Tricho-PIN - instructions for use, dose, side effects, contraindications

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 active in a relationship: Trichomonas vaginalis, Entamoeba histolytica, Gardnerella vaginalis, Giardia intestinal is, Lamblia spp., as well as obligate anaerobes Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonella spp,, Prevotella (P. bivia, P. buccae, P.disiens) and some Gram-positive microorganisms (Eubacterium spp., Clostridium 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 does not have a bactericidal effect for 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 is quickly and almost completely absorbed from the digestive tract, bioavailability of at least 80%. The presence of food reduces the rate of absorption and the 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. Volume of distribution the 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.

The 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 of metronidazole cumulation in serum can be observed (hence patients with severe renal impairment receiving frequency to be reduced).

Urine may have a dark or reddish-brown color due to the presence of water-soluble dyes.

Kidney excretion of metronidazole decreases in elderly patients.

Indications:

- Protozoal infections: trichomoniasis, extraintestinal amoebiasis, including amoebic liver abscess, intestinal amoebiasis (amoebic dysentery), giardiasis.

- Anaerobic bacterial infections (gynecological, including bacterial vaginosis, as well as abdominal infections, central nervous system infections, bacteremia, sepsis, endocarditis, infections of bones, joints, skin and soft tissues, periodontal infections, respiratory tract infections) caused by Bacteroides spp., Clostridium spp., Eubacterium spp., Peptococcus spp., Peptostreptococcus spp. and other anaerobes, sensitive to metronidazole (for adults and children).

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

- Treatment of enterocolitis caused by Clostridium difficile.

- 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 anamnesis).

- Organic damage to the central nervous system (including epilepsy).

- Hepatic insufficiency (in case of administration of large doses of the drug).

- Pregnancy (I trimester), lactation.

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

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

Carefully:

Pregnancy (II-III trimester), renal / hepatic 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 in 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 a meal (or squeezed milk), without chewing,

Trichomoniasis

Adults:

250 mg twice a day for 10 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 or increase the dose to 0.75 - 1.0 g per day. Between the courses should be a break in 3-4 weeks with the conduct of repeated control laboratory tests.

An alternative scheme of therapy is the appointment of 2 g once to the patient and his sexual partner.

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

Children: from 3 to 5 years - 250 mg (1 tablet) per day; from 5 to 10 years - 250 - 375 mg (1-1.5 tablets) per day; over 10 years old - 500 mg (2 tablets) per day.

The daily dose should be divided into 2 reception. The course of treatment is 10 days.

Amebiasis

Adults:

With asymptomatic amoebiasis (cyst), 500 mg (2 tablets) 2-3 times a day for 5-7 days.

In chronic amoebiasis, 500 mg (2 tablets) 3 times a day for 5-10 days.

In acute amoebic dysentery for 750 mg (3 tablets) 3 times a day until the symptoms stop.

With liver abscess, the maximum daily dose of 2.5 g in 1 or 2-3 doses, for 3-5 days, in combination with antibiotics (tetracyclines) and other methods of treatment.

Children: 3-7 years - 1/3 of the adult dose; 7-10 years old - 1/2 dose of an adult.

Lambliasis

Adults: 500 mg (2 tablets) 2 times a day.

Children: from 3 to 5 years: 250 mg (1 tablet) per day; from 6 to 10 years: 375 mg (1.5 tablets) per day; older than 10 years: 500 mg (2 tablets) per day.

The daily dose should be divided into 2 divided doses.

The course of treatment is usually 5-10 days.

If necessary, according to the doctor's decision, the treatment can be repeated after 4-6 weeks.

Eradication of Helicobacter pylori

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

Infections caused by anaerobic bacteria

Adults and children over 12 years of age: 250-500 mg (1-2 tablets) 3 times a day during or after meals.

Metronidazole can be used in monotherapy or in combination with other antibacterial drugs.

The average treatment period should not exceed 7 days.

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:

First 1 g (4 tablets of 250 mg) in a single dose, then 1 tablet 250 mg 3 times daily during or after a meal.

Children: from 6 to 12 years - 125 mg (1/2 tablet) every 8 hours for 2 days.

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

Side effects:

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

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

From the genitourinary system: a burning sensation in the urethra, dysuria, cystitis, polyuria, urinary incontinence, excessive development of fungal flora of the vagina (candidiasis), staining of urine in red-brown color.

Allergic reactions: skin rash, itching, hives, nasal congestion, fever.

From the side of the musculoskeletal system: arthralgia.

From the hematopoietic system: neutropenia, leukopenia.

Other: flattening of the T wave on the ECG.

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 action indirect anticoagulants, which leads to an increase in the time of prothrombin formation.

Similarly, disulfiram causes intolerance ethanol.

Simultaneous application with disulfiram can lead to the development of various neurological symptoms (the interval between the appointment - at least 2 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 stimulating enzymes of microsomal oxidation in the liver (phenobarbital, phenytoin), can accelerate the elimination of metronidazole, as a result of which its concentration in the plasma decreases.

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 with nondepolarizing muscle relaxants (vecuronium bromide).

Sulfonamides enhance 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.

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. Treatment does not stop during menstruation. 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).

In the period of treatment, the use of ethanol is contraindicated (it is possible to develop disulfiramo similar reactions: abdominal pain of a spastic nature, nausea, vomiting, headache, sudden rush of blood to the face).

Stains urine in a dark color.

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

Consider the possibility of developing dizziness when prescribing the drug to patients; whose activities are related to the management of mechanisms,especially to drivers of vehicles.

Form release / dosage:

Tablets, 250 mg.

Packaging:

10 tablets per contour cell pack.

On 2 contour cellular packings together with the instruction on application place in a pack from a cardboard.

Storage conditions:

In a dry, dark place, at a temperature of no higher than 25 FROM.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N0002272 / 01

Date of registration:10.04.2008

Expiration Date:Unlimited

The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia

Manufacturer: & nbsp

NORTH STAR, CJSC Russia

Representation: & nbspNORTH STAR CJSC NORTH STAR CJSC Russia

Information update date: & nbsp19.09.2016

Illustrated instructions

Instructions

Tricho-PIN® (Tricho-PIN®)