TRIZOL [Metronidazole] 500 g Film-coated tablets
TRIZOL
instructions for medical use of the medicinal product
Tradename
Trizol , Тризол
International non-proprietary name
Metronidazole,
Compound
Each film-coated tablet contains:
active substance: metronidazole 500 mg
excipients: dextrin, hydroxypropylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, silicon dioxide, talc, sodium starch glycolate , magnesium stearate.
Dosage form
Tablets.
Pharmacotherapeutic group
Antimicrobial and antiprotozoal agent.
Pharmacological properties
Pharmacodynamics
Antiprotozoal and antimicrobial drug, a derivative of 5-nitroimidazole. 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 deoxyribonucleic acid (DNA) of the microorganism cells, inhibiting the synthesis of their nucleic acids, which leads to the death of bacteria.
Active against Trihomonas vaginalis, Entamoeba histolica, Gardnerella vaginalis, Giardia intestinalis, Lamblia spp., and obligate anaerobes Bacteroides spp. (including Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides vulgatus), Fusobacterium spp., Veillonela spp., Prevotella (P. bivia, P. buccae, P. disiens), and some gram-positive microorganisms ( Eubacterium spp., Clostridium spp., Peptococcus spp., Peptostreptococcus spp.). The minimum inhibitory concentration for these strains is 0.125-6.25 µg/ml.
In combination with amoxicillin, it is active against Helicobacter pylori (amoxicillin inhibits the development of resistance to metronidazole).
Aerobic microorganisms and facultative anaerobes are not sensitive to metronidazole, but in the presence of mixed flora (aerobes and anaerobes), metronidazole acts synergistically with antibiotics, and is effective against ordinary aerobes.
Increases the sensitivity of tumors to radiation, causes sensitization to alcohol (disulfiram-like action), stimulates reparative processes.
Pharmacokinetics
When taken orally, metronidazole is rapidly and almost completely absorbed (approximately 80% in 1 hour). Simultaneous food intake does not affect the absorption of metronidazole. Bioavailability is at least 80%. After oral administration of metronidazole at a dose of 500 mg, its plasma concentration is 10 μg / ml after 1 hour, 13.5 μg / ml after 3 hours. Binding to blood proteins is insignificant and does not exceed 10-20%. Metronidazole rapidly penetrates tissues (lungs, kidneys, liver, skin, bile, cerebrospinal fluid, saliva, seminal fluid, vaginal secretion), into breast milk and passes through the placental barrier. About 30-60% of metronidazole is metabolized by hydroxylation, oxidation and glucuronidation. The main metabolite (2-oxymetronidazole) also has antiprotozoal and antimicrobial effects. 40-70% of metronidazole is excreted by the kidneys (unchanged - about 35% of a pleasant dose). The half-life is 8-10 hours. In patients with impaired renal function, a course of taking metronidazole may increase its concentration in the blood serum.
Indications for use
• Protozoal infections: extraintestinal amoebiasis (including amoebic liver abscess), intestinal amoebiasis (amebic dysentery), trichomoniasis.
• Infections caused by Bacteroides spp. (including Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides distasonis, Bacteroides vulgatus): bone and joint infections, central nervous system infections (including meningitis, brain abscess), bacterial endocarditis, pneumonia, empyema and lung abscess , sepsis.
• Infections caused by Clostridium spp., Peptococcus niger, Peptostreptococcus spp.: infections of the abdominal cavity (peritonitis, liver abscess), infections of the pelvic organs (endometritis, abscess of the fallopian tubes and ovaries, infections of the vaginal fornix).
• Pseudomembranous colitis associated with the use of antibiotics; gastritis or duodenal ulcer associated with Helicobacter pylori (as part of complex therapy);
• Prevention of postoperative complications (especially after interventions on the colon, pararectal region, appendectomy, and after gynecological operations).
Contraindications
• hypersensitivity to metronidazole, other nitroimidazole derivatives, imidazoles;
• organic lesions of the central nervous system (including epilepsy);
• leukopenia (including history);
• liver failure (in case of prescribing the drug in high doses);
• pregnancy (I trimester) , the period of breastfeeding.
Dosage and administration
Inside during or after a meal without chewing. Drink plenty of water.
Adults:
Anaerobic infections
Usually, treatment begins with intravenous infusions of metronidazole, followed by the transition to taking the drug inside. 500 mg 3 times a day. The duration of treatment is up to 7 days.
Trichomoniasis
With trichomoniasis in women (urethritis and vaginitis), the drug is used once at a dose of 2 g or as a course of treatment for 10 days: 250 mg 2 times a day. With trichomoniasis in men (urethritis), the drug is used once at a dose of 2 g or as a course of treatment for 10 days: 250 mg 2 times a day.
Pseudomembranous colitis
500 mg 3-4 times a day. The duration of treatment is determined by the doctor.
intestinal amoebiasis
1500 mg per day in three doses for 7 days. In acute amoebic dysentery - the daily dose is 2250 mg divided into three doses.
Liver abscess and other extraintestinal amoebiasis
The maximum daily dose is 2500 mg divided into 3 doses for 3-5 days in combination with tetracycline antibiotics and other therapies.
Gastritis or duodenal ulcer associated with Helicobacter pylori
500 mg 3 times a day as part of combination therapy, for example with amoxicillin.
Prevention of postoperative infections
750-1500 mg per day in 3 doses 3-4 days before surgery. 1-2 days after the operation (when ingestion is already allowed) - 750 mg per day for 7 days.
In renal failure (creatinine clearance less than 10 ml / min), the daily dose should be reduced by 2 times.
Children over 3 years old:
Anaerobic infections
20-30 mg/kg per day.
intestinal amoebiasis
30-40 mg / kg per day in three divided doses.
Liver abscess and other extraintestinal amoebiasis
30-40 mg / kg per day in three divided doses.
Special instructions and precautions
During the treatment period, ethanol is contraindicated (possible development of a disulfiram-like reaction: spastic abdominal pain, nausea, vomiting, headache, sudden rush of blood to the face).
In combination with amoxicillin, it is not recommended for use in patients under 18 years of age.
With prolonged therapy, it is necessary to control the blood picture. 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.
May immobilize treponema and lead to a false positive Nelson test.
Colors urine dark.
In the treatment of trichomonas vaginitis in women and trichomonas urethritis in men, it is necessary to refrain from sexual activity. Mandatory simultaneous treatment of sexual partners. Treatment does not stop during menstruation. After therapy for trichomoniasis, control tests should be carried out for three regular cycles before and after menstruation.
After treatment of giardiasis, if symptoms persist, perform 3 stool tests at intervals of several days after 3-4 weeks (in some successfully treated patients, lactose intolerance caused by invasion may persist for several weeks or months, resembling the symptoms of giardiasis).
During the treatment period, it is recommended to stop breastfeeding.
With caution prescribed for hepatic encephalopathy, acute and chronic diseases of the peripheral and central nervous system (the risk of worsening neurological symptoms), renal failure.
Use during pregnancy and during breastfeeding
Contraindicated in the first trimester of pregnancy, during breastfeeding.
II-III trimester of pregnancy, the use is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.
Interaction with other drugs
Enhances the effect of indirect anticoagulants, which leads to an increase in the time of formation of prothrombin.
Similar to disulfiram, it causes ethanol intolerance. Simultaneous use with disulfiram can lead to the development of various neurological symptoms (the interval between administration is 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 increase in the risk of side effects.
The simultaneous administration of drugs that stimulate microsomal oxidation enzymes in the liver (phenobarbital, phenytoin) can accelerate the elimination of metronidazole, resulting in a decrease in its plasma concentration. When taken simultaneously with lithium preparations, the concentration of the latter in plasma and the development of symptoms of intoxication may increase.
It is not recommended to combine with non-depolarizing muscle relaxants (vecuronium bromide).
Sulfonamides enhance the antimicrobial effect of metronidazole.
Side effect
From the digestive system: epigastric pain, nausea, vomiting, diarrhea; inflammation of the oral mucosa (glossitis, stomatitis), taste disturbances ("metallic" taste in the mouth), loss of appetite, anorexia, dryness of the oral mucosa, constipation; pancreatitis (reversible cases); discoloration of the tongue / "coated" tongue (due to excessive growth of fungal microflora).
From the immune system: angioedema, anaphylactic shock.
From the side of the nervous system: peripheral sensory neuropathy; headache, convulsions, dizziness; encephalopathy (eg, confusion, fever, headache, paralysis, photosensitivity, visual and movement disturbances, neck stiffness) and subacute cerebellar syndrome (eg, ataxia, dysatria, gait disturbance, nystagmus, and tremor), which regress after withdrawal drug; aseptic meningitis.
On the part of the psyche: psychotic disorders, including confusion, hallucinations; depression, insomnia, irritability, irritability.
On the part of the organ of vision: transient visual impairment, such as diplopia, myopia, blurred vision, decreased visual acuity, impaired color perception; optic neuritis.
On the part of the organ of hearing and labyrinth disorders: hearing impairment / hearing loss (including sensorineural deafness); noise in ears.
From the hemopoietic system: agranulocytosis, leukopenia, neutropenia, thrombocytopenia.
On the part of the liver and biliary tract: increased activity of liver enzymes (ACT and ALT, alkaline phosphatase), the development of cholestatic or mixed hepatitis, hepatocellular liver damage, sometimes accompanied by jaundice. In patients treated with metronidazole in combination with other antibiotics, cases of liver failure have been observed, requiring liver transplantation.
On the part of the skin and subcutaneous tissues: rash, itching, flushing of the skin, flushing of the skin, urticaria; pustular skin rash; acute generalized exanthematous pustulosis; fixed drug rash; Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the urinary system: it is possible to stain urine in a brownish-reddish color, due to the presence in the urine of a water-soluble metabolite of metronidazole; dysuria, polyuria, cystitis, urinary incontinence, candidiasis.
On the part of laboratory parameters and instrumental studies: flattening of the T wave on the ECG.
General reactions: fever, nasal congestion, arthralgia, weakness.
Overdose
Symptoms: vomiting, ataxia, slight disorientation, convulsions.
Treatment: gastric lavage, administration of activated charcoal, symptomatic and supportive therapy. There is no specific antidote, it is excreted from the body during hemodialysis.
Storage conditions
Store below 30ºC. Keep away from the world.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiry date stated on the packaging.
Holiday conditions
Released by prescription.
Release form
10 tablets in an aluminum foil blister. 2 blisters with instructions for use in a cardboard box.