.

Acute odontogenic infections

Adults and children over 10 years of age:

250 mg (1 tablet) 3 times a day for 3-7 days.

Infections caused by anaerobic bacteria

Treatment of anaerobic infections usually begins with intravenous infusions. As soon as it becomes possible, the treatment should be continued with pills.

Adults and children over 10 years of age: 500 mg (2 tablets) 3-4 times a day.

Children under 10 years of age In the treatment of anaerobic infections, the use of infusion solutions of metronidazole is recommended.

The duration of treatment should not exceed 7 days.

Eradication Helicobacter pylori

For 500 mg (2 tablets) 3 times a day for 7 days (as part of combination therapy, for example, with amoxicillin 2.25 g per day).

Prevention of infections caused by anaerobic bacteria (before surgical operations on the abdominal cavity, in gynecology and obstetrics)

Adults and children over 12 years of age:

For 250-500 mg (1-2 tablets) 3 times a day for 3-4 days before surgery.

1-2 days after the operation (when ingestion is already allowed) 250 mg (1 tablet) 3 times a day for 7 days.

With severe renal dysfunction (creatinine clearance less than 10 ml / min) daily dose of metronidazole should be reduced 2 times.

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, 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.

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

Overdose:

The lethal dose for a person is unknown.Too high doses can cause increased side effects, mainly nausea, vomiting and dizziness; in more severe cases, there may be ataxia, paresthesia and seizures.

In case of poisoning, use symptomatic and supportive treatment. There is no specific antidote.

Interaction:

Metronidazole enhances the effect of warfarin and other anticoagulants coumarinic series, so with the simultaneous administration of a dose of these drugs must be reduced.

Similarly, disulfiram causes intolerance to ethanol.

Simultaneous use with disulfiram can lead to the development of various neurologic symptoms (the interval between appointments is at least 2 weeks).

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 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.

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

With the combined use of metronidazole and cyclosporine, an increase in the concentration of cyclosporine in the blood plasma can be observed.

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

Sulfonamides increase the antimicrobial effect of metronidazole.

Special instructions:

Patients with severe hepatic insufficiency metronidazole should be administered with caution, because as a result of slowing metabolism, the concentration of metronidazole and its metabolites in plasma increases.

Because of the slowing down of excretion, care must be taken when choosing a dose of metronidazole in patients with renal insufficiency. In such patients, the dose should be reduced by half.

Metronidazole should be used with extreme caution in patients with bone marrow and central nervous system depression, as well as in elderly patients.

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

With prolonged therapy with metronidazole (more than 10 days), monitor the picture of peripheral blood and liver function.

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

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

Metronidazole should be avoided in patients with porphyria.

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. After trichomoniasis therapy, control tests should be performed for three consecutive cycles before and after menstruation.

After treatment of giardiasis, if symptoms persist, 3 feces analysis should be performed at intervals of several days in 3-4 weeks (in some successfully treated patients lactose intolerance caused by invasion can persist for several weeks or months, recalling the symptoms of giardiasis).

Patients should refrain from drinking alcohol during metronidazole therapy, and also for at least 48 hours after completion of treatment, because of the potential for developing disulfiram-like reactions: abdominal pain of a spastic nature, nausea, vomiting, headache, sudden rush of blood to the face.

During treatment with metronidazole urine may have a dark or reddish-brown color due to the presence of water-soluble dyes.

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

When taking the drug should be avoided potentially dangerous activities that require increased attention, rapid mental and motor reaction, especially driving vehicles and maintenance mechanisms.

Form release / dosage:

Tablets, 250 mg.

Packaging:

10 tablets in a blister of PVC / Al foil.

Two blisters together with instructions for use are placed in a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014703 / 01

Date of registration:18.08.2009 / 12.01.2015

Expiration Date:Unlimited

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: & nbsp12.09.2016

Illustrated instructions

Instructions

Trichopolol® (Trichopol®)